Usage
Umeclidinium is prescribed 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. It is a long-acting muscarinic antagonist (LAMA), also known as an anticholinergic bronchodilator. Umeclidinium works by blocking the action of acetylcholine at muscarinic receptors in the lungs, leading to bronchodilation (widening of the airways). This helps to improve airflow and reduce symptoms such as shortness of breath, wheezing, and coughing. It is not indicated for the relief of acute bronchospasm or asthma.
Alternate Names
- Umeclidinium bromide (chemical name)
- Incruse Ellipta (brand name)
How It Works
Pharmacodynamics: Umeclidinium acts as a competitive and reversible antagonist at M3 muscarinic receptors in the smooth muscle of the airways. By blocking the bronchoconstricting effect of acetylcholine, it promotes bronchodilation, thereby improving lung function.
Pharmacokinetics:
- Absorption: Following oral inhalation, umeclidinium reaches peak plasma concentrations within 5 to 15 minutes. The systemic absorption is low, minimizing systemic side effects.
- Metabolism: Umeclidinium is primarily metabolized by CYP2D6 to several metabolites. However, CYP2D6 poor metabolizers do not experience clinically meaningful differences in systemic exposure.
- Elimination: Umeclidinium is eliminated primarily via feces, with a small portion excreted in urine. The terminal elimination half-life is approximately 11 hours.
Dosage
Standard Dosage
Adults:
One inhalation (62.5 mcg) once daily, administered at the same time each day via the Incruse Ellipta inhaler. The maximum dose is one inhalation per 24 hours.
Children:
Umeclidinium is not recommended for use in pediatric patients under 18 years of age. Safety and effectiveness have not been established in this population.
Special Cases:
- Elderly Patients: No dosage adjustment is required.
- Patients with Renal Impairment: No dosage adjustment is required.
- Patients with Hepatic Dysfunction: No dosage adjustment is required for mild to moderate hepatic impairment. Umeclidinium has not been studied in patients with severe hepatic impairment and should be used with caution in this population.
- Patients with Comorbid Conditions: Use with caution in patients with narrow-angle glaucoma, prostatic hyperplasia, or bladder-neck obstruction.
Clinical Use Cases
Umeclidinium is not indicated for:
- Intubation
- Surgical Procedures
- Mechanical Ventilation
- Intensive Care Unit (ICU) Use
- Emergency Situations (e.g., status epilepticus, cardiac arrest)
Side Effects
Common Side Effects:
- Nasopharyngitis
- Upper respiratory tract infection
- Cough
- Arthralgia
- Headache
- Back pain
Rare but Serious Side Effects:
- Hypersensitivity reactions (e.g., anaphylaxis, angioedema, urticaria)
- Paradoxical bronchospasm
- Urinary retention
- Worsening of narrow-angle glaucoma
- Atrial fibrillation
- QT prolongation (rare)
Long-Term Effects:
Limited data are available on the long-term effects of umeclidinium.
Contraindications
- Hypersensitivity to umeclidinium or any of the excipients, including lactose.
- Severe hypersensitivity to milk proteins.
Drug Interactions
- Anticholinergic agents: Concomitant use with other anticholinergics can increase the risk of anticholinergic adverse effects.
- CYP2D6 and P-gp inhibitors: Although umeclidinium is a substrate of CYP2D6 and P-gp, no clinically relevant drug interactions are expected with inhibitors of these pathways.
Pregnancy and Breastfeeding
- Pregnancy: Insufficient data in pregnant women. Animal studies do not indicate direct or indirect harmful effects on reproductive toxicity. Use only if the potential benefit to the mother justifies the potential risk to the fetus.
- Breastfeeding: It is unknown whether umeclidinium is excreted in human milk. A risk to the breastfed infant cannot be excluded. A decision should be made whether to discontinue breastfeeding or discontinue the drug, taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.
Drug Profile Summary
- Mechanism of Action: Muscarinic antagonist (M3) causing bronchodilation.
- Side Effects: Nasopharyngitis, upper respiratory tract infection, cough, arthralgia, paradoxical bronchospasm.
- Contraindications: Hypersensitivity to umeclidinium or milk proteins.
- Drug Interactions: Other anticholinergics.
- Pregnancy & Breastfeeding: Insufficient data; use with caution.
- Dosage: 62.5 mcg once daily via inhalation.
- Monitoring Parameters: Lung function (FEV1), respiratory symptoms, heart rate, adverse events.
Popular Combinations
Umeclidinium is often combined with vilanterol (a long-acting beta2-agonist) in a single inhaler (Anoro Ellipta) for enhanced bronchodilation. It can also be found in combination with fluticasone furoate and vilanterol (Trelegy Ellipta).
Precautions
- Not for acute bronchospasm.
- Caution in patients with narrow-angle glaucoma, urinary retention, or prostatic hyperplasia.
- Monitor for paradoxical bronchospasm.
- Monitor for cardiovascular effects.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Umeclidinium?
A: The recommended dosage for adults is 62.5 mcg once daily via oral inhalation using the Incruse Ellipta inhaler.
Q2: Can Umeclidinium be used to treat asthma?
A: No, umeclidinium is not indicated for the treatment of asthma. Its efficacy in asthma has not been established.
Q3: What are the common side effects of Umeclidinium?
A: Common side effects include nasopharyngitis, upper respiratory tract infection, cough, and arthralgia.
Q4: How should patients be instructed to use the Incruse Ellipta inhaler?
A: Patients should be instructed to exhale completely before inhaling the dose, place the mouthpiece between their lips, and inhale deeply and steadily through the inhaler. They should hold their breath for 3-4 seconds after inhalation, then exhale slowly.
Q5: Are there any contraindications to using Umeclidinium?
A: Yes, contraindications include hypersensitivity to umeclidinium, severe hypersensitivity to milk proteins, and use in patients younger than 18 years of age.
Q6: Does Umeclidinium interact with other medications?
A: Concomitant use with other anticholinergic medications may increase the risk of anticholinergic adverse effects.
Q7: Can Umeclidinium be used during pregnancy or breastfeeding?
A: There are limited data available on the use of umeclidinium during pregnancy and breastfeeding. It should be used with caution in these populations, and only if the potential benefit to the mother outweighs the potential risks to the fetus or infant.
Q8: How does Umeclidinium differ from other LAMAs?
A: While all LAMAs share a similar mechanism of action, they may have different pharmacokinetic properties, durations of action, and side effect profiles. Umeclidinium is a once-daily LAMA known for its generally good tolerability and low systemic absorption.
Q9: What should patients do if they miss a dose of Umeclidinium?
A: Patients should skip the missed dose and take the next dose at their regularly scheduled time. They should not double the dose to catch up.
