Usage
Vilanterol is a long-acting beta2-adrenergic agonist (LABA) 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. It is also used to reduce exacerbations of COPD in patients with a history of exacerbations. Vilanterol is also indicated for the maintenance treatment of asthma in certain patients. It is not indicated for the relief of acute bronchospasm. It is always used in combination with an inhaled corticosteroid (ICS) like fluticasone furoate. Therefore, Vilanterol itself is not prescribed alone but as part of combination inhalers.
Alternate Names
Vilanterol trifenatate is the full chemical name. It’s primarily known by its generic name, vilanterol. Brand names of combination inhalers containing vilanterol include Breo Ellipta (with fluticasone furoate), Anoro Ellipta (with umeclidinium), and Relvar Ellipta (with fluticasone furoate).
How It Works
Pharmacodynamics: Vilanterol, a LABA, relaxes the smooth muscle in the airways. This bronchodilation effect results from its binding to beta2-adrenergic receptors on airway smooth muscle cells, leading to an increase in intracellular cyclic adenosine monophosphate (cAMP). Increased cAMP levels activate protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular calcium concentrations, causing relaxation of the airway smooth muscle.
Pharmacokinetics:
- Absorption: Following oral inhalation, vilanterol is systemically absorbed.
- Metabolism: Vilanterol is primarily metabolized by cytochrome P450 (CYP) 3A4 isoenzyme.
- Elimination: Vilanterol is eliminated through both renal and hepatic pathways. The effective half-life for accumulation, determined from inhalation administration, is approximately 16 hours in individuals with asthma and about 21 hours in individuals with COPD.
Dosage
Vilanterol is always administered in fixed-dose combination with an inhaled corticosteroid. The dosage information below refers to the vilanterol component within these combination inhalers:
Standard Dosage
Adults:
- COPD: 25 mcg vilanterol (in combination with 100 mcg fluticasone furoate or 62.5 mcg umeclidinium) inhaled once daily.
- Asthma: 25 mcg vilanterol (in combination with 50 mcg, 100 mcg or 200 mcg fluticasone furoate), inhaled once daily.
Children:
- Asthma (5-11 years): 25 mcg vilanterol (with 50 mcg fluticasone furoate) inhaled once daily.
- Asthma (12-17 years): 25 mcg vilanterol (with 100 mcg fluticasone furoate) inhaled once daily.
- COPD: Use is not recommended in children.
Special Cases:
- Elderly Patients: No dosage adjustment is required.
- Patients with Renal Impairment: No dosage adjustment is required.
- Patients with Hepatic Dysfunction: Caution should be exercised due to potential increased risk of systemic effects of the corticosteroid component. No dosage adjustment of vilanterol itself is required, though the concomitant ICS might require adjustment.
- Patients with Comorbid Conditions: Evaluate patient-specific factors and consider any necessary adjustments in the concomitant ICS dosage.
Clinical Use Cases
Vilanterol is not indicated for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations like status epilepticus or cardiac arrest. It is strictly for maintenance treatment of COPD and asthma.
Dosage Adjustments
No specific dosage adjustments are required based on age, renal impairment, or hepatic impairment.
Side Effects
Common Side Effects
Common side effects reported with vilanterol-containing inhalers include: Upper respiratory tract infections, nasopharyngitis, headache, bronchitis, influenza, sinusitis, back pain, oropharyngeal pain, cough.
Rare but Serious Side Effects
Rare but serious side effects can include: Paradoxical bronchospasm, hypersensitivity reactions (including angioedema, urticaria), cardiovascular effects (palpitations, tachycardia).
Long-Term Effects
Potential long-term effects might include: Decreased bone mineral density, increased risk of pneumonia (in COPD patients), growth suppression in children (with ICS use).
Adverse Drug Reactions (ADR)
Clinically significant ADRs necessitating immediate intervention include severe hypersensitivity reactions like angioedema.
Contraindications
- Hypersensitivity to vilanterol or any components of the combination inhaler.
- Primary treatment of status asthmaticus or other acute episodes of COPD or asthma where intensive measures are required.
Drug Interactions
- Beta-blockers: May antagonize the bronchodilating effects of vilanterol.
- CYP3A4 Inhibitors: May increase vilanterol exposure and potentially increase the risk of adverse effects.
- CYP3A4 Inducers: May decrease vilanterol exposure.
Pregnancy and Breastfeeding
Vilanterol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether vilanterol is excreted in human milk. Caution should be exercised when administering to nursing women.
Drug Profile Summary
- Mechanism of Action: LABA, binds to beta2-adrenergic receptors, relaxes airway smooth muscle.
- Side Effects: Upper respiratory tract infections, nasopharyngitis, headache, paradoxical bronchospasm, hypersensitivity reactions.
- Contraindications: Hypersensitivity to vilanterol, acute bronchospasm.
- Drug Interactions: Beta-blockers, CYP3A4 inhibitors/inducers.
- Pregnancy & Breastfeeding: Use with caution if benefits outweigh risks.
- Dosage: 25 mcg once daily (in combination with an ICS).
- Monitoring Parameters: COPD or asthma symptoms, lung function tests.
Popular Combinations
Vilanterol is commonly combined with:
- Fluticasone furoate: An inhaled corticosteroid that reduces airway inflammation.
- Umeclidinium: A long-acting muscarinic antagonist (LAMA) that also bronchodilates.
Precautions
- General Precautions: Monitor for paradoxical bronchospasm and cardiovascular effects.
- Specific Populations: Use with caution in pregnant/breastfeeding women and in patients with hepatic impairment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Vilanterol?
A: Vilanterol is always given in combination with another medicine. The dose of vilanterol is 25 mcg once daily, by inhalation.
Q2: How does Vilanterol work?
A: Vilanterol is a LABA. It relaxes the muscles around the airways in your lungs, making it easier to breathe.
Q3: Can Vilanterol be used for acute asthma attacks?
A: No, Vilanterol is not a rescue inhaler and should not be used to treat acute asthma attacks or COPD exacerbations. A short-acting beta2-agonist (SABA) like albuterol should be used for acute symptoms.
Q4: What are the common side effects of Vilanterol?
A: Common side effects can include upper respiratory tract infections, headache, nasopharyngitis, and cough.
Q5: Are there any drug interactions with Vilanterol?
A: Yes, Vilanterol can interact with beta-blockers and some medications metabolized by CYP3A4. It’s crucial to inform your doctor about all other medicines you are taking.
Q6: Can Vilanterol be used during pregnancy?
A: Vilanterol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Discuss the risks and benefits with your doctor.
Q7: Can Vilanterol be used in children?
A: Vilanterol, in combination with fluticasone furoate, is approved for use in children aged 5 years and older for asthma. It is not recommended for use in children with COPD.
Q8: What should patients know about using Vilanterol?
A: Patients should understand that Vilanterol is for maintenance treatment, not rescue. They should also be aware of potential side effects and drug interactions and report any concerns to their doctor. They should also be instructed on proper inhaler technique.
Q9: What if a patient develops paradoxical bronchospasm after using Vilanterol?
A: Paradoxical bronchospasm is a rare but serious side effect. If it occurs, Vilanterol should be discontinued immediately and alternative treatment sought.