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- Ritonavir (7)
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Ritonavir
From Wikipedia, the free encyclopedia
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Ritonavir
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| Systematic (IUPAC) name | |
| 1,3-thiazol-5-ylmethyl [3-hydroxy-5- [3-methyl-2-[methyl- [(2-propan-2-yl-1,3-thiazol- 4-yl)methyl] carbamoyl] amino-butanoyl] amino-1,6-diphenyl-hexan-2-yl] aminoformate | |
| Identifiers | |
| CAS number | |
| ATC code | J05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C37H48N6O5S2 |
| Mol. mass | 720.946 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 98-99% |
| Metabolism | ? |
| Half life | 3-5 hours |
| Excretion | mostly fecal |
| Therapeutic considerations | |
| Pregnancy cat. |
B (U.S.) |
| Legal status |
℞-only (U.S.) |
| Routes | ? |
Ritonavir, with trade name Norvir® (Abbott Laboratories), is an antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS.
Ritonavir is frequently prescribed with HAART, not for its antiviral action, but as it inhibits the same host enzyme that metabolizes other protease inhibitors. This inhibition leads to higher plasma concentrations of these latter drugs, allowing the clinician to lower their dose and frequency and improving their clinical efficacy.
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Ritonavir is manufactured as Norvir® by Abbott Laboratories. Research that led to the drug's development was financed by a $3,500,000 federal grant through the National Institutes of Health (NIH) and over $200,000,000 by Abbott Labs. The Food and Drug Administration (FDA) approved ritonavir on March 1, 1996, making it the seventh approved antiretroviral drug in the United States. In 2003, Abbott raised the price of a Norvir course from USD $1.71 per day to $8.57 per day, leading to claims of price gouging by patients' groups and some members of Congress. Consumer group Essential Inventions petitioned the NIH to override the Norvir patent, but the NIH announced on August 4, 2004 that it would not invoke its legal right to allow generic production of Norvir, citing potential adverse effects on the pharmaceutical market.[1]
Ritonavir was originally developped as an inhibitor of HIV protease. It is now rarely used for its own antiviral activity, but remains widely used as a booster of other protease inhibitors. More specifically, ritonavir is used to inhibit a particular liver enzyme that normally metabolizes away protease inhibitors, cytochrome P450-3A4 (CYP3A4). [2] The drug's molecular structure inhibits CYP3A4, so a low dose can be used to enhance other protease inhibitors. This discovery, which has drastically reduced the adverse effects and improved the efficacy of PI's and HAART, was first communicated in an article published in the AIDS Journal in 1997 by the University of Liverpool. This effect does come with a price: it also affects the strength of numerous other medications, making it difficult to know how to administer them concurrently. In addition it can cause a large number of side-effects on its own.
One puzzling side effect of ritonavir is hyperglycemia. It appears that it directly inhibits the GLUT4 insulin-regulated transporter, keeping glucose from entering fat and muscle cells. This can lead to insulin resistance and cause problems for Type I diabetics.
- ^ Ceci Connolly (2004-08-05). NIH Declines to Enter AIDS Drug Price Battle. Washington Post. Retrieved on 2006-01-16.
- ^ Zeldin RK, Petruschke RA (2004). "Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients". Journal of Antimicrobial Chemotherapy 53: 4-9.
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| Nucleoside & Nucleotide Reverse Transcriptase Inbitors (NRTI) |
Abacavir (ABC) • Didanosine • Emtricitabine • Lamivudine (3TC) • Stavudine • Zidovudine (AZT) • Adefovir • Tenofovir • Zalcitabine‡ |
| Non-Nucleoside Reverse Transcriptase Inhibitiors (NNRTI) |
Efavirenz • Nevirapine • Etravirine† • Rilpivarine† • Loviride‡ • Delavirdine‡ |
| Protease Inhibitors (PI) | Atazanavir • Darunavir • Fosamprenavir • Lopinavir • Nelfinavir • Ritonavir • Saquinavir • Tipranavir • Amprenavir‡ • Indinavir‡ |
| Entry/fusion inhibitors | Enfuvirtide • Maraviroc • Vicriviroc† |
| Integrase inhibitors | Raltegravir • Elvitegravir† |
| Combined formulations | Combivir • Atripla • Trizivir • Truvada • Kaletra |
| Other/experimental/unclassified agents | Synergistic enhancers • Epigallocatechin gallate • Portmanteau inhibitors • Globoidnan A • Bevirimat† |
| †Undergoing clinical trials, not FDA approved. ‡Formerly or rarely used agent. | |
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