Reverse transcriptase inhibitors tenofovir

Nucleotide reverse transcriptase inhibitor Tenofovir (TDF) 300 mg once daily >30 days-13 yrs 120 mg/m daily for 2 weeks, then 200 mg/m twice daily Safety and efficacy not well... 

IL-2 NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS-TENOFOVIR t adverse effects with tenofovir Uncertain Avoid if possible otherwise monitor renal function weekly... 

VANCOMYCIN NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS-TENOFOVIR, ZIDOVUDINE t adverse effects with zidovudine and possibly tenofovir Additive toxicity Monitor FBC and renal function closely (at least weekly)... 

AMPHOTERICIN NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - TENOFOVIR, ZIDOVUDINE Possibly T adverse effects with tenofovir and zidovudine Additive toxicity Avoid if possible otherwise monitor FBC and renal function (weekly). 1 doses as necessary... 

Tenofovir disoproxil fumarate is a nucleotide analog reverse transcriptase inhibitor. Tenofovir disoproxil fumarate is a... 

Lee WA, He GX, Eisenberg E, CUilar T, Swaminathan S, Mulato A, Cundy KC (2(X)5) Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue. Antimicrob Agents Chemothta 49 1898—1906... 

The 2, 3 -dideoxynucleoside (ddN) analogues (Fig. 3) encompass a vast group of compounds that have been found active against HIV and HBV, although they have been primarily pursued for the treatment of HIV infections (AIDS). They are targeted at the HIV-associated reverse transcriptase (RT) and therefore also referred to as nucleoside reverse transcriptase inhibitors (NRTIs). They have to be distinguished from the nucleotide reverse transcriptase inhibitors (NtRTIs) such as adefovir (PMEA) and tenofovir (PMPA) (see above) which, like the NRTIs, act as chain... 

TC, lamivudine ABC, abacavir APV, amprenavir AST, aspartate aminotransferase ALT, alanine aminotransferase ATV, atazanavir CBC, complete blood cell count D/C, discontinue ddl, didano-sine d4T, stavudine EFV, efavirenz FTC, emtricitabine P1BV, hepatitis B virus F1CV, hepatitis C vims HIV, human immunodeficiency virus IDV, indinavir IV, intravenous LFT, liver function tests LPV/r, lopinavir + ritonavir NNRTI, nonnucleoside reverse transcriptase inhibitor NRTI, nucleoside reverse transcriptase inhibitor NVP, nevirapine PI, protease inhibitor PT, prothrombin time T.bili, total bilirubin TDF, tenofovir disoproxiI fumarate TPV, tipranavir ULN, upper limit of normal ZDV, zidovudine. 

Zidovudine (ZDV or AZT) is a nucleoside reverse transcriptase inhibitor (NRTI) and it was the first anti-HIV agent to be introduced. Other NRTIs include stavudine (d4T), lamivudine (3TC), didano-sine (ddl), abacavir (ABC) and zalcitabine (ddC). Recent additions to this class are emtricitabine (FTC) which has a molecular structure similar to 3TC and tenofovir (TDF) a nucleotide reverse transcriptase inhibitor. 

Birkus G, Hitchcock MJ, Cihlar T. Assessment of mitochondrial toxicity in human cells treated with tenofovir comparison with other nucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother 2002 46 716-23. 

Raltegravir, or Isentress (1), is the first FDA-approved inhibitor of HIV integrase. HIV/AIDS drugs are categorized according to their mode of action as nucleoside and nucleotide reverse transcriptase inhibitors [NRTIs, e.g., tenofovir (2)], nonnucleotide reverse transcriptase inhibitors [NNRTIs, e.g., efavirenz (3)] protease inhibitors [Pis, e.g., ritonavir (4)], fusion inhibitors [e.g., enfuvirtide (5)], entry inhibitors... 

In 2001, tenofovir disoproxil fumarate 61, a prodrug of tenofovir was approved for treatment of HIV, subsequently being preregistered in the USA for treatment of hepatitis B. Emtricitabine 62, a reverse transcriptase inhibitor, was approved in 2003 for HIV. What is of import is that these compounds are now part of fixed dose combination therapies for treatment of HIV, either two drug (tenofovir disoproxil fumarate/emtricitabine) or three drug Atripla (tenofovir disoproxil fumarate/emtricitabine/efavirenz) formulations. Thus, even 50 + years after Bergmann s discovery of bioactive arabinose nucleosides, small molecules synthesised as result of his discoveries are still in clinical use and others are in clinical trials for treatment of viral diseases. 

EFAVIRENZ NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS-DIDANOSINE (ENTERIC-COATED), TENOFOVIR A high treatment failure rate is reported when tenofovir, enteric-coated didanosine and efavirenz are co administered Unknown Use this combination with caution... 

NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS GANCICLOVIRAfALGANCIC LOVIR 1. T adverse effects with tenofovir, zidovudine and possibly didanosine, lamivudine and zalcitabine 2. Possibly 1 efficacy of ganciclovir 1. Uncertain possibly additive toxicity. Lamivudine may compete for active tubular secretion in the kidneys 2. Uncertain L bioavailability 1. Avoid if possible otherwise monitor FBC and renal function weekly. It has been suggested that the dose of zidovudine should be halved from 600 mg to 300 mg daily. Monitor for peripheral neuropathy, particularly with zalcitabine 2. Uncertain clinical significance if in doubt, consider alternative cytomegalovirus prophylaxis... 

The nucleoside analogue reverse transcriptase inhibitors (NRTIs) include abacavir, didanosine, lamivudine, stavu-dine, tenofovir, zalcitabine, and zidovudine (all rINNs). The following abbreviations have been used and may still be encountered in published papers ... 

Tenofovir is a nucleotide (nucleoside monophosphate) analogue reverse transcriptase inhibitor, given as a prodrug, tenofovir disoproxU fumarate. In contrast to the other members of this class, it only needs to be phosphorylated twice intraceUularly before it is pharmacologically active. Adverse effects have been reported as flatulence, raised transaminases, raised creatine kinase activity, and rarely a raised serum creatinine (1). Tenofovir does not currently appear to be nephrotoxic. 

Nucleoside reverse transcriptase inhibitors (NRTIs) were the first class of medications approved for the management of HIV infection. They are structural analogues of nucleic acids. They undergo intracellular phosphorylation to a triphosphate metabolite and it is this metabolite that is pharmacologically active against reverse transcriptase. Drugs in this class include abacavir, adefovir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir, and zidovudine. 

Tenofovir is a nucleotide reverse transcriptase inhibitor (NtRTI). 

Droste JA, Kearney BP, Hekster YA, Burger DM. Assesanent of dn -dnig interactions between tenofovir disoproxil fumarate and the ncfinucleoside reverse transcriptase inhibitors nevirapine and efavirenz in HIV-infected patients. J Acquir Immune Defic Symb- (2006) 41,37-... 

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