Protease inhibitors block an enzyme called HIV protease

Protease inhibitors

Protease inhibitors block an enzyme called HIV protease, which prevents infected cells from producing more HIV. There are 11 U.S. FDA-approved protease inhibitors used to treat HIV. The use of two protease inhibitors in dual protease-inhibitor regimens is popular because of drug interactions that increase potency, reduce dose frequency, require fewer food restrictions, and lower the cost. Long term effects of dual protease-inhibitor regimens are unknown.

Blood levels of protease inhibitors drop significantly shortly after being taken. This makes frequent dosing necessary to maintain a level of the medication in the blood to destroy the virus. Missed doses lead to low blood levels of drug, allowing the virus to multiply, mutate, and develop resistance. Much of the focus of current studies is to develop new medications and new ways of taking medications that maintain proper drug levels, prevent resistance, and overcome the need for frequent dosing.

Protease inhibitors have been associated with new onset diabetes mellitus and may worsen pre-existing diabetes. All patients who are on antiretroviral therapy must be followed closely by a health care professional for treatment-related side effects. PIs can cause elevations in blood levels of sugar, as well as cholesterol and other fats and have been associated with lipodystrophy.