Stavudine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
HIV infection
Adult: <60 kg: 30 mg 12 hrly; ≥60 kg: 40 mg 12 hrly.
Child: Birth to 13 days 0.5 mg/kg 12 hrly; ≥14 days <30 kg: 1 mg/kg 12 hrly; ≥30 kg: Same as adult dose.
Suy thận
CrCl (mL/min) Dosage
<26 <60 kg: 15 mg 24 hrly; ≥60 kg: 20 mg 24 hrly. 
26-50 <60 kg: 15 mg 12 hrly; ≥60 kg: 20 mg 12 hrly.
Cách dùng
May be taken with or without food.
Hướng dẫn pha thuốc
Oral soln: Reconstitute w/ purified water to provide a soln containing 1 mg/mL.
Chống chỉ định
Hypersensitivity to stavudine. Lactation.
Thận trọng
Patient w/ hepatomegaly, hepatitis or other risk factors for liver disease (esp obese women); pre-existing bone marrow suppression; history of peripheral neuropathy; history of or risk factors for pancreatitis. Renal or hepatic impairment. Pregnancy.
Tác dụng không mong muốn
Peripheral neuropathy, abdominal pain, nausea, drowsiness, diarrhoea, dyspepsia, fatigue, dizziness, headache, abnormal dreams, depression, insomnia, pruritus, rash, immune reconstitution syndrome, lipodystrophy (including central obesity, facial and peripheral wasting, breast enlargement, cushingoid appearance, dorsocervical fat enlargement), metabolic abnormalities (e.g. hypertriglyceridaemia, hypercholesterolaemia, insulin resistance, hyperglycaemia, hyperlactataemia), mitochondrial dysfunction (manifesting as abnormal behaviour, convulsions, anaemia, hyperlipasaemia, hypertonia, neutropenia), myalgia, myositis, elevated creatine phosphokinase, osteonecrosis. Rarely, rhabdomyolysis.
Potentially Fatal: Lactic acidosis associated w/ severe hepatomegaly and steatosis. Rarely, hepatitis, hepatic failure, pancreatitis.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness and/or somnolence, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor LFTs, renal function tests, viral load, CD4 count.
Quá liều
Symptoms: Peripheral neuropathy and hepatic toxicity. Management: Supportive and symptomatic treatment.
Tương tác
Increased risk of pancreatitis, peripheral neuropathy and hepatotoxicity in combination w/ didanosine and hydroxycarbamide. Risk of hepatic decompensation w/ interferon and ribavirin. Risk of peripheral neuropathy w/ isoniazid. Zidovudine may decrease the phosphorylation of stavudine to its active triphosphate form. Doxorubicin and ribavirin may inhibit stavudine activation.
Tương tác với thức ăn
Food delays but does not reduce absorption.
Tác dụng
Description:
Mechanism of Action: Stavudine, a thymidine analogue, is converted intracellularly to the active metabolite stavudine triphosphate which inhibits HIV reverse transcriptase by competing w/ the natural substrate, thymidine triphosphate. It also inhibits viral DNA synthesis by causing DNA chain termination.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Bioavailability: Approx 86%. Time to peak plasma concentration: W/in 1 hr.
Distribution: Distributed into CSF. Crosses the blood-brain barrier and enters breast milk. Volume of distribution: 46 L.
Metabolism: Undergoes intracellular phosphorylation by thymidine kinase to the active metabolite, stavudine triphosphate.
Excretion: Via urine (95%, 74% as unchanged drug) and faeces (3%, 62% as unchanged drug). Elimination half-life: Approx 1-1.5 hr.
Đặc tính

Chemical Structure Image
Stavudine

Source: National Center for Biotechnology Information. PubChem Database. Stavudine, CID=18283, https://pubchem.ncbi.nlm.nih.gov/compound/Stavudine (accessed on Jan. 23, 2020)

Bảo quản
Store at 25°C. Reconstituted soln: Store between 2-8°C.
Phân loại MIMS
Thuốc kháng virus
Phân loại ATC
J05AF04 - stavudine ; Belongs to the class of nucleoside and nucleotide reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.
Tài liệu tham khảo
Anon. Stavudine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 10/02/2016 .

Buckingham R (ed). Stavudine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/02/2016 .

Joint Formulary Committee. Stavudine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/02/2016 .

McEvoy GK, Snow EK, Miller J et al (eds). Stavudine. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 10/02/2016 .

Stavudine Capsule (Mylan Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 10/02/2016 .

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