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23 Cards in this Set
- Front
- Back
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Mechanism of action OF: saquinavir, ritonavir, indinavir, nelfinavir, amprenavir
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Protease inhibitors; prevents maturation of new virus by cleaving polypeptide products of HIV mRNA into pieces
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Overall side effects (4) of protease inhibitors?
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1) GI intolerance
2) Inhibition of cytochrome p450 3) Lipid changes 4) thrombocytopenia |
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Which of the protease inhibitors have unfavorable glucose & lipid changes (3)?
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saquinavir, indinavir, amprenavir
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Retonavir is known for causing...
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pancreatitis
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Indinavir is associated with (2)...
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Kidney stones
Insignificant hyperbilirubinemia |
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What is the mechanism of action of zidovudine, didanosine, zalcitabine, stavudine, lamivudine, and abacavir?
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Nucleoside reverse transcriptase inhibitors; gets added to DNA chain and then causes termination bc it lacks a 3' OH group
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Which NRTI is/was given during pregnancy to reduce transmission?
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zidovudine (aka AZT)
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What is a unique side effect of zidovudine?
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Bone marrow suppression
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Which NRTIs (3) cause pancreatitis and peripheral neuropathy?
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Didanosine, stavudine, and zalcitabine
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What side effect is unique to dedanosine and stavudine?
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Hepatic steathosis (fatty change of liver)
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What is the "safest" or one of the safest NRTIs?
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Lamivudine
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Side effect of abacavir (and class of drug)?
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Hypersensitivity rash, it's an NRTI drug
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Describe two things that are different between NRTIs and NNRTIs?
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1) NRTIs need to be phosphorylated by thyrmidine kinase to be active, NNRTIs don't
2) DIT guy says that nucleosides are competitive inhibitors and NNRTIs are non-competitive |
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Name the three NNRTI drugs in FA.
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Nevirapine, Efavirenz, Declaviridine
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What is the general overall side effect of the NNRTIs?
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RASH
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What are two unique side effects of efavirenz?
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1) Test + for cannabinoids
2) CNS side effects like somnolence, confusion, agitation |
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What is the mechanism of action of maraviroc?
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CCR5 coreceptor antagonist that blocks infection of macrophages, aka "entry inhibitor"
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When does maroviroc work better?
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early infection, blocks the CCR5 receptor entry which is attacked by the R5 type virus which is more present earlier in infection.
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What is the mechanism of action of raltegravir?
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Integrase inhibitor; prevents HIV DNA from integrating into human genome
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What is the main side effect of raltegravir?
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unfavorable lipid profile
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What is the mechanism of action of enfuvirtide?
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- it binds the viral gp41 subunit and prevents it from making the confirmational change it needs to to complete fusion; blocking entry and replication
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What side effects would you expect with enfuvirtide (2)?
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1) Hypersensitivity reactions
2) Increased risk of bacterial pneumonia |
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Which category of HIV drug has lactic acidosis as a side effect?
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NRTIs
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