Dosing and uses of Incruse (umeclidinium bromide)
Adult dosage forms and strengths
powder for inhalation
- 62.5mcg/actuation
Chronic Obstructive Pulmonary Disease
Indicated for the long-term, once-daily, maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema
62.5 mcg (1 actuation) inhaled PO qDay
Dosage modifications
Renal impairment (including severe [CrCl <30 mL/min]): No dosage adjustment required
Moderate hepatic impairment (Child-Pugh 7-9): No dosage adjustment required
Severe hepatic impairment: Unknown, not evaluated
Geriatric patients: No dosage adjustment required
Administration
Inhaler is not reusable
Store at room temperature between 68-77°F (20-25°C); excursions permitted from 59-86°F (15-30°C)
Store in a dry place away from direct heat or sunlight
Before the inhaler is used for the first time, the counter should show the number 30 (7 if a sample or institutional pack); this is the number of doses in the inhaler
See prescribing information for detailed description regarding how to administer
Pediatric dosage forms and strengths
Safety and efficacy not established
Incruse (umeclidinium bromide) adverse (side) effects
1-10%
Nasopharyngitis (8%)
Upper respiratory tract infection (5%)
Cough (3%)
Arthralgia (2%
Toothache (1%)
Pharyngitis (1%)
Viral upper respiratory tract infection (1%)
Tachycardia (1%)
<1%
Atrial fibrillation
Warnings
Contraindications
Severe hypersensitivity to milk proteins
Demonstrated hypersensitivity to umeclidinium or any of the excipients
Cautions
Anaphylactic reactions reported in patients with severe milk protein allergy after inhalation of other powder products containing lactose (see Contraindications)
Do not initiate in patients during rapidly deteriorating or potentially life-threatening episodes of COPD; not be used for the relief of acute symptoms (ie, as rescue inhaler) from acute episodes of bronchospasm
Paradoxical bronchospasm reported; discontinue and treat immediately with an inhaled, prompt-acting bronchodilator (eg, albuterol)
Worsening of narrow-angle glaucoma may occur
Worsening of urinary retention may occur; caution in patients with prostatic hyperplasia or bladder-neck obstruction
Pregnancy and lactation
Pregnancy category: C
Lactation: Unknown if distributed in human breast milk
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.
Pharmacology of Incruse (umeclidinium bromide)
Mechanism of action
Long-acting muscarinic antagonist (LAMA) often referred to as an anticholinergic; blocks action of acetylcholine at muscarinic receptors (M1 to M5) in the bronchial airways (M3) by preventing increase in intracellular calcium concentration, leading to relaxation of airway smooth muscle, improved lung function, and decreased mucus secretion; dissociates slowly from M3 muscarinic receptors extending its duration of action
Absorption
Plasma levels not predictive of therapeutic effect
Peak plasma time: 5-15 minutes
Distribution
Following IV administration
Protein bound: 89% (umeclidinium)
Vd: 86 L (umeclidinium)
Metabolism
Primarily metabolized by CYP2D6 and is a substrate for the P-gp transporter
Primary metabolic routes for umeclidinium are oxidative (hydroxylation, O-dealkylation) followed by conjugation (eg, glucuronidation), resulting in a range of metabolites with either reduced pharmacological activity or for which the pharmacological activity has not been established
Systemic exposure to the metabolites is low
Elimination
Half-life: 11 hr
Umeclidinium (IV): 58% feces; 22% urine
Umeclidinium (PO): 92% feces; <1% urine
