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15 Cards in this Set
- Front
- Back
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Ribavirin
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Guanosine analog
Competitive inhibitor of DNA/RNA synthesis |
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Ribavirin administration
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Aerosol spray
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Ribavirin uses
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pneumonitis due to RSV
Combination with Interferon for Hep B & C minimal toxicity |
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Amantidine/Rimantidine
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cyclic amine
prevents uncoating of the virus inferes with release of genome |
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Amantidine/Rimantidine uses
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Influenza A tx and prophylaxis
also used for parkinson's resistance develops fast |
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Amantidine/Rimantidine Toxicity
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Reversible CNS defects
Rimantidine has fewer effects |
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Zanamavir
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neuraminidase inhibitor
active against influenza A&B Prophylactic treatment |
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Nucleoside Reverse Transcriptase Inhibitors (NRTI’s)
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Mechanism of all NRTI’s: competitive inhibition of reverse transcriptase and chain termination;
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Zidovudine (ZDV, Azidothymidine = AZT) / Retrovir
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thymidine analogue-historically first line agent for HIV infection
- competitive inhibitor of reverse transcriptase (RT) and DNA chain terminator |
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Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
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Non-nucleoside RT inhibitors (non-competitive); direct binding to
reverse transcriptase at an allosteric site that is different from the NRTIs. |
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Protease Inhibitors (peptide based structures)
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Inhibit HIV aspartic protease (an enzyme necessary in proteolytic
processing of the products of gag and gag-pol genes into functional core proteins and viral enzymes such as reverse transcriptase and integrase). Results in production of non-infectious virus |
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Protease inhibitors toxicity
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Lypodystrophy:
altered fat distribution/buffalo hump facial/peripheral atrophy truncal obesity |
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New compounds
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New protease inhibitor
–Tipranavir: just approved is a unique non-peptidic PI inhibitor that shows full or enhanced activity in vitro against HIV isolates resistant to most other protease inhibitors) • Nucleotide analogue Tenofovir—contains a phosphate and is less in need of intracellular phosphorylation • Viral-cell fusion inhibitor, Enfuvirtide (T20) |
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Highly Aggressive Anti-Retroviral Therapy (HAART), Drug Resistance
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HIV infected and immunocompromised patients at greatest risk of developing drug
related mutations in reverse transcriptase and the protease. Drug resistance is also a problem with the opportunistic infections that accompany full-blown AIDS like HSV, CMV, VZV, Influenza. (E.g., HSV Thymidine kinase, DNA polymerase). Because of the rapid development of resistance in HIV combination therapy (HAART) is essential. |
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Three categories of HAART:
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Three categories of HAART:
• 1 NNRTI + 2 NRTIs • 1 PI + 2 NRTIs • NRTIs |
