Template:Drugbox Indinavir (IDV; trade name Crixivan, manufactured by Merck) is a protease inhibitor used as a component of highly active antiretroviral therapy (HAART) to treat HIV infection and AIDS.
The Food and Drug Administration (FDA) approved indinavir March 13, 1996, making it the eighth approved antiretroviral. Indinavir was much more powerful than any prior antiretroviral drug; using it with dual NRTIs set the standard for treatment of HIV/AIDS and raised the bar on design and introduction of subsequent antiretroviral drugs. Protease inhibitors changed the very nature of the AIDS epidemic from one of a terminal illness to a somewhat manageable one.
Unfortunately, indinavir wears off quickly after dosing, therefore requiring very precise dosing every eight hours in order to thwart HIV from forming drug-resistant mutations, including resistances to other protease inhibitors. It has restrictions on what sorts of food may be eaten concurrently.
Most common side effects of indinavir include:
- General malaise and fatigue;
- Kidney stones, which sometimes may lead to more severe condition including kidney failure;
- Metabolic alterations including hyperlipidemia (cholesterol or triglyceride elevations) and hyperglycemia;
- Alterations in body shape (lipodystrophy), colloquially known as "Crix belly"
Endothelial cells produce nitric oxide (NO) which causes blood vessels to dilate, lowers blood pressure, allows oxygen to reach and nutrients to reach tissues, and allows carbon dioxide and metabolic waste to be removed. Nitric oxide is highly reactive and quickly reacts with molecular oxygen (O2) to form nitrogen dioxide (NO2).
- 2NO + O2 → 2NO2
A further reaction between nitrogen dioxide (NO2) and water (H2O) can produce nitrate (NO3). The nitrate is then removed from the body in the urine. The kidney is filled with small blood vessels. In the absence of nitric oxide, these blood vessels may become constricted, and the kidney may become ischemic, leading to kidney disease.
Indinavir inhibits urinary nitrous oxide production and may inhibit nitric oxide production. Treatment with this drug is frequently associated with renal abnormalities, sterile leukocyturia, and reduced creatinine clearance.