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Umeclidinium Bromide; Indications, Dosage, Side Effects, Interaction, Pregnancy

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.

Umeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD). It is also approved for this indication in combination with vilanterol

Mechanism of Action of Umeclidinium Bromide

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 the M3 receptor at the smooth muscle leading to bronchodilation.

Indications of Umeclidinium Bromide

Chronic Obstructive Pulmonary Disease (COPD)
Bronchiectasis
Bronchospasm Prophylaxis
Bronchial asthma,
Chronic bronchitis,
Chronic bronchopulmonary disorders
Airflow obstruction in patients with chronic obstructive pulmonary disease (COPD),
Chronic bronchitis and/or emphysema.
Indicated for the long-term, once-daily, maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD).
Incruse is indicated as a maintenance bronchodilator treatment to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD).
Rolufta is indicated as a maintenance bronchodilator treatment to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD).

Contra-Indications of Umeclidinium Bromide

Thyrotoxicosis
Low amount of potassium in the blood
Diabetes
Ketoacidosis
Excess Body Acid
Low amount of potassium in the blood
High blood pressure
Diminished blood flow through arteries of the Heart
Prolonged QT interval on EKG
Abnormal heart rhythm
Abnormal EKG with QT changes from Birth
Kidney disease with reduction in kidney function
Seizures
Paradoxical bronchospasm

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The dosage of Umeclidinium Bromide

Strengths: 62.5 mcg (0.0625 mg)/inh

Chronic Obstructive Pulmonary Disease – Maintenance

1 inhalation (62.5 mcg) orally once a day
Maximum dose: 1 inhalation every 24 hours

Side Effects

The most common

Arm, back, or jaw pain
Chest pain or tightness
dry mouth
trembling or shaking of the hands or feet
stomach pain or cramping
diarrhea
headache
dizziness
confusion
stomach pain;
back pain, joint or muscle pain.
problems with your vision (including color vision);
sudden chest pain or trouble breathing;
pain or swelling in one or both legs;
migraine headache;
pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or
feeling like you might pass out.

More common

Abdominal or stomach pain, discomfort, or tenderness
chills or fever
difficulty with moving
a headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
discomfort in arms, shoulders, neck or upper back
excessive sweating
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
rust colored urine
decreased amount of urine

Rare

Anxiety
change in vision
chest pain or tightness
confusion
a cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
fainting
hallucinations
a headache
irritability
lightheadedness
mood or mental changes
muscle pain or cramps
muscle spasm or jerking of all extremities
nervousness

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Drug Interactions

Umeclidinium bromide may interact with the following drugs, supplements & may change the efficacy of drugs

antihistamines (e.g, cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
beta 2 agonists (e.g., salbutamol, formoterol, terbutaline)
beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
long-acting beta agonists (e.g., indacaterol, salmeterol)
citalopram
decongestant cold medications (e.g., phenylephrine, pseudoephedrine)
oral steroids such as prednisone, dexamethasone methylprednisolone, and others
diuretics (e.g., furosemide, hydrochlorothiazide)
domperidone
escitalopram
ipratropium
macrolide antibiotics (e.g., clarithromycin, erythromycin, telithromycin)
methadone
mirabegron
monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine)
quinolone antibiotics (e.g., levofloxacin moxifloxacin ofloxacin)
serotonin antagonists (anti-emetic medications; e.g., ondansetron granisetron, )
theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
thiazide diuretics (water pills; e.g., hydrochlorothiazide, indapamide, metolazone)
tolterodine
tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
aminophylline
theophylline

Pregnancy Catagory

FDA Pregnancy Category C

Pregnancy

In animal studies, pregnant animals were given this medication and there was no evidence of problems for the mother or offspring. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

Lactation

It is not known if umeclidinium crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication.