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Encyclopedia > NRTI

Reverse transcriptase inhibitors (RTIs) are a class of antiretroviral drug used to treat HIV infection. RTIs inhibit activity of reverse transcriptase, a viral enzyme that HIV needs to reproduce. Antiretroviral drugs are medications for the treatment of infection by retroviruses, primarily HIV. Different classes of antiretroviral drugs act at different stages of the HIV life cycle. ... Human immunodeficiency virus, commonly known by the initialism HIV, is a retrovirus that primarily infects vital components of the human immune system such as CD4+ T cells, macrophages and dendritic cells. ... To meet Wikipedias quality standards, this article or section may require cleanup. ... Ribbon diagram of the catalytically perfect enzyme TIM. An enzyme is a protein that catalyzes, or speeds up, a chemical reaction. ...


When a retrovirus infects a cell, reverse transcriptase transcribes the viral RNA onto the host cell's DNA. The host's own processes then reproduce the virus. RTIs block reverse transcriptase from transcribing retroviral genetic information onto a host cell's DNA, thus preventing HIV from multiplying. Ribonucleic acid (RNA) is a nucleic acid polymer consisting of covalently bound nucleotides. ... Space-filling model of a section of DNA molecule Deoxyribonucleic acid (DNA) is a nucleic acid that contains the genetic instructions specifying the biological development of all cellular forms of life (and most viruses). ...


RTIs come in three forms:

  • Nucleoside analog reverse transcriptase inhibitors (NARTIs or NRTIs)
  • Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
  • Nucleotide analog reverse transcriptase inhibitors (NtARTIs or NtRTIs)

Nucleoside analog reverse transcriptase inhibitors

Nucleoside analog reverse transcriptase inhibitors (NARTIs or NRTIs) compose the first class of antiretroviral drugs developed.

Zidovudine 
Zidovudine, also called AZT, ZDV, and azidothymidine, has the trade name Retrovir®.
Didanosine 
Didanosine, also called ddI, with the trade names Videx® and Videx EC®, was the second FDA-approved antiretroviral drug.
Zalcitabine 
Zalcitabine, also called ddC and dideoxycytidine, has the trade name Hivid®.
Stavudine 
Stavudine, also called d4T, has trade names Zerit® and Zerit XR®.
Lamivudine 
Lamivudine, also called 3TC, has the trade name Epivir®.
Abacavir 
Abacavir, also called ABC, has the trade name Ziagen®, is an analog of guanosine.
Emtricitabine 
Emtricitabine, also called FTC, has the trade name Emtriva® (formerly Coviracil).

Zidovudine (INN) or azidothymidine (AZT) is an antiretroviral drug, the first one approved for treatment of HIV. It is also sold under the names Retrovir® and Retrovis®, and as an ingredient in Combivir® and Trizivir®. It is an analog of thymidine. ... Didanosine (2-3-dideoxyinosine, ddI, Videx®) differs from other nucleoside analogues, because it does not have any of the regular bases, instead it has hypoxanthine attached to the sugar ring. ... Zalcitabine (2-3-dideoxycytidine, ddC), is a derivative of the naturally existing deoxycytidine, made by replacing the hydroxyl group in position 3 with a hydrogen. ... Stavudine (2-3-didehydro-2-3-dideoxythymidine, d4T, brand name Zerit®) is a thymidine analogue active against HIV. It is phosphorylated by cellular kinases into active triphosphate. ... Lamivudine (2,3-dideoxy-3-thiacytidine, 3TC) is a potent reverse transcriptase inhibitor. ... Abacavir (ABC) is extremely potent reverse transcriptase inhibitor, meant for the treatment of AIDS. ABC is capable of crossing the blood-brain barrier. ... Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) for the treatment of HIV infection in adults. ...

Non-nucleoside reverse transcriptase inhibitors

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) compose the third class of antiretroviral drugs that were developed. In all cases, patents remain in force until beyond 2010.

Nevirapine 
Nevirapine has the trade name Viramune®.
Delavirdine 
Delavirdine has the trade name: Rescriptor®. It was approved by the FDA April 4, 1997 and is thus the eleventh approved antiretroviral.
Efavirenz 
Efavirenz has trade names Sustiva® and Stocrin®.

Nevirapine is a controversial AIDS drug. ... April 4 is the 94th day of the year in the Gregorian calendar (95th in leap years). ... 1997 (MCMXCVII) is a common year starting on Wednesday of the Gregorian calendar. ... This article needs to be cleaned up to conform to a higher standard of quality. ...

Nucleotide analog reverse transcriptase inhibitors

Normally, nucleoside analogs are converted into nucleotide analogs by the body. Taking Nucleotide Analog Reverse Transcriptase Inhibitors (NtARTIs or NtRTIs) directly allows conversion steps to be skipped, causing less toxicity.

Tenofovir 
Tenofovir, also known as tenofovir disoproxil fumarate, has the trade name Viread®.
Adefovir 
Adefovir, also known as bis-POM PMPA, has trade names Preveon® and Hepsera®. It is not approved by the FDA for treatment of HIV.

  Results from FactBites:
 
Safety and efficacy of switching to alternative nucleoside analogues following symptomatic hyperlactatemia and lactic ... (2230 words)
The NRTI that patients were receiving when symptomatic hyperlactatemia or lactic acidosis was diagnosed included stavudine and lamivudine (n = 6), stavudine and didanosine (n = 4), and stavudine and abacavir (n = 2).
The NRTI suspected to have caused symptomatic hyperlactatemia or lactic acidosis were replaced with alternative NRTI thought to have equivalent antiviral efficacy but less propensity to injure mitochondria.
NRTI (stavudine, didanosine) believed to have induced symptomatic hyperlactatemia or lactic acidosis were switched to alternative NRTI (zidovudine, abacavir, lamivudine) that have less propensity to cause mitochondrial dysfunction.
  More results at FactBites »

 
 

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