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36 Cards in this Set
- Front
- Back
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What are the targets of HIV treatment?
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Block CCR5 receptor
Block fusion and uncoating Block Reverse Transcriptase Block integrase Block maturation |
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What are the Anti-HIV Drug Classes?
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Nucleoside analogs
Nonnucleoside reverse transcriptase inhibitors Protease inhibitors Integrase inhibitors Fusion inhibitors Entry inhibitors (CCR5 antagonists) |
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What is combination therapy
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The ONLY approved mode of therapy
Use multiple drugs to insure no resistance development and long-term viral suppression |
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What combinations are used in triple combination therapy?
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NNRTI + 2 nukes
PI + 2 nukes II + 2 nukes |
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What is the NNRTI option?
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Efavirenz + Tenofovir + emtricitabine
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What are the Protease Inhibitor options?
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1) Atazanavir + ritonavir + Tenofovir + Emtricitabine
2) Darunavir + ritonavir + Tenofovir + Emtricitabine |
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What is the Integrase Inhibitor option?
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Raltergravir + Tenofovir + Emtricitabine
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What class does this belong in?
Lamivudine |
Nucleoside analog
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What class does this belong in?
Zidovudine |
Nucleoside analog
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What class does this belong in?
Stavudine |
Nucleoside analog
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What class does this belong in?
Didanosine |
Nucleoside analog
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What class does this belong in?
Ritonavir |
Protease inhibitors
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What class does this belong in?
Indinavir |
Protease inhibitors
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What class does this belong in?
Fosampernavir |
Protease inhibitors
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What class does this belong in?
Nelfinavir |
Protease inhibitors
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What class does this belong in?
Saquinavir |
Protease inhibitors
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What class does this belong in?
Efavirenz |
Nonnucleoside Reverse Transcriptase Inhibitors
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What class does this belong in?
Nevirapine |
Nonnucleoside Reverse Transcriptase Inhibitors
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What class does this belong in?
Enfuvirtide |
Fusion Inhibitor
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What class does this belong in?
Maraviroc |
Entry Inhibitor - CCR5 antagonist
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What class does this belong in?
Raltegravir |
Integrase Inhibitor
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What is the black box label warning on Nukes?
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Lactic acidosis with hepatic steatosis
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How are most nukes eliminated?
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Renal except Zidovudine and Abacavir
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What nuke has bone marrow degeneration as an adverse effect?
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Zidovudine
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What nuke has minimal toxicity?
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Lamivudine
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What is the preferred nuke in pregnant women?
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Zidovudine or lamivudine
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What Nonnucleoside Reverse Transcriptase Inhibitor is safe for use in pregnant women?
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Nevirapine
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What are some of the adverse effects associated with Efavirenz?
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Neurophychiatric
Teratogenic Metabolized by p450 |
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What are some of the adverse effects associated with Nevirapine?
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Rash including rare but serious hypersensitivity (stevens-johnson syndrome or toxic epidermal necrolysis)
Symptomatic hepatitis Metabolized by p450 |
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What is the protease inhibitor's mechanism of action?
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Competitive inhibition of viral protease
Irreversibly binds to protease active site |
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What compound is used to boost PK of protease inhibitors? How does it work?
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Ritonavir
Use every time! Improves bioavailability by blocking CYP3A4 |
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What are some adverse effects associated with Protease inhibitors?
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Hepatotoxicity
Lipodystrophy Hyperlipidemia Insulin resistance |
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What is the mechanism of action of Integrase Inhibitors?
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Blocks HIV integrase from inserting viral genome into host DNA
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What is the mechanism of action of HIV fusion inhibitors?
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Blocks the entry of HIV-1 into CD4+ cells by binding gp41 subunit HIV envelope gylcoprotein
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What is the primary population use of Enfuvirtide?
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Highly drug experienced patients
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What is the mechanism of action of entry inhibitors?
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CCR5 antagonist Maraviroc blocks the HIV gp120 from associating with the receptor
Only works in CCR5 cells!!! |
