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FIU - Anti-HIV drugs
Anti-HIV
17
Pharmacology
Professional
01/13/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
HIV Attachment/Fusion inhibitors examples
Definition
maraviroc, enfuvirtide
Term
maraviroc category, mode of action, screening, indication?
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.
Term
enfuvirtide category, mode of action
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
Term
HIV reverse transcriptase inhibitors: 2 categories, examples from each
Definition
nucleoside (zidovudine, didanosine, stavudine, abacavir, zalcitabine, emtricitabine, tenofovir) "TAZES DogZ"; non-nucleoside (nevirapine, delavirdine, efavirene) "DEN"
Term
nucleoside reverse transcriptase inhibitors mode of action, indication, SE (why)?
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"
Term
Zidovudine mode of action, tx, SE?
Definition
Nucleoside reverse transcriptase inhibitor; HIV combination therapy (use two different ones); SE: severe peripheral neuropathy
Term
Didanosine mode of action, tx, SE?
Definition
Nucleoside reverse transcriptase inhibitor; HIV combination therapy (use two different ones); SE: severe peripheral neuropathy, pancreatitis
Term
Stavudine mode of action, tx, SE?
Definition
Nucleoside reverse transcriptase inhibitor; HIV combination therapy (use two different ones); SE: severe peripheral neuropathy (71%) and lipo-atropy
Term
abacavir mode of action, tx, SE?
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%)
Term
non-nucleoside reverse transcriptase inhibitors root, mode of action, advantage, indication, metabolism, SEs (3)?
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
Term
Nevirapine mode of action, tx, SE?
Definition
Non-nucleoside reverse transcriptase inhibitor; HIV combination therapy (use one with two different NRTI); SE: rash, hepatitis
Term
Delavirdine mode of action, tx, SE?
Definition
Non-nucleoside reverse transcriptase inhibitor; HIV combination therapy (use one with two different NRTI); SE: rash
Term
Efavirene mode of action, tx, SE?
Definition
Non-nucleoside reverse transcriptase inhibitor; HIV combination therapy (use one with two different NRTI); SE: rash, CNS: insomnia, vivid dreams (53%)
Term
HIV integrase inhibitors mode of action, indication, example
Definition
blocks activity of HIV integrase; used in combination therapy; raltegravir
Term
HIV protease inhibitors ending, mode of action, indication, metabolism, SEs (4)?
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
Term
ritonavir mode of action, metabolism effect; use
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
Term
HAART? recommendation? signs of success? combinations to avoid?
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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