Acronyms
- Anticholinergic = Antimuscarinic
- ICS - Inhaled corticosteroid
- LABA - Long-acting beta agonist
- LAMA - Long-acting muscarinic antagonist
- NHLBI - National Heart, Lung, and Blood Institute
- RCT - Randomized controlled trial
- SABA - Short-acting beta agonist
- SAMA - Short-acting muscarinic antagonist
Ipratropium
Atrovent®
Atrovent®
Dosage forms
HFA Inhaler
- Delivers 17 mcg of ipratropium per actuation (200 actuations per inhaler)
Nebulizer
- Ipratropium 0.02% (0.5 mg/2.5 ml)
- Comes in package of 25 nebs
Dosing
COPD
- HFA inhaler
- Two puffs four times a day
- Max: 12 puffs in 24 hours
- Nebulizer
- One neb every 6 - 8 hours
Asthma Exacerbations
Generic / Price
- Atrovent HFA® - NO/$$$$
- Ipratropium nebs (25 nebs) - YES/$
Other
- Avoid spraying in eyes
- Ipratropium is an OCT2 inhibitor and may increase exposure to OCT2 substrates
Aclidinium
Tudorza Pressair®
Tudorza Pressair®
Dosage forms
Inhaler
- Delivers 400 mcg of aclidinium inhalation powder per actuation
- Comes in inhaler with 30 or 60 doses
Dosing
COPD
- One inhalation twice a day
- Discard inhaler 45 days after opening pouch
Efficacy
Generic / Price
- NO/$$$$
Other
- Avoid spraying in eyes
- Tudorza Pressair contains lactose and should not be used in severe milk allergy
Revefenacin
Yupelri®
Yupelri®
Dosage forms
Inhalation solution
- 175 mcg/3 ml vial
- Comes in carton with 30 vials
Dosing
COPD
- Dosing: One 175 mcg unit-dose vial once daily via nebulizer
- Do not mix with other nebulized medications
Efficacy
Generic / Price
- NO/$$$$
Other
- The active metabolite of revefenacin is an OATP1B1/B3 substrate, and OATP1B1/B3 inhibitors may increase its exposure. Co-administration is not recommended.
Tiotropium
Spiriva® Handihaler, Spiriva® Respimat
Spiriva® Handihaler, Spiriva® Respimat
Dosage forms
Spiriva® Handihaler
- Delivers 18 mcg of tiotropium inhalation powder per actuation
- Comes in carton with 30 or 90 capsules
Spiriva® Respimat
- Comes in two doses:
- Tiotropium 1.25 mcg/actuation
- Tiotropium 2.5 mcg/actuation
- Carton contains cartridge and inhaler
- Cartridge contains 60 metered sprays
Dosing - Handihaler
COPD
- One capsule once daily
- Two inhalations should be taken from device for each capsule
- May store at room temperature
- Use capsule immediately after removing from blister pack
Dosing - Respimat
COPD
- Two inhalations (5 mcg total) once daily
- Use 2.5 mcg inhaler in COPD
Asthma (≥ 6 years old)
- Two inhalations (2.5 mcg total) once daily
- Use 1.25 mcg inhaler in Asthma
- May take up to 8 weeks before full benefit is seen
Generic / Price
- NO/$$$$
Other
- Spiriva Handihaler® contains lactose and should not be used by patients with severe milk allergy
Umeclidinium
Incruse Ellipta®
Incruse Ellipta®
Dosage forms
Inhaler
- Delivers 62.5 mcg of umeclidinium inhalation powder per actuation
- Comes in package with 30 doses
Dosing
COPD
- One inhalation once daily
- Inhale at the same time each day
- Discard inhaler 6 weeks after opening foil pouch
Generic / Price
- NO/$$$$
Other
- Incruse Ellipta® contains lactose and should not be used by patients with severe milk allergy
Combivent Respimat®, Duoneb®
Albuterol + ipratropium
Albuterol + ipratropium
Dosage forms
Inhaler (Combivent Respimat®)
- Inhaler delivers 100 mcg of albuterol and 20 mcg of ipratropium per actuation
- Each inhaler contains 120 actuations
Nebulizer solution (Duoneb®)
- Ipratropium 0.5 mg/Albuterol 3 mg per 3 ml neb
- Comes in box of 30 or 60 nebs
Dosing - Respimat
Acute bronchospasm in COPD
- Dosing: One inhalation four times a day with up to two additional inhalations if required
- Max: Six inhalations in 24 hours
Acute asthma exacerbation
Dosing - Duoneb
Acute bronchospasm in COPD
- Dosing: One neb four times a day with up to two additional nebs if required
- Max: Six nebs in 24 hours
Acute asthma exacerbation
Generic / Price
- Combivent Respimat® - NO/$$$$
- Duoneb® - YES/$
Anoro Ellipta®
Vilanterol + umeclidinium
Vilanterol + umeclidinium
Dosage forms
Inhalation powder
- Each powder inhalation contains umeclidinium 62.5 mcg and vilanterol 25 mcg
- Inhaler comes with 30 inhalations
Dosing
COPD
- One inhalation once daily
Generic / Price
- NO/$$$$
Other
- Discard inhaler 6 weeks after opening the foil tray
- Anoro Ellipta® contains lactose and should not be used by patients with severe milk allergy
- Vilanterol is a CYP3A4 substrate, and strong CYP3A4 inhibitors may increase its exposure
- DO NOT USE in patients with congenital long QT syndrome [4]
Bevespi Aerosphere™
Formoterol + glycopyrrolate
Formoterol + glycopyrrolate
Dosage forms
Inhalation aerosol
- Device delivers 4.8 mcg of formoterol and 9 mcg of glycopyrrolate per actuation
- Each inhaler contains 120 inhalations
Dosing
COPD
- Two inhalations twice a day
Generic / Price
- NO/$$$$
Duaklir Pressair®
Aclidinium + formoterol
Aclidinium + formoterol
Dosage forms
Inhalation powder
- Device delivers 400 mcg of aclidinium and 12 mcg of formoterol powder per actuation
- Comes in 30 dose and 60 dose inhaler
- Inhaler is breath-actuated
Dosing
COPD
- One inhalation twice daily
Generic / Price
- NO/$$$$
Other
- Duaklir Pressair® contains lactose and should not be used by patients with severe milk allergy
- Inhaler is good for 2 months after removing from sealed bag
Stiolto® Respimat
Olodaterol + tiotropium)
Olodaterol + tiotropium)
Dosage forms
Inhalation spray
- Inhaler delivers tiotropium 3.124 mcg (equivalent to 2.5 mcg tiotropium) and olodaterol 2.736 mcg (equivalent to 2.5 mcg olodaterol) per spray
- Inhaler comes with 60 actuations
Dosing
COPD
- Two inhalations once daily
- Use at the same time every day
Generic
- NO/$$$$
Breztri Aerosphere™
Budesonide + glycopyrrolate + formoterol
Budesonide + glycopyrrolate + formoterol
Dosage forms
Inhalation aerosol
- Inhaler delivers 160 mcg of budesonide, 9 mcg of glycopyrrolate, and 4.8 mcg of formoterol per inhalation
- Inhaler comes with 120 inhalations
Dosing
COPD
- Two inhalations twice daily
Generic / Price
- NO/$$$$
Trelegy Ellipta®
Fluticasone + umeclidinium + vilanterol
Fluticasone + umeclidinium + vilanterol
Dosage forms
Inhalation powder
- Fluticasone / Umeclidinium / Vilanterol
- 100 mcg/62.5 mcg/25 mcg
- 200 mcg/62.5 mcg/25 mcg
- Inhaler comes with 30 inhalations
Dosing
COPD
- One inhalation once daily of 100/62.5/25 mcg
Asthma (adults)
- One inhalation once daily of 100/62.5/25 mcg or 200/62.5/25 mcg
- When choosing a dose consider disease severity and current dose of ICS
Generic / Price
- NO/$$$$
Other
- Trelegy Ellipta® contains lactose and should not be used by patients with severe milk allergy
- Vilanterol is a CYP3A4 substrate, and strong CYP3A4 inhibitors may increase its exposure
SIDE EFFECTS
- Overview
- Inhaled antimuscarinic side effects are generally mild and occur in less than 10% of patients
- Side effects include:
- Dry mouth
- Pupil dilation
- Cough
- Nasopharyngitis
- Rhinitis/sinusitis
- Urinary retention
- Headache
- Upper respiratory infection
PRECAUTIONS / CONTRAINDICATIONS
- Glaucoma - antimuscarinics may cause pupil dilation which can precipitate or worsen narrow-angle glaucoma
- Paradoxical bronchospasm - paradoxical bronchospasm after inhalation has been reported
- Benign prostatic hypertrophy (BPH) - antimuscarinics may worsen urinary retention associated with BPH
- Hypersensitivity reactions - hypersensitivity reactions including anaphylaxis have been reported
- Liver disease
- Ipratropium, Aclidinium, Revefenacin, Tiotropium: has not been studied extensively
- Umeclidinium: no dose adjustment necessary for Child-Pugh A or B; has not been studied in Child-Pugh C
- Kidney disease
- Ipratropium: has not been studied extensively
- Aclidinium, Revefenacin, Tiotropium, Umeclidinium: no dose adjustment necessary. Monitor for anticholinergic side effects.
DRUG INTERACTIONS
- NOTE: The drug interactions presented here are NOT all-inclusive. Other interactions may exist. Drug interaction checkers provide the most efficient and practical way to check for interactions among multiple medications. A free interaction checker is available from Drugs.com (see Drugs.com interactions checker).
- Anticholinergic medications - antimuscarinics have anticholinergic activity and may potentiate the effects of other anticholinergic drugs
NHLBI ASTHMA EXACERBATION TREATMENT RECOMMENDATIONS
PRICE ($) INFO
- $ = 0 - $50
- $$ = $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
| Patient Assistance Programs for Inhaled Antimuscarinics | ||||
|---|---|---|---|---|
| Drug | Manufacturer | Ships to | PAP info | Application |
| Anoro Ellipta® (vilanterol + umeclidinium) | GlaxoSmithKline | Patient or other | Link | Link |
| Atrovent® HFA (ipratropium) | Boehringer Ingelheim | Patient | Link | Link |
| Bevespi Aerosphere® (formoterol + glycopyrrolate) | AstraZeneca | Patient or doctor | Link | Link |
| Combivent® (albuterol + ipratropium) | Boehringer Ingelheim | Patient | Link | Link |
| Duaklir Pressair® (aclidinium + formoterol) | Circassia | N/A | N/A | N/A |
| Incruse Ellipta® (umeclidinium) | GlaxoSmithKline | Patient or other | Link | Link |
| Spiriva® handihaler and Respimat (tiotropium) | Boehringer Ingelheim | Patient | Link | Link |
| Stiolto Respimat® (olodaterol + tiotropium) | Boehringer Ingelheim | Patient | Link | Link |
| Trelegy Ellipta® (fluticasone + umeclidinium + vilanterol) | GlaxoSmithKline | Patient or other | Link | Link |
| Tudorza Pressair® (aclidinium) | Circassia | N/A | N/A | N/A |
| Yupelri® (revefenacin) | Mylan | N/A | N/A | N/A |
BIBLIOGRAPHY
- 1 - NHLBI 2007 asthma guidelines
- 2 - Manufacturer's package insert