Thông tin thuốc gốc
Chỉ định và Liều dùng
HIV infection
Adult: 500 mg (with ritonavir 200 mg) bid.
Cách dùng
Should be taken with food.
Chống chỉ định
Child-Pugh class B or C.
Thận trọng
Child-Pugh class A. Chronic hepatitis B or C co-infection. Not to be used in patients with pre-treatment liver enzymes levels >5 times the upper limit of normal. Monitor LFTs before and during treatment; more frequent monitoring is needed in patients with underlying hepatic diseases. Discontinue treatment if liver function worsens; stop permanently in patients with liver enzymes >10 times the upper limit of normal or those who develop signs/symptoms of clinical hepatitis. Patients at increased risk of bleeding or taking antiplatelet drugs or anticoagulants. Monitor cholesterol and triglyceride before and during therapy. Patients with known sulfonamide allergy. Pregnancy, lactation.
Phản ứng phụ
Diarrhoea, increased transaminases, hypertriglyceridaemia, hypercholesterolaemia, fever, fatigue, headache, rash, dehydration, nausea, vomiting, abdominal pain, wt loss, dehydration, myalgia, dyspnoea. Redistribution or accumulation of body fat.
Quá liều
Treatment: General supportive measures, monitoring of vital signs and observation of the patient's clinical status. Unabsorbed drug may be removed by emesis or gastric lavage. Activated charcoal may also be used. Dialysis is unlikely to be useful.
Tương tác
May decrease the levels/effects of abacavir, phenytoin, phenobarbitone, delavirdine, didanosine (separate admin by 2 hr), methadone, PPIs and omeprazole, theophylline derivatives, valproic acid, zidovudine. May increase the levels/effects of antifungal agents, benzodiazepines, calcium channel blockers, fluticasone, CYP3A4 substrates (e.g. ciclosporin, mirtazapine, nateglinide, nefazodone, sildenafil, tacrolimus and venlafaxine), digoxin, eplerenone, fentanyl, flecainide, HMG-CoA reductase inhibitors, immunosuppressive agents (e.g. sirolimus, tacrolimus), normeperidine, nefazodone, pimozide, propafenone, TCAs. Serum levels may be reduced by antacids, anticonvulsants, CYP3A4 inducers, nevirapine, rifampin derivatives, tenofovir. Serum levels may be increased by antifungal agents, cimetidine, clarithromycin, enfuvirtide, fusidic acid, protease inhibitors. Increased risk of rash when used with hormonal contraceptives.
Potentially Fatal: May increase toxicity (peripheral ischaemia, vasospasm) of ergot derivatives. Concurrent use with midazolam and triazolam is contraindicated due to increased risk of toxicity. May cause malignant arrhythmias when used with cisapride. Increased risk of myopathy/rhabdomyolysis when used with lovastatin and simvastatin. Concurrent use with quinidine, amiodarone or rifampin is contraindicated.
Food Interaction
St John's wort may reduce the levels of tipranavir/ritonavir; avoid concurrent use. High-dose vitamin E may increase the risk of bleeding.
Tác dụng
Description: Tipranavir is a non-peptide protease inhibitor that exerts its antiviral activity against HIV-1 by binding to the protease activity site and inhibits the enzymatic activity. In doing so, it prevents cleavage of these polyproteins, resulting in the formation of immature, noninfectious viral particles.
Absorption: Limited absorption after oral admin.
Distribution: About 99.9% bound to plasma proteins.
Metabolism: Metabolised by cytochrome P450 system, mainly CYP3A4.
Excretion: Mean elimination half-life: 4.8-6 hr.
Bảo quản
Store at 2-8°C.
Phân loại MIMS
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