Indinavir

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Indinavir
Systematic (IUPAC) name
1-[2-hydroxy-4- [(2-hydroxy-2,3-dihydro- 1H-inden-1-yl) carbamoyl]-5-phenyl-pentyl]-4- (pyridin-3-ylmethyl)- N-tert-butyl-piperazine-2-carboxamide
Identifiers
CAS number	150378-17-9
ATC code	J05 AE02
PubChem	5362440
DrugBank	APRD00069
Chemical data
Formula	C₃₆H₄₇N₅O₄
Mol. weight	613.79 g/mol
Pharmacokinetic data
Bioavailability	?
Protein binding	60%
Metabolism	Hepatic via CYP3A4
Half life	1.8 (± 0.4) hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	C(US)
Legal status
Routes	Oral

Indinavir (IDV) (trade name Crixivan®) (Merck) is a protease inhibitor used as a component of highly active antiretroviral therapy (HAART) to treat HIV infection and AIDS.

[edit] 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 the 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.

[edit] 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.

[edit] Side effects

Side effects include

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

Antivirals (primarily J05A, also S01AD and D06BB) edit

Anti-herpesvirus agents		Aciclovir, Cidofovir, Docosanol, Famciclovir, Fomivirsen, Foscarnet, Ganciclovir, Idoxuridine, Penciclovir, Trifluridine, Tromantadine, Valaciclovir, Valganciclovir, Vidarabine
Anti-influenza agents		Amantadine, Oseltamivir, Peramivir, Rimantadine, Zanamivir

Antiretroviral drugs	NRTIs	Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Zalcitabine, Zidovudine
	NtRTIs	Tenofovir
	NNRTIs	Efavirenz, Delavirdine, Nevirapine
	PIs	Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir
	Fusion inhibitors	Enfuvirtide

Other antiviral agents		Adefovir, Fomivirsen, Imiquimod, Inosine,Interferon, Podophyllotoxin, Ribavirin, Viramidine