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NRTIs Lamivudine

Saquinavir, the first anti-HIV drug as aPI 3TC (lamivudine) NRTI The FDA approves Saquinavir in a record 97 days... [Pg.24]

At present there are seven NRTIs, which have been formally approved for the treatment of AIDS 3 -azido-2, 3 -dideoxythymidine (AZT, zidovudine), 2, 3 -dideoxyinosine (ddl, didanosine), 2, 3 -dideoxycytidine (ddC, zalcitabine), 2, 3 -didehydro-2, 3 -dideoxythymidine (d4T, stavudine), (—)-L-3 -thia-2, 3 -dideoxycytidine (3TC, lamivudine), cyclopentenyl V -cyclopropylaminopurine (abacavir, ABC), and (—)-L-5-fluoro-3 -thia-2, 3 -dideoxycytidine ((—)FTC, emtricitabine) (De Clercq 2004a) (Fig. 3). [Pg.73]

In addition to the NRTI lamivudine (3TC) and the NtRTI adefovir dipivoxU and tenofovir disoproxil fumarate (which has been recently licensed for the treatment of chronic hepatitis B), two other nucleoside analogues, that is, entecavir and L-dT (tel-bivudine) (Fig.4aa), have been licensed for the treatment of HBV infections. Two other compounds 3 -Val-L-dC (valtorcitabine) and L-FMAU (clevudine) (Fig. 4aa) are in clinical development for the treatment of HBV infections, and yet two other compounds, that is, racivir and elvucitabine (Fig. 3), yield potential for the treatment of both HBV and HIV infections. [Pg.75]

There are currently six major antiretroviral drug families (Table 5). Nucleoside reverse transcriptase inhibitors (NRTI) are nucleoside analogs (discussed in more detail in chapter by De Clercq and Neyts, this volume) and were the first approved antiretroviral agents. They include drugs such as AZT, didanosine (ddl), stavudine (d4T), abacavir (ABC), and lamivudine (3TC), the latest used at doses of 300 mg daily as anti-HIV agent (lOOmg/day is the dosing approved for treatment of HBV... [Pg.334]

Triple NRTI therapy is recommended only when a first-line or alternative first-line therapy with either an NNRTI-based or Pi-based regimen cannot be used. Abacavir plus zidovudine plus lamivudine is the only regimen approved by the DHHS. The following triple nucleoside therapy combinations have shown poor or limited efficacy, and should be avoided abacavir plus tenofovir plus lamivudine (or emtricitabine), and didanosine plus tenofovir plus lamivudine (or emtricitabine). [Pg.1259]

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. [Pg.1271]

The present NRTIs available for the treatment of HIV are zidovudine (azidothymidine, AZT), stavu-dine (d4T), didanosine (ddl), lamivudine (3TC), dideoxycytidine (ddC, zalcitabine) and abacavir, emtricitabine and tenofovir disoproxil. Combination formulations are abcavir combined with zidovudine and lamivudine and the abacavir-lamivudine combination. [Pg.421]

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. [Pg.550]

As a class effect NRTIs are associated with lactic acidosis and hepatic steatosis, conditions which may occur more frequently in pregnant women. The individual NRTIs have their own adverse reactions. Pancreatitis is seen with lamivudine, stavudine, di-danosine and rarely with zalcitabine while the latter three agents can also induce peripheral neuropathy. [Pg.550]

Lamivudine is the best-tolerated NRTI. Its most common adverse effects include headache, malaise, fatigue, and insomnia. Pancreatitis is rare. Gastrointestinal complaints are common with lamivudine-zidovudine therapy but are probably mainly due to the zidovudine component. Lamivudine resistance sometimes occurs early in treatment. Cross-resistance to zal-citabine, didanosine, and abacavir can occur simultaneously. Withdrawal of lamivudine in patients infected with both hepatitis B virus and HIV can cause a flare-up of hepatitis symptoms. [Pg.588]

NRTIs) abacavir sulfate didanosine (ddl) lamivudine (3TC) stavudine (d4T) zalcitabine (ddC) zidovudine (AZT)... [Pg.617]

Several anti-HBV agents have anti-HIV activity as well, including lamivudine, adefovir dipivoxil, and tenofovir. Emtricitabine, an antiretroviral NRTI, is under clinical evaluation for HBV treatment. Because NRTI agents may be used in patients co-infected with HBV and HIV, it is important to note that acute exacerbation of hepatitis may occur upon discontinuation or interruption of these agents. [Pg.1084]

Antiretroviral nucleoside analogues have been associated with hepatic steatosis and lactic acidosis. These compounds require phosphorylation to active triphosphate derivatives by cellular phosphokinases. The triphosphate nucleotide inhibits the growing proviral DNA chain, but it also inhibits host DNA polymerases, and this can result in compensatory glycolysis and lactic acidosis. Abnormal mitochondrial oxidation of free fatty acids causes the accumulation of neutral fat in liver cells, and this manifests as hepatomegaly with macrovesicular steatosis. Hepatic steatosis and lactic acidosis have been reported previously with zidovudine, didanosine, zalcita-bine, Combivir (zidovudine plus lamivudine), and lamivudine. Of 349 Australian patients studied for 18 months (516 patient-years) taking NRTIs only two had severe lactic acidosis (847). [Pg.631]

At the present time, there are at least 14 compounds that have been formally approved for the treatment of human immunodeficiency virus (HIV) infections. There are six nucleoside reverse transcriptase inhibitors (NRTIs) that, after their intracellular conversion to the 5 -triphosphate form, are able to interfere as competitive inhibitors of the normal substrates (dNTPs). These are zidovudine (AZT), didanosine (ddl), zalcitabine (ddC), stavudine (d4T), lamivudine (3TC), and abacavir (ABC). There are three nonnucleoside reverse transcriptase inhibitors (NNRTIs) — nevirapine, delavirdine, and efavirenz — that, as such, directly interact with the reverse transcriptase at a nonsubstrate binding, allosteric site. There are five HIV protease inhibitors (Pis saquinavir, ritonavir, indinavir, nelfinavir, and amprenavir) that block the cleavage of precursor to mature HIV proteins, thus impairing the infectivity of the virus particles produced in the presence of these inhibitors. [Pg.387]

Nevirapine = Viramune] (dipyridodiazepinone) [NRTIs in clinical use Abacavir (ABC) Adefovir dipivoxil (9-[2-Phosphonomethoxy)ethyl] -adenine PMEA) AZT Didanosine (= 2, 3 -Dideoxyinosine) Lamivudine Stavudine Zalcitabine (2, 3 -Dideoxycytidine]... [Pg.386]

Preferred Pl-based regimens are lopinavir/ritonavir plus lamivudine or emtricitabine plus another NRTI, usually zidovudine, stavudine or abacavir. Alternative combinations include other Pis with or without ritonavir, and two NRTIs. The combination of a protease inhibitor with ritonavir provides inhibition of cytochrome p450 enzymes and permits less frequent dosing of amprenavir, indinavir, lopinavir and saquinavir. Use of ritonavir in this setting is also known as boosting. ... [Pg.610]

Zidovudine monotherapy was the only available treatment for HIV disease before the 1990s, and was used until 1992. Zidovudine monotherapy has been proven to be efficacious for both the treatment of HAD as well as for HIV-associated minor cognitive/motor disorder (MCMD) (Arendt et al., 1992 Sidtis et al., 1993 Tozzi et al., 1993). Unfortunately, the beneficial effect of zidovudine was transient and an addition of a second NRTI such as dideoxyinosine (ddl), lamivudine (3TC), or dideoxycytidine (ddC), may not further improve psychomotor performance. Stavudine was shown to improve motor performance even after pretreatment with zidovndine (Arendt et al., 2001). A study in 1998, using abacavir versns placebo showed no nenrologic deterioration in the abacavir group as compared with the placebo group (Lanier et al., 2001). However, there was no benefit when abacavir was added to a stable ART, despite good proven CNS penetration. [Pg.611]

In a multicenter trial, 128 chUdren were randomly assigned to one of three regimens zidovudine + lamivudine (n — 36), zidovudine + abacavir (n = 45), or lamivudine + abacavir (n — 47) (12). The children who were free of symptoms (n — 55) were also randomized to nelfinavir or placebo, while those with more advanced disease received open-label nelfinavir (n — 73). All 13 episodes of diarrhea occurred in those taking nelfinavir. Nelfinavir did not affect serum cholesterol or triglyceride concentrations and there were no cases of lipodystrophy. There were 24 serious adverse events six were in the symptom-free children (all taking nelfinavir), but all were attributed to the NRTIs. [Pg.2434]

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 ... [Pg.2586]

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. [Pg.387]

Three NRTI medications are Abacavir (Ziagen, ABC), Abacavir, and Lamivudine (Epzicom). [Pg.265]

There are currently a variety of nucleoside analogs (i.e., AZT [zidovudine] [3], DDC [zalcitabine] [4], DDI [didanosine] [4], D4T [stavudine] [5], and 3TC [lamivudine] [6] [also designated NRTIs or nucleoside RT inhibitors]) and two nonnucleoside RT inhibitors (i.e., nevirapine [viramune] and BHAP [delavirdine] [also designated NNRTIs] [7,8]) officially approved for treatment of HIV-infected individuals. It should be noted that the NNRTIs are uniquely active against HIV-1, but not HIV-2 RT, whereas the NRTIs inhibit both HIV-1 and HIV-2 RTs. In addition, several other structural classes of... [Pg.283]

I Lamivudine, 3TC Least toxic of the NRTIs, but some GI effects and neutropenia— active in hepatitis B... [Pg.212]

Mechanisms Like other NRTIs, lamivudine requires activation by host cell kinases and the drug is active against HIV-1, including strains resistant to zidovudine. Lamivudine is also effective in hepatitis B, and HBV nucleic acid is undetectable after treatment for 12 weeks. [Pg.431]


See other pages where NRTIs Lamivudine is mentioned: [Pg.198]    [Pg.10]    [Pg.73]    [Pg.1266]    [Pg.1275]    [Pg.461]    [Pg.1838]    [Pg.201]    [Pg.320]    [Pg.554]    [Pg.201]    [Pg.297]    [Pg.320]    [Pg.531]    [Pg.537]    [Pg.1134]    [Pg.140]    [Pg.198]    [Pg.325]    [Pg.610]    [Pg.610]    [Pg.610]    [Pg.610]    [Pg.610]    [Pg.896]    [Pg.2261]   
See also in sourсe #XX -- [ Pg.800 ]




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