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Reverse Transcriptase InhibitorsHIV Reverse TranscriptaseNucleosidesAnti-HIV AgentsDrug Resistance, ViralHIV-1BenzoxazinesNevirapineZidovudineHIV InfectionsDelavirdineOrganophosphonatesHIV Protease InhibitorsRNA-Directed DNA PolymeraseDideoxynucleosidesStavudinePurine NucleosidesAdenineDrug Resistance, Multiple, ViralDidanosineOxazinesPyrimidine NucleosidesNucleoside Transport ProteinsAntiretroviral Therapy, Highly ActiveLamivudineZalcitabinePyrimidinonesDideoxynucleotidesPyridazinesRitonavirPyranocoumarinsLopinavirViral LoadAnti-Retroviral AgentsEquilibrative Nucleoside Transporter 1MutationHIVCD4 Lymphocyte CountRNA, ViralDrug Therapy, CombinationAntiviral AgentsVirus ReplicationTreatment FailureNelfinavirThymine NucleotidesHIV ProteaseMolecular Sequence DataRibonuclease HHIV-Associated Lipodystrophy SyndromeHIV Integrase InhibitorsThioinosinePurine-Nucleoside PhosphorylaseTelomeraseReverse Transcriptase Polymerase Chain ReactionAcidosis, LacticDrug InteractionsBase SequenceDeoxyadenosinesReverse TranscriptionGuanosineMutation, Missensepol Gene Products, Human Immunodeficiency VirusIndinavirGenotypeCell LineUridineFuransSaquinavirIntegrase InhibitorsHIV-2Nucleoside-Diphosphate KinaseInosineDrug Resistance, MicrobialAcquired Immunodeficiency SyndromeKineticsPyrrolidinonesNitrilesAmino Acid SubstitutionNucleotidesAnilidesInhibitory Concentration 50BenzoxazolesMolecular StructurePyridinesProtease InhibitorsDeoxycytidinePyridonesNucleoside QDNA, ViralStructure-Activity RelationshipAvian myeloblastosis virusFoscarnetLipodystrophyCytidineAmino Acid SequenceEquilibrative-Nucleoside Transporter 2Chromatography, High Pressure LiquidNucleoside-TriphosphatasePyrimidinesTemplates, Genetic

NRTIsNRTINNRTIEmtricitabineEfavirenzTenofovirAnalog reverse transcripProtease inhibitorHAARTRegimensLamivudineEnzymeDidanosineInhibitionInfectionAntiretroviral drugsDrugsIntegrase inhibitorsSubstrateIndinavirPolymeraseAnalogueSimvastatinRegimenStatinsNucleotidesTreatmentPotentInhibitsBindInteractionsStructuralDrug-resistant

NRTIs11

• There are two classes of drugs that target the HIV-1 RT enzyme, nucleoside/nucleotide reverse-transcriptase inhibitors (NRTIs/NtRTIs) and non-nucleoside reverse-transcriptase inhibitors (NNRTIs). (wikipedia.org)
• Nucleoside reverse transcriptase inhibitors (NRTIs) block the action of an enzyme called reverse transcriptase, which HIV needs to replicate. (medicalnewstoday.com)
• Resistance to multiple nucleoside reverse transcriptase inhibitors (NRTIs) may result from several genotypically distinct pathways, including the Q151M (151 complex), the 69 insertion complex, two distinct thymidine analogue mutational pathways and the K65R mutation. (neb.com)
• Entecavir is used in the treatment of Hepatitis B and belongs to the drug class nucleoside reverse transcriptase inhibitors (NRTIs) . (drugs.com)
• Emtricitabine belongs to a group of drugs called nucleoside reverse transcriptase inhibitors (NRTIs) and tenofovir is a nucleotide reverse transcriptase inhibitor (NRTI). (rxwiki.com)
• Several classes of anti-HIV drugs interfere with this stage of HIV's life cycle: nucleoside reverse transcriptase inhibitors and nucleotide reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs). (aidsmap.com)
• Although newer classes of drugs are available, the most commonly used drugs approved for the treatment of HIV infection fall into three classes: nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs) and protease inhibitors (PIs). (canada.ca)
• PZA PZA include protease inhibitors, NRTIs, and NNRTIs. (cdc.gov)
• Most experience with nevirapine is in combination with nucleoside reverse transcriptase inhibitors (NRTIs). (who.int)
• Eligibility criteria For maternal outcomes, we considered randomised controlled trials (RCTs) comparing tenofovir-based regimens with those with alternative nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs). (bmj.com)
• Emtricitabine and tenofovir are in a class of medications called nucleoside reverse transcriptase inhibitors (NRTIs). (safemedication.com)

NRTI2

• Reverse transcriptase is the target for numerous approved anti-HIV drugs including both nucleoside inhibitor (NRTI) and non-nucleosides (NNRTI). (ox.ac.uk)
• Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI), emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI), and tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor (NtRTI). (aidsmap.com)

NNRTI4

• These inhibitors can inhibit reverse transcriptase by binding to NNRTI binding pocket (NNIBP). (immune-system-research.com)
• Such clustering implies a direct stereochemical basis for NNRTI resistance mechanisms, which is indeed observed in many cases such as the loss of key ring stacking interactions with inhibitors via mutations at Tyr181 and Tyr188. (ox.ac.uk)
• RESCRIPTOR tablets contain delavirdine mesylate, a synthetic non-nucleoside reverse transcriptase inhibitor (NNRTI) of the human immunodeficiency virus type 1 (HIV-1). (drugs.com)
• New non-nucleoside reverse transcriptase inhibitors (NNRTI), which are similar in structure to earlier described di(arylamino)pyrimidines but featuring a 2,6-di(arylamino)-3-fluoropyridine, 2,4-di(arylamino)-5-fluoropyrimidine, or 1,3-di(arylamino)-4-fluorobenzene moiety instead of a 2,4-disubstituted pyrimidine moiety, are reported. (itg.be)

Emtricitabine3

• Emtricitabine is a synthetic nucleoside cytosine analogue. (medscape.com)
• Here, the water-soluble nucleoside reverse transcriptase inhibitor emtricitabine (FTC) has been used as a novel A-B monomer in step-growth polymerisation with chloroformate functional C n monomers, to produce new poly(carbamate/carbonate) structures with varying architecture. (johnshopkins.edu)
• Raltegravir (Isentress) -- the sole approved integrase inhibitor -- plus tenofovir/emtricitabine remains the 'preferred' regimen. (hivandhepatitis.com)

Efavirenz2

• INH Daily for 2 weeks and INH 2 times/week for The patient should be monitored If the patient also is taking RFB then 2 times/week for RFB 4 months (18 weeks) carefully for RFB drug toxicity efavirenz, the daily or twice (arthalgia, uveitis,leukopenia) weekly dose of RFB is increased if RFB is used concurrently from 300mg to 450 mg. with protease inhibitors or NNRTIs. (cdc.gov)
• Efavirenz is in a class of medications non-nucleoside reverse transcriptase inhibitors (NNRTIs). (safemedication.com)

Tenofovir1

• Cochrane Abstracts , Evidence Central , evidence.unboundmedicine.com/evidence/view/Cochrane/432835/all/Tenofovir_or_zidovudine_in_three_drug_combination_therapy_with_one_nucleoside_reverse_transcriptase_inhibitor_and_one_non_nucleoside_reverse_transcriptase_inhibitor_for_initial_treatment_of_HIV_infection_in_antiretroviral_na��ve_individuals:_Cochrane_systematic_review. (unboundmedicine.com)

Analog reverse transcrip1

• The table contains 195 products whose active ingredient are classified under the same pharmacologic class Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor [EPC]. (ndclist.com)

Protease inhibitor7

• METHODS: Samples of semen and blood were obtained from a cohort of 12 nucleoside reverse transcriptase inhibitor experienced men before and during 25-68 weeks of combination therapy, which included the protease inhibitor indinavir. (bmj.com)
• 3000% increase in simvastatin concentrations, simvastatin should never be given concurrently with any protease inhibitor. (ebmconsult.com)
• However, use of simvastatin in HIV-infected patients receiving highly active antiretroviral therapy (HAART) is limited by the potential for this drug to interact with antiretroviral medications, specifically drugs from the protease inhibitor class. (ebmconsult.com)
• One key study showed a 3,059% increase in simvastatin exposure when coadministration with the protease inhibitor combo, saquinavir (Invirase) and ritonavir (Norvir).2 The mechanism for the interaction is potent inhibition of the cytochrome P450 3A4 enzyme by all known protease inhibitors. (ebmconsult.com)
• In particular, CYP450 3A4 is responsible for the vast majority of simvastatin metabolism and plasma clearance.3 Thus, protease inhibitor mediated inhibition of the CYP450 3A4 clearance pathway for simvastatin results in dangerously high concentrations of this statin. (ebmconsult.com)
• Dolutegravir-based treatment in PLHIV with pre-existing nucleoside reverse transcriptase inhibitor-mutations was non-inferior to protease inhibitor-based regimens. (lu.se)
• Insulin resistance (IR) is common in HIV-seropositive patients, particularly among those receiving protease inhibitor (PI) and is more prevalent among those with lipoatrophy or fat accumulation in the visceral region. (bvsalud.org)

HAART2

• Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are an important part of HAART. (immune-system-research.com)
• Increased risk of preterm delivery among HIV-infected women randomized to protease versus nucleoside reverse transcriptase inhibitor-based HAART during pregnancy. (bvsalud.org)

Regimens1

• The mean time on ART was 75.5 months (95% confidence interval [CI]: 69.0-81.9 months), and 93.7% of the patients were receiving non-nucleoside reverse transcriptase inhibitor-based regimens. (who.int)

Lamivudine1

• In drug combination studies of delavirdine with zidovudine, didanosine, zalcitabine, lamivudine, interferon-α, and protease inhibitors, additive to synergistic anti-HIV-1 activity was observed in cell culture. (drugs.com)

Enzyme5

• NNRTIs inhibit reverse transcriptase (RT), an enzyme that controls the replication of the genetic material of HIV. (wikipedia.org)
• The most popular target in the field of antiretroviral drug development is the HIV-1 reverse transcriptase (RT) enzyme. (wikipedia.org)
• Nucleoside reverse transcriptase inhibitors inhibit the enzyme that allows for reproduction of the virus. (medscape.com)
• Protease inhibitors (PIs) impede another enzyme called HIV protease. (medicalnewstoday.com)
• Use of simvastatin with protease inhibitors increases the risk of statin adverse effects such as liver enzyme elevations and even rhabdomyolysis. (ebmconsult.com)

Didanosine1

• It was also fueled by the fact that a lot of those early drugs, especially in the 1990s and early 2000s, were quite toxic - drugs like zidovudine (AZT) , stavudine (d4T), didanosine (ddI) , and the early protease inhibitors . (medscape.com)

Inhibition2

• Mechanism of inhibition of HIV-1 reverse transcriptase by non-nucleoside inhibitors. (ox.ac.uk)
• The relationship between the in vitro susceptibility of HIV-1 RT inhibitors and the inhibition of HIV replication in humans has not been established. (drugs.com)

Infection2

• TROGARZO, a CD4-directed post-attachment HIV-1 inhibitor, in combination with other antiretroviral(s), is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in heavily treatment-experienced adults with multidrug resistant HIV-1 infection failing their current antiretroviral regimen. (nih.gov)
• This guideline presents updated data about drug interactions between protease inhibitors and non-nucleoside reverse transcriptase inhibitors for treatment of HIV infection together with rifamycins for treatment of TB. (cdc.gov)

Antiretroviral drugs2

• Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV). (wikipedia.org)
• The development of NNRTIs improved quickly into the 1990s and they soon became the third class of antiretroviral drugs, following the protease inhibitors. (wikipedia.org)

Drugs3

• The most commonly used drugs used in ART target the reverse transcriptase (RT) and protease enzymes. (canada.ca)
• Lenacapavir belongs to a new class of anti-HIV drugs called capsid inhibitors. (catie.ca)
• Cardiovascular Drugs / Antilipemic Agents / HMG-CoA Reductase Inhibitors (i.e. (tevausa.com)

Integrase inhibitors2

• Long-acting injectable contraception is compatible with protease inhibitors and NNRTIs, but data are limited with integrase inhibitors. (medscape.com)
• Integrase inhibitors block this action. (medicalnewstoday.com)

Substrate1

• Zalcitabine inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. (pharmacycode.com)

Indinavir2

• Poor reduction of HIV-1 RNA titres in nucleoside reverse transcriptase inhibitor experienced patients treated with indinavir combination therapy. (bmj.com)
• Administration with protease inhibitors: indinavir should be administered at least 1 hour before or after ddI on an empty stomach. (cdc.gov)

Polymerase2

• Comparison with the structures of four different RT and non-nucleoside inhibitor complexes reveals that only minor domain rearrangements occur, but there is a significant repositioning of a three-stranded beta-sheet in the p66 subunit (containing the catalytic aspartic acid residues 110, 185 and 186) with respect to the rest of the polymerase site. (ox.ac.uk)
• Delavirdine binds directly to reverse transcriptase (RT) and blocks RNA-dependent and DNA-dependent DNA polymerase activities. (drugs.com)

Analogue2

• Reference: Nucleoside and nucleotide analogue reverse transcriptase inhibitors: a clinical review of antiretroviral resistance. (neb.com)
• This review summarizes research advances that further the understanding of nucleoside and nucleotide analogue resistance mutations, and their interplay. (neb.com)

Simvastatin1

• The reason why simvastatin use is contraindicated with protease inhibitors is related to the pharmacokinetic properties of both protease inhibitors and simvastatin. (ebmconsult.com)

Regimen1

• Enskyce™ (desogestrel and ethinyl estradiol tablets USP) provides an oral contraceptive regimen of 21 light orange round tablets each containing 0.15 mg desogestrel (13-ethyl-11-methylene-18,19-dinor-17 alpha-pregn-4-en-20-yn-17-ol) and 0.03 mg ethinyl estradiol (19-nor-17 alpha-pregna-1,3,5 (10)-trien-20-yne-3,17,diol). (nih.gov)

Statins1

• Pharmacokinetic interactions between protease inhibitors and statins in HIV seronegative volunteers: ACTG Study A5047. (ebmconsult.com)

Nucleotides2

• Nucleosides, Nucleotides and Nucleic Acids , 26 (10-12), 1543-1546. (elsevierpure.com)
• Nucleosides must be chemically changed into nucleotides before they can be used to make DNA or RNA. (aidsmap.com)

Treatment2

• Daklinza (daclatasvir) is a hepatitis C virus (HCV) NS5A inhibitor indicated for use with sofosbuvir for the treatment of chronic HCV genotype 3. (rxlist.com)
• Lower efficacy for protease inhibitors was not due to lower adherence to treatment. (lu.se)

Potent2

• 4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity. (adooq.com)
• The study based on the hypotheses proved the validity of the hypotheses and resulted in the development of 2′-deoxy-4′-C-ethynyl-2-fluoroadenosine, a nucleoside reverse transcriptase inhibitor, with highly potent activity against all HIV-1, very favorable toxic profiles, and stability in plasma. (elsevierpure.com)

Inhibits1

• ZLM-66 inhibits wild type (WT) HIV-1 reverse transcriptase (RT) with an IC 50 of 41 nM, as well as suppresses multiple HIV-1 mutant strains with EC 50 s of 13 nM, 13 nM, 24 nM, 25 nM and 58 nM against HIV-1 WT, K103N, L1001, E138K, and Y181C, respectively. (immune-system-research.com)

Bind1

• Non-nucleoside reverse transcriptase inhibitors (NNRTIs) bind to reverse transcriptase and prevent HIV from replicating. (medicalnewstoday.com)

Interactions1

• Such factors include reduced interactions with Tyr181, the presence of inhibitor/main-chain H-bonds and ability to undergo conformational flexing and rearrangement within the mutated drug site. (ox.ac.uk)

Structural1

• Structural basis for drug resistance mechanisms for non-nucleoside inhibitors of HIV reverse transcriptase. (ox.ac.uk)

Drug-resistant1

• The nucleoside will prevent or delay the emergence of drug-resistant HIV-1 variants and be an ideal therapeutic agent for both HIV-1 and HBV infections. (elsevierpure.com)