Chronic obstructive pulmonary disease:
62.5 mcg (1 inhalation) oral inhalation once daily
General Dosage Information:
Safety and efficacy are not established in pediatric patients.
Chronic obstructive pulmonary disease
Mechanism of Action
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 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
Upper respiratory infection (5%)
Severe hypersensitivity to milk proteins
umeclidinium or any product component
Anticholinergics There are potential for an additive interaction with concomitantly used
medicines. Therefore, avoid coadministration of
Umeclidinium with other
anticholinergic-containing drugs as this may lead to an increase in
Time for Maximum Plasma Concentration (Tmax):
Inhalation: 5 to 15 minutes
Protein binding: 89%
Volume of Distribution (Vd): 86 L
Metabolism: oxidation followed by conjugation
Substrate of CYP2D6 and P-glycoprotein
Renal: less than 1% (oral) to 22% (IV)
Fecal: 58% (IV) to 92% (oral)
Avoid co administration with other
Hypersensitivity reactions (anaphylaxis, angioedema, pruritus, rash, and urticaria) have been reported; discontinue use with occurrence
Worsening narrow-angle glaucoma may occur; monitoring recommended
urinary retention may occur, especially in patients with prostatic hyperplasia or bladder-neck obstruction; monitoring recommended
Acute bronchospasm; avoid use
Loss of bronchoconstriction control may indicate
disease deterioration; immediate re-evaluation recommended
paradoxical bronchospasm may occur; symptomatic
treatment and discontinuation required
Infant risk cannot be ruled out.
Improvement or maintenance of
respiratory function in patients with COPD may indicate efficacy
Respiratory function, with symptoms suggestive of
How to Take or Administration
For oral inhalation only
at the same time
Opening and closing the device without an inhalation will result in a lost dose
When ready for a dose, open the cover
of the inhaler; a click will be heard and the counter will decrease to indicate the device is ready
Before inhaling the dose, breathe out fully;
do not exhale into the device
Place device firmly between lips and inhale with a long, deep, steady breath through the mouth;
do not breathe in through nose or cover air vent on the inhaler
Hold breath for 3 to 4 seconds or for as long as comfortable, and exhale slowly
is not reusable; discard 6 weeks after opening, or when dose counter reads zero (whichever comes first)
62.5 MCG/1 Actuation
Mild to Moderate Toxicity:
The vast majority of pharmaceutical overdoses that produce the
anticholinergic toxidrome requires only supportive care; administer
activated charcoal if the patient presents shortly after ingestion; sedate patients with benzodiazepines for agitation and delirium. Hypertension and tachycardia are generally
mild and well tolerated, and
do not require specific
treatment. Physostigmine can
be used to establish a diagnosis; it may help avoid an invasive, costly work-up, but should only be given in a setting where intensive monitoring and resuscitation is possible, and should NOT be given if the history or ECG (QRS widening) suggests tricyclic antidepressant poisoning.
Management of Severe Toxicity:
Orotracheal intubation for airway protection should be performed early. May benefit from gastric lavage if patient presents soon after a large ingestion; administer
activated charcoal. GI decontamination should only be performed in patients who can protect their airway or who are intubated. Severe delirium may develop and require large
doses of benzodiazepines for sedation. Seizures (may progress to status epilepticus) may require aggressive
use of benzodiazepines, propofol and/or barbiturates. Monitor core temperature and
treat hyperthermia with aggressive benzodiazepine sedation to control agitation, and external cooling. Clinical manifestations may be prolonged due to prolonged absorption
in the setting of
Varies with the specific medication. In general, patients will have to ingest large
doses of plant products (or make a tea) to develop symptoms.
Patient Counselling or Clinical Teaching
Instruct patient to seek immediate medical attention if their symptoms get worse or if they need more inhalations from their rescue inhaler than usual.
Advise patient that drug
is not to
be used to relieve
acute symptoms and extra
doses should not
be used for that purpose. Instruct patient to treat
acute symptoms with a short-acting beta-agonist rescue inhaler..
Side effects may include
upper respiratory tract infection, cough, joint pain, muscle pain, or upper abdominal pain.
Advise patient to report signs/symptoms of acute narrow-angle glaucoma (e.g., eye pain or discomfort, blurred vision, visual halos or colored images in association with red eyes from conjunctival congestion and corneal edema).
Instruct patient to report signs/symptoms of
urinary retention (e.g., difficulty passing urine, painful urination).
to take drug
at the same time
every day and not use it more than once every
Advise patient on proper preparation
of the delivery device, and inhalation technique.
Advise patient that there are multiple significant drug-drug interactions for this drug. Consult a healthcare professional prior to new drug use (including over-the-counter and herbal drugs).
Category of Umeclidinium :