INHALED ANTIMUSCARINICS








Ipratropium (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

Dosing - Asthma Exacerbations

Generic / Price

  • Atrovent HFA® - NO/$$$$
  • Ipratropium nebs (25 nebs) - YES/$

Other

Atrovent HFA®
  • Does not require shaking
  • Prime before first use by releasing 2 test sprays
  • Re-prime inhaler if not used for more than 3 days
  • Avoid spraying in eyes
Nebulizer
  • May mix with albuterol. Use within one hour after mixing.
  • Protect nebs from sunlight

Mechanism of action

  • Anticholinergic - blocks muscarinic receptors on bronchial smooth muscle and reduces intrinsic vagal tone of the airway

FDA-approved indication

  • Chronic Obstructive Pulmonary Disease (COPD)
  • NHLBI 2007 asthma guidelines state that anticholinergic agents provide additive benefit to SABA in moderate-to-severe asthma exacerbations, and may be used as an alternative bronchodilator for patients who do not tolerate SABA

Side effects



Side effect Ipratropium Placebo
Bronchitis 10% 6%
Shortness of breath 8% 4%
Dizziness 3% 2%
Dry mouth 4% 2%
Nausea 4% 2%
Anticholinergic side effects
  • Pupil dilation - may cause pupils to dilate. Avoid spraying in eyes.
  • Urinary retention - may cause urinary retention
  • See anticholinergic medications for more

Drug interactions

Contraindications / Precautions

  • Glaucoma - ipratropium may cause pupil dilation which can precipitate or worsen narrow-angle glaucoma
  • Paradoxical bronchospasm - paradoxical bronchospasm has occurred in some patients
  • Benign prostatic hypertrophy (BPH) - ipratropium may worsen urinary retention seen in BPH
  • Liver disease - has not been studied extensively
  • Kidney disease - has not been studied extensively


Aclidinium (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/$$$$

Mechanism of action

  • Anticholinergic - blocks muscarinic receptors on bronchial smooth muscle and reduces intrinsic vagal tone of the airway

FDA-approved indication

  • Chronic Obstructive Pulmonary Disease (COPD)
  • Aclidinium is NOT indicated to treat acute bronchospasm

Side effects



Side effect Aclidinium Placebo
Headache 6.6% 5%
Nasopharyngitis 5.5% 3.9%
Cough 3% 2.2%
Diarrhea 2.7% 1.4%
Sinusitis 1.7% 0.8%
Rhinitis 1.6% 1.2%
Anticholinergic side effects
  • Pupil dilation - may cause pupils to dilate. Avoid spraying in eyes.
  • Urinary retention - may cause urinary retention
  • See anticholinergic medications for more

Drug interactions

Contraindications / Precautions

  • Severe allergy to milk proteins - DO NOT USE. Contains lactose.
  • Hypersensitivity reactions - hypersensitivity reactions including anaphylaxis have occurred
  • Glaucoma - aclidinium may cause pupil dilation which can precipitate or worsen narrow-angle glaucoma
  • Paradoxical bronchospasm - paradoxical bronchospasm has occurred in some patients
  • Benign prostatic hypertrophy (BPH) - aclidinium may worsen urinary retention seen in BPH
  • Liver disease - has not been studied extensively
  • Kidney disease - no dose adjustment necessary

Revefenacin (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/$$$$

Mechanism of action

  • Anticholinergic - blocks muscarinic receptors on bronchial smooth muscle and reduces intrinsic vagal tone of the airway

FDA-approved indication

  • Chronic Obstructive Pulmonary Disease (COPD)
  • Revefenacin is NOT indicated to treat acute bronchospasm

Side effects


Side effect Revefenacin
(N=395)		 Placebo
(N=418)
Cough 4% 4%
Nasopharyngitis 4% 2%
Upper respiratory tract infection 3% 2%
Headache 4% 3%
Back pain 2% 1%
Anticholinergic side effects
  • Pupil dilation - may cause pupils to dilate. Avoid spraying in eyes.
  • Urinary retention - may cause urinary retention
  • See anticholinergic medications for more

Drug interactions

Contraindications / Precautions

  • Hypersensitivity reactions - hypersensitivity reactions including anaphylaxis have occurred
  • Glaucoma - revefenacin may cause pupil dilation which can precipitate or worsen narrow-angle glaucoma
  • Paradoxical bronchospasm - paradoxical bronchospasm has occurred in some patients
  • Benign prostatic hypertrophy (BPH) - revefenacin may worsen urinary retention seen in BPH
  • Liver disease - has not been studied. Not recommended.
  • Kidney disease - no dose adjustment necessary. Monitor for systemic antimuscarinic side effects in patients with severe renal impairment.

Tiotropium | 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/$$$$

Mechanism of action

  • Anticholinergic - blocks muscarinic receptors on bronchial smooth muscle and reduces intrinsic vagal tone of the airway

FDA-approved indications

Spiriva® Handihaler
  • Chronic Obstructive Pulmonary Disease (COPD) - long-term maintenance and prevention of COPD exacerbations
  • Tiotropium is NOT indicated to treat acute bronchospasm
Spiriva® Respimat
  • Chronic Obstructive Pulmonary Disease (COPD) - tiotropium is indicated for long-term maintenance and prevention of COPD exacerbations
  • Asthma - maintenance treatment of asthma in patients 6 years of age and older
  • Tiotropium is NOT indicated to treat acute bronchospasm

Side effects



Side effect Spiriva Handihaler Placebo
Upper Respiratory infection 41% 37%
Dry mouth 16% 3%
Sinusitis 11% 9%
Pharyngitis 9% 7%
Chest pain 7% 5%
Urinary tract infection 7% 5%
Shortness of breath 6% 5%
Abdominal pain 5% 3%
Anticholinergic side effects
  • Pupil dilation - may cause pupils to dilate. Avoid spraying in eyes.
  • Urinary retention - may cause urinary retention
  • See anticholinergic medications for more
Side effect Spiriva Respimat Placebo
Pharyngitis 11.5% 10.1%
Cough 5.8% 5.5%
Dry mouth 4.1% 1.6%
Sinusitis 3.1% 2.7%
Anticholinergic side effects
  • Pupil dilation - may cause pupils to dilate. Avoid spraying in eyes.
  • Urinary retention - may cause urinary retention
  • See anticholinergic medications for more

Drug interactions

Contraindications / Precautions

  • Severe allergy to milk proteins (Handihaler® only) - DO NOT USE. Contains lactose.
  • Glaucoma - tiotropium may cause pupil dilation which can precipitate or worsen narrow-angle glaucoma
  • Paradoxical bronchospasm - paradoxical bronchospasm has occurred in some patients
  • Benign prostatic hypertrophy (BPH) - ipratropium may worsen urinary retention seen in BPH
  • Liver disease - has not been studied extensively
  • Kidney disease - CrCl ≤ 60 ml/min - monitor patient closely for anticholinergic side effects

Umeclidinium (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/$$$$

Mechanism of action

  • Anticholinergic - blocks muscarinic receptors on bronchial smooth muscle and reduces intrinsic vagal tone of the airway

FDA-approved indications

  • Chronic Obstructive Pulmonary Disease (COPD)
  • Umeclidinium is NOT indicated to treat acute bronchospasm

Side effects



Side effect Umeclidinium Placebo
Nasopharyngitis 8% 7%
Upper respiratory infection 5% 4%
Cough 3% 2%
Arthralgia 2% 1%
Anticholinergic side effects
  • Pupil dilation - may cause pupils to dilate. Avoid spraying in eyes.
  • Urinary retention - may cause urinary retention
  • See anticholinergic medications for more

Drug interactions

Contraindications / Precautions

  • Severe allergy to milk proteins - DO NOT USE. Contains lactose.
  • Glaucoma - umeclidinium may cause pupil dilation which can precipitate or worsen narrow-angle glaucoma
  • Paradoxical bronchospasm - paradoxical bronchospasm has occurred in some patients
  • Benign prostatic hypertrophy (BPH) - umeclidinium may worsen urinary retention seen in BPH
  • Kidney disease - no dose adjustment necessary
  • Liver disease
    • Mild-to-moderate (Child-Pugh A/B): no dose adjustment necessary
    • Severe (Child-Pugh C): has not been studied


Combivent Respimat® | Duoneb® | 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/$

Other

  • Combivent Respimat® is good for 3 months after first use
  • See Combivent Respimat® patient insert for priming instructions

FDA-approved indications

  • Chronic Obstructive Pulmonary Disease (COPD)
  • Relief of bronchospasm


Anoro Ellipta® (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

  • See Anoro Ellipta® PI for complete prescribing information
  • Discard inhaler 6 weeks after opening the foil tray
  • DO NOT USE in patients with severe milk allergy
  • Vilanterol is a CYP3A4 substrate. Use caution with strong CYP3A4 inhibitors.
  • DO NOT USE in patients with congenital long QT syndrome [4]

FDA-approved indications

  • Maintenance treatment of Chronic Obstructive Pulmonary Disease (COPD)
  • NOT for relief of acute bronchospasm

Bevespi Aerosphere™ (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/$$$$

Other

  • Inhaler must be primed. See package insert for instructions.
  • See Bevespi Aerosphere PI for complete prescribing information
  • Inhaler is good for 3 months after removal from foil pouch

FDA-approved indications

  • Chronic Obstructive Pulmonary Disease (COPD)
  • NOT for relief of acute bronchospasm

Duaklir Pressair® (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 a day

Generic / Price

- NO/$$$$

Other

  • Do not use in patients with severe milk allergy. Contains lactose.
  • Inhaler is good for 2 months after removing from sealed bag

FDA-approved indications

  • Chronic Obstructive Pulmonary Disease (COPD)
  • NOT for relief of acute bronchospasm

Stiolto® Respimat (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/$$$$

Other

  • See Stiolto® PI for complete prescribing information
  • Inhaler should be primed. See patient instructions for details

FDA-approved indications

  • Maintenance treatment of Chronic Obstructive Pulmonary Disease (COPD)
  • NOT for relief of acute bronchospasm


Breztri Aerosphere™ (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/$$$$

FDA-approved indication

  • Maintenance treatment of Chronic Obstructive Pulmonary Disease (COPD)
  • NOT for relief of acute bronchospasm

Trelegy Ellipta® (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

  • See Trelegy Ellipta® PI for complete prescribing information
  • Discard inhaler 6 weeks after opening the foil tray
  • DO NOT USE in patients with severe milk allergy
  • Vilanterol is a CYP3A4 substrate. Use caution with strong CYP3A4 inhibitors.

FDA-approved indication

  • Chronic Obstructive Pulmonary Disease (COPD) - maintenance treatment
  • Asthma - maintenance treatment in adults
  • NOT for relief of acute bronchospasm




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

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