Drug information of Umeclidinium


Drug group:

Umeclidinium is a long-acting muscarinic antagonist (LAMA) used as maintenance treatment for symptoms of chronic obstructive pulmonary disease (COPD). It is available as a once-daily inhalation monotherapy or as a fixed-dose combination product with the long-acting beta2-agonist vilanterol.
COPD is a progressive obstructive lung disease characterized by shortness of breath, cough, sputum production, and chronically poor airflow with a forced expiratory volume in 1 second (FEV1) of less than 80%. By blocking the M3 muscarinic receptor which is highly expressed in airway smooth muscle of the lungs, umeclidinium inhibits the binding of acetylcholine and thereby opens up the airways by preventing bronchoconstriction. Its use has been shown to provide clinically significant, sustained improvements in lung function

:Dosage Forms & Strengths
Powder for inhalation: 62.5 mcg/actuation

Mechanism of effect

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


Not Available


Plasma levels not predictive of therapeutic effect
Peak plasma time: 5-15 minutes

Following IV administration
Protein bound: 89%
Vd: 86 L

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

Half-life: 11 hr
Umeclidinium (IV): 58% feces; 22% urine
Umeclidinium (PO): 92% feces; <1% urine


62.5mcg (1 actuation) inhaled PO qDay


Anaphylactic reactions reported in patients with severe milk protein allergy after inhalation of other powder products containing lactose

Hypersensitivity reactions such as anaphylaxis, angioedema, pruritus, rash, and urticaria may occur; discontinue if reactions occur

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

Points of recommendation

:Adverse Effects
Nasopharyngitis, Upper respiratory tract infection, Cough, Arthralgia, Toothache, Pharyngitis, Viral upper respiratory tract infection, Tachycardia, Atrial fibrillation, Hypersensitivity reactions, Eye pain, Glaucoma, Vision blurred, Dysuria and Urinary retention

:Drug Interactions
Serious, Use Alternative: glucagon, glucagon intranasal, revefenacin
Monitor Closely: abobotulinumtoxinA, acetylcholine, aclidinium, amantadine, atropine, atropine IV/IM, atropine ophthalmic, belladonna alkaloids, bethanechol, carbachol, dicyclomine, echothiophate iodide, glycopyrrolate, glycopyrrolate inhaled, glycopyrronium tosylate topical, homatropine, hyoscyamine, hyoscyamine spray, ipratropium, methscopolamine, neostigmine, physostigmine, pilocarpine, pilocarpine ophthalmic, propantheline, pyridostigmine, scopolamine, tiotropium

Severe hypersensitivity to milk proteins
Demonstrated hypersensitivity to umeclidinium or any of the excipients

Pregnancy level

There are insufficient data on use in pregnant women to inform a drug-associated risk

:Animal Data
Administered via inhalation or subcutaneously to pregnant rats and rabbits was not associated with adverse effect on embryofetal development at exposures approximately 50 and 200 times, respectively, the human exposure at maximum recommended human daily inhaled dose » MRHDID

Breast feeding warning

There is no information available on presence of drug in human milk, effects on breastfed child, or on milk production; the drug was detected in plasma of offspring of lactating rats treated with umeclidinium suggesting its presence in maternal milk;
developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from umeclidinium or from underlying maternal condition

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