Indinavir
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Indinavir
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| 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 | |
| ATC code | J05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C36H47N5O4 |
| Mol. mass | 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 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.
[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) | |
|---|---|
| Anti-herpesvirus | Aciclovir, Cidofovir, Docosanol, Famciclovir, Fomivirsen, Foscarnet, Ganciclovir, Idoxuridine, Penciclovir, Trifluridine, Tromantadine, Valaciclovir, Valganciclovir, Vidarabine |
| Anti-influenza agents | Amantadine, Arbidol, Oseltamivir, Peramivir, Rimantadine, Zanamivir |
| Antiretrovirals: NRTIs | Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Zalcitabine, Zidovudine |
| Antiretrovirals: NtRTIs | Tenofovir |
| Antiretrovirals: NNRTIs | Efavirenz, Delavirdine, Nevirapine, Loviride |
| Antiretrovirals: PIs | Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir |
| Antiretrovirals: Fusion inhibitors | Enfuvirtide |
| Other antiviral agents | Adefovir, Fomivirsen, Imiquimod, Inosine, Interferon, Podophyllotoxin, Ribavirin, Viramidine |
| Merck & Co., Inc. |
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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 |
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Key products: Indinavir | Aprepitant | Alendronate | Rizatriptan | Finasteride | Montelukast | Rofecoxib | Ezetimibe/simvastatin | Ezetimibe | Simvastatin | The Merck Index | The Merck Manual |
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Annual Revenue: $22.9 billion USD ( |
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