Term
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Definition
MOA: CCR5 co-receptor antagonist attachment inhibitor
Use: HIV |
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Term
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Definition
MOA: binds to gp41 and prevents membrane fusion, blocks entry
Use: HIV |
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Term
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Definition
| determines if HIV enters T-cells via CCR5, CXCR4 or both |
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Term
| Nucleoside/tide Reverse transcriptase inhibitors (N-RTIs); MOA, use, ADRs |
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Definition
MOA: competatively inhibit the incorporation of native nucleotides and also by terminating elongation
Use: HIV-1 or HIV-2
ADRs: bone marrow suppression, pancreatitis, and peripheral neuropathy |
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Term
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Definition
N-RTI
also has dose-limiting hematotoxicity |
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Term
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Definition
N-RTI
dose limiting peripheral neuropathy (20%) and pancreatitis (7%) |
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Term
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Definition
N-RTI
dose-limiting peripheral neuropathy (71% w/ monotherapy) and lipo-atrophy (skinny cheeks) |
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Term
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Definition
N-RTI
hypersensitivity, in multi organ system
Syx occur in first 6 weeks - fever, rash, GI, constitutional, and respiratory, can cause life threatening complications if continued through symptoms or restarted later.
Screen for HLA-B*5701 genotype |
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Term
| Stavudine cannot be combined w/ which other drugs? why? |
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Definition
Didanosine - additive toxicity of peripheral neuropathy
Zidovudine - both are thymidine analogues and will compete for activation and activity |
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Term
| Non-Nucleotide Reverse Transcriptase Inhibitors (NN-RTIs); use, MOA, ADRs |
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Definition
use: HIV-1 specific
MOA: active drugs, highly selective for viral RT, non-competative inhibit HIV-1 RT. bind to site adjacent to active site leading to a conformation change that inhibits the enzyme
ADRs: rash, CYP3A4 metabolized so interaction w/ inducers and inhibitors |
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Term
| SEs of Nevirapine, Delaviridine and Efavirenz |
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Definition
Nevirapine - rash (16%), hepatitis (14%)
Delavirdine - rash (18-36%)
Efavirenz - rash (27%), CNS (53%) such as insomnia and vivid dreams but disappear after 1 month |
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Term
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Definition
| MOA: block the catylitic activity of HIV integrase, which incorporates proviral DNA into the host chromosomal DNA |
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Term
| Protease inhibitors; MOA, metabolism, ADRs |
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Definition
-navirs
block the incorporation of proteases into long chain peptides, that would normally cleave the chain into smaller active proteins, thus preventing maturation and making the noninfections
All are 3A4 substrates and inhibitors
ADR: lipodystrophy, Metabolic syndrome, Diarrhea, Night sweats |
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Term
| which protease inhibitor is combined with other 3A4 metabolized drugs to decrease their metabolism and increase their activity? |
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Definition
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Term
| HAART standard of therapy? benefits |
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Definition
2 NRTIs + 1 PI
or
2 NRTIs + 1 NNRTI
decreased viral RNA concentration
reverse CD4 count declines
Decreased opportunistic infections
Decrease rate of emergence of drug resistance |
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