OPIOID MEDICATIONS




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Benzhydrocodone (Apadaz®)

Dosage forms

Tablet
  • Benzhydrocodone : Acetaminophen
    • 4.08 mg : 325 mg
    • 6.12 mg : 325 mg
    • 8.16 mg : 325 mg

Dosing

Adults (opiate-naïve)
  • 1 - 2 tablets every 4 - 6 hours as needed for pain
  • Do not exceed 12 tablets in 24 hours
Converting from Hydrocodone
Hydrocodone dose Apadaz equivalent
5 mg 4.08 mg
7.5 mg 6.12 mg
10 mg 8.16 mg

Generic / Price

  • Generic available
  • 30 tablets - $

Other

  • DEA Schedule II
  • Benzhydrocodone is a prodrug of hydrocodone
  • Benzhydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase benzhydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining benzhydrocodone with an inhibitor, consider reducing the benzhydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the benzhydrocodone dose may need to be increased. When combining benzhydrocodone with an inducer, consider increasing the benzhydrocodone dose and monitoring efficacy. If an inducer is discontinued, the benzhydrocodone dose may need to be decreased.
  • Benzhydrocodone is partially metabolized by CYP2D6. If CYP2D6 inhibitors are taken with CYP3A4 inhibitors, the increase in benzhydrocodone exposure may be potentiated.


Buprenorphine (Belbuca®)

Dosage forms

Buccal film
  • 75 mcg
  • 150 mcg
  • 300 mcg
  • 450 mcg
  • 600 mcg
  • 750 mcg
  • 900 mcg
  • Comes in carton of 60 films

Dosing

Severe pain requiring long-term treatment (opiate-naïve or opioid-non-tolerant adults)
  • Starting: 75 mcg once daily or 75 mcg every 12 hours (if tolerated) for at least 4 days. Increase to 150 mcg every 12 hours after 4 days.
  • Further dose increases should be in increments of 150 mcg every 12 hours at intervals of no less than 4 days
  • Doses up to 450 mcg every 12 hours were studied in opiate-naïve patients in clinical trials. Do not exceed 900 mcg every 12 hours due to potential for QT prolongation.
  • Oral mucositis - patients with oral mucositis from chemotherapy may absorb Belbuca more rapidly. Reduce starting dose and titration dose by half, from 150 mcg to 75 mcg.
  • Severe liver disease (Child-Pugh C): reduce starting dose and titration dose by half, from 150 mcg to 75 mcg
Converting from other opiates
  • To reduce the risk of opioid withdrawal, taper patients to no more than 30 mg of oral morphine sulfate equivalent daily before beginning Belbuca
  • Dose increases should be in increments of no more than 150 mcg every 12 hours at intervals of no less than 4 days
  • Do not exceed 900 mcg every 12 hours due to potential for QT prolongation

Prior daily dose of MSE before taper to 30 mg MSE Initial Belbuca dose
< 30 mg 75 mcg once daily or every 12 hours
30 - 89 mg 150 mcg every 12 hours
90 - 160 mg 300 mcg every 12 hours
> 160 mg Consider alternative

Generic / Price

  • No generic
  • 60 films - $$$$

Other

  • DEA Schedule III
  • Buprenorphine is a partial agonist at mu opioid receptors
  • Belbuca is placed against the inside of the cheek. Belbuca film dissolves within 30 minutes. Do not eat or drink until film is dissolved.
  • Buprenorphine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase buprenorphine exposure, and CYP3A4 inducers may decrease exposure. When combining buprenorphine with an inhibitor, consider reducing the buprenorphine dose and monitoring for toxicity. If an inhibitor is discontinued, the buprenorphine dose may need to be increased. When combining buprenorphine with an inducer, consider increasing the buprenorphine dose and monitoring efficacy. If an inducer is discontinued, the buprenorphine dose may need to be decreased.
  • Prolonged QT interval - in trials, some patients treated with Belbuca had QT prolongation. Belbuca doses should not exceed 900 mcg every 12 hours because higher doses increase the risk. Use caution in patients at increased risk for QT prolongation (e.g. hypokalemia, hypomagnesemia, bradycardia, recent conversion from atrial fibrillation, CHF, digitalis therapy, hypomagnesemia, long QT syndrome). The risk of combining buprenorphine with other QT-prolonging drugs is unknown.
  • Dental problems (products that dissolve in the mouth) - dental problems, including tooth decay, cavities, dental abscesses/infection, tooth erosion, and tooth loss, have been reported in patients using buprenorphine medications that dissolve in the mouth. Problems have occurred in patients with no prior history of dental issues. Measures that may help prevent problems include taking a large sip of water after the product fully dissolves, swishing it gently around the teeth and gums, and swallowing it. Patients should also wait at least one hour before brushing their teeth after using the product. Regular visits to a dentist are also recommended.
  • Hepatotoxicity - buprenorphine has been associated with liver toxicity, especially in high-risk patients (e.g. alcoholism, hepatitis C, etc.). Baseline and periodic LFTs are recommended in susceptible patients.

Buprenorphine hydrochloride (Subutex®)

Dosage forms

Sublingual tablet
  • 2 mg
  • 8 mg

Dosing

Opiate withdrawal and OUD treatment

Generic / Price

  • Generic (60 tablets): $-$$ for #60

Other

  • DEA Schedule III
  • See buprenorphine for side effects, precautions, drug interactions, and more

Buprenorphine hydrochloride (Butrans®)

Dosage forms

Transdermal patch
  • 5.0 mcg/hr
  • 7.5 mcg/hr
  • 10 mcg/hr
  • 15 mcg/hr
  • 20 mcg/hr
  • Comes in carton with 4 patches

Dosing

Severe pain requiring long-term treatment (opiate-naïve adults)
  • Starting: one 5 mcg/hour patch
  • Patches are intended to be worn for 7 days
  • Increase dose at intervals of ≥ 72 hours. Dose adjustments may be made in 5 mcg/hr, 7.5 mcg/hr, or 10 mcg/hr increments by using no more than two patches of the 5 mcg/hr, or 7.5 mcg/hr, or 10 mcg/hr system(s). The total dose from both patches should not exceed 20 mcg/hr. For the use of two patches, instruct patients to remove their current patch, and apply the two new patches at the same time, adjacent to one another at a different application site
  • Maximum dose is 20 mcg/hr because of prolonged QT interval risk
Converting from other opiates
  • Initiate Butrans at the next dosing interval. See oral morphine sulfate equivalence table.
  • Oral morphine equivalent < 30 mg/day: start with 5 mcg/hr
  • Oral morphine equivalent 30 - 80 mg/day: before beginning Butrans, taper current opioids for up to 7 days to no more than 30 mg oral morphine equivalent per day. Initiate Butrans at 10 mcg/hr.
  • Oral morphine equivalent > 80 mg/day: 20 mcg/hr may not provide adequate analgesia. Consider the use of an alternate analgesic.

Generic / Price

  • Generic available
  • 4 patches - $$$

Other

  • DEA Schedule III
  • Buprenorphine is a partial agonist at mu opioid receptors
  • Apply to upper outer arm, upper chest, upper back or the side of the chest. These 4 sites (each present on both sides of the body) provide 8 possible application sites. Rotate Butrans among the 8 described skin sites. After Butrans removal, wait a minimum of 21 days before reapplying to the same skin site. Apply Butrans to a hairless or nearly hairless skin site. If none are available, the hair at the site should be clipped, not shaven.
  • Do not expose patch to direct heat because absorption may be increased
  • Patients with fever may absorb more buprenorphine from the patch
  • Buprenorphine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase buprenorphine exposure, and CYP3A4 inducers may decrease exposure. When combining buprenorphine with an inhibitor, consider reducing the buprenorphine dose and monitoring for toxicity. If an inhibitor is discontinued, the buprenorphine dose may need to be increased. When combining buprenorphine with an inducer, consider increasing the buprenorphine dose and monitoring efficacy. If an inducer is discontinued, the buprenorphine dose may need to be decreased.
  • Prolonged QT interval - in a trial, Butrans 40 mcg/hr was found to prolong the QT interval by a maximum of 9.2 msec. Butrans dosing should not exceed 20 mcg/hr. Use caution in patients at increased risk for QT prolongation (e.g. hypokalemia, hypomagnesemia, bradycardia, recent conversion from atrial fibrillation, CHF, digitalis therapy, hypomagnesemia, long QT syndrome). The risk of combining buprenorphine with other QT-prolonging drugs is unknown.
  • Hepatotoxicity - buprenorphine has been associated with liver toxicity, especially in high-risk patients (e.g. alcoholism, hepatitis C, etc.). Baseline and periodic LFTs are recommended in susceptible patients.

Buprenorphine hydrochloride (Probuphine®)

Dosage forms

Subdermal implant
  • Each implant contains 80 mg of buprenorphine HCL
  • Comes in kit with 4 implants and disposable applicator

Dosing

OUD maintenance therapy

Efficacy

Generic / Price

  • No generic
  • 1 kit - $$$$

Other

  • DEA Schedule III
  • See buprenorphine for side effects, precautions, drug interactions, and more

Buprenorphine hydrochloride (Sublocade®)

Dosage forms

Prefilled syringe
  • 100 mg/0.5 ml
  • 300 mg/1.5 ml

Dosing

OUD maintenance therapy

Efficacy

Generic / Price

  • No generic
  • 1 syringe - $$$$

Other

  • DEA Schedule III
  • See buprenorphine for side effects, precautions, drug interactions, and more


Buprenorphine and Naloxone | Suboxone® | Zubsolv®

Dosage forms

Suboxone® - sublingual tablet
  • Buprenorphine (mg) : Naloxone (mg)
    • 2 mg : 0.5 mg
    • 8 mg : 2.0 mg
Suboxone® - sublingual/buccal film
  • Buprenorphine : Naloxone
    • 2 mg : 0.5 mg
    • 4 mg : 1.0 mg
    • 8 mg : 2 mg
    • 12 mg: 3 mg
    • May be administered sublingually or buccally
Zubsolv® - sublingual tablet
  • Buprenorphine : Naloxone
    • 0.7 mg : 0.18 mg
    • 1.4 mg : 0.36 mg
    • 5.7 mg : 1.4 mg
    • 8.6 mg : 2.1 mg
    • 11.4 mg : 2.9 mg

Dosing

Opiate withdrawal and OUD treatment

Generic / Price

  • Suboxone generic (60 tablets): $$-$$$
  • Suboxone generic (30 films): $$$
  • Zubsolv (30 tablets): $$$$

Other

  • DEA Schedule III
  • See buprenorphine for side effects, precautions, drug interactions, and more


Butorphanol tartrate (Stadol®)

Dosage forms

Nasal spray
  • 1 mg/spray
  • Comes in 2.5 ml bottle at a concentration of 10 mg/ml
  • On average, one bottle delivers 14 - 15 one milligram doses

Dosing

Adults
  • 1 - 2 mg (one or two sprays)
  • May repeat in 3 - 4 hours as needed
  • When giving more than 1 spray, give in separate nostrils
Elderly or patients with renal or hepatic impairment
  • 1 mg (one spray)
  • May give an additional 1 mg in 90 - 120 minutes
  • May repeat in 6 hours as needed
Discontinuation after chronic dosing
  • Reduce dose by 25 - 50% every 2 - 4 days to prevent withdrawal

Generic / Price

  • Generic (1 bottle) - $

Other

  • DEA Schedule IV
  • Butorphanol is a partial opioid agonist at the mu opioid receptor and a full agonist at the kappa opioid receptor
  • Butorphanol is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase butorphanol exposure, and CYP3A4 inducers may decrease exposure. When combining butorphanol with an inhibitor, consider reducing the butorphanol dose and monitoring for toxicity. If an inhibitor is discontinued, the butorphanol dose may need to be increased. When combining butorphanol with an inducer, consider increasing the butorphanol dose and monitoring efficacy. If an inducer is discontinued, the butorphanol dose may need to be decreased.


Codeine - APAP | Tylenol #3 | Tylenol #4

Dosage forms

Tablet
  • Codeine phosphate : Acetaminophen
    • 15 mg : 300 mg
    • 30 mg: 300 mg (Tylenol® #3)
    • 60 mg : 300 mg (Tylenol® #4)

Dosing

Acute pain (adults)
  • 15 - 60 mg every 4 hours as needed
  • Do not exceed 360 mg in 24 hours
Acute pain (children ≥ 12 years)
  • Standard
    • 0.5 mg/kg/dose every 4 hours as needed
  • Alternative
    • < 50 kg: 0.5 - 1 mg/kg every 3 - 4 hours [5]
    • ≥ 50 kg: 30 - 60 mg every 3 - 4 hours [5]

Generic / Price

  • Generic (30 tablets) - $

Other

  • DEA Schedule III
  • CYP2D6 poor/rapid metabolizers - codeine has no analgesic activity until it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, codeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of codeine to morphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - codeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take codeine because it may cause somnolence and breathing issues in breastfed infants
  • Codeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase codeine exposure, and CYP3A4 inducers may decrease exposure. When combining codeine with an inhibitor, consider reducing the codeine dose and monitoring for toxicity. If an inhibitor is discontinued, the codeine dose may need to be increased. When combining codeine with an inducer, consider increasing the codeine dose and monitoring efficacy. If an inducer is discontinued, the codeine dose may need to be decreased.

Codeine - APAP solution

Dosage forms

Solution
  • Codeine 12 mg and acetaminophen 120 mg per 5 ml

Dosing

Acute pain (adults)
  • 15 ml every 4 hours as needed
Acute pain (children)
  • 3 - 6 years: 5 ml three to four times daily
  • 7 - 12 years: 10 ml three to four times daily
  • NOTE: in 2018, the FDA declared that codeine products are contraindicated in children < 12 years old

Generic / Price

  • Generic (120 ml) - $

Other

  • DEA Schedule V
  • CYP2D6 poor/rapid metabolizers - codeine has no analgesic activity until it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, codeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of codeine to morphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - codeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take codeine because it may cause somnolence and breathing issues in breastfed infants
  • Codeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase codeine exposure, and CYP3A4 inducers may decrease exposure. When combining codeine with an inhibitor, consider reducing the codeine dose and monitoring for toxicity. If an inhibitor is discontinued, the codeine dose may need to be increased. When combining codeine with an inducer, consider increasing the codeine dose and monitoring efficacy. If an inducer is discontinued, the codeine dose may need to be decreased.

Cheratussin DAC®

Dosage forms

Liquid
  • Codeine 10 mg, guaifenesin 100 mg, pseudoephedrine 30 mg per 5 ml
  • Contains 2.1% alcohol

Dosing

Cough and congestion (adults and children ≥ 12 years)
  • 10 ml every 4 hours as needed
  • Do not take more than 4 doses in 24 hours
Cough and congestion (children 6 - 11 years old)
  • 5 ml every 4 hours as needed
  • Do not take more than 4 doses in 24 hours
  • NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old

Generic / Price

  • Generic (120 ml) - $

Other

  • DEA Schedule V
  • Guaifenesin is an expectorant. Pseudoephedrine is a decongestant.
  • CYP2D6 poor/rapid metabolizers - codeine has no analgesic activity until it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, codeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of codeine to morphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - codeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take codeine because it may cause somnolence and breathing issues in breastfed infants
  • Codeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase codeine exposure, and CYP3A4 inducers may decrease exposure. When combining codeine with an inhibitor, consider reducing the codeine dose and monitoring for toxicity. If an inhibitor is discontinued, the codeine dose may need to be increased. When combining codeine with an inducer, consider increasing the codeine dose and monitoring efficacy. If an inducer is discontinued, the codeine dose may need to be decreased.

Phenergan® with codeine

Dosage forms

Syrup
  • Codeine 10 mg and promethazine 6.25 mg per 5 ml
  • Contains 7% alcohol

Dosing

Cough and congestion (adults and children ≥ 12 years)
  • 5 ml every 4 - 6 hours as needed
  • Do not take more than 30 ml in 24 hours
Cough and congestion (children 6 - 11 years old
  • 2.5 - 5 ml every 4 - 6 hours as needed
  • Do not take more than 30 ml in 24 hours
  • NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old

Generic / Price

  • Generic (120 ml) - $

Other

  • DEA Schedule V
  • Promethazine is an antihistamine/anticholinergic medication
  • CYP2D6 poor/rapid metabolizers - codeine has no analgesic activity until it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, codeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of codeine to morphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - codeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take codeine because it may cause somnolence and breathing issues in breastfed infants
  • Codeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase codeine exposure, and CYP3A4 inducers may decrease exposure. When combining codeine with an inhibitor, consider reducing the codeine dose and monitoring for toxicity. If an inhibitor is discontinued, the codeine dose may need to be increased. When combining codeine with an inducer, consider increasing the codeine dose and monitoring efficacy. If an inducer is discontinued, the codeine dose may need to be decreased.

Phenergan® VC with codeine

Dosage forms

Syrup
  • Codeine 10 mg, phenylephrine 5 mg, and promethazine 6.25 mg per 5 ml
  • Contains 7% alcohol

Dosing

Cough and congestion (adults and children ≥ 12 years)
  • 5 ml every 4 - 6 hours as needed
  • Do not take more than 30 ml in 24 hours
Cough and congestion (children 6 - 11 years old)
  • 2.5 - 5 ml every 4 - 6 hours as needed
  • Do not take more than 30 ml in 24 hours
  • NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old

Generic / Price

  • Generic (120 ml) - $

Other

  • DEA Schedule V
  • Phenylephrine is a decongestant. Promethazine is an antihistamine/anticholinergic medication.
  • CYP2D6 poor/rapid metabolizers - codeine has no analgesic activity until it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, codeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of codeine to morphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - codeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take codeine because it may cause somnolence and breathing issues in breastfed infants
  • Codeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase codeine exposure, and CYP3A4 inducers may decrease exposure. When combining codeine with an inhibitor, consider reducing the codeine dose and monitoring for toxicity. If an inhibitor is discontinued, the codeine dose may need to be increased. When combining codeine with an inducer, consider increasing the codeine dose and monitoring efficacy. If an inducer is discontinued, the codeine dose may need to be decreased.

Robitussin® AC

Dosage forms

Liquid / solution
  • Codeine 10 mg and guaifenesin 100 mg per 5 ml
  • Solution is alcohol free
  • Liquid contains 3 - 4% alcohol

Dosing

Cough and congestion (adults and children ≥ 12 years)
  • 10 ml every 4 hours as needed
  • Do not take more than 6 doses in 24 hours
Cough and congestion (children 6 - 11 years old)
  • 5 ml every 4 hours as needed
  • Do not take more than 6 doses in 24 hours
  • NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old

Generic / Price

  • Generic (120 ml) - $

Other

  • DEA Schedule V
  • Guaifenesin is an expectorant
  • Other brand names: Cheratussin AC®, Guaiatussin AC®, Virtussin AC®
  • CYP2D6 poor/rapid metabolizers - codeine has no analgesic activity until it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, codeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of codeine to morphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - codeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take codeine because it may cause somnolence and breathing issues in breastfed infants
  • Codeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase codeine exposure, and CYP3A4 inducers may decrease exposure. When combining codeine with an inhibitor, consider reducing the codeine dose and monitoring for toxicity. If an inhibitor is discontinued, the codeine dose may need to be increased. When combining codeine with an inducer, consider increasing the codeine dose and monitoring efficacy. If an inducer is discontinued, the codeine dose may need to be decreased.

Tuzistra™ XR

Dosage forms

Suspension, extended-release
  • Codeine 14.7 mg and chlorpheniramine 2.8 mg per 5 ml

Dosing

Cough and congestion (adults 18 years and older)
  • 10 ml every 12 hours as needed
  • Do not exceed 20 ml in 24 hours

Generic / Price

  • No generic
  • Brand (120 ml) - $$$

Other

  • DEA Schedule III
  • Chlorpheniramine is an antihistamine
  • CYP2D6 poor/rapid metabolizers - codeine has no analgesic activity until it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, codeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of codeine to morphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - codeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take codeine because it may cause somnolence and breathing issues in breastfed infants
  • Codeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase codeine exposure, and CYP3A4 inducers may decrease exposure. When combining codeine with an inhibitor, consider reducing the codeine dose and monitoring for toxicity. If an inhibitor is discontinued, the codeine dose may need to be increased. When combining codeine with an inducer, consider increasing the codeine dose and monitoring efficacy. If an inducer is discontinued, the codeine dose may need to be decreased.

Codeine Sulfate (CII)

Dosage forms

Tablet
  • 15 mg
  • 30 mg
  • 60 mg

Dosing

Acute pain (opiate-naïve adults)
  • 15 - 60 mg every 4 hours as needed
  • Do not exceed 360 mg in 24 hours
Acute pain (children > 6 months old)
  • < 50 kg: 0.5 - 1 mg/kg/dose every 3 - 4 hours [5]
  • ≥ 50 kg: 30 - 60 mg every 3 - 4 hours [5]
  • NOTE: In 2017, the FDA declared that all codeine products are contraindicated in children < 12 years old

Generic / Price

  • Generic (30 tablets) - $

Other

  • DEA Schedule II
  • CYP2D6 poor/rapid metabolizers - codeine has no analgesic activity until it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, codeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of codeine to morphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - codeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take codeine because it may cause somnolence and breathing issues in breastfed infants
  • Codeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase codeine exposure, and CYP3A4 inducers may decrease exposure. When combining codeine with an inhibitor, consider reducing the codeine dose and monitoring for toxicity. If an inhibitor is discontinued, the codeine dose may need to be increased. When combining codeine with an inducer, consider increasing the codeine dose and monitoring efficacy. If an inducer is discontinued, the codeine dose may need to be decreased.

Fioricet® with codeine

Dosage forms

Capsule
  • Codeine 30 mg, acetaminophen 325 mg, butalbital 50 mg, caffeine 40 mg per capsule
Capsule
  • Codeine 30 mg, acetaminophen 300 mg, butalbital 50 mg, caffeine 40 mg per capsule

Dosing

Tension headache (adults)
  • 1 - 2 capsules every 4 hours as needed
  • Do not exceed 6 capsules in 24 hours

Generic / Price

  • Generic (30 capsules) - $
  • NOTE: product with 300 mg of acetaminophen is $$$$

Other

  • DEA Schedule III
  • Butalbital is a barbiturate
  • CYP2D6 poor/rapid metabolizers - codeine has no analgesic activity until it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, codeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of codeine to morphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - codeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take codeine because it may cause somnolence and breathing issues in breastfed infants
  • Codeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase codeine exposure, and CYP3A4 inducers may decrease exposure. When combining codeine with an inhibitor, consider reducing the codeine dose and monitoring for toxicity. If an inhibitor is discontinued, the codeine dose may need to be increased. When combining codeine with an inducer, consider increasing the codeine dose and monitoring efficacy. If an inducer is discontinued, the codeine dose may need to be decreased.

Fiorinal® with codeine

Dosage forms

Capsule
  • Codeine 30 mg, aspirin 325 mg, butalbital 50 mg, caffeine 40 mg per capsule

Dosing

Tension headache (adults)
  • 1 - 2 capsules every 4 hours as needed
  • Do not exceed 6 capsules in 24 hours

Generic / Price

  • Generic (30 capsules) - $

Other

  • DEA Schedule III
  • Butalbital is a barbiturate
  • CYP2D6 poor/rapid metabolizers - codeine has no analgesic activity until it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, codeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of codeine to morphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - codeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take codeine because it may cause somnolence and breathing issues in breastfed infants
  • Codeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase codeine exposure, and CYP3A4 inducers may decrease exposure. When combining codeine with an inhibitor, consider reducing the codeine dose and monitoring for toxicity. If an inhibitor is discontinued, the codeine dose may need to be increased. When combining codeine with an inducer, consider increasing the codeine dose and monitoring efficacy. If an inducer is discontinued, the codeine dose may need to be decreased.

Soma® Compound with codeine

Dosage forms

Tablet
  • Codeine 16 mg, aspirin 325 mg, and carisoprodol 200 mg per tablet

Dosing

Acute, painful musculoskeletal conditions (adults)
  • 1 - 2 tablets four times daily as needed

Generic / Price

  • Generic (30 capsules) - $ - $$

Other

  • DEA Schedule III
  • Carisoprodol is a centrally-acting muscle relaxant. See carisoprodol for more.
  • CYP2D6 poor/rapid metabolizers - codeine has no analgesic activity until it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, codeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of codeine to morphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - codeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take codeine because it may cause somnolence and breathing issues in breastfed infants
  • Codeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase codeine exposure, and CYP3A4 inducers may decrease exposure. When combining codeine with an inhibitor, consider reducing the codeine dose and monitoring for toxicity. If an inhibitor is discontinued, the codeine dose may need to be increased. When combining codeine with an inducer, consider increasing the codeine dose and monitoring efficacy. If an inducer is discontinued, the codeine dose may need to be decreased.


Trezix® (dihydrocodeine)

Dosage forms

Capsule
  • Dihydrocodeine 16 mg, Caffeine 30 mg, Acetaminophen 320.5 mg per capsule

Dosing

Moderate to severe pain (adults)
  • 2 capsules every 4 hours as needed for pain
  • Do not exceed 10 capsules in 24 hours

Generic / Price

  • Generic (30 capsules) - $$

Other

  • DEA Schedule III
  • CYP2D6 poor/rapid metabolizers - dihydrocodeine has no analgesic activity until it is metabolized into dihydromorphine by CYP2D6. Poor metabolizers may not receive any pain relief from dihydrocodeine, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, dihydrocodeine is contraindicated in children less than 12 years old.
  • CYP2D6 inhibitors - CYP2D6 inhibitors can decrease the conversion of dihydrocodeine to dihydromorphine and reduce its analgesic effect. Avoid concomitant use.
  • Adolescents 12 - 18 years old with respiratory disease - dihydrocodeine is not recommended in adolescents who are obese or have conditions such as obstructive sleep apnea or severe lung disease
  • Nursing mothers - nursing mothers should not take dihydrocodeine because it may cause somnolence and breathing issues in breastfed infants
  • Dihydrocodeine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase dihydrocodeine exposure, and CYP3A4 inducers may decrease exposure. When combining dihydrocodeine with an inhibitor, consider reducing the dihydrocodeine dose and monitoring for toxicity. If an inhibitor is discontinued, the dihydrocodeine dose may need to be increased. When combining dihydrocodeine with an inducer, consider increasing the dihydrocodeine dose and monitoring efficacy. If an inducer is discontinued, the dihydrocodeine dose may need to be decreased.


Diphenoxylate | Lomotil® | Lonox®

Dosage forms

Tablet
  • Diphenoxylate 2.5 mg and atropine 0.025 mg per tablet
Solution
  • Diphenoxylate 2.5 mg and atropine 0.025 mg per 5 ml

Dosing

Diarrhea (adults)
  • Tablet - 2 tablets four times daily as needed
  • Liquid - 10 ml four times daily as needed
Diarrhea (children 2 - 13 years old)
  • Use liquid in children
  • 0.3 - 0.4 mg/kg/day (diphenoxylate component) given in 4 divided doses

Age (years) Weight (kg) Weight (pounds) Dose in milliliters
(4 times daily as needed)
2 11 - 14 24 - 31 1.5 - 3.0
3 12 - 16 26 - 35 2.0 - 3.0
4 14 - 20 31 - 44 2.0 - 4.0
5 16 - 23 35 - 51 2.5 - 4.5
6 - 8 17 - 32 38 - 71 2.5 - 5.0
9 - 12 23 - 55 51 - 121 3.5 - 5.0

Generic / Price

  • Generic (30 tablets or 120ml) - $

Other

  • DEA Schedule V
  • Atropine is added to discourage deliberate overdose. It has no effect in normal dosing.
  • Young children may be more susceptible to diphenoxylate and atropine side effects


Fentanyl (Actiq®)

Dosage forms

Lozenge
  • 200 mcg
  • 400 mcg
  • 600 mcg
  • 800 mcg
  • 1200 mcg
  • 1600 mcg

Dosing

Opioid-tolerant cancer patients
  • The Actiq PI (sec 2) contains a dose titration schedule
  • Fentanyl products are not recommended in opiate-naïve patients, and they should only be used in opiate-tolerant cancer patients for breakthrough pain
  • See opiate-tolerant definition for more

Generic / Price

  • Generic (30 lozenges) - $$$$

Other

  • DEA Schedule II
  • Providers and patients must enroll in the TIRF REMS Access program for outpatient use
  • Special lozenge disposal instructions are provided to prevent accidental exposures
  • Fentanyl may cause bradycardia. Use caution in susceptible patients.
  • Fentanyl is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase fentanyl exposure, and CYP3A4 inducers may decrease exposure. When combining fentanyl with an inhibitor, consider reducing the fentanyl dose and monitoring for toxicity. If an inhibitor is discontinued, the fentanyl dose may need to be increased. When combining fentanyl with an inducer, consider increasing the fentanyl dose and monitoring efficacy. If an inducer is discontinued, the fentanyl dose may need to be decreased.

Fentanyl (Duragesic®)

Dosage forms

Patch
  • 12 mcg/hour
  • 25 mcg/hour
  • 37.5 mcg/hour
  • 50 mcg/hour
  • 62.5 mcg/hour
  • 75 mcg/hour
  • 87.5 mcg/hour
  • 100 mcg/hour

Dosing

Opioid-tolerant cancer patients
  • The Duragesic PI (sec 2) contains an extensive table for converting from other opioids to fentanyl patch
  • Fentanyl products are not recommended in opiate-naïve patients, and they should only be used in opiate-tolerant cancer patients for breakthrough pain
  • See opiate-tolerant definition for more

Generic / Price

  • Generic available. Comes in carton with 5 patches.
  • 12 mcg/hr, 50 mcg/hr, 75 mcg/hr, 100 mcg/hr (10 patches) - $$-$$$
  • 25 mcg/hr (10 patches) - $
  • 37.5 mcg/hr, 62.5 mcg/hr, 87.5 mcg/hr (10 patches) - $$$$

Other

  • DEA Schedule II
  • Old patch is removed and new patch is applied every 72 hours. Apply new patch to different skin site.
  • Apply to chest, back, flank, or upper arm. Hair at application site may be clipped (not shaved).
  • Flush used patches down the toilet to prevent accidental exposure
  • Do not expose patch to direct heat because absorption may be increased
  • Patients with fever may absorb more fentanyl from the patch
  • Fentanyl may cause bradycardia. Use caution in susceptible patients.
  • Fentanyl is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase fentanyl exposure, and CYP3A4 inducers may decrease exposure. When combining fentanyl with an inhibitor, consider reducing the fentanyl dose and monitoring for toxicity. If an inhibitor is discontinued, the fentanyl dose may need to be increased. When combining fentanyl with an inducer, consider increasing the fentanyl dose and monitoring efficacy. If an inducer is discontinued, the fentanyl dose may need to be decreased.

Fentanyl (Fentora®)

Dosage forms

Buccal / sublingual tablet
  • 100 mcg
  • 200 mcg
  • 400 mcg
  • 600 mcg
  • 800 mcg
  • Comes in cartons containing 7 blister cards with 4 tablets per card

Dosing

Opioid-tolerant cancer patients
  • The Fentora PI (sec 2) contains a dose titration schedule
  • Fentanyl products are not recommended in opiate-naïve patients, and they should only be used in opiate-tolerant cancer patients for breakthrough pain
  • See opiate-tolerant definition for more

Generic / Price

  • Generic available
  • 30 tablets - $$$$

Other

  • DEA Schedule II
  • Providers and patients must enroll in the TIRF REMS Access program for outpatient use
  • Tablet can be placed above a rear molar, between the upper cheek and gum, or under the tongue
  • Special disposal instructions are provided to prevent accidental exposure
  • Fentanyl may cause bradycardia. Use caution in susceptible patients.
  • Fentanyl is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase fentanyl exposure, and CYP3A4 inducers may decrease exposure. When combining fentanyl with an inhibitor, consider reducing the fentanyl dose and monitoring for toxicity. If an inhibitor is discontinued, the fentanyl dose may need to be increased. When combining fentanyl with an inducer, consider increasing the fentanyl dose and monitoring efficacy. If an inducer is discontinued, the fentanyl dose may need to be decreased.

Fentanyl (Lazanda®)

Dosage forms

Nasal spray
  • 100 mcg/100 mcL
  • 400 mcg/100 mcL
  • Each bottle contains 8 sprays of 100 mcL

Dosing

Opioid-tolerant cancer patients
  • The Lazanda PI (sec 2) contains a dose titration schedule
  • Fentanyl products are not recommended in opiate-naïve patients, and they should only be used in opiate-tolerant cancer patients for breakthrough pain
  • See opiate-tolerant definition for more

Generic / Price

  • No generic
  • 1 bottle - $$$$

Other

  • DEA Schedule II
  • Providers and patients must enroll in the TIRF REMS Access program for outpatient use
  • Special disposal instructions are provided to prevent accidental exposure
  • Fentanyl may cause bradycardia. Use caution in susceptible patients.
  • Fentanyl is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase fentanyl exposure, and CYP3A4 inducers may decrease exposure. When combining fentanyl with an inhibitor, consider reducing the fentanyl dose and monitoring for toxicity. If an inhibitor is discontinued, the fentanyl dose may need to be increased. When combining fentanyl with an inducer, consider increasing the fentanyl dose and monitoring efficacy. If an inducer is discontinued, the fentanyl dose may need to be decreased.

Fentanyl (Subsys®)

Dosage forms

Sublingual spray
  • 100 mcg
  • 200 mcg
  • 400 mcg
  • 600 mcg
  • 800 mcg
  • 1200 mcg
  • 1600 mcg

Dosing

Opioid-tolerant cancer patients
  • The Subsys PI (sec 2) contains a dose titration schedule
  • Fentanyl products are not recommended in opiate-naïve patients, and they should only be used in opiate-tolerant cancer patients for breakthrough pain
  • See opiate-tolerant definition for more

Generic / Price

  • No generic. Comes in cartons of 10 and 30 sprays.
  • 30 sprays - $$$$

Other

  • DEA Schedule II
  • Providers and patients must enroll in the TIRF REMS Access program for outpatient use
  • Each dose comes in an individual sprayer
  • Special disposal instructions are provided to prevent accidental exposure
  • Fentanyl may cause bradycardia. Use caution in susceptible patients.
  • Fentanyl is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase fentanyl exposure, and CYP3A4 inducers may decrease exposure. When combining fentanyl with an inhibitor, consider reducing the fentanyl dose and monitoring for toxicity. If an inhibitor is discontinued, the fentanyl dose may need to be increased. When combining fentanyl with an inducer, consider increasing the fentanyl dose and monitoring efficacy. If an inducer is discontinued, the fentanyl dose may need to be decreased.


Hydrocodone - APAP | Vicodin® | Norco® | Lortab®

Dosage forms

Tablet
  • Hydrocodone : Acetaminophen
  • 2.5 mg : 325 mg
  • 5.0 mg : 325 mg
  • 7.5 mg : 325 mg
  • 10 mg : 325 mg
  • 5.0 mg : 300 mg
  • 7.5 mg : 300 mg
  • 10 mg : 300 mg
Solution
  • Hydrocodone 7.5 mg and acetaminophen 325 mg per 15ml

Dosing

Adults (opiate-naïve)
  • 5 - 10 mg every 4 - 6 hours as needed
  • Do not to exceed 50 mg a day
Children ≥ 2 years (opiate-naïve)
  • 0.135 mg/kg/dose every 4 - 6 hours as needed
  • Do not exceed 6 doses a day

  • *Based on 7.5 mg/15 ml solution
Weight (kg) Dose every 4 - 6 hours
12 - 15 1.875 mg (3.75 ml*)
16 - 22 2.5 mg (5 ml*)
23 - 31 3.75 mg (7.5 ml*)
32 - 45 5 mg (10 ml*)

Generic / Price

  • Hydrocodone/APAP tab #30 - $
  • Hydrocodone/APAP solution #240 ml - $

Other

  • DEA Schedule II
  • Duration of action: 3 - 5 hours
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Hydrocodone - Ibuprofen (Vicoprofen®)

Dosage forms

Tablet
  • Hydrocodone : Ibuprofen
    • 2.5 mg : 200 mg
    • 5.0 mg : 200 mg
    • 7.5 mg : 200 mg
    • 10 mg : 200 mg

Dosing

Adults (opiate-naïve)
  • 5 - 10 mg every 4 - 6 hours as needed
  • Do not to exceed 50 mg a day

Generic / Price

  • Generic available
  • Hydrocodone/Ibuprofen tab #30: $-$$

Other

  • DEA Schedule II
  • Duration of action: 3 - 5 hours
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Flowtuss®

Dosage forms

Solution
  • Hydrocodone 2.5 mg and guaifenesin 200 mg per 5 ml

Dosing

Cough (adults)
  • 10 ml every 4 - 6 hours as needed
  • Do not exceed 60 ml in 24 hours

Generic / Price

  • No generic
  • 120 ml - $$$

Other

  • DEA Schedule II
  • Guaifenesin is an expectorant
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Hycodan® syrup

Dosage forms

Syrup
  • Hydrocodone 5 mg and homatropine 1.5 mg per 5 ml

Dosing

Cough (adults)
  • 5 ml every 4 - 6 hours as needed
  • Do not exceed 30 ml in 24 hours
Cough (children 6 - 12 years)
  • 2.5 ml every 4 - 6 hours as needed
  • Do not exceed 15 ml in 24 hours
  • NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old

Generic / Price

  • Generic 120 ml - $

Other

  • DEA Schedule II
  • Homatropine is an anticholinergic medication that is included to discourage overdose
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Hycodan® tablets

Dosage forms

Tablet
  • Hydrocodone 5 mg and homatropine 1.5 mg per tablet

Dosing

Cough (adults)
  • 1 tablet every 4 - 6 hours as needed
  • Do not exceed 6 tablets in 24 hours
Cough (children 6 - 12 years)
  • One-half (1/2) tablet every 4 - 6 hours as needed
  • Do not exceed 3 tablets in 24 hours
  • NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old

Generic / Price

  • Generic 30 tablets - $

Other

  • DEA Schedule II
  • Homatropine is an anticholinergic medication that is included to discourage overdose
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Hycofenix®

Dosage forms

Solution
  • Hydrocodone 2.5 mg, pseudoephedrine 30 mg, and guaifenesin 200 mg per 5 ml

Dosing

Cough (adults)
  • 10 ml every 4 - 6 hours as needed
  • Do not exceed 40 ml in 24 hours

Generic / Price

  • No generic
  • 120 ml - $$$

Other

  • DEA Schedule II
  • Guaifenesin is an expectorant. Pseudoephedrine is a decongestant
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Obredon®

Dosage forms

Solution
  • Hydrocodone 2.5 mg and guaifenesin 200 mg per 5 ml

Dosing

Cough (adults)
  • 10 ml every 4 - 6 hours as needed
  • Do not exceed 60 ml in 24 hours

Generic / Price

  • No generic
  • 120 ml - $$$

Other

  • DEA Schedule II
  • Guaifenesin is an expectorant
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Rezira®

Dosage forms

Solution
  • Hydrocodone 5 mg and pseudoephedrine 60 mg per 5 ml

Dosing

Cough (adults)
  • 5 ml every 4 - 6 hours as needed
  • Do not exceed 20 ml in 24 hours

Generic / Price

  • No generic
  • 120 ml - $

Other

  • DEA Schedule II
  • Pseudoephedrine is a decongestant
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Tussicaps®

Dosage forms

Capsule, extended-release
  • Hydrocodone 5 mg and chlorpheniramine 4 mg per capsule
  • Hydrocodone 10 mg and chlorpheniramine 8 mg per capsule

Dosing

Cough (adults and children ≥ 12 years)
  • 1 capsule (hydrocodone 10 mg) every 12 hours as needed
  • Do not exceed 2 capsules in 24 hours
  • NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old
Cough (children 6 - 11 years)
  • 1 capsule (hydrocodone 5 mg) every 12 hours as needed
  • Do not exceed 2 capsules in 24 hours
  • Only hydrocodone 5 mg capsule should be used in this age group
  • NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old

Generic / Price

  • No generic
  • 30 capsules - $$$$

Other

  • DEA Schedule II
  • Chlorpheniramine is an antihistamine
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Tussionex®

Dosage forms

Suspension, extended-release
  • Hydrocodone 10 mg and chlorpheniramine 8 mg per 5 ml

Dosing

Cough (adults and adolescents ≥ 12 years)
  • 5 ml every 12 hours
  • Do not exceed 10 ml in 24 hours
  • NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old
Cough (children 6 - 11 years)
  • 2.5 ml every 12 hours
  • Do not exceed 5 ml in 24 hours
  • NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old

Generic / Price

  • Generic 120ml - $

Other

  • DEA Schedule II
  • Chlorpheniramine is an antihistamine
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Vituz®

Dosage forms

Solution
  • Hydrocodone 5 mg and chlorpheniramine 4 mg per 5 ml

Dosing

Cough (adults)
  • 5 ml every 4 - 6 hours as needed
  • Do not exceed 20 ml in 24 hours

Generic / Price

  • No generic
  • 120 ml - $

Other

  • DEA Schedule II
  • Chlorpheniramine is an antihistamine
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Zutripro®

Dosage forms

Solution
  • Hydrocodone 5 mg, chlorpheniramine 4 mg, pseudoephedrine 60 mg per 5 ml

Dosing

Cough (adults)
  • 5 ml every 4 - 6 hours as needed
  • Do not exceed 20 ml in 24 hours

Generic / Price

  • Generic (120 ml) - $-$$

Other

  • DEA Schedule II
  • Chlorpheniramine is an antihistamine. Pseudoephedrine is a decongestant.
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.

Hydrocodone (Hysingla® ER)

Dosage forms

Tablet, extended-release
  • 20 mg
  • 30 mg
  • 40 mg
  • 60 mg
  • 80 mg
  • 100 mg
  • 120 mg

Dosing

Adults (opiate-naïve)
  • 20 mg once daily
  • Increase dose by 10 - 20 mg every 3 - 5 days as needed
Converting other hydrocodone formulations to Hysingla
  • Total daily hydrocodone dose is given as once daily Hysingla dose
Converting from other opioids

Generic / Price

- YES/$$

Other

  • DEA Schedule II
  • Do not crush, cut, chew, or dissolve tablet
  • Abuse-deterrent properties - when tablet is crushed and mixed with water, it forms a gel that is difficult to pull through a needle
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.
  • QT prolongation has been observed in patients receiving Hysingla doses of ≥ 160 mg. Do not use Hysingla in patients with congenital long QT syndrome. If patients develop QT prolongation while taking Hysingla, consider reducing the dose by 33 - 50% or changing analgesics.

Hydrocodone (Zohydro® ER)

Dosage forms

Capsule, extended-release
  • 10 mg
  • 15 mg
  • 20 mg
  • 30 mg
  • 40 mg
  • 50 mg

Dosing

Adults (opiate-naïve)
  • 10 mg every 12 hours
  • Increase dose by 10 mg every 3 - 7 days as needed
Converting other HC formulations to Zohydro
  • Total daily hydrocodone dose is divided by 2 and given once every 12 hours
Converting from other opioids

Generic / Price

  • No generic
  • 30 capsules - $$$$

Other

  • DEA Schedule II
  • Do not crush, open, chew, or dissolve capsules
  • Hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase hydrocodone exposure, and CYP3A4 inducers may decrease exposure. When combining hydrocodone with an inhibitor, consider reducing the hydrocodone dose and monitoring for toxicity. If an inhibitor is discontinued, the hydrocodone dose may need to be increased. When combining hydrocodone with an inducer, consider increasing the hydrocodone dose and monitoring efficacy. If an inducer is discontinued, the hydrocodone dose may need to be decreased.
  • QT prolongation has been seen in patients receiving extended-release hydrocodone products. Use caution in at-risk patients.


Hydromorphone IR (Dilaudid®)

Dosage forms

Tablet
  • 2 mg
  • 4 mg
  • 8 mg
Solution
  • 5 mg/5 ml

Dosing

Adults (opiate-naïve)
  • 2 - 4 mg every 4 - 6 hours as needed
Children ≥ 6 months (opiate-naïve)
  • < 50 kg: 0.040 - 0.080 mg/kg every 3 - 4 hours as needed
  • ≥ 50 kg: 2 - 4 mg every 3 - 4 hours as needed [2]
Liver disease
  • Child-Pugh A/B: start with 25% - 50% of the usual dose; titrate slowly and monitor closely
  • Child-Pugh C: has not been studied
Kidney disease
  • Start with 25% - 50% of the usual dose, depending on the degree of impairment. Titrate slowly and monitor closely.

Generic / Price

  • Generic tablets (#30): $
  • Generic solution (200 ml): $

Other

  • DEA Schedule II
  • Solution and tablet are bioequivalent
  • Sulfite sensitivity - hydromorphone contains sulfites. Do not use in sulfite-sensitive patients.

Hydromorphone ER (Exalgo®)

Dosage forms

Tablet, extended-release
  • 8 mg
  • 12 mg
  • 16 mg
  • 32 mg

Dosing

Adults (opiate-naïve)
  • Not recommended
Converting from other oral hydromorphone products
  • Give total daily dose of hydromorphone as once daily Exalgo® dose
Converting from other opioids
Liver disease
  • Child-Pugh B: start with 25% of the usual dose; titrate slowly and monitor closely
  • Child-Pugh C: not recommended
Kidney disease
  • CrCl 30 - 60 ml/min: start with 50% of the usual dose; titrate slowly and monitor closely
  • CrCl < 30 ml/min: start with 25% of the usual dose; titrate slowly and monitor closely

Generic / Price

  • Generic (30 tablets): $$-$$$$

Other

  • DEA Schedule II
  • May take without regard to food
  • Do not crush, cut, or chew tablets
  • Sulfite sensitivity - hydromorphone contains sulfites. Do not use in sulfite-sensitive patients.


Meperidine hydrochloride (Demerol®)

Dosage forms

Tablet
  • 50 mg
  • 100 mg
Solution
  • 50 mg/5 ml

Dosing

Adults (opiate-naïve)
  • 50 - 150 mg every 3 - 4 hours as needed
Children ≥ 6 months
  • Standard
    • 1.1 - 1.8 mg/kg (max 150 mg/dose) every 3 - 4 hours as needed [dosing from package insert]
  • Alternative
    • < 50 kg: 2 - 3 mg/kg every 3 - 4 hours [5]
    • ≥ 50 kg: 100 - 150 mg every 3 - 4 hours [5]

Generic / Price

  • Generic (30 tablets) - $

Other

  • DEA Schedule II
  • Prolonged use of meperidine may cause accumulation of its metabolite, normeperidine. Normeperidine has been associated with an increased risk of seizures.
  • Meperidine should only be used for acute pain. It should not be used for chronic pain.
  • Serotonin syndrome - meperidine has serotonergic activity and may increase the risk of serotonin syndrome. Use caution in susceptible patients, particularly those who are taking other serotonergic drugs.
  • Supraventricular tachycardia (SVT) - meperidine may increase the ventricular response rate in patients with SVT. Use caution.
  • Meperidine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase meperidine exposure, and CYP3A4 inducers may decrease exposure. When combining meperidine with an inhibitor, consider reducing the meperidine dose and monitoring for toxicity. If an inhibitor is discontinued, the meperidine dose may need to be increased. When combining meperidine with an inducer, consider increasing the meperidine dose and monitoring efficacy. If an inducer is discontinued, the meperidine dose may need to be decreased.
  • Meperidine is a CYP2B6 sensitive substrate. CYP2B6 inhibitors may increase meperidine exposure, and CYP2B6 inducers may decrease exposure. When combining meperidine with an inhibitor, consider reducing the meperidine dose and monitoring for toxicity. If an inhibitor is discontinued, the meperidine dose may need to be increased. When combining meperidine with an inducer, consider increasing the meperidine dose and monitoring efficacy. If an inducer is discontinued, the meperidine dose may need to be decreased.
  • Acyclovir - acyclovir may increase meperidine exposure. Monitor patients for toxicity when combining and reduce the meperidine dose if necessary.

Methadone | Methadose® | Dolophine®

Dosage forms

Tablet
  • 5 mg
  • 10 mg
Dispersible tablet for suspension (Methadose®)
  • 40 mg
Solution
  • 5 mg/5 ml
  • 10 mg/5 ml
Concentrate (Methadose®)
  • 10 mg/1 ml

Dosing

Chronic pain, opiate-naïve (children 1 - 12 years)
  • 0.100 mg/kg (max 5 mg/dose) every 6 - 8 hours
  • Increase dose every 5 - 7 days [4]
  • May also be dosed every 12 hours
Chronic pain, opiate-naïve (adults)
  • 2.5 mg every 8 hours
  • Increase dose no more than 5 mg/day every 5 - 7 days [4]
  • May also be dosed every 12 hours
Opiate withdrawal and OUD treatment
Converting from other opiates to methadone (chronic pain)
  • See morphine milligram equivalent table
  • Patients taking < 40 – 60 mg/day of morphine or equivalent:
    • Start methadone 2.5 mg three times a day
    • Increase dose no more than 5 mg/day every 5 to 7 days
  • Patients taking > 60 mg/day of morphine or equivalent:
    • Start methadone therapy at a dose 75 to 90% less than the calculated equianalgesic dose and at no higher than 30 to 40 mg/day
    • Increases dose no more than 10 mg/day every 5 to 7 days [4]
Discontinuing methadone
  • Patients taking > 100 mg/day
    • Reduce dose by 5 mg/day down to 100 mg, then reduce by 3 mg/day to 0 mg
    • Based on PMID 26028120
  • Patients taking ≤ 100 mg/day

Generic / Price

  • Tablets (#90): YES/$
  • Solution (180 ml): YES/$
  • Concentrate (240 ml): YES/$

Other

  • DEA Schedule II
  • See methadone for side effects, precautions, drug interactions, and more


Morphine sulfate IR

Dosage forms

Tablet
  • 15 mg
  • 30 mg
Solution
  • 10 mg/5 ml
  • 20 mg/5 ml
  • 100 mg/5 ml

Dosing

Adults (opiate-naïve)
  • Tablet: 15 - 30 mg every 4 hours as needed
  • Solution: 10 - 20 mg every 4 hours as needed
Children 1 - 12 years (opiate-naïve)
  • Standard
    • 0.2 - 0.5 mg/kg every 4 hours as needed (max 5 mg) [2]
  • Alternative
    • < 50 kg: 0.3 mg/kg every 3 - 4 hours as needed [5]
    • ≥ 50 kg: 15 - 20 mg every 3 - 4 hours as needed [5]
Converting from parenteral to oral
  • Anywhere from 3 to 6 mg of oral morphine sulfate may be required to provide pain relief equivalent to 1 mg of parenteral morphine
  • In chronic dosing, 3 mg of oral morphine for every 1 mg of parenteral morphine may be sufficient [3]
Discontinuation
  • Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
  • Do not discontinue abruptly

Generic / Price

  • Generic (30 tablets or 120 ml) - $

Other

  • DEA Schedule II
  • Duration of action: 3 - 4 hours
  • P-glycoprotein inhibitors - morphine is a p-glycoprotein substrate, and p-glycoprotein inhibitors may increase its exposure. Monitor patients for toxicity when combining and decrease dose if necessary.

Morphine sulfate ER (Avinza®)

Dosage forms

Capsule, extended-release
  • 30 mg
  • 45 mg
  • 60 mg
  • 75 mg
  • 90 mg
  • 120 mg

Dosing

Adults (opiate-naïve)
  • 30 mg once daily
  • Increase in increments not greater than 30 mg every 4 days
Converting from other oral morphine meds
  • Total daily morphine dose can be given as once daily Avinza dose
Converting from parenteral morphine to oral
  • Anywhere from 3 to 6 mg of oral morphine sulfate may be required to provide pain relief equivalent to 1 mg of parenteral morphine
  • In chronic dosing, 3 mg of oral morphine for every 1 mg of parenteral morphine may be sufficient [3]
Discontinuation
  • Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
  • Do not discontinue abruptly

Generic / Price

  • Generic (30 capsules): $$$$

Other

  • DEA Schedule II
  • Avinza may be opened and sprinkled on applesauce. Swallow whole. Do not chew or crush beads.
  • Daily dose should not exceed 1600 mg because of fumaric acid content of drug
  • P-glycoprotein inhibitors - morphine is a p-glycoprotein substrate, and p-glycoprotein inhibitors may increase its exposure. Monitor patients for toxicity when combining and decrease dose if necessary.

Morphine sulfate ER (Kadian®)

Dosage forms

Capsule, extended-release
  • 10 mg
  • 20 mg
  • 30 mg
  • 40 mg
  • 50 mg
  • 60 mg
  • 80 mg
  • 100 mg

Dosing

Adults (opiate-naïve)
  • 30 mg once daily
  • Kadian daily dose may also be divided in half and given every 12 hours
  • Increase dose at intervals of every 1 - 2 days
Converting from other oral morphine meds
  • Total daily morphine dose can be given as once daily Kadian dose or divided by 2 and given every 12 hours
Converting from parenteral morphine to oral
  • Anywhere from 3 to 6 mg of oral morphine sulfate may be required to provide pain relief equivalent to 1 mg of parenteral morphine
  • In chronic dosing, 3 mg of oral morphine for every 1 mg of parenteral morphine may be sufficient [3]
Discontinuation
  • Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
  • Do not discontinue abruptly

Generic / Price

  • Generic (30 capsules) - $-$$$$ depending on strength

Other

  • DEA Schedule II
  • Kadian may be opened and sprinkled on applesauce. Swallow whole. Do not chew or crush beads.
  • P-glycoprotein inhibitors - morphine is a p-glycoprotein substrate, and p-glycoprotein inhibitors may increase its exposure. Monitor patients for toxicity when combining and decrease dose if necessary.

Morphine sulfate ER (MS Contin®)

Dosage forms

Tablet, extended-release
  • 15 mg
  • 30 mg
  • 60 mg
  • 100 mg
  • 200 mg

Dosing

Adults (opiate-naïve)
  • 15 mg every 12 hours
  • Increase dose at intervals of every 1 - 2 days
Children 1 - 12 years (opiate-naïve)
  • 0.2 - 0.8 mg/kg every 12 hours [2]
Converting from other oral morphine meds
  • Total daily morphine dose can be divided in half and given every 12 hours
  • Total daily morphine dose may also be divided into thirds and given every 8 hours
Converting from parenteral morphine to oral
  • Anywhere from 3 to 6 mg of oral morphine sulfate may be required to provide pain relief equivalent to 1 mg of parenteral morphine
  • In chronic dosing, 3 mg of oral morphine for every 1 mg of parenteral morphine may be sufficient [3]
Discontinuation
  • Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
  • Do not discontinue abruptly

Generic / Price

  • Generic (60 tablets) - $-$$$ depending on strength

Other

  • DEA Schedule II
  • Do not crush, cut, or chew tablets
  • P-glycoprotein inhibitors - morphine is a p-glycoprotein substrate, and p-glycoprotein inhibitors may increase its exposure. Monitor patients for toxicity when combining and decrease dose if necessary.


Methylnaltrexone (Relistor®)

Dosage forms

Tablet
  • 150 mg
Prefilled syringe
  • 8 mg/0.4 ml
  • 12 mg/0.6 ml
  • Comes in carton of 7 syringes
Single-dose vial
  • 12 mg/0.6 ml

Dosing

Opioid-induced constipation in patients with chronic non-cancer pain
  • Tablet: 450 mg once daily in the morning
  • Injection: 12 mg subcutaneously once daily
  • Tablets should be taken with water on an empty stomach at least 30 minutes before the first meal of the day
  • Kidney and liver disease - see Relistor PI for dosing
Opioid-induced constipation in patients with advanced illness
  • Only the injection is approved for advanced illness
  • Dosing is weight-based (see table)
  • Dose in given every other day as needed
  • Use single-dose vial for doses other than 8 and 12 mg
  • Kidney and liver disease - see Relistor PI for dosing

  • Give dose every other day as needed
Weight Dose
< 38 kg 0.15 mg/kg
38 to < 62 kg 8 mg
62 to 114 kg 12 mg
> 114 kg 0.15 mg/kg

Generic / Price

  • No generic
  • 28 syringes or 90 tablets - $$$$

Other

  • Injection is given in upper arm, abdomen, or thigh. Rotate injection sites.
  • Contraindicated in patients with GI obstruction and those at increased risk of obstruction
  • May increase risk of gastrointestinal perforation
  • Discontinue all laxatives before starting. Laxatives may be added after 3 days if response to Relistor is suboptimal

Mechanism of action

  • Methylnaltrexone is a selective antagonist of opioid binding at the mu-opioid receptor. As a quaternary amine, the ability of methylnaltrexone to cross the blood-brain barrier is restricted. This allows methylnaltrexone to function as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids without impacting opioid-mediated analgesic effects on the central nervous system (CNS).

Naloxegol (Movantik®)

Dosage forms

Tablet
  • 12.5 mg
  • 25 mg

Dosing

Opioid-induced constipation in patients with chronic non-cancer pain
  • Dosing: 25 mg once daily in the morning. Patients who cannot tolerate 25 mg may try 12.5 mg once daily.
  • Take on an empty stomach at least 1 hour prior to the first meal of the day or 2 hours after the meal
  • Kidney disease (CrCl < 60 ml/min: start with 12.5 mg once daily. If well tolerated, may increase to 25 mg once daily.
  • Strong CYP3A4 inhibitors: DO NOT COMBINE
  • Moderate CYP3A4 inhibitors: Not recommended. If must combine, use 12.5 mg once daily.

Generic / Price

  • No generic
  • 30 tablets - $$$$

Other

  • Tablet may be crushed and mixed with 120 ml of water
  • Contraindicated in patients with GI obstruction and those at increased risk of obstruction
  • May increase risk of gastrointestinal perforation
  • Discontinue all laxatives before starting. Laxatives may be added after 3 days if response to Movantik is suboptimal
  • Patients receiving opioids for less than 4 weeks may be less responsive

Mechanism of action

  • Naloxegol is an antagonist of opioid binding at the mu-opioid receptor. When administered at the recommended dose levels, naloxegol functions as a peripherally-acting mu-opioid receptor antagonist in tissues, such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids.
  • Naloxegol is a PEGylated derivative of naloxone and is a substrate for the P-glycoprotein transporter (P-gp). Also, the presence of the PEG moiety in naloxegol reduces its passive permeability as compared with naloxone. Due to the reduced permeability and increased efflux of naloxegol across the blood-brain barrier, related to P-gp substrate properties, the CNS penetration of naloxegol is expected to be negligible at the recommended dose levels limiting the potential for interference with centrally mediated opioid analgesia.

Naloxone injection

Dosage forms

Vial
  • 0.4 mg/ml
  • Comes in 1 ml single-dose vial and 10 ml multi-dose vial
Prefilled syringe
  • 1 mg/ml
  • Comes in 2 ml single-dose syringe

Dosing

Acute opiate overdose (adults)
  • May be given intravenously, intramuscularly, or subcutaneously
  • Give an initial dose of 0.4 - 2 mg. If the desired degree of counteraction and improvement in respiratory functions are not obtained, it may be repeated at two-to-three-minute intervals. If no response is observed after 10 mg of naloxone hydrochloride have been administered, the diagnosis of opioid-induced or partial opioid-induced toxicity should be questioned.
  • Seek immediate medical help. Naloxone may wear off and opiate-induced respiratory depression may return.
  • Reversal of partial agonists or mixed/antagonists such as buprenorphine and pentazocine may be incomplete and require higher doses
  • See who should carry naloxone below for recommendations on which patients should receive a prescription for naloxone

Generic / Price

  • Generic available
  • Syringes and vials - $

Pharmacokinetics

  • Time to max concentration: 15 minutes
  • Half-life: 1.36 hours

Mechanism of action

  • Naloxone hydrochloride is an opioid antagonist that antagonizes opioid effects by competing for the same receptor sites. Naloxone hydrochloride reverses the effects of opioids, including respiratory depression, sedation, and hypotension. Also, it can reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine.

Naloxone (Evzio®)

Dosage forms

Single-dose auto-injector
  • 2 mg
  • Comes in carton with 2 auto-injectors
  • Store at room temp

Dosing

Acute opioid overdose (adult and pediatric patients)
  • Dosing for adults and pediatric patients is the same
  • When activated, auto-injector gives voice instructions
  • Place the patient in the supine position (on back with face-up)
  • Inject intramuscularly or subcutaneously into the anterolateral aspect of the thigh. Inject through clothing if necessary. After injection, place the patient in the lateral recumbent position (lying on their side).
  • If the desired response is not obtained after 2 or 3 minutes, an additional dose may be administered. If there is still no response or the patient relapses back into respiratory depression, additional doses may be administered every 2 to 3 minutes until emergency medical assistance arrives.
  • Overdoses from partial agonists or mixed agonist/antagonists, such as buprenorphine and pentazocine, may require higher and/or more frequent doses
  • Patients < 1 year of age: in pediatric patients under the age of one year, the caregiver should pinch the thigh muscle while administering the dose. Carefully observe the administration site for signs of infection following resolution of the opioid emergency.
  • See who should carry naloxone below for recommendations on which patients should receive a prescription for naloxone

Generic / Price

  • Generic available
  • Carton of 2 auto-injectors - $$$

Pharmacokinetics

  • Time to max concentration: 15 minutes
  • Half-life 1.5 hours

Mechanism of action

  • Naloxone hydrochloride is an opioid antagonist that antagonizes opioid effects by competing for the same receptor sites. Administration of naloxone hydrochloride reverses the effects of opioids, including respiratory depression, sedation and hypotension. It can also reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine.

Naloxone (Zimhi®)

Dosage forms

Single-dose prefilled syringe
  • 5 mg/0.5 ml
  • Comes in carton with 2 syringes
  • Store at room temp

Dosing

Acute opioid overdose (adult and pediatric patients)
  • Dosing for adults and pediatric patients is the same
  • Place the patient in the supine position (on back with face-up)
  • Inject intramuscularly or subcutaneously into the anterolateral aspect of the thigh. Inject through clothing if necessary. After injection, place the patient in the lateral recumbent position (lying on their side).
  • If the desired response is not obtained after 2 or 3 minutes, an additional dose may be administered. If there is still no response or the patient relapses back into respiratory depression, additional doses may be administered every 2 to 3 minutes until emergency medical assistance arrives.
  • Overdoses from partial agonists or mixed agonist/antagonists, such as buprenorphine and pentazocine, may require higher and/or more frequent doses
  • Patients < 1 year of age: In pediatric patients under the age of one year, the caregiver should pinch the thigh muscle while administering Zimhi. Carefully observe the administration site for signs of infection following resolution of the opioid emergency.
  • See who should carry naloxone below for recommendations on which patients should receive a prescription for naloxone

Generic / Price

  • No generic
  • Carton of 2 syringes - $$$

Pharmacokinetics

  • Time to max concentration (intramuscular): 15 minutes
  • Half-life 1.5 hours

Mechanism of action

  • Naloxone hydrochloride is an opioid antagonist that antagonizes opioid effects by competing for the same receptor sites. Administration of naloxone hydrochloride reverses the effects of opioids, including respiratory depression, sedation and hypotension. It can also reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine.

Naloxone (Narcan®)

Dosage forms

Nasal spray
  • 4 mg single-use spray
  • Comes in a carton with 2 single-use sprays

Dosing

Acute opiate overdose (adult and pediatric patients)
  • Dosing for adults and pediatric patients is the same
  • Place patient on their back and provide support to the back of the neck to allow the head to tilt back before giving. Administer one spray in one nostril. Place patient on their side after giving.
  • May give an additional spray every 2 - 3 minutes depending on response. Alternate nostrils. Each spray device only provides one dose.
  • Seek immediate medical help. Naloxone may wear off and opiate-induced respiratory depression may return.
  • Reversal of partial agonists or mixed agonist/antagonists such as buprenorphine and pentazocine may be incomplete and require higher doses
  • See who should carry naloxone below for recommendations on which patients should receive a prescription for naloxone

Generic / Price

  • Generic available
  • Carton of 2 sprays - $-$$

Pharmacokinetics

  • Time to max concentration:
    • One spray (4 mg): 30 minutes
    • Two sprays (8 mg): 20 minutes
  • Half-life: 1.85 hours

Mechanism of action

  • Naloxone hydrochloride is an opioid antagonist that antagonizes opioid effects by competing for the same receptor sites. Naloxone hydrochloride reverses the effects of opioids, including respiratory depression, sedation, and hypotension. It can also reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine.

Naloxone (Kloxxado®)

Dosage forms

Nasal spray
  • 8 mg single-use spray
  • Comes in a carton with 2 single-use sprays

Dosing

Acute opiate overdose (adult and pediatric patients)
  • Dosing for adults and pediatric patients is the same
  • Place patient on their back and provide support to the back of the neck to allow the head to tilt back before giving. Administer one spray in one nostril. Place patient on their side after giving.
  • May give an additional spray every 2 - 3 minutes depending on response. Alternate nostrils. Each spray device only provides one dose.
  • Seek immediate medical help. Naloxone may wear off and opiate-induced respiratory depression may return.
  • Reversal of partial agonists or mixed agonist/antagonists such as buprenorphine and pentazocine may be incomplete and require higher doses
  • See who should carry naloxone below for recommendations on which patients should receive a prescription for naloxone

Generic / Price

  • No generic
  • Carton of 2 sprays - $$$

Pharmacokinetics

  • Time to max concentration: 15 minutes
  • Half-life 1.8 hours

Mechanism of action

  • Naloxone hydrochloride is an opioid antagonist that antagonizes opioid effects by competing for the same receptor sites. Administration of naloxone hydrochloride reverses the effects of opioids, including respiratory depression, sedation and hypotension. It can also reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine.

Naltrexone (Revia®)

Dosage forms

Tablet
  • 50 mg

Dosing

Alcohol use disorder
OUD maintenance therapy

Generic / Price

  • Generic (30 tablets): $

Naltrexone (Vivitrol®)

Dosage forms

Injectable suspension
  • 380 mg vial
  • Carton comes with vial, diluent, special needle and syringe

Dosing

Alcohol use disorder
OUD maintenance therapy

Generic / Price

  • No generic
  • One injection - $$$$

Efficacy

Methamphetamine abuse Opiate abuse

Naldemedine (Symproic®)

Dosage forms

Tablet
  • 0.2 mg

Dosing

Treatment of opioid-induced constipation
  • 0.2 mg once daily
  • Patients receiving opioids for less than 4 weeks may be less responsive
  • May take with or without food
  • Naldemedine is a CYP3A4 sensitive substrate. Do not use with strong CYP3A4 inducers, and monitor for adverse reactions when combining with moderate or strong CYP3A4 inhibitors.
  • Naldemedine is a P-glycoprotein substrate. Monitor for adverse reactions when combining with P-glycoprotein inhibitors.

Generic / Price

  • No generic
  • Tablets (#30) - $$$$

Efficacy

Opioid-induced constipation

Other

  • Contraindicated in patients with GI obstruction and those at increased risk of obstruction
  • May increase risk of gastrointestinal perforation
  • Cases of opioid withdrawal have been reported, and patients with disruptions of the blood-brain barrier may be at greater risk
  • Side effects include abdominal pain (8%), diarrhea (7%), and nausea (4%)

Mechanism of action

  • Naldemedine is an opioid antagonist with binding affinities for mu-, delta-, and kappa-opioid receptors. Naldemedine functions as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids.
  • Naldemedine is a derivative of naltrexone to which a side chain has been added that increases the molecular weight and the polar surface area, thereby reducing its ability to cross the blood-brain barrier (BBB). Naldemedine is also a substrate of the P-glycoprotein (P-gp) efflux transporter. Based on these properties, the CNS penetration of naldemedine is expected to be negligible at the recommended dose levels, limiting the potential for interference with centrally-mediated opioid analgesia.


Oxycodone IR (Roxicodone®)

Dosage forms

Tablet
  • 5 mg
  • 10 mg
  • 15 mg
  • 20 mg
  • 30 mg
Capsule
  • 5 mg
Solution
  • 5 mg/5 ml
  • 100 mg/5 ml

Dosing

Adults (opiate-naïve)
  • 5 - 15 mg every 4 - 6 hours as needed
  • Do not exceed 60 mg in 24 hours
Children 1 - 12 years (opiate-naïve)
  • 0.125 - 0.200 mg/kg every 4 hours as needed (max 5 mg/dose) [2]
Discontinuing therapy
  • If patients have been taking regularly, taper the dose gradually, by 25% to 50% every 2 to 4 days and monitor for withdrawal symptoms

Generic / Price

  • Generic solution (120 ml) - $
  • Generic capsules/tablets (#30) - $

Other

  • DEA Schedule II
  • Duration of action: 3 - 5 hours
  • Liver disease - oxycodone clearance is decreased in mild-to-moderate liver disease by as much as 50%. Initiate dosing at lower than usual doses (1/3 to 1/2) and titrate slowly.
  • Kidney disease - oxycodone clearance is decreased in moderate kidney disease (CrCl < 60 ml/min) by as much as 50%. Initiate dosing at lower than usual doses and titrate slowly.
  • Oxycodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase oxycodone exposure, and CYP3A4 inducers may decrease exposure. When combining oxycodone with an inhibitor, consider reducing the oxycodone dose and monitoring for toxicity. If an inhibitor is discontinued, the oxycodone dose may need to be increased. When combining oxycodone with an inducer, consider increasing the oxycodone dose and monitoring efficacy. If an inducer is discontinued, the oxycodone dose may need to be decreased.
  • Oxycodone is partially metabolized by CYP2D6. If CYP2D6 inhibitors are taken with CYP3A4 inhibitors, the increase in oxycodone exposure may be potentiated.

Oxycodone - APAP IR | Percocet® | Roxicet®

Dosage forms

Tablet
  • Oxycodone : Acetaminophen
  • 2.5 mg: 325 mg
  • 5.0 mg: 325 mg
  • 7.5 mg: 325 mg
  • 10 mg: 325 mg
  • 2.5 mg: 300 mg
  • 5.0 mg: 300 mg
  • 7.5 mg: 300 mg
  • 10 mg: 300 mg
Solution
  • Oxycodone 5 mg and acetaminophen 325 mg per 5 ml

Dosing

Adults (opiate-naïve)
  • 2.5 - 5 mg every 6 hours as needed
  • Do not exceed 60 mg of oxycodone in 24 hours
  • Do not exceed 4000 mg of acetaminophen in 24 hours
Discontinuing therapy
  • If patients have been taking regularly, taper the dose gradually, by 25% to 50% every 2 to 4 days and monitor for withdrawal symptoms

Generic / Price

  • Generic tablets (#30), solution (120ml) - $

Other

  • DEA Schedule II
  • Duration of action: 3 - 5 hours
  • Liver disease - oxycodone clearance is decreased in mild-to-moderate liver disease by as much as 50%. Initiate dosing at lower than usual doses (1/3 to 1/2) and titrate slowly.
  • Kidney disease - oxycodone clearance is decreased in moderate kidney disease (CrCl < 60 ml/min) by as much as 50%. Initiate dosing at lower than usual doses and titrate slowly.
  • Oxycodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase oxycodone exposure, and CYP3A4 inducers may decrease exposure. When combining oxycodone with an inhibitor, consider reducing the oxycodone dose and monitoring for toxicity. If an inhibitor is discontinued, the oxycodone dose may need to be increased. When combining oxycodone with an inducer, consider increasing the oxycodone dose and monitoring efficacy. If an inducer is discontinued, the oxycodone dose may need to be decreased.
  • Oxycodone is partially metabolized by CYP2D6. If CYP2D6 inhibitors are taken with CYP3A4 inhibitors, the increase in oxycodone exposure may be potentiated.

Oxycodone - Aspirin IR (Percodan®)

Dosage forms

Tablet
  • Oxycodone : Aspirin
    • 4.8355 mg : 325 mg

Dosing

Adults (opiate-naïve)
  • One tablet every 6 hours as needed
  • Do not exceed 60 mg of oxycodone in 24 hours
  • Do not exceed 4000 mg of aspirin in 24 hours
Discontinuing therapy
  • If patients have been taking regularly, taper the dose gradually, by 25% to 50% every 2 to 4 days and monitor for withdrawal symptoms

Generic / Price

  • Generic tablets (#30) - $

Other

  • DEA Schedule II
  • Duration of action: 3 - 5 hours
  • Liver disease - oxycodone clearance is decreased in mild-to-moderate liver disease by as much as 50%. Initiate dosing at lower than usual doses (1/3 to 1/2) and titrate slowly.
  • Kidney disease - oxycodone clearance is decreased in moderate kidney disease (CrCl < 60 ml/min) by as much as 50%. Initiate dosing at lower than usual doses and titrate slowly.
  • Oxycodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase oxycodone exposure, and CYP3A4 inducers may decrease exposure. When combining oxycodone with an inhibitor, consider reducing the oxycodone dose and monitoring for toxicity. If an inhibitor is discontinued, the oxycodone dose may need to be increased. When combining oxycodone with an inducer, consider increasing the oxycodone dose and monitoring efficacy. If an inducer is discontinued, the oxycodone dose may need to be decreased.
  • Oxycodone is partially metabolized by CYP2D6. If CYP2D6 inhibitors are taken with CYP3A4 inhibitors, the increase in oxycodone exposure may be potentiated.

Oxycodone - Ibuprofen IR

Dosage forms

Tablet
  • Oxycodone : Ibuprofen
    • 5 mg : 400 mg

Dosing

Adults (opiate-naïve)
  • 5 mg every 6 hours as needed
  • Do not exceed 4 tablets in 24 hours
Discontinuing therapy
  • If patients have been taking regularly, taper the dose gradually, by 25% to 50% every 2 to 4 days and monitor for withdrawal symptoms

Generic / Price

  • Generic tablets (#30) - $

Other

  • DEA Schedule II
  • Duration of action: 3 - 5 hours
  • Liver disease - oxycodone clearance is decreased in mild-to-moderate liver disease by as much as 50%. Initiate dosing at lower than usual doses (1/3 to 1/2) and titrate slowly.
  • Kidney disease - oxycodone clearance is decreased in moderate kidney disease (CrCl < 60 ml/min) by as much as 50%. Initiate dosing at lower than usual doses and titrate slowly.
  • Oxycodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase oxycodone exposure, and CYP3A4 inducers may decrease exposure. When combining oxycodone with an inhibitor, consider reducing the oxycodone dose and monitoring for toxicity. If an inhibitor is discontinued, the oxycodone dose may need to be increased. When combining oxycodone with an inducer, consider increasing the oxycodone dose and monitoring efficacy. If an inducer is discontinued, the oxycodone dose may need to be decreased.
  • Oxycodone is partially metabolized by CYP2D6. If CYP2D6 inhibitors are taken with CYP3A4 inhibitors, the increase in oxycodone exposure may be potentiated.

Oxycodone IR (Oxaydo®)

Dosage forms

Tablet
  • 5 mg
  • 7.5 mg

Dosing

Adults (opiate-naïve)
  • 5 - 15 mg every 4 - 6 hours as needed
  • Do not exceed 60 mg in 24 hours
Discontinuing therapy
  • If patients have been taking regularly, taper the dose gradually, by 25% to 50% every 2 to 4 days and monitor for withdrawal symptoms

Generic / Price

  • No generic
  • Tablets (#30) - $$$$

Other

  • DEA Schedule II
  • Duration of action: 3 - 4 hours
  • Liver disease - oxycodone clearance is decreased in mild-to-moderate liver disease by as much as 50%. Initiate dosing at lower than usual doses (1/3 to 1/2) and titrate slowly.
  • Kidney disease - oxycodone clearance is decreased in moderate kidney disease (CrCl < 60 ml/min) by as much as 50%. Initiate dosing at lower than usual doses and titrate slowly.
  • Oxycodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase oxycodone exposure, and CYP3A4 inducers may decrease exposure. When combining oxycodone with an inhibitor, consider reducing the oxycodone dose and monitoring for toxicity. If an inhibitor is discontinued, the oxycodone dose may need to be increased. When combining oxycodone with an inducer, consider increasing the oxycodone dose and monitoring efficacy. If an inducer is discontinued, the oxycodone dose may need to be decreased.
  • Oxycodone is partially metabolized by CYP2D6. If CYP2D6 inhibitors are taken with CYP3A4 inhibitors, the increase in oxycodone exposure may be potentiated.

Oxycodone ER (Oxycontin®)

Dosage forms

Tablet, extended-release
  • 10 mg
  • 15 mg
  • 20 mg
  • 30 mg
  • 40 mg
  • 60 mg
  • 80 mg

Dosing

Adults (opiate-naïve)
  • 10 mg every 12 hours
  • Increase dose every 1 - 2 days in increments of 25 - 50% of the current dose
Children ≥ 11 years
  • Opiate-naïve
    • Not recommended
  • Opiate-tolerant
    • Patients must be receiving opioids for at least 5 consecutive days
    • Patients must be receiving ≥ 20 mg/day of oxycodone or its equivalent for the 2 days prior to starting
    • See Oxycontin PI sec 2.4 for dose conversion table from other opioids
Converting from other oxycodone products
  • Total daily oxycodone dose can be divided in half and given every 12 hours
Discontinuing therapy
  • Taper the dose gradually, by 25% to 50% every 2 to 4 days and monitor for withdrawal symptoms

Generic / Price

  • Generic (30 tablets) - $-$$$$, depending on the strength

Other

  • DEA Schedule II
  • Abuse-deterrent properties - when tablet is crushed and mixed with water, it forms a gel that is difficult to pull through a needle
  • Liver disease - oxycodone clearance is decreased in mild-to-moderate liver disease by as much as 50%. Initiate dosing at lower than usual doses (1/3 to 1/2) and titrate slowly.
  • Kidney disease - oxycodone clearance is decreased in moderate kidney disease (CrCl < 60 ml/min) by as much as 50%. Initiate dosing at lower than usual doses and titrate slowly.
  • Oxycodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase oxycodone exposure, and CYP3A4 inducers may decrease exposure. When combining oxycodone with an inhibitor, consider reducing the oxycodone dose and monitoring for toxicity. If an inhibitor is discontinued, the oxycodone dose may need to be increased. When combining oxycodone with an inducer, consider increasing the oxycodone dose and monitoring efficacy. If an inducer is discontinued, the oxycodone dose may need to be decreased.
  • Oxycodone is partially metabolized by CYP2D6. If CYP2D6 inhibitors are taken with CYP3A4 inhibitors, the increase in oxycodone exposure may be potentiated.

Oxycodone ER (Xtampza® ER)

Dosage forms

Capsule, extended-release
  • 9 mg (equivalent to 10 mg oxycodone)
  • 13.5 mg (equivalent to 15 mg oxycodone)
  • 18 mg (equivalent to 20 mg oxycodone)
  • 27 mg (equivalent to 30 mg oxycodone)
  • 36 mg (equivalent to 40 mg oxycodone)

Dosing

Adults (opiate-naïve)
  • Starting dose is 9 mg every 12 hours with food
  • Increase dose every 1 - 2 days in increments of 25 - 50% of the current dose
  • Maximum daily dose is 288 mg/day
Converting from other oxycodone meds
  • Total daily oxycodone dose can be divided in half and given every 12 hours
Discontinuing therapy
  • Taper the dose gradually, by 25% to 50% every 2 to 4 days and monitor for withdrawal symptoms

Generic / Price

  • No generic
  • Capsules (#30) - $$$-$$$$, depending on the strength

Other

  • DEA Schedule II
  • Each dose of Xtampza should be taken with approximately the same amount of food in order to ensure consistent plasma levels are achieved. Food increases absorption, and absorption is higher with high-fat, high-calorie foods.
  • Capsules may be opened and sprinkled on a small amount of soft food (e.g. applesauce, pudding). Swallow whole and do not chew. Rinse mouth.
  • Contents of capsule may be given through feeding tube
  • Abuse-deterrent properties - microspheres are difficult to manipulate for misuse and abuse
  • Liver disease - oxycodone clearance is decreased in mild-to-moderate liver disease by as much as 50%. Initiate dosing at lower than usual doses (1/3 to 1/2) and titrate slowly.
  • Kidney disease - oxycodone clearance is decreased in moderate kidney disease (CrCl < 60 ml/min) by as much as 50%. Initiate dosing at lower than usual doses and titrate slowly.
  • Oxycodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase oxycodone exposure, and CYP3A4 inducers may decrease exposure. When combining oxycodone with an inhibitor, consider reducing the oxycodone dose and monitoring for toxicity. If an inhibitor is discontinued, the oxycodone dose may need to be increased. When combining oxycodone with an inducer, consider increasing the oxycodone dose and monitoring efficacy. If an inducer is discontinued, the oxycodone dose may need to be decreased.
  • Oxycodone is partially metabolized by CYP2D6. If CYP2D6 inhibitors are taken with CYP3A4 inhibitors, the increase in oxycodone exposure may be potentiated.


Oxymorphone IR (Opana®)

Dosage forms

Tablet
  • 5 mg
  • 10 mg

Dosing

Adults (opiate-naïve)
  • 10 - 20 mg every 4 - 6 hours as needed
  • Take on an empty stomach, at least one hour prior to or two hours after eating
  • Kidney disease (CrCl < 50 ml/min): Use caution. Start with 5 mg dose.
  • Liver disease (Child-Pugh A): Use caution. Start with 5 mg dose.
  • Liver disease (Child-Pugh B/C): DO NOT USE
Converting from parenteral oxymorphone
  • Given Opana’s absolute oral bioavailability of approximately 10%, patients receiving parenteral oxymorphone may be converted to oral Opana by administering 10 times the patient’s total daily parenteral oxymorphone dose as Opana, in four or six equally divided doses (e.g., [IV dose x 10] divided by 4 or 6)
  • For example, approximately 10 mg of Opana four times daily may be required to provide pain relief equivalent to a total daily IM dose of 4 mg oxymorphone
Discontinuation
  • Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
  • Do not discontinue abruptly

Generic / Price

  • Generic (30 tablets) - $$

Other

  • DEA Schedule II
  • Half-life: 9 - 11 hours

Oxymorphone ER (Opana® ER)

Dosage forms

Tablet, extended-release
  • 5 mg
  • 7.5 mg
  • 10 mg
  • 15 mg
  • 20 mg
  • 30 mg
  • 40 mg

Dosing

Adults (opiate-naïve)
  • 5 mg every 12 hours
  • Adjust dose in increments of 5 - 10 mg every 12 hours, every 3 to 7 days
  • Take on an empty stomach, at least one hour prior to or two hours after eating
  • Kidney disease (CrCl < 50 ml/min): Use caution. Start with 5 mg dose. For patients on prior opioid therapy, start Opana ER at 50% lower than the starting dose for a patient with normal renal function.
  • Liver disease (Child-Pugh A): Use caution. Start with 5 mg dose. For patients on prior opioid therapy, start Opana ER at 50% lower than the starting dose for a patient with normal hepatic function.
  • Liver disease (Child-Pugh B/C): DO NOT USE
Converting from Opana® to Opana® ER
  • Total daily dose remains the same. Administer half the total daily Opana dose as Opana ER, every 12 hours.
Converting from parenteral oxymorphone
  • The absolute oral bioavailability of Opana ER is approximately 10%. Convert patients receiving parenteral oxymorphone to Opana ER by administering 10 times the patient's total daily parenteral oxymorphone dose as Opana ER in two equally divided doses (e.g., [IV dose x 10] divided by 2).
Converting from other opioids to Opana ER
Discontinuation
  • Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
  • Do not discontinue abruptly

Generic / Price

  • No generic
  • 60 tablets - $$-$$$$, depending on strength

Other

  • DEA Schedule II
  • Do not crush, cut, chew, or dissolve tablets


Pentazocine + Naloxone (Talwin NX®)

Dosage forms

Tablet
  • Pentazocine 50 mg and naloxone 0.5 mg per tablet

Dosing

Adults
  • One tablet every 3 - 4 hours
  • May increase to 2 tablets when needed
  • Do not exceed 12 tablets in 24 hours

Generic / Price

  • Generic (30 tablets) - $

Other

  • DEA Schedule IV
  • Pentazocine is an opioid agonist/antagonist
  • Pentazocine may antagonize the effects of stronger opiates (e.g. morphine, methadone)
  • Pentazocine 50 mg is equivalent in analgesic activity to 60 mg of codeine
  • Naloxone is an opioid antagonist. It has no effect when taken orally, but acts as an opioid antagonist when injected.


Tapentadol IR (Nucynta®)

Dosage forms

Tablet
  • 50 mg
  • 75 mg
  • 100 mg

Dosing

Adults (opiate-naïve)
  • 50 - 100 mg every 4 - 6 hours as needed
  • On the first day of dosing, the second dose may be administered as soon as one hour after the first dose if adequate pain relief is not attained with the first dose. Subsequent dosing is 50 mg, 75 mg, or 100 mg every 4 to 6 hours and should be adjusted to maintain adequate analgesia with acceptable tolerability.
  • Do not exceed 700 mg on the first day of therapy, and do not exceed 600 mg/day on subsequent days
Discontinuation
  • Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
  • Do not discontinue abruptly

Generic / Price

  • No generic
  • 30 tablets - $$$$

Other

  • DEA Schedule II
  • Tapentadol is a centrally-acting synthetic analgesic. Although its exact mechanism is unknown, analgesic efficacy is thought to be due to mu-opioid agonist activity and the inhibition of norepinephrine reuptake.
  • The minimum effective plasma concentration of tapentadol for analgesia varies widely among patients
  • Tapentadol should not be consumed with alcohol. Alcohol increases blood levels and can lead to overdose.

Tapentadol ER (Nucynta® ER)

Dosage forms

Tablet, extended-release
  • 50 mg
  • 100 mg
  • 150 mg
  • 200 mg
  • 250 mg

Dosing

Adults (opiate-naïve)
  • 50 mg every 12 hours
  • Increase dose in increments of 50 mg at intervals of ≥ 3 days
  • Do not exceed 500 mg/day
Converting from Nucynta® to Nucynta® ER
  • Total daily dose of Nucynta® can be divided in half and given every 12 hours as Nucynta® ER
  • Do not exceed 500 mg/day of Nucynta® ER
Discontinuation
  • Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
  • Do not discontinue abruptly

Generic / Price

  • No generic
  • 60 tablets - $$$$

Other

  • DEA Schedule II
  • Do not crush, cut, chew, or dissolve tablets
  • Tapentadol is a centrally-acting synthetic analgesic. Although its exact mechanism is unknown, analgesic efficacy is thought to be due to mu-opioid agonist activity and the inhibition of norepinephrine reuptake.
  • The minimum effective plasma concentration of tapentadol for analgesia varies widely among patients
  • Tapentadol should not be consumed with alcohol. Alcohol increases blood levels and can lead to overdose.


Tramadol IR | Ultram® | Qdolo®

Dosage forms

Tablet (Ultram®)
  • 50 mg
Solution (Qdolo®)
  • 5 mg/ml
  • Comes in 473 ml bottle
  • Store at room temperature

Dosing

Pain not requiring rapid analgesia (adults)
  • Start with 25 mg/day and titrate in 25 mg increments as separate doses every 3 days to reach 100 mg/day (25 mg four times a day). Thereafter the total daily dose may be increased by 50 mg as tolerated every 3 days to reach 200 mg/day (50 mg four times a day).
  • Do not exceed 300 mg/day in patients > 75 years old
  • Do not exceed 400 mg in 24 hours
Pain requiring rapid analgesia (adults)
  • 50 - 100 mg every 4 - 6 hours as needed
  • Do not exceed 300 mg/day in patients > 75 years old
  • Do not exceed 400 mg in 24 hours
Liver disease
  • Child-Pugh C: recommended dose in 50 mg every 12 hours
Kidney disease
  • CrCl < 30 ml/min: increase dosing interval to every 12 hours; max dose is 200 mg/day

Generic / Price

  • Tablets (#30) - YES/$
  • Solution (250 ml) - NO/$$$$

Other

  • DEA Schedule IV
  • Tablets are scored so they can be halved
  • Patients who are allergic to opiates should not receive tramadol
  • Tramadol is a synthetic opioid that acts at opiate receptors in the central nervous system
  • Tramadol has been shown to inhibit reuptake of norepinephrine and serotonin. Use caution when combining with other serotonergic drugs (see serotonin syndrome).
  • CYP2D6 poor/rapid metabolizers - CYP2D6 metabolizes tramadol to an active metabolite (M1) that has more potent opioid activity than the parent compound. Poor CYP2D6 metabolizers may not receive as much pain relief from tramadol, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, tramadol is contraindicated in children under 12 years old and those 12 to 18 years old with respiratory conditions.
  • CYP2D6 inhibitors - concomitant CYP2D6 inhibitors may decrease the conversion of tramadol to its active metabolite and reduce its analgesic effect. Conversely, stopping CYP2D6 inhibitors may increase levels of the active metabolite. Consider the effects of starting and stopping CYP2D6 inhibitors on the efficacy and toxicity of tramadol and make appropriate dose adjustments.
  • Tramadol is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase tramadol exposure, and CYP3A4 inducers may decrease exposure. When combining tramadol with an inhibitor, consider reducing the tramadol dose and monitoring for toxicity. If an inhibitor is discontinued, the tramadol dose may need to be increased. When combining tramadol with an inducer, consider increasing the tramadol dose and monitoring efficacy. If an inducer is discontinued, the tramadol dose may need to be decreased.
  • Nursing mothers - Not recommended. May cause somnolence and breathing issues in breastfed infants.
  • Hyponatremia - hyponatremia, including severe cases (< 120 mEq/L), has occurred in patients receiving tramadol. In some patients, the cause was determined to be the syndrome of inappropriate antidiuretic hormone secretion (SIADH). If symptoms of hyponatremia develop (e.g. headache, fatigue, nausea, vomiting), or if significant hyponatremia is noted on lab work, tramadol should be discontinued.
  • Hypoglycemia - hypoglycemia, including severe cases requiring hospitalization, has been reported in patients receiving tramadol. Patients with risk factors (e.g. diabetes medications) may be at greater risk. If unexplained and/or dangerous hypoglycemia occurs, consider stopping tramadol.

Tramadol - APAP IR (Ultracet®)

Dosage forms

Tablet
  • Tramadol 37.5 mg and acetaminophen 325 mg per tablet

Dosing

Adults
  • 2 tablets every 4 - 6 hours as needed
  • Do not exceed 8 tablets in 24 hours
Kidney disease
  • CrCl < 30 ml/min: do not exceed 2 tablets every 12 hours
Liver disease
  • Not recommended

Generic / Price

  • Generic (30 tablets) - $

Other

  • DEA Schedule IV
  • Patients who are allergic to opiates should not receive tramadol
  • Tramadol is a synthetic opioid that acts at opiate receptors in the central nervous system
  • Tramadol has been shown to inhibit reuptake of norepinephrine and serotonin. Use caution when combining with other serotonergic drugs (see serotonin syndrome).
  • CYP2D6 poor/rapid metabolizers - CYP2D6 metabolizes tramadol to an active metabolite (M1) that has more potent opioid activity than the parent compound. Poor CYP2D6 metabolizers may not receive as much pain relief from tramadol, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, tramadol is contraindicated in children under 12 years old and those 12 to 18 years old with respiratory conditions.
  • CYP2D6 inhibitors - concomitant CYP2D6 inhibitors may decrease the conversion of tramadol to its active metabolite and reduce its analgesic effect. Conversely, stopping CYP2D6 inhibitors may increase levels of the active metabolite. Consider the effects of starting and stopping CYP2D6 inhibitors on the efficacy and toxicity of tramadol and make appropriate dose adjustments.
  • Tramadol is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase tramadol exposure, and CYP3A4 inducers may decrease exposure. When combining tramadol with an inhibitor, consider reducing the tramadol dose and monitoring for toxicity. If an inhibitor is discontinued, the tramadol dose may need to be increased. When combining tramadol with an inducer, consider increasing the tramadol dose and monitoring efficacy. If an inducer is discontinued, the tramadol dose may need to be decreased.
  • Nursing mothers - Not recommended. May cause somnolence and breathing issues in breastfed infants.
  • Hyponatremia - hyponatremia, including severe cases (< 120 mEq/L), has occurred in patients receiving tramadol. In some patients, the cause was determined to be the syndrome of inappropriate antidiuretic hormone secretion (SIADH). If symptoms of hyponatremia develop (e.g. headache, fatigue, nausea, vomiting), or if significant hyponatremia is noted on lab work, tramadol should be discontinued.
  • Hypoglycemia - hypoglycemia, including severe cases requiring hospitalization, has been reported in patients receiving tramadol. Patients with risk factors (e.g. diabetes medications) may be at greater risk. If unexplained and/or dangerous hypoglycemia occurs, consider stopping tramadol.

Tramadol ER (Ultram® ER)

Dosage forms

Tablet, extended-release
  • 100 mg
  • 200 mg
  • 300 mg

Dosing

Adults
  • 100 mg once daily
  • Increase dose in 100 mg increments every 5 days as needed
  • Do not exceed 300 mg once daily
Kidney disease
  • CrCl < 30 ml/min: not recommended
Liver disease
  • Child-Pugh C: not recommended

Generic / Price

  • Generic (30 tablets) - $

Other

  • DEA Schedule IV
  • Do not crush, cut, or chew tablet
  • Patients who are allergic to opiates should not receive tramadol
  • Tramadol is a synthetic opioid that acts at opiate receptors in the central nervous system
  • Tramadol has been shown to inhibit reuptake of norepinephrine and serotonin. Use caution when combining with other serotonergic drugs (see serotonin syndrome).
  • CYP2D6 poor/rapid metabolizers - CYP2D6 metabolizes tramadol to an active metabolite (M1) that has more potent opioid activity than the parent compound. Poor CYP2D6 metabolizers may not receive as much pain relief from tramadol, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, tramadol is contraindicated in children under 12 years old and those 12 to 18 years old with respiratory conditions.
  • CYP2D6 inhibitors - concomitant CYP2D6 inhibitors may decrease the conversion of tramadol to its active metabolite and reduce its analgesic effect. Conversely, stopping CYP2D6 inhibitors may increase levels of the active metabolite. Consider the effects of starting and stopping CYP2D6 inhibitors on the efficacy and toxicity of tramadol and make appropriate dose adjustments.
  • Tramadol is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase tramadol exposure, and CYP3A4 inducers may decrease exposure. When combining tramadol with an inhibitor, consider reducing the tramadol dose and monitoring for toxicity. If an inhibitor is discontinued, the tramadol dose may need to be increased. When combining tramadol with an inducer, consider increasing the tramadol dose and monitoring efficacy. If an inducer is discontinued, the tramadol dose may need to be decreased.
  • Nursing mothers - Not recommended. May cause somnolence and breathing issues in breastfed infants.
  • Hyponatremia - hyponatremia, including severe cases (< 120 mEq/L), has occurred in patients receiving tramadol. In some patients, the cause was determined to be the syndrome of inappropriate antidiuretic hormone secretion (SIADH). If symptoms of hyponatremia develop (e.g. headache, fatigue, nausea, vomiting), or if significant hyponatremia is noted on lab work, tramadol should be discontinued.
  • Hypoglycemia - hypoglycemia, including severe cases requiring hospitalization, has been reported in patients receiving tramadol. Patients with risk factors (e.g. diabetes medications) may be at greater risk. If unexplained and/or dangerous hypoglycemia occurs, consider stopping tramadol.

Tramadol ER (Conzip®)

Dosage forms

Capsule, extended-release
  • 100 mg
  • 200 mg
  • 300 mg

Dosing

Adults
  • 100 mg once daily
  • Increase dose in 100 mg increments every 5 days as needed
  • Do not exceed 300 mg once daily
Kidney disease
  • CrCl < 30 ml/min: not recommended
Liver disease
  • Child-Pugh C: not recommended

Generic / Price

  • No Generic
  • Price (30 capsules) - $$$$

Other

  • DEA Schedule IV
  • Do not crush, cut, chew, or open capsule
  • Patients who are allergic to opiates should not receive tramadol
  • Tramadol is a synthetic opioid that acts at opiate receptors in the central nervous system
  • Tramadol has been shown to inhibit reuptake of norepinephrine and serotonin. Use caution when combining with other serotonergic drugs (see serotonin syndrome).
  • CYP2D6 poor/rapid metabolizers - CYP2D6 metabolizes tramadol to an active metabolite (M1) that has more potent opioid activity than the parent compound. Poor CYP2D6 metabolizers may not receive as much pain relief from tramadol, while rapid metabolizers may experience toxicity. Given this unforeseeable risk, tramadol is contraindicated in children under 12 years old and those 12 to 18 years old with respiratory conditions.
  • CYP2D6 inhibitors - concomitant CYP2D6 inhibitors may decrease the conversion of tramadol to its active metabolite and reduce its analgesic effect. Conversely, stopping CYP2D6 inhibitors may increase levels of the active metabolite. Consider the effects of starting and stopping CYP2D6 inhibitors on the efficacy and toxicity of tramadol and make appropriate dose adjustments.
  • Tramadol is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase tramadol exposure, and CYP3A4 inducers may decrease exposure. When combining tramadol with an inhibitor, consider reducing the tramadol dose and monitoring for toxicity. If an inhibitor is discontinued, the tramadol dose may need to be increased. When combining tramadol with an inducer, consider increasing the tramadol dose and monitoring efficacy. If an inducer is discontinued, the tramadol dose may need to be decreased.
  • Nursing mothers - Not recommended. May cause somnolence and breathing issues in breastfed infants.
  • Hyponatremia - hyponatremia, including severe cases (< 120 mEq/L), has occurred in patients receiving tramadol. In some patients, the cause was determined to be the syndrome of inappropriate antidiuretic hormone secretion (SIADH). If symptoms of hyponatremia develop (e.g. headache, fatigue, nausea, vomiting), or if significant hyponatremia is noted on lab work, tramadol should be discontinued.
  • Hypoglycemia - hypoglycemia, including severe cases requiring hospitalization, has been reported in patients receiving tramadol. Patients with risk factors (e.g. diabetes medications) may be at greater risk. If unexplained and/or dangerous hypoglycemia occurs, consider stopping tramadol.

Seglentis® (celecoxib + tramadol)

Dosage forms

Tablet
  • Celecoxib - Tramadol
    • 56 mg - 44 mg

Dosing

Acute pain (adults)
  • Dosing: 2 tablets every 12 hours as needed
  • May take without regard to food
  • Celecoxib is a selective NSAID. See celecoxib for more.

Generic / Price

- NO/$$$ for #30










  • ✝Multiply the dose of the opioid by the conversion factor to get the equivalent dose in morphine. For example, 20 mg of oxycodone would be equivalent to 30 mg of morphine (20 mg X 1.5 = 30 mg)
  • NOTE: THIS TABLE IS NOT FOR CONVERTING BETWEEN DOSES OF DIFFERENT OPIOIDS. There are no established conversion ratios for converting from one opioid to another. See individual drug package inserts for recommendations on converting between drugs.
  • Reference [12]
Oral morphine milligram equivalent doses for commonly prescribed opioids
Opioid Conversion factor✝
Codeine 0.15
Fentanyl transdermal (in mcg/hr) 2.4
Hydrocodone 1
Hydromorphone 5
Methadone 4.7
Morphine 1
Oxycodone 1.5
Oxymorphone 3
Tapentadol 0.4
Tramadol 0.2


  • PMID 29114811 - Interpretation of Urine Drug Screens: Metabolites and Impurities, JAMA (2017)
URINARY METABOLITES OF OPIATES
Opiate Urinary metabolite Comment
Codeine
  • Morphine
  • Hydrocodone (< 10%)
  • Norcodeine
  • Codeine is metabolized to morphine
Buprenorphine
  • Norbuprenorphine
Fentanyl
  • Norfentanyl
Heroin
  • 6-Monoacetylmorphine
  • Morphine
  • Normorphine
  • Morphine may be the only metabolite detected after heroin use
Hydrocodone
  • Hydromorphone
  • Norhydrocodone
  • Dihydrocodeine
Hydromorphone
  • Hydromorphone-3-glucuronide
Methadone
  • 2-Ethylidene-1
  • 5-dimethyl-3
  • 3-diphenylpyrrolidine
Morphine
  • Normorphine
  • Hydromorphone (< 10%)
  • Morphine-6-glucuronide
  • Morphine-3-glucuronide
  • Codeine is sometimes a contaminant of morphine during manufacturing
  • Codeine contamination is typically 0.04% - 0.5% of morphine concentrations
Oxycodone
  • Oxymorphone
  • Noroxycodone
  • Hydrocodone is sometimes a contaminant of oxycodone during manufacturing
  • Hydrocodone contamination is typically < 0.1% of oxycodone concentrations
Oxymorphone
  • Oxymorphone-3-glucuronide
  • 6-hydroxy-oxymorphone








Pricing legend
  • $ = 0 - $50
  • $$ = $51 - $100
  • $$$ = $101 - $150
  • $$$$ = > $151
  • Pricing based on one month of therapy at standard dosing in an adult
  • Pricing based on information from GoodRX.com®
  • Pricing may vary by region and availability