tipranavir

Tipranavir is a protease inhibitor used in the treatment of HIV-1 infection. It is a non-peptide protease inhibitor that is typically prescribed in combination with ritonavir to boost its plasma levels, forming a boosted regimen known as tipranavir/ritonavir. It is primarily indicated for treatment-experienced adults and, in some settings, pediatric patients who have limited options due to resistance to other antiretroviral drugs.

Tipranavir works by inhibiting the HIV-1 protease enzyme, which is essential for the maturation of infectious virions. By blocking protease activity, it prevents the formation of mature, infectious HIV particles. The drug retains activity against certain HIV-1 strains that are resistant to other protease inhibitors, but resistance can still develop with continued use. Because of its metabolism and interactions, tipranavir is usually given with ritonavir to achieve sufficient drug exposure.

Administration and pharmacology notes: boosted tipranavir/ritonavir is administered twice daily, with dosing adjusted for aspects such as age and weight in pediatric patients. Tipranavir is extensively metabolized by the liver and is a significant inhibitor and substrate of cytochrome P450 enzymes, leading to many potential drug interactions. Careful review of concomitant medications is required to avoid harmful interactions, including certain lipid-lowering agents, antiarrhythmics, sedatives, and herbal supplements.

Safety and adverse effects: tipranavir/ritonavir has been associated with hepatotoxicity and pancreatitis, as well as lipid abnormalities, nausea, diarrhea, rash, and other adverse events. Serious liver injury and intracranial hemorrhage have been reported in some cases. Liver function tests, lipid panels, and pancreatic enzymes should be monitored regularly. Tipranavir is contraindicated in certain hepatic conditions and requires careful assessment of drug interactions and patient risk factors.