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Flashcards in Antiretrovirals Deck (31):
1

Drug that interferes with entry of HIV-1 into cells. HIV enters a cell by attachment of gp120 to the CD4 receptor, followed by binding to either the CCR5 or CXCR4 receptor. This drug binds to the CCR5 receptor preventing the interaction between HIV-1 gp120 and CCR5 receptor

Maraviroc

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Maraviroc

Interferes with entry of HIV-1 into cells by binding to the CCR5 receptor preventing the interaction between HIV-1 gp120 and CCR5 receptor

3

Dosing adjustments: Maraviroc

No dose adjustment for renal/hepatic insufficiency, but avoid in significant renal dysfunction

4

Drug-Drug Interactions: Maraviroc

No significant effect on other drugs, but inhibitors of CYP3A increase maraviroc levels (Protease inhibitors) and Inducers of CYP3A decrease maraviroc levels (Efavirenz/Etravirine, rifapentine, and St. John's wort)

5

Toxicity: Maraviroc

Allergic reactions, rash, hepatotoxicity

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Drug that interferes with entry of HIV-1 into cells. Inhibits fusion of viral and cellular membranes. Binds to the first heptad repeat in the gp41 subunit of the virus

Enfuvirtide

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Delivery and dosing adjustments: Enfuvirtide

Subcutaneous injection. Catabolism to constituent amino acids. No dose adjustment for renal/hepatic insufficiency

8

Drug-Drug Interactions: Enfuvirtide

No drug-drug interactions

9

Toxicity: Enfuvirtide

Injection site reactions. Bacterial pneumonia. Hypersensitivity ? 1%

10

Nucleoside (Thymidine) analog(s) reverse transcriptase inhibitor(s) (NRTI)

Zidovudine

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Excretion and dosing adjustments: Nucleoside analog reverse transcriptase inhibitors (NRTIs)

Renal excretion. Dose adjustment for renal insufficiency except for abacavir. Adjustment for abacavir in hepatic insufficiency

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Nucleoside (Guanosine) analog(s) reverse transcriptase inhibitor(s) (NRTI)

Abacavir

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Abacavir can cause what unique side effect

A hypersensitivity reaction

14

Nucleoside (Cytidine) analog(s) reverse transcriptase inhibitor(s) (NRTI)

Lamivudine & Emtricitabine

15

Tenofovir can cause what unique side effect

Renal insufficiency

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Toxicities: Nucleoside analog reverse transcriptase inhibitors (NRTIs)

Mitochondrial toxicity with lactic acidosis (Onset over months. Vague GI symptoms, malaise. Can progress to multiorgan failure and death), Hepatotoxicity (Onset over months to years), Steatosis

17

NucleoTide (Adenine) analog(s) reverse transcriptase inhibitor(s) (NRTI)

Tenofovir

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What, if administered with didanosine (a guanosine analog reverse transcriptase inhibitor), wil increase didanosine levels

Tenofovir

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Zidovudine antagonizes phosphorylation of what

Stavudine, a nucleoside (thymidine) analog(s) reverse transcriptase inhibitor (NRTI)

20

Drug that requires no intracellular metabolism for activation. Reversible non-competitive inhibitor of HIV reverse transcriptase. Binding to reverse transcriptase blocks RNA- and DNA-dependent DNA polymerase action of the enzyme

Efavirenz (non-nucleoside reverse transcriptase inhibitor: NNRTI)

21

Metabolism and dosing adjustments: Efavirenz

Metabolized by cytochrome P450 (CYP3A4). No dose adjustment for renal insufficiency. Caution with hepatic insufficiency (more so when taking related drug nevirapine)

22

Drug-Drug Interactions: Efavirenz

It is both metabolized by and an inducer of CYP3A4. Simultaneous use of protease inhibitors (Inducers of P450 3A4) may require dose adjustment. Avoid sedatives such as midazolam and alprazolam (these are metabolized by CYP3A4 and will not function properly when administered with efavirenz)

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Toxicity: Efavirenz

Can cause some CNS side effects and it may be teratogenic. Skin Rash with onset in days to weeks. Stevens-Johnson Syndrome/Toxic Epidermal necrosis, Hepatotoxicity (all worse with nevirapine, a different NNRTI )

24

Drug that interferes with HIV-1 integrase. Prevents insertion of linear HIV-1 DNA into host DNA. Prevents formation of HIV-1 provirus

Raltegravir (Integrase Inhibitor)

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Metabolism and dosing adjustment: Raltegravir

Metabolized by hepatic UGT1A1 glucuronidation. No dose change

26

Drug-drug interaction: Raltegravir

Increase dose when taken w/rifampin

27

Toxicities: Raltegravir

Nausea, headache, diarrhea, Fever, increased CPK (muscle pain/inflammation), Rare rash, hypersensitivity

28

Drug(s) that block protease cleavage of viral gag and gag-pol polyproteins. Immature noninfectious viral particles. No intracellular metabolism. Active in resting and infected cells

Protease Inhibitors (Atazanavir and Darunavir)

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Dosing adjustment: Protease Inhibitors (Atazanavir and Darunavir)

No dose adjustment for renal insufficiency. Caution with hepatic insufficiency. Not recommended if significant liver impairment

30

Drug-drug interaction: Protease Inhibitors (Atazanavir and Darunavir)

Protease inhibitors are metabolized by cytochrome P450 3A4. In general avoid rifampin and other rifamycins. Avoid sedatives such as midazolam and alprazolam. Avoid fluticasone nasal spray with all ritonavir-boosted PI regimens (Adrenal suppression and Cushing's syndrome). Avoid proton pump inhibitors with atazanavir (Lowers absorption significantly)

31

Toxicities: Protease Inhibitors (Atazanavir and Darunavir)

Increased bleeding episodes in hemophiliacs, Hepatotoxicity, Possible Lipodystrophy (fat redistribution), Premature coronary artery disease, Hyperlipidemia, Osteonecrosis