Umeclidinium + Vilanterol


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Thận trọng
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.
Phản ứng phụ
Significant: Hypersensitivity reactions (e.g. anaphylaxis, angioedema, rash, urticaria), blood pressure and tachycardia, atrial fibrillation, hyperglycaemia, diabetes mellitus and ketoacidosis exacerbation; hypokalaemia, urinary retention, narrow-angle glaucoma, bladder outlet obstruction, CNS stimulation/excitation; thyrotoxicosis exacerbation.
Gastrointestinal disorders: Constipation, dry mouth, diarrhoea, abdominal pain, nausea, toothache.
Musculoskeletal and connective tissue disorders: Muscle pain, pain in extremity, neck pain.
Nervous system disorders: Headache, vertigo, tremor, dysgeusia.
Renal and urinary disorders: UTI.
Respiratory, thoracic and mediastinal disorders: Sinusitis, nasopharyngitis, pharyngitis, upper respiratory tract infection, cough, pleuritic chest pain.
Potentially Fatal: Increased risk of asthma-related deaths. Rarely, paradoxical bronchospasm.
Inhalation/Respiratory: C
MonitoringParameters
Monitor pulmonary function test (e.g. FEV1, peak flow). Obtain blood pressure and heart rate. Assess ocular changes and signs of CNS stimulation.
Tương tác
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).
Tác dụng
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.
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Umeclidinium, CID=11519070, https://pubchem.ncbi.nlm.nih.gov/compound/Umeclidinium (accessed on Jan. 23, 2020)


Chemical Structure Image
Vilanterol

Source: National Center for Biotechnology Information. PubChem Database. Vilanterol, CID=10184665, https://pubchem.ncbi.nlm.nih.gov/compound/Vilanterol (accessed on Jan. 23, 2020)

Bảo quản
Store between 20-25°C. Protect from direct heat or sunlight.
Phân loại ATC
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.
References
Anon. Umeclidinium and Vilanterol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/03/2018.

Anon. Umeclidinium. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/03/2018.

Anoro Ellipta Powder (GlaxoSmithKline LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Buckingham R (ed). Umeclidinium Bromide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/03/2018.

Buckingham R (ed). Vilanterol Trifenatate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/03/2018.

Joint Formulary Committee. Umeclidinium with Vilanterol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/03/2018.

McEvoy GK, Snow EK, Miller J et al (eds). Umeclidinium Bromide. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 05/03/2018.

McEvoy GK, Snow EK, Miller J et al (eds). Vilanterol Trifenatate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 05/03/2018.

Thông báo miễn trừ trách nhiệm: Thông tin này được MIMS biên soạn một cách độc lập dựa trên thông tin của Umeclidinium + Vilanterol từ nhiều nguồn tài liệu tham khảo và được cung cấp chỉ cho mục đích tham khảo. Việc sử dụng điều trị và thông tin kê toa có thể khác nhau giữa các quốc gia. Vui lòng tham khảo thông tin sản phẩm trong MIMS để biết thông tin kê toa cụ thể đã qua phê duyệt ở quốc gia đó. Mặc dù đã rất nỗ lực để đảm bảo nội dung được chính xác nhưng MIMS sẽ không chịu trách nhiệm hoặc nghĩa vụ pháp lý cho bất kỳ yêu cầu bồi thường hay thiệt hại nào phát sinh do việc sử dụng hoặc sử dụng sai các thông tin ở đây, về nội dung thông tin hoặc về sự thiếu sót thông tin, hoặc về thông tin khác. © 2021 MIMS. Bản quyền thuộc về MIMS. Phát triển bởi MIMS.com
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in