Tipranavir


Concise Prescribing Info
Indications/Uses
HIV infection.
Dosage/Direction for Use
Adult : PO Combined w/ ritonavir: 500 mg twice daily.
Dosage Details
Oral
HIV infection
Adult: 500 mg (with ritonavir 200 mg) bid.
Administration
Should be taken with food.
Contraindications
Child-Pugh class B or C.
Special Precautions
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.
Adverse Reactions
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.
Overdosage
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.
Drug Interactions
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.
Action
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.
Pharmacokinetics:
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.
Storage
Store at 2-8°C.
MIMS Class
Disclaimer: This information is independently developed by MIMS based on Tipranavir from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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