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Flashcards in HIV Drugs Deck (16):
1

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.

2

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.

3

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

4

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.

5

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.

6

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,

7

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

8

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.

9

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.

10

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.

11

Raltegravir

Integrase Inhibitor. Binds integrase to inhibit strand transfer, the final step of provirus integration. Few drug interactions.

12

Maraviroc

CCR5 receptor antagonist. Prevents HIV-1 entry into the host cell by binding CCR5 and CXCR4 coreceptors. AE: pyrexia, rash, postural dizziness.

13

Ritonavir

Inhibitor of CYP3A4 and is used at lowdoses to increase serum concentrations of other protease inhibitors.

14

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

15

pol gene

Enzyme gene, transcribed as large preproteins and cut into proteins by reverse transcriptase, protease and integrase

16

env gene

envelope glycoproteins gp120 and gp41