Indinavir

Indinavir

File:Indinavir.svg
Systematic (IUPAC) name
(2S)-1-[(2S,4R)-4-benzyl-2-hydroxy-4-{[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]carbamoyl}butyl]-N-tert-butyl-4-(pyridin-3-ylmethyl)piperazine-2-carboxamide
Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]	US FDA: Indinavir
Pregnancy category	US: C (Risk not ruled out)
Routes of administration	Oral
Pharmacokinetic data
Protein binding	60%
Metabolism	Hepatic via CYP3A4
Biological half-life	1.8 (± 0.4) hours
Identifiers
CAS Number	150378-17-9
ATC code	J05AE02 (WHO)
PubChem	CID 5362440
DrugBank	APRD00069
Chemical data
Formula	C36H47N5O4
Molar mass	613.79 g/mol[[]]

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.

History

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.

Increasingly, it is being replaced by newer drugs that are more convenient to take and less likely to promote resistant virus, such as lopinavir or atazanavir.

Administration

Unfortunately, indinavir wears off quickly after dosing and therefore requires dosing very precisely 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.

Side effects

Side effects include

• Kidney stones
• Metabolic abnormalities including hyperlipidemia (cholesterol or triglyceride elevations)
• alterations in body shape known as lipodystrophy

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