10 Questions
What is the major issue with chronic administration of HIV protease inhibitors?
Fat maldistribution, including loss of fat from the extremities
Why are drug interactions a common problem with HIV protease inhibitors?
They are potent inhibitors of CYP450 isoenzymes
How does resistance develop to HIV protease inhibitors?
Accumulation of stepwise mutations of the protease gene
What are the drawbacks of using HIV protease inhibitors alone?
Drug resistance
Why is poor patient compliance a concern with HIV protease inhibitors?
High number of capsules needed to be taken (pill burden)
What is the mechanism of action of HIV protease inhibitors?
HIV protease inhibitors bind to the site where protein cutting occurs, preventing the enzyme from releasing individual core proteins, thus hindering the maturation of new viral particles.
How are HIV protease inhibitors metabolized in the body?
HIV protease inhibitors are metabolized by the CYP3A4 isoenzyme and other CYP450 isoenzymes, with hepatic metabolism being extensive.
What are some adverse effects of HIV protease inhibitors?
Adverse effects include GI disturbances (nausea, vomiting, diarrhea), hyperglycemia, hyperlipidemia, and hepatic injury.
Why should HIV protease inhibitors not be used with Lovastatin and simvastatin?
Lovastatin and simvastatin levels are elevated by protease inhibitors, increasing the risk of complications in coronary heart disease.
Why are dosage adjustments unnecessary in renal impairment when using HIV protease inhibitors?
Dosage adjustments are unnecessary in renal impairment because the inhibitors are primarily eliminated through biliary excretion and are not excreted unchanged in urine.
Explore the mechanism of action of HIV protease inhibitors like Darunavir and Atazanavir, and how Ritonavir and Cobicistat are used as pharmacokinetic boosters. Learn how these inhibitors prevent the enzyme protease from cutting viral proteins, essential for forming mature viral proteins.
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