Adverse effects hiv protease inhibitors

Protease inhibitors commonly cause paresthesias, nausea, vomiting, and diarrhea Disturbances in glucose and lipid metabolism also occur, including diabetes, hypertriglyceridemia, and hypercholesterolemia. Chronic administration results in fat redistribution, including loss of fat from the extremities, fat accumulation in the abdomen and the base of the neck (“buffalo hump”), and breast enlargement. These physical changes may indicate to others that an individual is HIV infected.Drug interactions are a common problem for all protease inhibitors, because they are not only substrates but also potent inhibitors of CYP isozymes. The inhibitory potency of the compounds lies between that of ritonavir, the most potent, and that of saquinavir, the least potent Drugs that rely on metabolism for their termination of action may accumulate to toxic levels. Examples of potentially dangerous interactions from drugs that are contraindicated with protease inhibitors include rhabdomyolysis from simvastatin or lovastatin, excessive sedation from midazolam or triazolam, and respiratory depression from fentanyl Other drug interactions that require dosage modification and cautious use include warfarin, sildenafi l, and phenytoin inducers of CYP isozymes may result in the lowering of protease inhibitor plasma concentrations to suboptimal levels, contributing to treatment failures. Thus, drugs such as rifampin and St. John’s wort are also contraindicated with protease inhibitors. Meticulous attention must be paid to all of these detrimental interactions.A peripheral neuropathy, skin rash, and hyperbilirubinemia. Prolongation of the QTc interval may occur at high doses. Unlike most PIs, atazanavir does not appear to be associated with dyslipidemias, fat deposition, or a metabolic syndrome. However, it is a potent inhibitor of CYP3A4 and CYP2C9.