Pulmonary – Anti-cholinergic agents (Inhaled)

Drug:  TUDORZA ® PRESSAIR ® (aclidinium bromide inhalation powder)
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ABBREVIATED MONOGRAPH - SEE PACKAGE INSERT.

Initial U.S. Approval:  2012

Mechanism of Action: Aclidinium bromide is a long-acting antimuscarinic agent, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo studies, prevention of acetylcholine-induced bronchoconstriction effects was dose-dependent and lasted longer than 24 hours. The clinical relevance of these findings is unknown. The bronchodilation following inhalation of aclidinium bromide is predominantly a site-specific effect.

INDICATIONS AND USAGE
TUDORZA PRESSAIR is an anticholinergic indicated for the long-term maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema.

DOSAGE AND ADMINISTRATION
For oral inhalation only

One inhalation of TUDORZA PRESSAIR 400 mcg twice daily.

DOSAGE FORMS AND STRENGTHS
Inhalation powder; The multi-dose device is a dry powder inhaler metering 400 mcg of aclidinium bromide per actuation.

CONTRAINDICATIONS
None.

WARNINGS AND PRECAUTIONS

Not for acute use: Not for use as a rescue medication. ( 5.1)
Paradoxical bronchospasm: Discontinue TUDORZA PRESSAIR and consider other treatments if paradoxical bronchospasm occurs. ( 5.2)
Worsening of narrow-angle glaucoma may occur. Use with caution in patients with narrow-angle glaucoma and instruct patients to consult a physician immediately if this occurs. ( 5.3)
Worsening of urinary retention may occur. Use with caution in patients with prostatic hyperplasia or bladder-neck obstruction and instruct patients to consult a physician immediately if this occurs. ( 5.4)
Immediate hypersensitivity reactions: Discontinue TUDORZA PRESSAIR at once and consider alternatives if immediate hypersensitivity reactions, including angioedema, bronchospasm, or anaphylaxis, occur. Use with caution in patients with severe hypersensitivity to milk proteins. ( 5.5)

Drug UPDATES:  SEEBRI™ NEOHALER® (glycopyrrolate) inhalation powder, for oral inhalation use
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U.S. Approval:  2015  [Initial U.S. Approval: 1961]

Mechanism of Action:  Glycopyrrolate is a long-acting muscarinic antagonist which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, glycopyrrolate exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo studies, prevention of methacholine-induced bronchoconstrictive effects was dose-dependent and lasted longer than 24 hours. The clinical relevance of these findings is unknown. The bronchodilation following inhalation of glycopyrrolate is predominantly a site-specific effect.

INDICATIONS AND USAGE:  SEEBRI™ NEOHALER® is indicated for the long-term, maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema.

HOW SUPPLIED: Inhalation powder: SEEBRI capsules contain 15.6 mcg of glycopyrrolate inhalation powder for use with the NEOHALER device

INDICATIONS AND USAGE
ATROVENT HFA Inhalation Aerosol is indicated as a bronchodilator for maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease, including chronic bronchitis and emphysema

Mechanism of Action
Ipratropium bromide is an anticholinergic (parasympatholytic) agent which, based on animal studies, appears to inhibit vagally mediated reflexes by antagonizing the action of acetylcholine, the transmitter agent released from the vagus nerve. Anticholinergics prevent the increases in intracellular concentration of cyclic guanosine monophosphate (cyclic GMP) which are caused by interaction of acetylcholine with the muscarinic receptor on bronchial smooth muscle.

Dosing (Adults):  (usual): Nebulization: 500 mcg (one vial) 3-4 times/day with doses 6-8 hours apart. Metered dose inhaler: 2 puffs 4 times/day - up to 12 puffs /24 hours.

Supplied: Nebulization (soln): 0.02% (2.5 ml). MDI: 18 mcg/actuation.

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ATROVENT HFA Inhalation Aerosol is supplied in a 12.9 g pressurized stainless steel canister as a metered-dose inhaler with a white mouthpiece that has a clear, colorless sleeve and a green protective cap (NDC 0597-0087-17).

The ATROVENT HFA Inhalation Aerosol canister is to be used only with the accompanying ATROVENT HFA Inhalation Aerosol mouthpiece. This mouthpiece should not be used with other aerosol medications. Similarly, the canister should not be used with other mouthpieces. Each actuation of ATROVENT HFA Inhalation Aerosol delivers 21 mcg of ipratropium bromide from the valve and 17 mcg from the mouthpiece. Each 12.9 gram canister provides sufficient medication for 200 actuations. The canister should be discarded after the labeled number of actuations has been used. The amount of medication in each actuation cannot be assured after this point, even though the canister is not completely empty.

Mechanism of Action
Tiotropium is a long-acting, antimuscarinic agent, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors, M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3-receptors at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo studies, prevention of methacholine-induced bronchoconstriction effects were dose-dependent and lasted longer than 24 hours. The bronchodilation following inhalation of tiotropium is predominantly a site-specific effect.

INDICATIONS AND USAGE
SPIRIVA HandiHaler (tiotropium bromide inhalation powder) is indicated for the long-term, once-daily, maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema.

CONTRAINDICATIONS
SPIRIVA® HandiHaler® (tiotropium bromide inhalation powder) is contraindicated in patients with a history of hypersensitivity to atropine or its derivatives, including ipratropium, or to any component of this product.

Dosing:
Oral inhalation: Adults: Contents of 1 capsule (18 mcg) inhaled once daily using HandiHaler® device

Supplied:
Powder for oral inhalation [capsule]: 18 mcg/capsule [contains lactose; packaged in 6s or 30s with HandiHaler® device]

Drug UPDATES:  SPIRIVA® RESPIMAT® (tiotropium bromide) inhalation spray, for oral inhalation
Initial U.S. Approval: 2004
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U.S. Approval:  2014

Mechanism of Action: Tiotropium is a long-acting, antimuscarinic agent, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors, M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3-receptors at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo studies, prevention of methacholine-induced bronchoconstriction effects was dose-dependent and lasted longer than 24 hours. The bronchodilation following inhalation of tiotropium is predominantly a site-specific effect.

INDICATIONS AND USAGE:  SPIRIVA RESPIMAT is an anticholinergic indicated for:
The long-term, once-daily, maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD), and for reducing COPD exacerbations (1.1)
The long-term, once-daily, maintenance treatment of asthma in patients 12 years of age and older (1.2)
Limitation of Use:
Not indicated for relief of acute bronchospasm.

DOSAGE AND ADMINISTRATION
To receive the full dose of medication, SPIRIVA RESPIMAT must be administered as two inhalations once-daily. Do not take more than one dose (2 inhalations) in 24 hours.

Prior to first use, the SPIRIVA RESPIMAT cartridge is inserted into the SPIRIVA RESPIMAT inhaler and the unit is primed. When using the unit for the first time, patients are to actuate the inhaler toward the ground until an aerosol cloud is visible and then repeat the process three more times. The unit is then considered primed and ready for use. If not used for more than 3 days, patients are to actuate the inhaler once to prepare the inhaler for use. If not used for more than 21 days, patients are to actuate the inhaler until an aerosol cloud is visible and then repeat the process three more times to prepare the inhaler for use [see Patient Counseling Information (17)].

2.1 Chronic Obstructive Pulmonary Disease
The recommended dosage for patients with COPD is 2 inhalations of SPIRIVA RESPIMAT 2.5 mcg per actuation once-daily; total dose equals 5 mcg of SPIRIVA RESPIMAT.

2.2 Asthma
The recommended dosage for patients with asthma is 2 inhalations of SPIRIVA RESPIMAT 1.25 mcg per actuation once-daily; total dose equals 2.5 mcg of SPIRIVA RESPIMAT. In the treatment of asthma, the maximum benefits in lung function may take up to 4 to 8 weeks of dosing [see Patient Counseling Information (17)].

2.3 Special Populations
No dosage adjustment is required for geriatric, hepatically-impaired, or renally-impaired patients. However, patients with moderate to severe renal impairment given SPIRIVA RESPIMAT should be monitored closely for anticholinergic effects [see Warnings and Precautions (5.6), Use in Specific Populations (8.5, 8.6, 8.7), and Clinical Pharmacology (12.3)].

HOW SUPPLIED: Inhalation spray: 1.25 mcg or 2.5 mcg tiotropium per actuation with the SPIRIVA RESPIMAT inhaler. Two actuations equal one dose (2.5 mcg or 5 mcg).

Drug UPDATES:  INCRUSE ELLIPTA (umeclidinium inhalation powder) FOR ORAL INHALATION USE
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Initial U.S. Approval:  2013-2014

Mechanism of Action: Umeclidinium is a long-acting, antimuscarinic agent, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through the inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo studies, prevention of methacholine and acetylcholine-induced bronchoconstrictive effects was dose-dependent and lasted longer than 24 hours. The clinical relevance of these findings is unknown. The bronchodilation following inhalation of umeclidinium is predominantly a site-specific effect.

INDICATIONS AND USAGE:   INCRUSE ELLIPTA is an anticholinergic indicated for the long-term, once-daily, maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD).

HOW SUPPLIED: Inhalation Powder. Inhaler containing a double-foil blister strip of powder formulation for oral inhalation. Each blister contains umeclidinium 62.5 mcg.
INCRUSE ELLIPTA should be stored inside the unopened moisture-protective foil tray and only removed from the tray immediately before initial use. Discard INCRUSE ELLIPTA 6 weeks after opening the foil tray or when the counter reads "0" (after all blisters have been used), whichever comes first. The inhaler is not reusable. Do not attempt to take the inhaler apart.