Inhalation/Respiratory Maintenance therapy in chronic obstructive pulmonary disease
Adult: Available preparations:
Dry powder inhaler releasing Umeclidinium 62.5 mcg and vilanterol 25 mcg per actuation
Dry powder inhaler releasing Umeclidinium 55 mcg and vilanterol 22 mcg per actuation
1 inhalation once daily.
Chống chỉ định
Asthma. Acute episodes of bronchospasm or acutely deteriorating COPD. Concomitant use with other long-acting β2-agonists.
Patient with CV disease (e.g. cardiac insufficiency, arrhythmias, hypertension), diabetes mellitus, narrow-angle glaucoma, hypokalaemia, prostatic hyperplasia/bladder neck obstruction, seizure disorders, thyrotoxicosis. Concomitant use with other long-acting muscarinic antagonists. Not indicated for the relief of acute bronchospasm or for asthma treatment. Pregnancy and lactation.
Monitor pulmonary function test (e.g. FEV1, peak flow). Obtain blood pressure and heart rate. Assess ocular changes and signs of CNS stimulation.
Umeclidinium: Additive effect with other anticholinergic drugs.
Vilanterol: Increased exposure with strong CYP3A4 inhibitors (e.g. ketoconazole, clarithromycin). Increased risk of hypokalaemia with methylxanthine derivative, steroids or non-K-sparing diuretics. Diminished bronchodilatory effect with β-adrenergic blockers. Increased risk of CV adverse effects with MAOIs, and TCAs. Potentially Fatal: Enhanced adverse effect with other long-acting β2-adrenergic agonists (e.g. formoterol, salmeterol).
Description: Umeclidinium is a long-acting quaternary ammonium antimuscarinic agent. It competitively and reversibly inhibits acetylcholine at type 3 muscarinic (M3) receptors in the bronchial smooth muscles thereby causing bronchodilation.
Vilanterol is a selective, long-acting β2-adrenergic agonist. It stimulates the production of cyclic adenosine-3’,5’-monophosphate (cAMP) by activation of adenyl cyclase which results in the relaxation of bronchial smooth muscle. Pharmacokinetics: Absorption: Rapidly absorbed via lungs. Time to peak plasma concentration: 5-15 minutes.
Umeclidinium: Absolute bioavailability: Approx 13%.
Vilanterol: Absolute bioavailability: Approx 27%. Distribution: Umeclidinium: Volume of distribution: 86 L. Plasma protein binding: Approx 89%.
Vilanterol: Volume of distribution: 165 L. Plasma protein binding: Approx 94%. Metabolism: Umeclidinium: Metabolised in the liver by CYP2D6 by oxidation via hydroxylation and O-dealkylation, followed by glucuronidation into metabolites and is a substrate of P-glycoprotein transporter.
Vilanterol: Undergoes extensive 1st pass metabolism in the liver by CYP3A4 via O-dealkylation into metabolites. Excretion: Umeclidinium: Mainly via faeces (92%); urine (<1%). Plasma elimination half-life: 11 hours.
Vilanterol: Mainly via urine (70% as metabolites); faeces (30% as metabolites). Plasma elimination half-life: Approx 11 hours.
Store between 20-25°C. Protect from direct heat or sunlight.
R03AL03 - vilanterol and umeclidinium bromide ; Belongs to the class of combination of adrenergics with anticholinergics, that may also include a corticosteroid. Used in the treatment of obstructive airway diseases.
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