glycopyrrolate inhaled (Rx)

1-10%

Upper respiratory tract infection (3.4%)

Nasopharyngitis (2.1%)

Oropharyngeal pain (1.8%)

Urinary tract infection (1.4%)

Sinusitis (1.4%)

Contraindications

Hypersensitivity

Cautions

Should not be initiated in patients with acutely deteriorating or potentially life-threatening episodes of COPD; also do not use for the relief of acute symptoms (ie, as rescue therapy) for treating acute episodes of bronchospasm

Can produce paradoxical bronchospasm that may be life-threatening

Immediate hypersensitivity reactions have been reported after administration of indacaterol or glycopyrrolate

Worsening of narrow-angle glaucoma or urinary retention may occur; use with caution in patients with prostatic hyperplasia, or bladder-neck obstruction and instruct patients to contact a physician immediately if symptoms occur

Drug interaction overview

• Concomitant use with anticholinergic medications may cause additive anticholinergic effects; if possible, avoid coadministration

Pregnancy

There are no adequate and well-controlled studies in humans

Animal studies have not shown teratogenicity

Lactation

Unknown if distributed in human breast milk

Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Long-acting muscarinic antagonist (LAMA); often referred to as an anticholinergic; produces bronchodilation by inhibiting acetylcholine’s effect on muscarinic receptors in the airway smooth muscle

Absorption

Absolute bioavailability: 40%

Peak plasma time: 5 minutes

Distribution

Protein bound: 38-41%

Vd: 83-376 L

Metabolism

Hydroxylated to a variety of mono-and bishydroxylated metabolites and direct hydrolysis results in the formation of a carboxylic acid derivative (M9)

M9 is hydrolyzed by multiple CYP isoenzymes

Elimination

Half-life: 33-53 hr (glycopyrrolate inhaled)

Excretion: 60-70% urine; 30-40% nonrenal (mostly by metabolism; also biliary)

Oral Inhalation

Encapsulated powder for inhalation

• Do not swallow the capsules, as the intended effects on the lungs will not be obtained
• Seebri capsules should only be used with the Neohaler device
• Should be administered at the same time of the day, (1 capsule in the morning and 1 capsule in the evening), every day
• More frequent administration or a greater number of inhalations (>1 capsule BID) is not recommended

Solution for inhalation

• Lonhala vials should be used with Magnair device for nebulization only; do not use Magnair with any other vials
• Should be administered at the same time of the day, (1 vial in the morning and 1 vial in the evening), every day

Storage

Encapsulated powder for inhalation

• Store in a dry place at controlled room temperature (25°C [77°F]); excursions permitted to 15-30°C (59-86°F)
• Store capsules in the blister package that they are packaged in, and only remove immediately before use with the Neohaler device

Solution for inhalation

• Store vials in the protective foil pouch at 20-25°C (68-77°F)
• After opening the foil pouch, unused unit-dose vials should be returned to, and stored in, the foil pouch
• Once a foil pouch is opened, discard the vials if not used within 7 days
• An opened unit-dose vial should be used right away
• Discard any unit-dose vial if the solution is not colorless