Article: 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 J05AE02
PubChem 5362440
DrugBank APRD00069
Chemical data
Formula C36H47N5O4
Mol. weight 613.79 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 60%
Metabolism  ?
Half life 1.8 (┬▒ 0.4) hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

Indinavir (IDV) (Crixivan®) (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 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.

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)
  • Bizarre alterations in body shape known as lipodystrophy


Merck & Co., Inc.

Corporate Directors: Lawrence Bossidy | William Bowen | Richard Clark | Johnnetta Cole | William Harrison | William Kelley | Rochelle Lazarus | Thomas Shenk | Anne Tatlock | Samuel Thier | Wendell Weeks | Peter Wendell

Key products: Indinavir | Aprepitant | Alendronate | Rizatriptan | Finasteride | Montelukast | Rofecoxib | Ezetimibe/simvastatin | Ezetimibe | Simvastatin | The Merck Index | The Merck Manual

Annual Revenue: $22.9 billion USD (5916-10px-green-arrow-up-svg-indinavir.png2% FY 2004) | Employees: 63,000 | Stock Symbol: NYSE: MRK | Website: www.merck.com


Retrieved from "http://en.wikipedia.org/wiki/Indinavir"

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