Zafirlukast


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Chronic asthma
Adult: 20 mg bid.
Child: 5-11 years old 10 mg bid. ≥12 years old Same as adult dose.
Hepatic Impairment
Contraindicated.
Cách dùng
Should be taken on an empty stomach. Take at least 1 hr before or 2 hr after meals.
Chống chỉ định
Hepatic impairment including hepatic cirrhosis.
Thận trọng
Not indicated for use in the reversal of bronchospasm in acute asthma attacks. Avoid abruptly substitution to oral or inhaled corticosteroids. Renal impairment. Pregnancy and lactation.
Phản ứng phụ
Systemic eosinophilia, eosinophilic pneumonia or w/ clinical features of systemic vasculitis consistent w/ Churg-Strauss syndrome; neuropsychiatric adverse events (e.g. insomnia, depression); headache, resp tract infection, GI disturbances, arthralgia, myalgia, fever, malaise, insomnia, dizziness, elevated liver enzyme values, hypersensitivity reactions (e.g. rashes, pruritus, urticaria, angioedema), agranulocytosis, bleeding, bruising, oedema.
Potentially Fatal: Severe hepatotoxicity.
Monitoring Parameters
Monitor for improvements in air flow; monitor closely for sign/symptoms of hepatic injury; periodic monitoring of LFTs.
Quá liều
Symptoms: Rash and stomach upset. Management: Supportive and symptomatic treatment. Empty the stomach by inducing emesis or by gastric lavage. May administer activated charcoal to prevent absorption of unrecovered drug.
Tương tác
May enhance anticoagulant activity of warfarin resulting to increased prothrombin time. Decreased plasma levels w/ theophylline, terfenadine and erythromycin. Increased plasma levels w/ fluconazole and high dose aspirin.
Food Interaction
Food reduces the rate and extent of absorption.
Tác dụng
Description: Zafirlukast is a selective and competitive leukotriene-receptor antagonist (LTRA) of leukotriene D4 and E4 (LTD4 and LTE4), components of slow-reacting substance of anaphylaxis (SRSA). Cysteinyl leukotriene production and receptor occupation have been correlated w/ the pathophysiology of asthma, including airway oedema, smooth muscle constriction, and altered cellular activity associated w/ the inflammatory process, which contribute to the signs and symptoms of asthma.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Food reduces the rate and extent of absorption. Time to peak plasma concentration: Approx 3 hr.
Distribution: Volume of distribution: Approx 70 L. Plasma protein binding: Approx 99% (primarily to albumin).
Metabolism: Extensively metabolised in the liver, mainly by CYP2C9 isoenzyme.
Excretion: Mainly via faeces (approx 90%) as unchanged drug and metabolites and urine (approx 10%) as metabolites. Terminal elimination half-life: Approx 10 hr.
Đặc tính

Chemical Structure Image
Zafirlukast

Source: National Center for Biotechnology Information. PubChem Database. Zafirlukast, CID=5717, https://pubchem.ncbi.nlm.nih.gov/compound/Zafirlukast (accessed on Jan. 24, 2020)

Bảo quản
Store between 20-25°C. Protect from light and moisture.
References
Accolate Tablet. U.S. FDA. https://www.fda.gov/. Accessed 30/09/2014.

Anon. Zafirlukast. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/10/2014.

Buckingham R (ed). Zafirlukast. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/09/2014.

McEvoy GK, Snow EK, Miller J et al (eds). Zafirlukast. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 30/09/2014.

Zafirlukast Tablet, Film-Coated (AstraZeneca Pharmaceuticals LP). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 30/09/2014.

Thông báo miễn trừ trách nhiệm: Thông tin này được MIMS biên soạn một cách độc lập dựa trên thông tin của Zafirlukast 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