Darunavir


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
HIV-1 infection
Adult: Treatment-naive or treatment-experienced patients w/o duranavir resistance associated mutations (DRV-RAMs): 800 mg once daily, given in combination w/ ritonavir 100 mg or cobicistat 150 mg. Treatment-experienced patients w/ ≥1 DRV-RAMs or if genotype testing is not possible: 600 mg bid, given in combination w/ ritonavir 100 mg.
Child: 3-17 yr Treatment-naive or treatment-experienced patients w/o DRV-RAMs (given in combination w/ ritonavir 100 mg): ≥15-<30 kg: 600 mg once daily; ≥30-<40 kg: 675 mg once daily; ≥40 kg: 800 mg once daily. Treatment-experienced patients (given in combination w/ ritonavir 50 mg): ≥15-<30 kg: 375 mg bid; ≥30-<40 kg: 450 mg bid; ≥40 kg: 600 mg bid.
Special Patient Group
Pregnant patients: 600 mg bid, given in combination w/ ritonavir 100 mg.
Hepatic Impairment
Severe (Child-Pugh Class C): Contraindicated.
Cách dùng
Should be taken with food.
Chống chỉ định
Hypersensitivity to darunavir. Severe hepatic (Child-Pugh Class C) impairment. Lactation. Concomitant use w/ strong CYP3A4 enzyme inducers and narrow therapeutic index (NTI) drugs that are highly dependent on CYP3A4 enzyme for clearance.
Thận trọng
Patient w/ advanced HIV infection, immune reconstitution syndrome, sulfonamide allergy, chronic active hepatitis B or C, cirrhosis, haemophilia A and B, DM, history of pancreatitis, elevated triglycerides. Patient on multiple medications. Mild to moderate hepatic impairment. Pregnancy.
Phản ứng phụ
Significant: Fat redistribution (e.g. Cushingoid appearance, buffalo hump, peripheral and facial wasting, breast enlargement), mild to moderate rash, immune reconstitution syndrome, bleeding, hyperglycaemia, hypertriglyceridaemia, hypercholesterolaemia, pancreatitis, new onset or exacerbation of DM, hypersensitivity reactions (e.g. angioedema, erythema multiforme, toxic epidermal necrolysis, bronchospasm, rarely, drug rash w/ eosinophilia and systemic symptoms (DRESS) and Stevens-Johnson syndrome).
Nervous: Asthenia, dizziness, insomnia, headache, somnolence, vertigo, peripheral neuropathy.
CV: MI, tachycardia, TIA.
GI: Abdominal pain, diarrhoea, nausea, vomiting.
Resp: Nasopharyngitis.
Genitourinary: Polyuria.
Endocrine: Insulin resistance, hyperlactataemia, wt gain.
Haematologic: Anaemia, thrombocytopenia, neutropenia.
Musculoskeletal: Osteonecrosis, osteopenia, osteoporosis, myalgia, myositis.
Dermatologic: Folliculitis.
Others: Fatigue.
Potentially Fatal: Drug-induced hepatitis (e.g. acute hepatitis, cytolytic hepatitis).
MonitoringParameters
Perform LFTs prior to and during therapy. Perform baseline genotypic and phenotypic testing in treatment-experienced patients if possible. Monitor viral load, CD4, transaminase, triglyceride, and cholesterol levels prior to and during therapy.
Tương tác
Enhanced systemic exposure w/ ritonavir and cobicistat. Increased plasma concentration w/ CYP3A4 enzyme inhibitors (e.g. ketoconazole, clotrimazole, indinavir).
Potentially Fatal: Strong CYP3A4 enzyme inducers (e.g. rifampicin, lopinavir, carbamazepine, phenobarbital, phenytoin) may reduce plasma concentration of darunavir leading to loss of therapeutic effect and development of resistance. May inhibit elimination and increase exposure of NTI drugs that are highly dependent on CYP3A4 enzyme for clearance (e.g. sildenafil [when used for pulmonary HTN], salmeterol, alfuzosin, amiodarone, bepridil, systemic lidocaine, quinidine, terfenadine, astemizole, sertindole, pimozide, ergot derivatives, cisapride, oral midazolam, triazolam, simvastatin, lovastatin) leading to serious or life-threatening events.
Food Interaction
Absorption and bioavailability are increased w/ food. Concomitant use w/ St. John’s wort is not recommended since it may reduce plasma concentration of darunavir leading to loss of therapeutic effect and development of resistance.
Tác dụng
Description: Darunavir is a sulfonamide derivative that inhibits HIV-1 replication. It selectively blocks viral protease, inhibiting the cleavage of Gag-Pol polypeptides into infectious viral proteins, thereby forming non-functional, immature, and non-infectious virions.
Pharmacokinetics:
Absorption: Rapidly absorbed. Bioavailability: 82%. Increased absorption and bioavailability w/ food. Time to peak plasma concentration: W/in 2.5-4 hr.
Distribution: Plasma protein binding: Approx 95%, mainly to α1-acid glycoprotein.
Metabolism: Metabolised in the liver via oxidation, mainly by CYP3A4 enzyme to at least 3 active metabolites.
Excretion: Via faeces (approx 80%, 41.2% as unchanged drug) and urine (approx 14%, 7.7% as unchanged drug). Terminal elimination half-life: Approx 15 hr.
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Darunavir, CID=213039, https://pubchem.ncbi.nlm.nih.gov/compound/Darunavir (accessed on Jan. 20, 2020)

Bảo quản
Store at 25°C. Oral susp: Do not refrigerate, freeze, or expose to excessive heat.
Phân loại MIMS
Phân loại ATC
J05AE10 - darunavir ; Belongs to the class of protease inhibitors. Used in the systemic treatment of viral infections.
References
Anon. Darunavir. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/04/2017.

Buckingham R (ed). Darunavir. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/04/2017.

Joint Formulary Committee . Darunavir. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/04/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Darunavir. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 03/04/2017.

Prezista Tablet, Film Coated and Suspension (Janssen Products LP). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/04/2017.

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