Nevirapine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
HIV-1 infection
Adult: In combination with other antiretroviral agents: Initially, 200 mg once daily for 14 days. Maintenance: As conventional tab: 200 mg bid. As extended release tab: 400 mg once daily.
Child: As conventional tablet or suspension in combination with other antiretroviral agents: Initially, 150 mg/m2 once daily for 14 days. Maintenance: 150 mg/m2 bid or as extended-release tab 400 mg once daily. ≥16 years or weighing ≥50 kg or with BSA >1.25 m2: Same as adult dose.
Suy thận
Patient on haemodialysis: An additional 200 mg should be given after dialysis treatment.
Suy gan
Moderate to severe (Child Pugh class B or C): Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Hypersensitivity. History of severe rash or rash accompanied by constitutional symptoms or clinical hepatitis caused by nevirapine. Use in postexposure prophylaxis (PEP) regimens. Moderate to severe hepatic impairment (Child Pugh class B or C). Lactation. Concomitant use with St. John’s wort.
Thận trọng
Patient with high CD4+ counts (>250 cells/mm3 in females or >400 cell/mm3 in males, chronic hepatitis B or C. Mild hepatic impairment (Child-Pugh class A). Pregnancy.
Tác dụng không mong muốn
Significant: Immune reconstitution syndrome, fat redistribution (e.g. central obesity, buffalo hump, peripheral wasting, facial wasting, breast enlargement, cushingoid appearance), rhabdomyolysis, elevated transaminase.
Blood and lymphatic system disorders: Granulocytopenia, neutropenia.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain.
General disorders and administration site conditions: Fever, fatigue.
Hepatobiliary disorders: Hepatitis.
Investigations: Increased serum cholesterol, LDL cholesterol, serum alanine aminotransferase, serum aspartate aminotransferase, amylase.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia.
Nervous system disorders: Headache.
Potentially Fatal: Stevens-Johnson syndrome, toxic epidermal necrolysis, hypersensitivity reactions with rash and organ dysfunction, hepatotoxicity.
Thông tin tư vấn bệnh nhân
This drug may cause fatigue, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor for signs of adverse skin reactions and hepatotoxicity for the first 18 weeks of treatment, particularly in the first 6 weeks. Monitor CBC, viral load; liver function at baseline then prior and after 2 weeks of dose escalation. Immediately evaluate transaminases level in patients with rash.
Tương tác
Increased risk of toxicity with efavirenz. May decrease serum concentration of atazanavir and lopinavir, boceprevir, telaprevir, clarithromycin, and methadone. Increased exposure with fluconazole.
Tương tác với thức ăn
Reduced plasma concentrations with St. John’s wort.
Tác dụng
Description:
Mechanism of Action: Nevirapine, a non-nucleoside reverse transcriptase inhibitor which binds directly to reverse transcriptase which inhibits the RNA-dependent and DNA-dependent DNA polymerase activities including HIV-1 replication.
Pharmacokinetics:
Absorption: Readily absorbed from the gastrointestinal tract. Bioavailability: 93% (conventional tab); approx 75% (extended release tab); 91% (oral solution). Time to peak plasma concentration: 4 hours (conventional tab/oral solution); approx 24 hours (extended release tab).
Distribution: Crosses placenta, enters breast milk and distributed in the CSF. Volume of distribution: 1.2 L/kg. Plasma protein binding: Approx 60%.
Metabolism: Extensively metabolised in the liver by CYP3A4 and CYP2B6 into several hydroxylated metabolites; undergoes enterohepatic recycling.
Excretion: Mainly via urine (approx 81% as metabolites; <3% as unchanged drug); faeces (approx 10%). Elimination half-life: 45 hours as single dose; decreases to 25-30 hours after multiple doses.
Đặc tính

Chemical Structure Image
Nevirapine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4463, Nevirapine. https://pubchem.ncbi.nlm.nih.gov/compound/Nevirapine. Accessed Apr. 28, 2021.

Bảo quản
Store at 25°C.
Phân loại MIMS
Thuốc kháng virus
Phân loại ATC
J05AG01 - nevirapine ; Belongs to the class of non-nucleoside reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.
Tài liệu tham khảo
Anon. Nevirapine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 23/09/2020.

Anon. Nevirapine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 23/09/2020.

Buckingham R (ed). Nevirapine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/09/2020.

Joint Formulary Committee. Nevirapine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/09/2020.

Nevirapine 200 mg Tablets (Accord Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 23/09/2020.

Nevirapine Mylan 400 mg Prolonged-Release Tablets (Generics UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 23/09/2020.

Viramune (Boehringer Ingelheim International GmbH). MIMS Singapore. http://www.mims.com/singapore. Accessed 23/09/2020.

Viramune Tablet and Oral Suspension (Boehringer Ingelheim Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 23/09/2020.

Viramune XR Extended-Release Tablet (Boehringer Ingelheim Roxane Inc.). MIMS Philippines. http://www.mims.com/philippines. Accessed 23/09/2020.

Viramune XR Extended-Release Tablets (Boehringer Ingelheim Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 23/09/2020.

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