HIV Drugs Flashcards
Zidovudine
Nucleoside reverse transcriptase inhibitor. Competitively inhibits reverse transcriptase, can be incorporated into viral DNA chain and cause termination. Requires “P” by cellular enzymes to activate. AE: lactic acidosis w/ hepatic steatosis, mitochondrial tox., hyperlipidemia, granulocytopenia, anemia headache, Nausea, maliase.
Lamivudine
Nucleoside reverse transcriptase inhibitor. Competitively inhibits reverse transcriptase, can be incorporated into viral DNA chain and cause termination. Requires “P” by cellular enzymes to activate. AE: lactic acidosis w/ hepatic steatosis, mitochondrial tox., Also effective against Hep B. Well tolerated.
Abacavir
Nucleoside reverse transcriptase inhibitor. Competitively inhibits reverse transcriptase, can be incorporated into viral DNA chain and cause termination. Requires “P” by cellular enzymes to activate. AE: lactic acidosis w/ hepatic steatosis, mitochondrial tox., hypersensitivity rxns test HLA b5701
Emtricitabine
Nucleoside reverse transcriptase inhibitor. Competitively inhibits reverse transcriptase, can be incorporated into viral DNA chain and cause termination. Requires “P” by cellular enzymes to activate. AE: lactic acidosis w/ hepatic steatosis, mitochondrial tox., Also effective against Hep B. Well tolerated.
Tenofovir
NucleoTide Reverse transcriptase inhibitor. Competitively inhibits reverse transcriptase, can be incorporated into viral DNA chain and cause termination. AE: N/V, diarrhea, renal failure, lactic acidosis.
Etravirine
Non-nucleoside reverse transcriptase inhibitor. Binds directly to the reverse transcriptase at a site different from nucleotide rev. transcriptase inhibs. The enzyme cannot then produce viral DNA. No “P” required. No cross resistance with other drugs. AE: severe rashes, CYP450, nausea, peripherial neuropathy,
Efavirenz
Non-nucleoside reverse transcriptase inhibitor. Binds directly to the reverse transcriptase at a site different from nucleotide rev. transcriptase inhibs. The enzyme cannot then produce viral DNA. No “P” required. No cross resistance with other drugs. AE: severe rashes, CYP450, once daily dosing, CNS effects, vivid dreams, hallucinations
Atazanavir
Protease Inhibitor, given with ritonavir. Prevent viral protease action required for maturation of the fully assembled virus. Prevents cleavage of polypeptide precursors for structural proteins, viral maturation, effective agains strains resistant to reverse transcriptase inhibitors. AE: GI, hepatoxicity, hyperglycemia, insulin res., hyperlipidemia, CYP3A4.
Darunavir
Protease Inhibitor, given with ritonavir. Prevent viral protease action required for maturation of the fully assembled virus. Prevents cleavage of polypeptide precursors for structural proteins, viral maturation, effective agains strains resistant to reverse transcriptase inhibitors. AE: GI, hepatoxicity, hyperglycemia, insulin res., hyperlipidemia, CYP3A4.
Enfuvirtide
(T-20) Fusion inhibitor. Is a synthetic peptide which binds gp41 preventing conformational change in the viral envelope precenting fusion of viral and host membrane and inhibiting entry of the virus into the cell. SubQ admin bid.
Raltegravir
Integrase Inhibitor. Binds integrase to inhibit strand transfer, the final step of provirus integration. Few drug interactions.
Maraviroc
CCR5 receptor antagonist. Prevents HIV-1 entry into the host cell by binding CCR5 and CXCR4 coreceptors. AE: pyrexia, rash, postural dizziness.
Ritonavir
Inhibitor of CYP3A4 and is used at lowdoses to increase serum concentrations of other protease inhibitors.
gag gene
capsid proteins (p24 et al)-diagnostic target for sandwich ELISA as a confirmatory test. Antibodies to p24 via indirect ELISA is initial test
pol gene
Enzyme gene, transcribed as large preproteins and cut into proteins by reverse transcriptase, protease and integrase
