Ritonavir: Difference between revisions
| Line 29: | Line 29: | ||
==Mechanism of Action== | ==Mechanism of Action== | ||
Ritonavir was originally developed as an [[enzyme inhibitor|inhibitor]] of [[HIV protease]]. It is one of the most complex inhibitors. It is now rarely used for its own antiviral activity, but remains widely used as a booster of other [[Protease inhibitor (pharmacology)|protease inhibitor]]s. More specifically, ritonavir is used to inhibit a particular liver enzyme that normally [[metabolize]]s protease inhibitors, [[CYP3A4|cytochrome P450-3A4]] (CYP3A4).<ref>{{cite journal |url=http://jac.oxfordjournals.org/cgi/content/full/53/1/4 | author=Zeldin RK, Petruschke RA |title=Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients |journal= [[Journal of Antimicrobial Chemotherapy]] | volume=53 | pages=4–9 | year=2004 | doi=10.1093/jac/dkh029 | pmid=14657084 | issue=1}}</ref> 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 protease inhibitors and HAART, was first communicated in an article published in the journal [[AIDS (journal)|''AIDS'']] in 1997 by researchers at the [[University of Liverpool]].<ref>{{cite journal | journal = AIDS | year = 1997 | volume = 11 | issue = 4 | pages = F29–F33 | url = http://www.aidsonline.com/pt/re/aids/fulltext.00002030-199704000-00001.htm;jsessionid=GzjRLZg2JD63hFQWx2LLZVLJzWLGwz72zpQ290nsQ4FywKbR5X5h!3145886!-949856145!8091!-1 | title = Saquinavir pharmacokinetics alone and in combination with ritonavir in HIV-infected patients | author = Merry, Concepta; Barry, Michael G.; Mulcahy, Fiona; Ryan, Mairin; Heavey, Jane; Tjia, John F.; Gibbons, Sara E.; Breckenridge, Alasdair M.; Back, David J. | doi = 10.1097/00002030-199704000-00001 | pmid = 9084785}}</ref> This effect does come with a price: it also affects the efficacy 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. | |||
==References== | ==References== | ||
Revision as of 17:12, 9 January 2014
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Chetan Lokhande, M.B.B.S [2]
Overview
Ritonavir, with trade name Norvir (AbbVie, Inc.), 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.
Category
US Brand Names
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Overdosage | Clinical Studies | Dosage and Administration | How Supplied | Labels and Packages
Mechanism of Action
Ritonavir was originally developed as an inhibitor of HIV protease. It is one of the most complex inhibitors. 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 protease inhibitors, cytochrome P450-3A4 (CYP3A4).[1] 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 protease inhibitors and HAART, was first communicated in an article published in the journal AIDS in 1997 by researchers at the University of Liverpool.[2] This effect does come with a price: it also affects the efficacy 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.
References
- ↑ Zeldin RK, Petruschke RA (2004). "Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients". Journal of Antimicrobial Chemotherapy. 53 (1): 4–9. doi:10.1093/jac/dkh029. PMID 14657084.
- ↑ Merry, Concepta; Barry, Michael G.; Mulcahy, Fiona; Ryan, Mairin; Heavey, Jane; Tjia, John F.; Gibbons, Sara E.; Breckenridge, Alasdair M.; Back, David J. (1997). "Saquinavir pharmacokinetics alone and in combination with ritonavir in HIV-infected patients". AIDS. 11 (4): F29–F33. doi:10.1097/00002030-199704000-00001. PMID 9084785.