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- NOTE: All dosing for adults unless otherwise specified
- ACRONYMS AND DEFINITIONS
- APAP - Acetaminophen (Tylenol®)
- ER - Extended release
- CII - DEA Schedule II
- CP - Codeine phosphate
- HC - Hydrocodone
- IR - Immediate release
- OC - Oxycodone
- P = Drugs with pediatric dosing recommendations
- SL - Sublingual
- XR - Extended release
- BENZHYDROCODONE
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 sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
- BUPRENORPHINE
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
- Adults (opiate-naïve)
- Approved to treat severe pain that requires long-term treatment
- 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
Converting from other opiates
- To reduce the risk of opioid withdrawal, taper patients to no more than 30 mg of oral morphine sulfate equivalent (MSE) 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 - $$$$
Other
- DEA Schedule III
- Buprenorphine is a partial agonist at mu opioid receptors
- FDA-approved for the treatment of severe pain requiring long-term treatment
- Belbuca is placed against the inside of the cheek
- Belbuca film dissolves within 30 minutes
- Do not eat or drink until film is dissolved
- Buprenorphine is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
Buprenorphine hydrochloride (Subutex®)
Dosage forms
Sublingual tablet
- 2 mg
- 8 mg
Dosing
Opiate withdrawal and maintenance
- Used to prevent withdrawal symptoms in patients who are being treated for opiate addiction
- Dosage will vary depending on the patient and their addiction characteristics
- Given as a once daily dose
- Initial dose is usually 4 - 8 mg on Day 1 given 12 - 48 hours after most recent opioid use while patient is having withdrawal symptoms
- On Day 2, dose may be increased up to 16 mg. On days 3 - 7, dose may be increased up to 30 mg.
- Maintenance dose is typically 16 - 24 mg/day
- During maintenance phase, patients should be switched to a buprenorphine-naloxone product
- Consider weaning after 1 year [9]
Generic / Price
- Generic (60 tablets) - $$
Other
- DEA Schedule III
- Buprenorphine is an opioid partial agonist. It prevents symptoms of opiate withdrawal, but its maximal effects are less than those seen with heroin, methadone, etc.
- Buprenorphine has been associated with liver toxicity, especially in high-risk patients (alcoholism, hepatitis C, etc). Baseline and periodic LFTs are recommended.
- Buprenorphine is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
- Providers must obtain waiver and complete special training in order to prescribe - see SAMHSA website
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 of 4 patches
Dosing
Severe pain
- Adults (opiate-naïve)
- Approved to treat severe pain that requires long-term treatment
- One 5 mcg/hour patch every 7 days
- Increase dose at an interval of ≥ 72 hours
- Maximum dose is 20 mcg/hour because of prolonged QT interval risk
Converting from other opiates
- Initiate Butrans at the next dosing interval
- 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 - $$$
Other
- DEA Schedule III
- Buprenorphine is a partial agonist at mu opioid receptors
- FDA-approved for the treatment of severe pain requiring long-term treatment
- Buprenorphine is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
- Apply to upper outer arm, upper chest, upper back or the side of the chest. These 4 sites (each present on both sides of the body) provide 8 possible application sites. Rotate Butrans among the 8 described skin sites. After Butrans removal, wait a minimum of 21 days before reapplying to the same skin site.
- Apply Butrans to a hairless or nearly hairless skin site. If none are available, the hair at the site should be clipped, not shaven.
- Do not expose patch to direct heat because absorption may be increased
- Patients with fever may absorb more buprenorphine from the patch
- Special disposal instructions are provided to prevent accidental exposure. Used patches may be flushed down toilet.
Buprenorphine hydrochloride (Probuphine®)
Dosage forms
Subdermal implant
- Each implant contains 80 mg of buprenorphine HCL
- Comes in kit with 4 implants and disposable applicator
Dosing
Maintenance of opioid dependence
- Approved for the maintenance treatment of opioid dependence
- Four implants inserted subdermally in the inner side of the upper arm every 6 months
- Patients should be on stable (≥ 3 months) maintenance doses of ≤ 8 mg/day of Subutex or Suboxone. For Bunavail, stable maintenance doses should be ≤ 4.2 mg/0.7 mg. For Zubsolv, stable maintenance doses should be ≤ 5.7 mg/1.4 mg.
- If another insertion is desired after 6 months, the opposite arm should be used
- After one insertion in each arm, patients should be transitioned back to transmucosal buprenorphine. Reinserting Probuphine in a previously-treated arm has not been studied.
Efficacy
Generic / Price
- No generic
- 1 kit - $$$$
Other
- DEA Schedule III
- Providers must be certified in the Probuphine REMS program in order to prescribe Probuphine
Buprenorphine hydrochloride (Sublocade®)
Dosage forms
Prefilled syringe, single-dose
- 100 mg/0.5 ml
- 300 mg/1.5 ml
Dosing
Maintenance of opioid dependence
- Indicated for patients who have initiated treatment with a transmucosal buprenorphine-containing product, followed by dose adjustment for a minimum of 7 days. Patients should be receiving the equivalent of 8 to 24 mg of buprenorphine daily. One Suboxone® (buprenorphine and naloxone) 8 mg/2 mg sublingual tablet provides equivalent buprenorphine exposure to one Subutex® (buprenorphine HCl) 8 mg sublingual tablet or one Bunavail® (buprenorphine and naloxone) 4.2 mg/0.7 mg buccal film or one Zubsolv® (buprenorphine and naloxone) 5.7 mg/1.4 mg sublingual tablet.
- For abdominal subcutaneous administration only
- Should only be administered by healthcare provider
- Dosing: 300 mg monthly for the first two months followed by a maintenance dose of 100 mg monthly.
- Maintenance dose may be increased to 300 mg monthly for patients who tolerate the 100 mg dose, but do not demonstrate a satisfactory clinical response
- There should be a minimum of 26 days between doses
- A patient who misses a dose should receive the next dose as soon as possible, with the following dose given no less than 26 days later. Occasional delays in dosing up to 2 weeks are not expected to have a clinically significant impact on treatment effect.
- For patients in established treatment of 100 mg monthly, there may be instances when allowance for a two-month dosing interval may be appropriate (e.g., extended travel); in those instances, a single 300 mg dose may be given to cover a two-month period. Thereafter, the 100 mg monthly regimen would resume. Patients should be cautioned that the peak plasma level after injection of a 300 mg dose will be higher than their usual monthly dose and that they may experience sedation or other buprenorphine related effects
Efficacy
Generic / Price
- No generic
- 1 syringe - $$$$
Other
- DEA Schedule III
- Subclocade is injected as a liquid, and the subsequent precipitation of the poly polymer creates a solid depot which contains buprenorphine. The depot disintegrates over time, but may be surgically excised under local anesthesia within 14 days of injection.
- After steady-state has been achieved (4-6 months), patients discontinuing Sublocade may have detectable plasma levels of buprenorphine for twelve months or longer
- Providers must be certified in the Sublocade REMS program in order to prescribe Sublocade
- BUPRENORPHINE + NALOXONE
Buprenorphine and Naloxone | Suboxone® | Zubsolv® | Bunavail®
Dosage forms
Suboxone® - sublingual tablet
- Buprenorphine (mg) : Naloxone (mg)
- 2 mg : 0.5 mg
- 8 mg : 2.0 mg
Suboxone® - sublingual film
- Buprenorphine : Naloxone
- 2 mg : 0.5 mg
- 4 mg : 1.0 mg
- 8 mg : 2 mg
- 12 mg: 3 mg
Zubsolv® - sublingual tablet
- Buprenorphine : Naloxone
- 1.4 mg : 0.36 mg
- 5.7 mg : 1.4 mg
- 8.6 mg : 2.1 mg
- 11.4 mg : 2.9 mg
Bunavail® - buccal film
- Buprenorphine : Naloxone
- 2.1 mg : 0.3 mg
- 4.2 mg : 0.7 mg
- 6.3 mg : 1.0 mg
Dosing
Opiate withdrawal and maintenance
- Used to prevent withdrawal symptoms in patients who are being treated for opiate addiction
- Buprenorphine/naloxone is preferred after induction with buprenorphine alone
- Naloxone is included to deter injection of buprenorphine. Naloxone has no effect when taken orally, but acts as an opioid antagonist when injected.
- Dosage will vary depending on the patient and their addiction characteristics
- Given as once daily dose
- Maintenance dose is typically 4 - 24 mg/day of buprenorphine, except for Zubsolv and Bunavail which have slightly different conversion ratios. See Zubsolv PI (sec 2) and Bunavail PI (sec 2).
Generic / Price
- Suboxone generic (30 tablets) - $
- Suboxone generic (30 films) - $$
- Zubsolv (30 tablets) - $$$$
- Bunavail (30 films) - $$$$
Other
- DEA Schedule III
- Buprenorphine is an opioid partial agonist. It prevents symptoms of opiate withdrawal, but its maximal effects are less than those seen with heroin, methadone, etc.
- Naloxone is an opioid antagonist. It has no effect when taken orally, but acts as an opioid antagonist when injected.
- Buprenorphine has been associated with liver toxicity, especially in high-risk patients (alcoholism, hepatitis C, etc). Baseline and periodic LFTs are recommended.
- Buprenorphine is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
- Providers must obtain waiver and complete special training in order to prescribe - see SAMHSA website
- BUTORPHANOL (STADOL®)
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
- Store at room temperature
- Bottle must be primed if not used for ≥ 48 hours
- CODEINE
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
Adults
- 15 - 60 mg every 4 hours as needed
- Do not exceed 360 mg in 24 hours
Children
- 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]
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 III
- Codeine has no analgesic activity unless it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine while rapid metabolizers may experience toxicity. Because of the risk for toxicity, codeine is contraindicated for postoperative pain in children.
Codeine - APAP solution
Dosage forms
Solution
- Codeine 12 mg and acetaminophen 120 mg per 5 ml
Dosing
Adults
- 15 ml every 4 hours as needed
Children
- 3 - 6 years: 5 ml three to four times daily
- 7 - 12 years: 10 ml three to four times daily
NOTE: In 2017, the FDA declared that all codeine products are contraindicated in children < 12 years old
Generic / Price
- Generic (120 ml) - $
Other
- DEA Schedule V
- Codeine has no analgesic activity unless it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine while rapid metabolizers may experience toxicity. Because of the risk for toxicity, codeine is contraindicated for postoperative pain in children.
Cheratussin DAC®
Dosage forms
Liquid
- Codeine 10 mg, guaifenesin 100 mg, pseudoephedrine 30 mg per 5 ml
- Contains 2.1% alcohol
Dosing
Adults and children ≥ 12 years
- 10 ml every 4 hours as needed
- Do not take more than 4 doses in 24 hours
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
Phenergan® with codeine
Dosage forms
Syrup
- Codeine 10 mg and promethazine 6.25 mg per 5 ml
- Contains 7% alcohol
Dosing
Adults and children ≥ 12 years
- 5 ml every 4 - 6 hours as needed
- Do not take more than 30 ml in 24 hours
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
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
Adults and children ≥ 12 years
- 5 ml every 4 - 6 hours as needed
- Do not take more than 30 ml in 24 hours
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
Robitussin® AC
Dosage forms
Liquid / solution
- Codeine 10 and guaifenesin 100 per 5 ml
- Solution is alcohol free
- Liquid contains 3 - 4% alcohol
Dosing
Adults and children ≥ 12 years
- 10 ml every 4 hours as needed
- Do not take more than 6 doses in 24 hours
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®
Tuzistra™ XR
Dosage forms
Suspension, extended-release
- Codeine 14.7 mg and chlorpheniramine 2.8 mg per 5 ml
Dosing
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
Codeine Sulfate (CII)
Dosage forms
Tablet
- 15 mg
- 30 mg
- 60 mg
Dosing
Adults (opiate-naïve)
- 15 - 60 mg every 4 hours as needed
- Do not exceed 360 mg in 24 hours
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
- Codeine has no analgesic activity unless it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine while rapid metabolizers may experience toxicity. Because of the risk for toxicity, codeine is contraindicated for postoperative pain in children.
- Duration of action: 3 - 4 hours
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
- 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 $$$$
Other
- DEA Schedule III
- Butalbital is a barbiturate
- Codeine has no analgesic activity unless it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine while rapid metabolizers may experience toxicity.
Fiorinal® with codeine
Dosage forms
Capsule
- Codeine 30 mg, aspirin 325 mg, butalbital 50 mg, caffeine 40 mg per capsule
Dosing
Tension headache
- 1 - 2 capsules every 4 hours as needed
- Do not exceed 6 capsules in 24 hours
Generic / Price
- Generic (30 capsules) - $
Other
- DEA Schedule III
- Butalbital is a barbiturate
- Codeine has no analgesic activity unless it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine while rapid metabolizers may experience toxicity.
Soma® Compound with codeine
Dosage forms
Tablet
- Codeine 16 mg, aspirin 325 mg, and carisoprodol 200 mg per tablet
Dosing
Acute, painful musculoskeletal conditions
- 1 - 2 tablets four times daily as needed
Generic / Price
- Generic (30 capsules) - $ - $$
Other
- DEA Schedule III
- Carisoprodol is a centrally-acting muscle relaxant. See carisoprodol for more.
- Codeine has no analgesic activity unless it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine while rapid metabolizers may experience toxicity.
- DIHYDROCODEINE
Synalgos®-DC
Dosage forms
Capsule
- Dihydrocodeine 16 mg, Caffeine 30 mg, Aspirin 356.4 mg per capsule
Dosing
Moderate to severe pain
- 2 capsules every 4 hours as needed for pain
Generic / Price
- Generic (30 capsules) - $
Other
- DEA Schedule III
- Dihydrocodeine has no analgesic activity unless it is metabolized into dihydromorphine by CYP2D6. Poor metabolizers may not receive any pain relief from dihydrocodeine while rapid metabolizers may experience toxicity.
Trezix®
Dosage forms
Capsule
- Dihydrocodeine 16 mg, Caffeine 30 mg, Acetaminophen 320.5 mg per capsule
Dosing
Moderate to severe pain
- 2 capsules every 4 hours as needed for pain
- Do not exceed 10 capsules in 24 hours
Generic / Price
- Generic (30 capsules) - $$
Other
- DEA Schedule III
- Dihydrocodeine has no analgesic activity unless it is metabolized into dihydromorphine by CYP2D6. Poor metabolizers may not receive any pain relief from dihydrocodeine while rapid metabolizers may experience toxicity.
- DIPHENOXYLATE
Diphenoxylate | Lomotil® | Lonox®
Dosage forms
Tablet
- Diphenoxylate 2.5 mg and atropine 0.025 mg per tablet
Solution
- Diphenoxylate 2.5 mg and atropine 0.025 mg per 5 ml
Dosing - Diarrhea
Adults
- Tablet - 2 tablets four times daily as needed
- Liquid - 10 ml four times daily as needed
Children 2 - 13 years
- Use liquid in children
- 0.3 - 0.4 mg/kg/day (diphenoxylate component) given in 4 divided doses
Age (years) | Weight (kg) | Weight (pounds) | Dose in milliliters (4 times daily as needed) |
---|---|---|---|
2 | 11 - 14 | 24 - 31 | 1.5 - 3.0 |
3 | 12 - 16 | 26 - 35 | 2.0 - 3.0 |
4 | 14 - 20 | 31 - 44 | 2.0 - 4.0 |
5 | 16 - 23 | 35 - 51 | 2.5 - 4.5 |
6 - 8 | 17 - 32 | 38 - 71 | 2.5 - 5.0 |
9 - 12 | 23 - 55 | 51 - 121 | 3.5 - 5.0 |
Generic / Price
- Generic (30 tablets or 120ml) - $
Other
- DEA Schedule V
- Atropine is added to discourage deliberate overdose. It has no effect in normal dosing.
- Young children may be more susceptible to diphenoxylate and atropine side effects
- FENTANYL
Fentanyl (Abstral®)
Dosage forms
Sublingual tablet
- 100 mcg
- 200 mcg
- 300 mcg
- 400 mcg
- 600 mcg
- 800 mcg
- Comes in packets of 12 (100, 200, 300, 400 mcg strengths only) or 32 tablets (all strengths)
Dosing
- The Abstral PI (sec 2) contains a dose titration schedule
- Fentanyl products are not recommended in opiate-naïve patients, and they should only be used in opiate-tolerant cancer patients for breakthrough pain
- See opiate-tolerant definition for more
Generic / Price
- No generic
- 30 tablets - $$$$
Other
- DEA Schedule II
- Providers and patients must enroll in the TIRF REMS Access program for outpatient use
- Tablet is placed under the tongue
- Special disposal instructions are provided to prevent accidental exposure
- Fentanyl is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
Fentanyl (Actiq®)
Dosage forms
Lozenge
- 200 mcg
- 400 mcg
- 600 mcg
- 800 mcg
- 1200 mcg
- 1600 mcg
Dosing
Opioid-tolerant cancer patients
- The Actiq PI (sec 2) contains a dose titration schedule
- Fentanyl products are not recommended in opiate-naïve patients, and they should only be used in opiate-tolerant cancer patients for breakthrough pain
- See opiate-tolerant definition for more
Generic / Price
- Generic (30 lozenges) - $$$$
Other
- DEA Schedule II
- Providers and patients must enroll in the TIRF REMS Access program for outpatient use
- Special lozenge disposal instructions are provided to prevent accidental exposures
- Fentanyl is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
Fentanyl (Duragesic®)
Dosage forms
Patch
- 12 mcg/hour
- 25 mcg/hour
- 37.5 mcg/hour
- 50 mcg/hour
- 62.5 mcg/hour
- 75 mcg/hour
- 87.5 mcg/hour
- 100 mcg/hour
Dosing
Opioid-tolerant cancer patients
- The Duragesic PI (sec 2) contains an extensive table for converting from other opioids to fentanyl patch
- Fentanyl products are not recommended in opiate-naïve patients, and they should only be used in opiate-tolerant cancer patients for breakthrough pain
- See opiate-tolerant definition for more
Generic / Price
- Generic available
- 12 mcg/hr, 50 mcg/hr, 75 mcg/hr, 100 mcg/hr (10 patches) - $$-$$$
- 25 mcg/hr (10 patches) - $
- 37.5 mcg/hr, 62.5 mcg/hr, 87.5 mcg/hr (10 patches) - $$$$
Other
- DEA Schedule II
- Old patch is removed and new patch is applied every 72 hours. Apply new patch to different skin site.
- Apply to chest, back, flank, or upper arm. Hair at application site may be clipped (not shaved).
- Flush used patches down the toilet to prevent accidental exposure
- Do not expose patch to direct heat because absorption may be increased
- Patients with fever may absorb more fentanyl from the patch
- Fentanyl is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
Fentanyl (Fentora®)
Dosage forms
Buccal / sublingual tablet
- 100 mcg
- 200 mcg
- 400 mcg
- 600 mcg
- 800 mcg
- Comes in cartons containing 7 blister cards with 4 tablets per card
Dosing
Opioid-tolerant cancer patients
- The Fentora PI (sec 2) contains a dose titration schedule
- Fentanyl products are not recommended in opiate-naïve patients, and they should only be used in opiate-tolerant cancer patients for breakthrough pain
- See opiate-tolerant definition for more
Generic / Price
- No generic
- 30 tablets - $$$$
Other
- DEA Schedule II
- Providers and patients must enroll in the TIRF REMS Access program for outpatient use
- Tablet can be placed above a rear molar, between the upper cheek and gum, or under the tongue
- Special disposal instructions are provided to prevent accidental exposure
- Fentanyl is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
Fentanyl (Lazanda®)
Dosage forms
Nasal spray
- 100 mcg/100 mcL
- 400 mcg/100 mcL
- Each bottle contains 8 sprays of 100 mcL
Dosing
Opioid-tolerant cancer patients
- The Lazanda PI (sec 2) contains a dose titration schedule
- Fentanyl products are not recommended in opiate-naïve patients, and they should only be used in opiate-tolerant cancer patients for breakthrough pain
- See opiate-tolerant definition for more
Generic / Price
- No generic
- 1 bottle - $$$$
Other
- DEA Schedule II
- Providers and patients must enroll in the TIRF REMS Access program for outpatient use
- Special disposal instructions are provided to prevent accidental exposure
- Fentanyl is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
Fentanyl (Subsys®)
Dosage forms
Sublingual spray
- 100 mcg
- 200 mcg
- 400 mcg
- 600 mcg
- 800 mcg
- 1200 mcg
- 1600 mcg
- Comes in cartons of 10 and 30 sprays
Dosing
Opioid-tolerant cancer patients
- The Subsys PI (sec 2) contains a dose titration schedule
- Fentanyl products are not recommended in opiate-naïve patients, and they should only be used in opiate-tolerant cancer patients for breakthrough pain
- See opiate-tolerant definition for more
Generic / Price
- No generic
- 30 sprays - $$$$
Other
- DEA Schedule II
- Providers and patients must enroll in the TIRF REMS Access program for outpatient use
- Each dose comes in an individual sprayer
- Special disposal instructions are provided to prevent accidental exposure
- Fentanyl is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
- HYDROCODONE
Hydrocodone - APAP | Vicodin® | Norco® | Lortab®
Dosage forms
Tablet
- Hydrocodone : Acetaminophen
- 2.5 mg : 325 mg
- 5.0 mg : 325 mg
- 7.5 mg : 325 mg
- 10 mg : 325 mg
- 5.0 mg : 300 mg
- 7.5 mg : 300 mg
- 10 mg : 300 mg
Solution
- Hydrocodone 7.5 mg and acetaminophen 325 mg per 15ml
Dosing
Adults (opiate-naïve)
- 5 - 10 mg every 4 - 6 hours as needed
- Do not to exceed 50 mg a day
Children ≥ 2 years (opiate-naïve)
- 0.135 mg/kg/dose every 4 - 6 hours as needed
- Do not exceed 6 doses a day
Weight (kg) | Dose every 4 - 6 hours |
---|---|
12 - 15 | 1.875 mg (3.75 ml*) |
16 - 22 | 2.5 mg (5 ml*) |
23 - 31 | 3.75 mg (7.5 ml*) |
32 - 45 | 5 mg (10 ml*) |
Generic / Price
- Hydrocodone/APAP tab #30 - $
- Hydrocodone/APAP solution #240 ml - $
Other
- DEA Schedule II
- Duration of action: 3 - 5 hours
- Hydrocodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
Hydrocodone - Ibuprofen (Vicoprofen®)
Dosage forms
Tablet
- Hydrocodone : Ibuprofen
- 2.5 mg : 200 mg
- 5.0 mg : 200 mg
- 7.5 mg : 200 mg
- 10 mg : 200 mg
Dosing
Adults (opiate-naïve)
- 5 - 10 mg every 4 - 6 hours as needed
- Do not to exceed 50 mg a day
Generic / Price
- Generic available
- Hydrocodone/Ibuprofen tab #30: $-$$
Other
- DEA Schedule II
- Duration of action: 3 - 5 hours
- Hydrocodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
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 - $$$
Other
- DEA Schedule II
- Guaifenesin is an expectorant
Hycodan® syrup
Dosage forms
Syrup
- Hydrocodone 5 mg and homatropine 1.5 mg per 5 ml
Dosing
Cough (adults)
- 5 ml every 4 - 6 hours as needed
- Do not exceed 30 ml in 24 hours
Cough (children 6 - 12 years)
- 2.5 ml every 4 - 6 hours as needed
- Do not exceed 15 ml in 24 hours
NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old
Generic / Price
- Generic 120 ml - $
Other
- DEA Schedule II
- Homatropine is an anticholinergic medication that is included to discourage overdose
Hycodan® tablets
Dosage forms
Tablet
- Hydrocodone 5 mg and homatropine 1.5 mg per tablet
Dosing
Cough (adults)
- 1 tablet every 4 - 6 hours as needed
- Do not exceed 6 tablets in 24 hours
Cough (children 6 - 12 years)
- One-half (1/2) tablet every 4 - 6 hours as needed
- Do not exceed 3 tablets in 24 hours
NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old
Generic / Price
- Generic 30 tablets - $
Other
- DEA Schedule II
- Homatropine is an anticholinergic medication that is included to discourage overdose
Hycofenix®
Dosage forms
Solution
- Hydrocodone 2.5 mg, pseudoephedrine 30 mg, and guaifenesin 200 mg per 5 ml
Dosing
Cough (adults)
- 10 ml every 4 - 6 hours as needed
- Do not exceed 40 ml in 24 hours
Generic / Price
- No generic
- 120 ml - $$$
Other
- DEA Schedule II
- Guaifenesin is an expectorant
- Pseudoephedrine is a decongestant
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 - $$$
Other
- DEA Schedule II
- Guaifenesin is an expectorant
Rezira®
Dosage forms
Solution
- Hydrocodone 5 mg and pseudoephedrine 60 mg per 5 ml
Dosing
Cough (adults)
- 5 ml every 4 - 6 hours as needed
- Do not exceed 20 ml in 24 hours
Generic / Price
- No generic
- 120 ml - $
Other
- DEA Schedule II
- Pseudoephedrine is a decongestant
Tussicaps®
Dosage forms
Capsule, extended-release
- Hydrocodone 5 mg and chlorpheniramine 4 mg per capsule
- Hydrocodone 10 mg and chlorpheniramine 8 mg per capsule
Dosing
Cough (adults and children ≥ 12 years)
- 1 capsule (hydrocodone 10 mg) every 12 hours as needed
- Do not exceed 2 capsules in 24 hours
Cough (children 6 - 11 years)
- 1 capsule (hydrocodone 5 mg) every 12 hours as needed
- Do not exceed 2 capsules in 24 hours
- Only hydrocodone 5 mg capsule should be used in this age group
NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old
Generic / Price
- No generic
- 30 capsules - $$$$
Other
- DEA Schedule II
- Chlorpheniramine is an antihistamine
Tussionex®
Dosage forms
Suspension, extended-release
- Hydrocodone 10 mg and chlorpheniramine 8 mg per 5 ml
Dosing
Cough (adults and adolescents ≥ 12 years)
- 5 ml every 12 hours
- Do not exceed 10 ml in 24 hours
Cough (children 6 - 11 years)
- 2.5 ml every 12 hours
- Do not exceed 5 ml in 24 hours
NOTE: In 2018, the FDA declared that all opiate-containing cough/cold medications should not be used in patients < 18 years old
Generic / Price
- Generic 120ml - $
Other
- DEA Schedule II
- Chlorpheniramine is an antihistamine
Vituz®
Dosage forms
Solution
- Hydrocodone 5 mg and chlorpheniramine 4 mg per 5 ml
Dosing
Cough (adults)
- 5 ml every 4 - 6 hours as needed
- Do not exceed 20 ml in 24 hours
Generic / Price
- No generic
- 120 ml - $
Other
- DEA Schedule II
- Chlorpheniramine is an antihistamine
Zutripro®
Dosage forms
Solution
- Hydrocodone 5 mg, chlorpheniramine 4 mg, pseudoephedrine 60 mg per 5 ml
Dosing
Cough (adults)
- 5 ml every 4 - 6 hours as needed
- Do not exceed 20 ml in 24 hours
Generic / Price
- Generic (120 ml) - $-$$
Other
- DEA Schedule II
- Chlorpheniramine is an antihistamine
- Pseudoephedrine is a decongestant
Hydrocodone (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
- Instructions for converting from other opioids are available in the Hysingla PI sec 2.2
Generic / Price
- YES/$$Other
- DEA Schedule II
- Do not crush, cut, chew, or dissolve tablet
- Abuse-deterrent properties - when tablet is crushed and mixed with water, it forms a gel that is difficult to pull through a needle
- Hydrocodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
- Prolonged QT interval has been seen with Hysingla doses of ≥ 160 mg
Hydrocodone (Zohydro® ER)
Dosage forms
Capsule, extended-release
- 10 mg
- 15 mg
- 20 mg
- 30 mg
- 40 mg
- 50 mg
Dosing
Adults (opiate-naïve)
- 10 mg every 12 hours
- Increase dose by 10 mg every 3 - 7 days as needed
Converting other HC formulations to Zohydro
- Total daily hydrocodone dose is divided by 2 and given once every 12 hours
Converting from other opioids
- A conversion table is available in the Zohydro PI sec 2.1
Generic / Price
- No generic
- 30 capsules - $$$$
Other
- DEA Schedule II
- Do not crush, open, chew, or dissolve capsules
- Hydrocodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
- Extended-release hydrocodone products have been associated with prolonged QT interval
- HYDROMORPHONE
Hydromorphone IR (Dilaudid®)
Dosage forms
Tablet
- 2 mg
- 4 mg
- 8 mg
Solution
- 5 mg/5 ml
Dosing
Adults (opiate-naïve)
- 2 - 4 mg every 4 - 6 hours as needed
Children ≥ 6 months (opiate-naïve)
- < 50 kg: 0.040 - 0.080 mg/kg every 3 - 4 hours as needed
- ≥ 50 kg: 2 - 4 mg every 3 - 4 hours as needed [2]
Generic / Price
- Generic (30 tablets) - $
- Generic (200 ml) - $
Other
- DEA Schedule II
- Solution and tablet are bioequivalent
Hydromorphone ER (Exalgo®)
Dosage forms
Tablet, extended-release
- 8 mg
- 12 mg
- 16 mg
- 32 mg
Dosing
Adults (opiate-naïve)
- Not recommended
Converting from other oral hydromorphone products
- Give total daily dose of hydromorphone as once daily Exalgo® dose
Converting from other opioids
- The Exalgo® PI sec 2.1 contains information on converting from other opioids
Generic / Price
- Generic (30 tablets): $$-$$$$
Other
- DEA Schedule II
- May take without regard to food
- Do not crush, cut, or chew tablets
- MEPERIDINE
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.
Methadone | Methadose® | Dolophine®
Dosage forms
Tablet
- 5 mg
- 10 mg
Tablet for suspension (dispersible)
- 40 mg
Solution
- 5 mg/5 ml
- 10 mg/5 ml
Concentrate
- 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
Converting from other opiates to methadone (chronic pain)
- 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]
Maintenance therapy in opiate dependence
- Start with 15 - 30 mg/day and increase by 10 - 15 mg every 3 - 5 days up to 50 - 80 mg/day
- At weeks 3 - 6, dose may need to be increased to 80 - 100 mg/day if tolerance develops and cravings increase
- Consider tapering after 1 year [9]
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
- Reduce dose by 3 mg/day down to 0 mg
- Based on PMID 26028120
Generic / Price
- Tablets (#90) - YES/$
- Solution (180 ml) - YES/$
- Concentrate (240 ml) - YES/$
Other
- DEA Schedule II
- Methadone has a long half-life. Typical range is 15 - 60 hours, but may be as long as 120 hours in some individuals.
- Risk of adverse events is higher during first 4 - 5 days of therapy
- Doses above 30 mg/day should only be done in appropriate settings
- Methadone may prolong the QT interval. (see prolonged QT interval). Baseline and periodic EKG may be appropriate in patients at increased risk. [3,4]
- Methadone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
- Tablets for suspension are intended for dispersion in a liquid immediately prior to observed intake
- MORPHINE SULFATE
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
Morphine sulfate (Arymo® ER)
Dosage forms
Tablet, extended-release
- 15 mg
- 30 mg
- 60 mg
Dosing
Adults (opiate-naïve)
- 15 mg every 8 - 12 hours
- Increase dose every 1 - 2 days as needed
Converting from other oral morphine meds
- Total daily morphine dose will remain the same. Dose may given in halves every twelve hours or thirds every 8 hours.
Converting from parenteral morphine to oral
- Between 2 to 6 mg of oral morphine may be required to provide analgesia equivalent to 1 mg of parenteral morphine. Typically, a dose of morphine that is approximately three times the previous daily parenteral morphine requirement is sufficient.
- 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
- No generic
- 30 tablets - $$$$
Other
- DEA Schedule II
- Do not crush, cut, dissolve, or chew tablets. Swallow tablets whole.
Morphine sulfate ER (Avinza®)
Dosage forms
Capsule, extended-release
- 30 mg
- 45 mg
- 60 mg
- 75 mg
- 90 mg
- 120 mg
Dosing
Adults (opiate-naïve)
- 30 mg once daily
- Increase in increments not greater than 30 mg every 4 days
Converting from other oral morphine meds
- Total daily morphine dose can be given as once daily Avinza dose
Converting from parenteral morphine to oral
- Anywhere from 3 to 6 mg of oral morphine sulfate may be required to provide pain relief equivalent to 1 mg of parenteral morphine
- In chronic dosing, 3 mg of oral morphine for every 1 mg of parenteral morphine may be sufficient [3]
Discontinuation
- Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
- Do not discontinue abruptly
Generic / Price
- Generic (30 capsules) - $$-$$$$ depending on the strength
Other
- DEA Schedule II
- Avinza may be opened and sprinkled on applesauce. Swallow whole. Do not chew or crush beads.
- Daily dose should not exceed 1600 mg because of fumaric acid content of drug
Morphine sulfate - Naltrexone ER (Embeda®)
Dosage forms
Capsule, extended-release
- Morphine : Naltrexone
- 20 mg: 0.8 mg
- 30 mg: 1.2 mg
- 50 mg: 2 mg
- 60 mg: 2.4 mg
- 80 mg: 3.2 mg
- 100 mg: 4 mg
Dosing
Adults (opiate-naïve)
- 20/0.8 mg every 24 hours
- Embeda daily dose may also be divided in half and given every 12 hours
- Increase dose at intervals of every 1 - 2 days
Converting from other oral morphine meds
- Total daily morphine dose can be given as once daily Embeda dose or divided by 2 and given every 12 hours
Converting from parenteral to oral
- Anywhere from 3 to 6 mg of oral morphine sulfate may be required to provide pain relief equivalent to 1 mg of parenteral morphine
- In chronic dosing, 3 mg of oral morphine for every 1 mg of parenteral morphine may be sufficient [3]
Discontinuation
- Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
- Do not discontinue abruptly
Generic / Price
- No generic
- 30 capsules - $$$$
Other
- DEA Schedule II
- Embeda may be opened and sprinkled on applesauce. Swallow whole. Do not chew or crush pellets.
- Naltrexone is an opioid antagonist that is added as an abuse-deterrent. When pellets are crushed, naltrexone is released and the euphoric effect of the drug is reduced. If pellets are not crushed, naltrexone remains sequestered and inactive.
Morphine sulfate ER (Kadian®)
Dosage forms
Capsule, extended-release
- 10 mg
- 20 mg
- 30 mg
- 40 mg
- 50 mg
- 60 mg
- 80 mg
- 100 mg
Dosing
Adults (opiate-naïve)
- 30 mg once daily
- Kadian daily dose may also be divided in half and given every 12 hours
- Increase dose at intervals of every 1 - 2 days
Converting from other oral morphine meds
- Total daily morphine dose can be given as once daily Kadian dose or divided by 2 and given every 12 hours
Converting from parenteral morphine to oral
- Anywhere from 3 to 6 mg of oral morphine sulfate may be required to provide pain relief equivalent to 1 mg of parenteral morphine
- In chronic dosing, 3 mg of oral morphine for every 1 mg of parenteral morphine may be sufficient [3]
Discontinuation
- Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
- Do not discontinue abruptly
Generic / Price
- Generic (30 capsules) - $-$$$$ depending on strength
Other
- DEA Schedule II
- Kadian may be opened and sprinkled on applesauce. Swallow whole. Do not chew or crush beads.
Morphine sulfate (Morphabond™ ER)
Dosage forms
Tablet, extended-release
- 15 mg
- 30 mg
- 60 mg
- 100 mg
Dosing
Adults (opiate-naïve)
- 15 mg every 8 - 12 hours
- Increase dose every 1 - 2 days as needed
Converting from other oral morphine meds
- Total daily morphine dose will remain the same. Dose may given in halves every twelve hours or thirds every 8 hours.
Converting from parenteral morphine to oral
- Between 2 to 6 mg of oral morphine may be required to provide analgesia equivalent to 1 mg of parenteral morphine. Typically, a dose of morphine that is approximately three times the previous daily parenteral morphine requirement is sufficient.
- In chronic dosing, 3 mg of oral morphine for every 1 mg of parenteral morphine may be sufficient [3]
Discontinuation
- Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
- Do not discontinue abruptly
Generic / Price
- No generic
- 30 tablets - $$$$
Other
- DEA Schedule II
- Do not crush, cut, chew, or dissolve tablets. Swallow tablets whole.
- Tablet shell containing inactive ingredients may be seen in stool
Morphine sulfate ER (MS Contin®)
Dosage forms
Tablet, extended-release
- 15 mg
- 30 mg
- 60 mg
- 100 mg
- 200 mg
Dosing
Adults (opiate-naïve)
- 15 mg every 12 hours
- Increase dose at intervals of every 1 - 2 days
Children 1 - 12 years (opiate-naïve)
- 0.2 - 0.8 mg/kg every 12 hours [2]
Converting from other oral morphine meds
- Total daily morphine dose can be divided in half and given every 12 hours
- Total daily morphine dose may also be divided into thirds and given every 8 hours
Converting from parenteral morphine to oral
- Anywhere from 3 to 6 mg of oral morphine sulfate may be required to provide pain relief equivalent to 1 mg of parenteral morphine
- In chronic dosing, 3 mg of oral morphine for every 1 mg of parenteral morphine may be sufficient [3]
Discontinuation
- Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
- Do not discontinue abruptly
Generic / Price
- Generic (60 tablets) - $-$$$ depending on strength
Other
- DEA Schedule II
- Do not crush, cut, or chew tablets
- OPIOID ANTAGONISTS
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
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 - $$$$
Other
- Injection is given in upper arm, abdomen, or thigh. Rotate injection sites.
- Contraindicated in patients with GI obstruction and in those at increased risk of obstruction
- May increase risk of gastrointestinal perforation
- Discontinue all laxatives before starting. Laxatives may be added after 3 days if response to Relistor is suboptimal
Mechanism of action
- Methylnaltrexone is a selective opioid antagonist. It binds and blocks mu-opioid receptors in the periphery, but it does not cross the blood-brain barrier.
- Methylnaltrexone can help alleviate opioid-induced constipation by blocking mu-opioid receptors in the gastrointestinal tract. Since it does not enter the central nervous system, it does not affect the analgesic properties of opioids.
Naloxegol (Movantik®)
Dosage forms
Tablet
- 12.5 mg
- 25 mg
Dosing
Opioid-induced constipation in patients with chronic non-cancer pain
- Dosing: 25 mg once daily in the morning. Patients who cannot tolerate 25 mg may try 12.5 mg once daily.
- Take on an empty stomach at least 1 hour prior to the first meal of the day or 2 hours after the meal
- Kidney disease (CrCl < 60 ml/min: start with 12.5 mg once daily. If well tolerated, may increase to 25 mg once daily.
- Strong CYP3A4 inhibitors: DO NOT COMBINE
- Moderate CYP3A4 inhibitors: Not recommended. If must combine, use 12.5 mg once daily.
Generic / Price
- No generic
- 30 tablets - $$$$
Other
- Tablet may be crushed and mixed with 120 ml of water
- Contraindicated in patients with GI obstruction and in 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 a selective opioid antagonist. It binds and blocks mu-opioid receptors in the periphery, but its central nervous system (CNS) penetration is negligible.
- Naloxegol can help alleviate opioid-induced constipation by blocking mu-opioid receptors in the gastrointestinal tract. Since it does not penetrate the CNS well at recommended doses, it does not affect the analgesic properties of opioids.
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 (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)
- Initial: administer one spray in one nostril
- May give an additional spray every 2 - 3 minutes depending on response. Alternate nostrils.
- Use each nasal spray only one time
- Place patient on their back and provide support to the back of the neck to allow the head to tilt back before giving. Place patient on their side after giving.
- 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
- No generic
- 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)
- Initial: administer one spray in one nostril
- May give an additional spray every 2 - 3 minutes depending on response. Alternate nostrils.
- Use each nasal spray only one time
- Place patient on their back and provide support to the back of the neck to allow the head to tilt back before giving. Place patient on their side after giving.
- 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
- No generic
- Carton of 2 sprays - $$$
Pharmacokinetics
- Time to max concentration: 15 minutes
- Half-life 1.8 hours
Mechanism of action
- Naloxone hydrochloride is an opioid antagonist that antagonizes opioid effects by competing for the same receptor sites. Administration of naloxone hydrochloride reverses the effects of opioids, including respiratory depression, sedation and hypotension. It can also reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine.
Naltrexone (Revia®)
Dosage forms
Tablet
- 50 mg
Dosing
Alcohol use disorder
Opiate dependence
- Start with 25 mg once daily
- If no withdrawal signs occur, the dose may be increased to 50 mg once daily
- Naltrexone should not be used during acute opiate withdrawal
Generic / Price
- Generic - $
Other
- Naltrexone 50 mg a day should block the action of most parenterally administered opiates
- After stopping naltrexone, patients may be more sensitive to opioids and at greater risk for adverse events
Mechanism of action
- Naltrexone is an opioid antagonist. Naltrexone binds to opiate receptors and blocks the effects of opioid medications.
- The mechanism of action of naltrexone hydrochloride in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone hydrochloride, an opioid receptor antagonist, competitively binds to such receptors and may block the effects of endogenous opioids.
Naltrexone (Vivitrol®)
Dosage forms
Injectable suspension
- 380 mg vial
- Carton comes with vial, diluent, special needle and syringe
Dosing
Alcohol use disorder
Opiate dependence
- 380 mg intramuscularly every 4 weeks
- Naltrexone should not be used during acute opiate withdrawal
Generic / Price
- No generic
- One injection - $$$$
Other
- Dose should be administered by a healthcare provider
- Dose is given in the gluteus. Alternate buttocks with each injection.
- Vivitrol should only be administered with the needle and diluent that comes with it
- Allow Vivitrol to reach room temperature before injecting
- Vivitrol should be refrigerated. Vivitrol is good for 7 days when kept at room temperature.
- After stopping naltrexone, patients may be more sensitive to opioids and at greater risk for adverse events
Mechanism of action
- Naltrexone is an opioid antagonist. Naltrexone binds to opiate receptors and blocks the effects of opioid medications.
- The mechanism of action of naltrexone hydrochloride in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone hydrochloride, an opioid receptor antagonist, competitively binds to such receptors and may block the effects of endogenous opioids.
Efficacy
Methamphetamine abuse
Opiate abuse
- OXYCODONE
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
- Oxycodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
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
- Oxycodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
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
- Oxycodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
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
- Oxycodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
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) - $$$$
Other
- DEA Schedule II
- Duration of action: 3 - 4 hours
- Oxycodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
Oxycodone ER (Oxycontin®)
Dosage forms
Tablet, extended-release
- 10 mg
- 15 mg
- 20 mg
- 30 mg
- 40 mg
- 60 mg
- 80 mg
Dosing
Adults (opiate-naïve)
- 10 mg every 12 hours
- Increase dose every 1 - 2 days in increments of 25 - 50% of the current dose
Children ≥ 11 years
- Opiate-naïve
- Not recommended
- Opiate-tolerant
- Patients must be receiving opioids for at least 5 consecutive days
- Patients must be receiving ≥ 20 mg/day of oxycodone or its equivalent for the 2 days prior to starting
- See Oxycontin PI sec 2.4 for dose conversion table from other opioids
Converting from other oxycodone products
- Total daily oxycodone dose can be divided in half and given every 12 hours
Discontinuing therapy
- Taper the dose gradually, by 25% to 50% every 2 to 4 days and monitor for withdrawal symptoms
Generic / Price
- Generic (30 tablets) - $-$$$$, depending on the strength
Other
- DEA Schedule II
- Abuse-deterrent properties - when tablet is crushed and mixed with water, it forms a gel that is difficult to pull through a needle
- Oxycodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
Oxycodone ER (Xartemis® XR)
Dosage forms
Tablet, extended-release
- Oxycodone : Acetaminophen
- 7.5 mg: 325 mg
Dosing
Adults (opiate-naïve)
- Starting: 2 tablets every 12 hours
- The second dose of 2 tablets may be given as early as 8 hours after the initial dose in patients without adequate relief. Subsequent doses are to be administered 2 tablets every 12 hours.
- May take without regard to food
- In patients with renal and/or hepatic impairment, start with 1 tablet every 12 hours and titrate as needed
Discontinuing therapy
- Taper the dose gradually, by 25% to 50% every 2 to 4 days and monitor for withdrawal symptoms
Generic / Price
- No generic
- Tablet (#30) - $$
Other
- DEA Schedule II
- Xartemis is not interchangeable with other oxycodone products
- Do not break, chew, crush, cut, dissolve or split the tablets
- Do not exceed 4000 mg of acetaminophen/day
- Oxycodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
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) - $$$-$$$$, depending on the strength
Other
- DEA Schedule II
- Each dose of Xtampza should be taken with approximately the same amount of food in order to ensure consistent plasma levels are achieved. Food increases absorption, and absorption is higher with high-fat, high-calorie foods.
- Capsules may be opened and sprinkled on a small amount of soft food (e.g. applesauce, pudding). Swallow whole and do not chew. Rinse mouth.
- Contents of capsule may be given through feeding tube
- Abuse-deterrent properties - microspheres are difficult to manipulate for misuse and abuse
- Oxycodone is a sensitive CYP3A4 substrate. Use caution with CYP3A4 inducers and inhibitors.
- OXYMORPHONE
Oxymorphone IR (Opana®)
Dosage forms
Tablet
- 5 mg
- 10 mg
Dosing
Adults (opiate-naïve)
- 10 - 20 mg every 4 - 6 hours as needed
- Take on an empty stomach, at least one hour prior to or two hours after eating
- Kidney disease (CrCl < 50 ml/min): Use caution. Start with 5 mg dose.
- Liver disease (Child-Pugh A): Use caution. Start with 5 mg dose.
- Liver disease (Child-Pugh B/C): DO NOT USE
Converting from parenteral oxymorphone
- Given Opana’s absolute oral bioavailability of approximately 10%, patients receiving parenteral oxymorphone may be converted to oral Opana by administering 10 times the patient’s total daily parenteral oxymorphone dose as Opana, in four or six equally divided doses (e.g., [IV dose x 10] divided by 4 or 6)
- For example, approximately 10 mg of Opana four times daily may be required to provide pain relief equivalent to a total daily IM dose of 4 mg oxymorphone
Discontinuation
- Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
- Do not discontinue abruptly
Generic / Price
- Generic (30 tablets) - $$
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 - $$-$$$$, depending on strength
Other
- DEA Schedule II
- Do not crush, cut, chew, or dissolve tablets
- PENTAZOCINE
Pentazocine (Talwin NX®)
Dosage forms
Tablet
- Pentazocine 50 mg and naloxone 0.5 mg per tablet
Dosing
Adults
- One tablet every 3 - 4 hours
- May increase to 2 tablets when needed
- Do not exceed 12 tablets in 24 hours
Generic / Price
- Generic (30 tablets) - $
Other
- DEA Schedule IV
- Pentazocine is an opioid agonist/antagonist
- Pentazocine may antagonize the effects of stronger opiates (e.g. morphine, methadone)
- Pentazocine 50 mg is equivalent in analgesic activity to 60 mg of codeine
- Naloxone is an opioid antagonist. It has no effect when taken orally, but acts as an opioid antagonist when injected.
- TAPENTADOL
Tapentadol IR (Nucynta®)
Dosage forms
Tablet
- 50 mg
- 75 mg
- 100 mg
Dosing
Adults (opiate-naïve)
- 50 - 100 mg every 4 - 6 hours as needed
- On the first day of dosing, the second dose may be administered as soon as one hour after the first dose if adequate pain relief is not attained with the first dose. Subsequent dosing is 50 mg, 75 mg, or 100 mg every 4 to 6 hours and should be adjusted to maintain adequate analgesia with acceptable tolerability.
- Do not exceed 700 mg on the first day of therapy, and do not exceed 600 mg/day on subsequent days
Discontinuation
- Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
- Do not discontinue abruptly
Generic / Price
- No generic
- 30 tablets - $$$$
Other
- DEA Schedule II
- Tapentadol is a centrally-acting synthetic analgesic. Although its exact mechanism is unknown, analgesic efficacy is thought to be due to mu-opioid agonist activity and the inhibition of norepinephrine reuptake.
- The minimum effective plasma concentration of tapentadol for analgesia varies widely among patients
- Tapentadol should not be consumed with alcohol. Alcohol increases blood levels and can lead to overdose.
Tapentadol ER (Nucynta® ER)
Dosage forms
Tablet, extended-release
- 50 mg
- 100 mg
- 150 mg
- 200 mg
- 250 mg
Dosing
Adults (opiate-naïve)
- 50 mg every 12 hours
- Increase dose in increments of 50 mg at intervals of ≥ 3 days
- Do not exceed 500 mg/day
Converting from Nucynta® to Nucynta® ER
- Total daily dose of Nucynta® can be divided in half and given every 12 hours as Nucynta® ER
- Do not exceed 500 mg/day of Nucynta® ER
Discontinuation
- Taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal
- Do not discontinue abruptly
Generic / Price
- No generic
- 60 tablets - $$$$
Other
- DEA Schedule II
- Do not crush, cut, chew, or dissolve tablets
- Tapentadol is a centrally-acting synthetic analgesic. Although its exact mechanism is unknown, analgesic efficacy is thought to be due to mu-opioid agonist activity and the inhibition of norepinephrine reuptake.
- The minimum effective plasma concentration of tapentadol for analgesia varies widely among patients
- Tapentadol should not be consumed with alcohol. Alcohol increases blood levels and can lead to overdose.
- TRAMADOL
Tramadol IR | Ultram® | Qdolo®
Dosage forms
Tablet (Ultram®)
- 50 mg
Solution (Qdolo®)
- 5 mg/ml
- Comes in 473 ml bottle
- Store at room temperature
Dosing
Patients not requiring rapid analgesia
- Start with 25 mg/day and titrate in 25 mg increments as separate doses every 3 days to reach 100 mg/day (25 mg four times a day). Thereafter the total daily dose may be increased by 50 mg as tolerated every 3 days to reach 200 mg/day (50 mg four times a day).
- Do not exceed 300 mg/day in patients > 75 years old
- Do not exceed 400 mg in 24 hours
- 50 - 100 mg every 4 - 6 hours as needed
- Do not exceed 300 mg/day in patients > 75 years old
- Do not exceed 400 mg in 24 hours
Generic / Price
- Tablets (#30) - YES/$
- Solution (250 ml) - NO/$$$$
Other
- DEA Schedule IV
- Tablets are scored so they can be halved
- 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. Tramadol should be used with caution when taken with other serotonergic drugs (see serotonin syndrome for more).
- Patients who are allergic to opiates should not receive tramadol
- Tramadol lowers the seizure threshold and increases the risk of seizures. Seizure risk may also be increased when taken with SSRIs, TCAs, other opioids, MAO inhibitors, and neuroleptics.
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
Generic / Price
- Generic (30 tablets) - $
Other
- DEA Schedule IV
- 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. Tramadol should be used with caution when taken with other serotonergic drugs (see serotonin syndrome for more).
- Patients who are allergic to opiates should not receive tramadol
- Tramadol lowers the seizure threshold and increases the risk of seizures. Seizure risk may also be increased when taken with SSRIs, TCAs, other opioids, MAO inhibitors, and neuroleptics.
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
Generic / Price
- Generic (30 tablets) - $
Other
- DEA Schedule IV
- Do not crush, cut, or chew tablet
- 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. Tramadol should be used with caution when taken with other serotonergic drugs (see serotonin syndrome for more).
- Patients who are allergic to opiates should not receive tramadol
- Tramadol lowers the seizure threshold and increases the risk of seizures. Seizure risk may also be increased when taken with SSRIs, TCAs, other opioids, MAO inhibitors, and neuroleptics.
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
Generic / Price
- No Generic
- Price (30 capsules) - $$$$
Other
- DEA Schedule IV
- Do not crush, cut, chew, or open capsule
- Tramadol is a synthetic opioid that acts at opiate receptors in the central nervous system
- Tramadol has been shown to inhibit reuptake of norepinephrine and serotonin. Tramadol should be used with caution when taken with other serotonergic drugs (see serotonin syndrome for more).
- Patients who are allergic to opiates should not receive tramadol
- Tramadol lowers the seizure threshold and increases the risk of seizures. Seizure risk may also be increased when taken with SSRIs, TCAs, other opioids, MAO inhibitors, and neuroleptics.
Seglentis® (celecoxib + tramadol)
Dosage forms
Tablet
- Celecoxib - Tramadol
- 56 mg - 44 mg
Dosing
Acute pain (adults)
- Dosing: 2 tablets every 12 hours as needed
- May take without regard to food
- Celecoxib is a selective NSAID. See celecoxib for more.
Generic / Price
- NO/$$$ for #30- SIDE EFFECTS
- Respiratory depression - all opiates can suppress respiratory drive and cause death. Patients and caregivers should be able to recognize symptoms of respiratory depression (e.g. shallow breathing, confusion, decreased alertness, blue skin) and be prepared to call 911 should they occur. Naloxone should also be made available to highly susceptible patients.
- Constipation - most common side effect of opiates. Typically does not improve with continued use. Increased fiber, stool softeners, and laxatives may be necessary in some patients.
- Nausea and vomiting - common side effect. Typically diminishes with continued use.
- Urinary retention - occurs through both central and peripheral mechanism. Naltrexone reverses opioid-induced urinary retention.
- Pruritus (itching) - thought to occur through central mu-opioid receptor-mediated mechanisms. Presence of rash or hives may indicate true opiate allergy as opposed to side effect. May treat with antihistamines, promethazine, or naloxone in severe cases.
- Mental status changes - delirium, sedation, confusion, and impaired cognitive function may occur with all opiates. Elderly patients may be more susceptible.
- Male hypogonadism - chronic opiate use suppresses GnRH synthesis and may lead to hypogonadism (low testosterone) in males
- Infertility - prolonged opiate use may reduce fertility in males and females. It is unknown if these effects are reversible upon discontinuation.
- Hypotension (low blood pressure) - opiates may lower blood pressure in some patients
- Adrenal insufficiency - cases of adrenal insufficiency have been associated with opiate use, particularly chronic use. Presentation of adrenal insufficiency may include non-specific symptoms and signs including nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure.
- PRECAUTIONS / CONTRAINDICATIONS
- All opiates
- Drug addiction and abuse - opiates are both physically and psychologically addictive. Use with caution in susceptible patients.
- Central sleep apnea - opiates can cause or worsen central sleep apnea. Use caution.
- Pulmonary disease - opiates suppress respiratory drive and may lead to hypoxia and even death in patients with respiratory disease. Use with caution in susceptible patients.
- Intestinal disorders - opiates inhibit bowel peristalsis and can worsen some bowel conditions. Use with caution in patients with intestinal disorders.
- Withdrawal syndrome - abruptly stopping opiates after chronic therapy may lead to withdrawal reactions including diarrhea, nausea and vomiting, confusion, somnolence, visual hallucinations, and dysphoria. Taper dose slowly depending on the situation and medication.
- Head injury and increased intracranial pressure - use caution in patients with head injuries or increased intracranial pressure. Opiates may suppress respiratory drive causing CO₂ retention which increases intracranial pressure.
- Elderly patients - elderly patients are more susceptible to the side effects of opiates. Use caution.
- Hypotension - opiates may cause severe hypotension. Use caution in susceptible patients (e.g. dehydration, heart disease, etc.).
- Pregnancy - prolonged use of opioids in pregnancy can lead to neonatal opioid withdrawal syndrome which may be life-threatening
- Seizure disorders - opiates may lower the seizure threshold in some patients
- Biliary disease - opiates may cause spasm of the sphincter of Oddi. Use caution in patients with biliary disease or pancreatitis. Meperidine and pentazocine may not have this effect.
- Kidney disease - opiate clearance is decreased in kidney disease. Use caution.
- Liver disease - opiate clearance is decreased in liver disease. Use caution.
- Buprenorphine
- Prolonged QT interval - buprenorphine can prolong the QT interval, particularly at higher doses. Use caution in patients at increased risk for QT prolongation (e.g. heart disease, hypokalemia, hypomagnesemia). Do not use in patients with history of Long QT Syndrome or an immediate family member with this condition.
- 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.
- Oral mucositis (Belbuca®) - 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.
- 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.
- Liver disease (Belbuca®)
- Severe liver disease (Child-Pugh C): reduce starting dose and titration dose by half, from 150 mcg to 75 mcg
- Codeine
- Children < 12 years old - DO NOT USE. May cause breathing difficulties and death.
- Adolescents 12 - 18 years old who are obese or have conditions such as obstructive sleep apnea or severe lung disease - Not recommended. May cause breathing problems.
- Nursing mothers - Not recommended. May cause somnolence and breathing issues in breastfed infants.
- CYP2D6 poor/rapid metabolizers - Codeine has no analgesic activity unless it is metabolized into morphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine while rapid metabolizers may experience toxicity. Because of the risk for toxicity, codeine is contraindicated for postoperative pain in children.
- Dihydrocodeine
- Dihydrocodeine has no analgesic activity unless it is metabolized into dihydromorphine by CYP2D6. Poor metabolizers may not receive any pain relief from codeine while rapid metabolizers may experience toxicity. Because of the risk for toxicity, dihydrocodeine is contraindicated for postoperative pain in children.
- Fentanyl
- Bradycardia (slow heart rate) - fentanyl may cause bradycardia. Use caution in at-risk patients.
- Hydrocodone
- Prolonged QT interval - extended-release hydrocodone products (e.g. Hysingla, Zohydro) may cause QT prolongation. Do not use in patients with congenital long QT syndrome. [8]
- Hydromorphone (Dilaudid®, Exalgo®)
- Sulfites - hydromorphone contains sulfites. Do not use in sulfite-sensitive patients.
- Liver disease (Exalgo®)
- Moderate liver disease (Child-Pugh B): start with 25% of the usual Exalgo dose; titrate slowly and monitor closely
- Severe liver disease (Child-Pugh C): consider alternative
- Kidney disease (Exalgo®)
- Moderate kidney disease (CrCl 40 - 60 ml/min): start with 50% of the usual Exalgo dose; titrate slowly and monitor closely
- Severe kidney disease (CrCl < 30 ml/min): start with 25% of the usual Exalgo dose; titrate slowly and monitor closely
- Meperidine
- Seizures - prolonged use of meperidine may cause accumulation of its metabolite, normeperidine. Normeperidine has been associated with an increased risk of seizures.
- Serotonin syndrome - meperidine has serotonergic activity. Use caution in susceptible patients.
- Supraventricular tachycardia (SVT) - meperidine may increase the ventricular response rate in patients with SVTs. Use caution.
- Methadone
- Prolonged QT interval - methadone can prolong the QT interval. Baseline and periodic EKG may be indicated in patients at increased risk.
- Naltrexone
- Liver toxicity - naltrexone has been associated with cases of hepatitis. Patients with liver disease (hepatitis C, alcoholism, etc.) may be at greater risk.
- Oxycodone
- Liver disease - clearance is decreased. Use 1/3 to 1/2 the recommended starting dose.
- Pentazocine
- Hypertension - pentazocine may raise blood pressure in some patients
- Tramadol
- Children < 12 years old - DO NOT USE. May cause breathing difficulties and death.
- Children < 18 years old to treat pain after surgery to remove the tonsils and/or adenoids - DO NOT USE. May cause breathing difficulties and death.
- Adolescents 12 - 18 years old who are obese or have conditions such as obstructive sleep apnea or severe lung disease - Not recommended. May cause breathing problems.
- Nursing mothers - Not recommended. May cause somnolence and breathing issues in breastfed infants.
- Seizure risk - tramadol lowers the seizure threshold and increases the risk of seizures. Seizure risk may also be increased when taken with SSRIs, TCAs, other opioids, MAO inhibitors, and neuroleptics.
- Serotonin syndrome- tramadol has been shown to inhibit reuptake of norepinephrine and serotonin. Tramadol should be used with caution when taken with other serotonergic drugs.
- 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.
- Kidney disease
- CrCl < 30 ml/min: increase dosing interval to every 12 hours, max dose is 200 mg/day (standard-release products only, do not use extended-release products)
- Cirrhosis - recommended dose in 50 mg every 12 hours (standard-release products only, do not use extended-release products)
- DRUG INTERACTIONS
- All opiates
- Central Nervous System (CNS) Depressants - opiates may potentiate the effects of other CNS depressants (e.g., sedatives, alcohol, anxiolytics, hypnotics, neuroleptics, other opioids)
- Benzodiazepines - combined use of benzodiazepines and opiates may result in profound sedation, respiratory depression, coma, and death. Use caution when combining and strongly consider prescribing naloxone for emergency use.
- Muscle relaxers - opiates may enhance the neuromuscular blocking action of skeletal muscle relaxants and increase the risk of respiratory depression. Use caution when combining and strongly consider prescribing naloxone for emergency use.
- Anticholinergic medications - opiates may potentiate the urinary retention and constipating effects of anticholinergic medications
- MAO inhibitors - MAO inhibitors may potentiate the effects of opiates and vice versa
- Tricyclic antidepressants - tricyclic antidepressants may potentiate the effects of opiates and vice versa
- Diuretics - opiates may reduce the efficacy of diuretics by inducing ADH release
- Serotonergic drugs - opiates may potentiate the effects of serotonergic medications and increase the risk of serotonin syndrome
- Cimetidine (Tagamet®) - cimetidine may potentiate the respiratory depression seen with opiate medications. Use caution.
- Benzhydrocodone (Apadaz®)
- CYP3A4 inhibitors and inducers - benzhydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase blood levels and the risk of adverse effects. CYP3A4 inducers may decrease blood levels. Stopping concomitant CYP3A4 inducers may increase benzhydrocodone blood levels.
- Buprenorphine
- CYP3A4 inhibitors and inducers - buprenorphine is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may raise blood levels of buprenorphine and increase the risk of adverse effects. CYP3A4 inducers may decrease blood levels of buprenorphine. Stopping concomitant CYP3A4 inducers may raise buprenorphine blood levels and increase the risk of adverse effects.
- Benzodiazepines - benzodiazepines may potentiate the respiratory-depressing effects of buprenorphine. Deaths have been reported when combined. Use caution.
- Drugs that prolong the QT interval - buprenorphine may prolong the QT interval. Do not take buprenorphine with other medications that may prolong the QT interval.
- Butorphanol
- CYP3A4 inhibitors and inducers - butorphanol is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may raise blood levels of butorphanol and increase the risk of adverse effects. CYP3A4 inducers may decrease blood levels of butorphanol. Stopping concomitant CYP3A4 inducers may raise butorphanol blood levels and increase the risk of adverse effects.
- Benzodiazepines - benzodiazepines may potentiate the respiratory-depressing effects of butorphanol. Deaths have been reported when combined. Use caution.
- Codeine
- CYP3A4 inducers - may decrease effectiveness of codeine
- CYP2D6 inhibitors - codeine is metabolized by CYP2D6 to morphine. CYP2D6 inhibitors may decrease the effectiveness of codeine.
- Dihydrocodeine
- CYP2D6 inhibitors - dihydrocodeine is metabolized by CYP2D6 to dihydromorphine. CYP2D6 inhibitors may decrease the effectiveness of dihydrocodeine.
- Fentanyl
- CYP3A4 inhibitors and inducers - fentanyl is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase blood levels and the risk of adverse effects. CYP3A4 inducers may decrease blood levels. Stopping concomitant CYP3A4 inducers may increase fentanyl blood levels.
- Hydrocodone
- CYP3A4 inhibitors and inducers - hydrocodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase blood levels and the risk of adverse effects. CYP3A4 inducers may decrease blood levels. Stopping concomitant CYP3A4 inducers may increase hydrocodone blood levels.
- Drugs that prolong the QT interval - extended-release hydrocodone products (e.g. Hysingla, Zohydro) may cause QT prolongation. Use caution if combining with other QT interval prolonging drugs. [8]
- Meperidine
- Serotonergic drugs - meperidine has serotonergic activity. Use caution when combining with other serotonergic medications.
- Acyclovir - acyclovir may increase blood levels of meperidine
- Cimetidine (Tagamet®) - cimetidine may reduce the clearance of meperidine
- Phenytoin - phenytoin may increase the clearance of meperidine and increase levels of normeperidine
- Ritonavir - ritonavir may increase exposure to normeperidine
- Methadone
- CYP3A4 inhibitors and inducers - methadone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase blood levels and the risk of adverse effects. CYP3A4 inducers may decrease blood levels. Stopping concomitant CYP3A4 inducers may increase methadone blood levels.
- Drugs that prolong the QT interval - methadone may prolong the QT interval. Use caution if prescribed with other QT-prolonging drugs
- Antiretroviral agents - abacavir, amprenavir, efavirenz, nelfinavir, nevirapine, ritonavir, lopinavir+ritonavir combination - may increase the clearance of methadone; didanosine and stavudine - methadone may decrease levels; zidovudine - methadone may increase levels
- Morphine
- P-glycoprotein inhibitors - p-glycoprotein inhibitors may increase exposure to morphine. Use caution when combining.
- Oxycodone
- CYP3A4 inhibitors and inducers - oxycodone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors may increase blood levels and the risk of adverse effects. CYP3A4 inducers may decrease blood levels. Stopping concomitant CYP3A4 inducers may increase oxycodone blood levels.
- CYP2D6 inhibitors - oxycodone is a minor substrate of CYP2D6. If oxycodone is taken with a CYP2D6 inhibitor and a CYP3A4 inhibitor, exposure may be increased. Use caution.
- Tapentadol
- Alcohol - do not consume alcohol with tapentadol. Alcohol can increase blood levels of tapentadol leading to overdose
- Serotonergic drugs - serotonin syndrome has occurred in patients taking tapentadol with other serotonergic drugs. Use caution.
- Tramadol
- CYP3A4 inhibitors and inducers - tramadol is a CYP3A4 substrate. CYP3A4 inhibitors and inducers may affect tramadol levels.
- CYP2D6 inhibitors and inducers - tramadol is a CYP2D6 substrate. CYP2D6 inhibitors and inducers may affect tramadol levels.
- Drugs that lower seizure threshold - tramadol lowers the seizure threshold and increases the risk of seizures. Seizure risk may also be increased when taken with SSRIs, TCAs, other opioids, MAO inhibitors, and neuroleptics.
- Drugs with serotonergic activity - tramadol has been shown to inhibit reuptake of norepinephrine and serotonin. Tramadol should be used with caution when taken with other serotonergic drugs.
- OPIATE-TOLERANT DEFINITION
- Opiate-tolerant is defined as receiving one of the following around-the-clock on a regular basis:
- ≥ 60 mg of oral morphine daily
- ≥ 30 mg of oral oxycodone daily
- ≥ 8 mg of oral hydromorphone daily
- ≥ 25 mcg/hour of transdermal fentanyl
- ≥ 25 mg of oral oxymorphone daily
- An equianalgesic dose of another opioid for a week or longer [3,6]
- OPIOID ANALGESIC EQUIVALENCE TABLE
Analgesic equivalent doses for select opioids | |
---|---|
Opioid | Equivalent analgesic oral dose |
Morphine | 30 mg |
Oxycodone | 15 - 20 mg |
Hydrocodone | 30 - 45 mg |
Hydromorphone | 7.5 mg |
Codeine | 200 mg |
Pentazocine | 166 mg |
Fentanyl (transdermal) | every 2 mg/day of morphine is approximately equivalent to 1 mcg/hr of transdermal fentanyl |
Methadone | See Methadone dosing in opiate table |
- URINARY METABOLITES OF OPIATES
URINARY METABOLITES OF OPIATES | ||
---|---|---|
Opiate | Urinary metabolite | Comment |
Codeine |
|
|
Buprenorphine |
|
|
Fentanyl |
|
|
Heroin |
|
|
Hydrocodone |
|
|
Hydromorphone |
|
|
Methadone |
|
|
Morphine |
|
|
Oxycodone |
|
|
Oxymorphone |
|
|
- WHO SHOULD CARRY NALOXONE
- Overview
- The U.S. Department of Health and Human Services recommends patients who meet any of the criteria below be prescribed naloxone injection or nasal spray (see naloxone) for use in cases of accidental overdose
- Patients Prescribed Opioids Who:
- Are receiving opioids at a dosage of 50 morphine milligram equivalents (MME) per day or greater (see opiate equivalence table)
- Have respiratory conditions such as chronic obstructive pulmonary disease (COPD) or obstructive sleep apnea (regardless of opioid dose)
- Have been prescribed benzodiazepines (regardless of opioid dose)
- Have a non-opioid substance use disorder, report excessive alcohol use, or have a mental health disorder (regardless of opioid dose)
- Patients at high risk for experiencing or responding to an opioid overdose, including individuals:
- Using heroin, illicit synthetic opioids or misusing prescription opioids
- Using other illicit drugs such as stimulants, including methamphetamine and cocaine, which could potentially be contaminated with illicit synthetic opioids like fentanyl
- Receiving treatment for opioid use disorder, including medication-assisted treatment with methadone, buprenorphine, or naltrexone
- With a history of opioid misuse that were recently released from incarceration or other controlled settings where tolerance to opioids has been lost [11]
- OPIATE TAPERING RECOMMENDATIONS
- Overview
- In 2016, the U.S. Veteran's Administration issued broad recommendations for tapering opiates in order to avoid withdrawal symptoms and rebound pain. Those guidelines are summarized below.
- Slowest taper - Consider for patients taking high doses of long-acting opiates for many years
- Reduce dose by 2 - 10% every 4 - 8 weeks with pauses in taper as needed
- Slower taper - Appropriate for most patients
- Reduce dose by 5 - 20% every 4 weeks with pauses in taper as needed
- Faster taper - May cause withdrawal symptoms that need to be treated
- Reduce dose by 10 - 20% every week
- Fastest taper - May cause withdrawal symptoms that need to be treated
- Reduce dose by 20 - 50% on first day, then reduce dose by 10 - 20% every day [10]
- OPIATE WITHDRAWAL TREATMENT
TREATMENT OF OPIATE WITHDRAWAL | ||
---|---|---|
Symptoms | Medication | Dosing |
Autonomic overactivity (elevated pulse and blood pressure, anxiety, chills, piloerection) |
Clonidine |
|
Lofexidine (Lucemyra™) |
|
|
Alternative treatments |
|
|
Insomnia | Temazepam |
|
Trazodone |
|
|
Anxiety | Diazepam |
|
Hydroxyzine |
|
|
Lacrimation, rhinorrhea | Hydroxyzine |
|
Diphenhydramine |
|
|
Diarrhea | Loperamide (Imodium®) |
|
Joint pain, body aches | NSAIDs / Acetaminophen |
|
Nausea and vomiting | Antiemetics |
|
Abdominal cramping | Dicyclomine |
|
- DEA SCHEDULES
- Schedule I
- The drug or other substance has a high potential for abuse
- The drug or other substance has no currently accepted medical use in treatment in the United States
- There is a lack of accepted safety for use of the drug or other substance under medical supervision
- Examples: cocaine, heroin, lsd, etc.
- Schedule II
- The drug or other substance has a high potential for abuse
- The drug or other substance has a currently accepted medical use in treatment in the United States or a currently accepted medical use with severe restrictions
- Abuse of the drug or other substances may lead to severe psychological or physical dependence
- Schedule III
- The drug or other substance has a potential for abuse less than the drugs or other substances in schedules I and II
- The drug or other substance has a currently accepted medical use in treatment in the United States
- Abuse of the drug or other substance may lead to moderate or low physical dependence or high psychological dependence
- Schedule IV
- The drug or other substance has a low potential for abuse relative to the drugs or other substances in schedule III
- The drug or other substance has a currently accepted medical use in treatment in the United States
- Abuse of the drug or other substance may lead to limited physical dependence or psychological dependence relative to the drugs or other substances in schedule III
- Schedule V
- The drug or other substance has a low potential for abuse relative to the drugs or other substances in schedule IV
- The drug or other substance has a currently accepted medical use in treatment in the United States
- Abuse of the drug or other substance may lead to limited physical dependence or psychological dependence relative to the drugs or other substances in schedule IV
- PRICE ($) INFO
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
- BIBLIOGRAPHY
- 1 - Package insert for drug unless otherwise specified
- 2 - PMID 23720867 - WHO guidelines on the pharmacological treatment of persisting pain in children with medical illnesses
- 3 - PMID 23946177 NCCN Adult Cancer Pain GL
- 4 - PMID 24685458 - APS methadone GL
- 5 - PMID 12362012 NEJM pediatric pain review
- 6 - Actiq PI
- 7 - Pentazocine PI
- 8 - CredibleMeds website
- 9 - PMID 27464203 - opiate withdrawal
- 10 - Pain Management Opioid Taper Decision Tool: A VA Clinician's Guide, (2016)
- 11 - PMID 34751711 - Higher-Dose Naloxone Nasal Spray (Kloxxado) for Opioid Overdose, JAMA (2021)