Term
HIV Attachment/Fusion inhibitors examples |
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Definition
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Term
maraviroc category, mode of action, screening, indication? |
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Definition
anti HIV attachment/fusion inhibitor; CCR5 receptor antagonist, blocks attachment of HIV pg120 to T-cell; must do CCR5 tropism test as some HIV use CCR5 while others use CXCR4 co-receptor on T-cell; use only in combination therapy if other drugs fail. |
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Term
enfuvirtide category, mode of action |
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Definition
anti HIV attachment/fusion inhibitor; binds to HIV's intracellular gp41 and prevents fusion of HIV capsid and T-cell cell membrane AFTER HIV has attached to T-cell via gp120 and T-cell CD4 receptor |
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Term
HIV reverse transcriptase inhibitors: 2 categories, examples from each |
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Definition
nucleoside (zidovudine, didanosine, stavudine, abacavir, zalcitabine, emtricitabine, tenofovir) "TAZES DogZ"; non-nucleoside (nevirapine, delavirdine, efavirene) "DEN" |
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Term
nucleoside reverse transcriptase inhibitors mode of action, indication, SE (why)? |
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Definition
competes with native nucleotides, resulting in termination of DNA synthesis; for HIV 1 or 2 (West African); SE: b/c human gamma DNA polymerase in mitochondia has some affinity for these drugs...1)severe peripheral neuropathy 2) pancreatitis 3) hematoxicity "HIV HaPpeNs" |
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Term
Zidovudine mode of action, tx, SE? |
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Definition
Nucleoside reverse transcriptase inhibitor; HIV combination therapy (use two different ones); SE: severe peripheral neuropathy |
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Term
Didanosine mode of action, tx, SE? |
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Definition
Nucleoside reverse transcriptase inhibitor; HIV combination therapy (use two different ones); SE: severe peripheral neuropathy, pancreatitis |
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Term
Stavudine mode of action, tx, SE? |
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Definition
Nucleoside reverse transcriptase inhibitor; HIV combination therapy (use two different ones); SE: severe peripheral neuropathy (71%) and lipo-atropy |
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Term
abacavir mode of action, tx, SE? |
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Definition
Nucleoside reverse transcriptase inhibitor; HIV combination therapy (use two different ones); SE: If HLA-B*5701 gene-> multisystem hypersensitivity -> becomes life threatening (screen, 5-8%) |
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Term
non-nucleoside reverse transcriptase inhibitors root, mode of action, advantage, indication, metabolism, SEs (3)? |
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Definition
-vir-; non competitive inhibitors of HIV reverse transcriptase; don't have to be phosphorylated, highly selective; only for HIV 1; CYP450 3A4 (inhibit: azole antifungal, cimetidine, erythromycin, grapefruit juice; induce: rifampin, carbamazepine, phenytoin, St. John's wort); SE: 1)temporary rash 2) hepatitis 3) CNS (temporary insomnia, vivid dreams)...RHC Really Hard Core HIV |
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Term
Nevirapine mode of action, tx, SE? |
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Definition
Non-nucleoside reverse transcriptase inhibitor; HIV combination therapy (use one with two different NRTI); SE: rash, hepatitis |
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Term
Delavirdine mode of action, tx, SE? |
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Definition
Non-nucleoside reverse transcriptase inhibitor; HIV combination therapy (use one with two different NRTI); SE: rash |
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Term
Efavirene mode of action, tx, SE? |
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Definition
Non-nucleoside reverse transcriptase inhibitor; HIV combination therapy (use one with two different NRTI); SE: rash, CNS: insomnia, vivid dreams (53%) |
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Term
HIV integrase inhibitors mode of action, indication, example |
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Definition
blocks activity of HIV integrase; used in combination therapy; raltegravir |
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Term
HIV protease inhibitors ending, mode of action, indication, metabolism, SEs (4)? |
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Definition
-navir; aspartyl proteases that cleave nacent HIV proteins into active proteins are inhibited, rendering virus non-infectious; combination therapy (one PI with two different NRTIs); CYP450 3A4 (also inhibits: saquinavir least, ritonavir most inhibiting...ritonavir boost increases action of other PIs); SE: 1) Lipodystrophy (buffalo hump: gain, facial wasting: loss, crix belly/protease paunch from Crixivan aka indinavir. 2) metabolic syndrome (X): central obesity, increased bp, increased TG, decreased HDL, insulin resistance (inhibits carb metabolism) -> increased risk of cardiovascular disease 3) diarrhea 4) night sweats ... LMDN Let Me Die Now from HIV |
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Term
ritonavir mode of action, metabolism effect; use |
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Definition
HIV protease inhibitor; most inhibiting of CYP450 3A4 (which metabolizes protease inhibitors); can be used as a ritonavir boost to increase activity of other HIV protease inhibitors |
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Term
HAART? recommendation? signs of success? combinations to avoid? |
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Definition
Highly active antiretroviral therapy; 2 NRTI + 1 NNRTI (or 1 PI); decreased viral load, resistance, opportunistic infections, increased CD4 count (T-cells); NO: stavudine + didanosine (same side effects: dose limited peripheral neuropathy) AND NO: stavudine + zidovudine (thymidine analogs that compete for HIV reverse transcriptase binding) |
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