I&I Antivirals, HIV & TB
Terms
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- Properties of base analogs
-
(typical antiviral agents)
activated in cell by phosphorylation
widely distributed
eliminated by kidney
usually non-specific & non-toxic - 2 drugs for Influenza A
- Amantidine & Rimantidine
- Amantidine & Rimantidine MOA
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Inhibition of uncoating
amines inhibit viral proton translocator
Used with L dopa in Parkinsons - 2 drugs for Influenza A & B
- Zanamivir & Oseltamivir
- Zanamivir & Oseltamivir MOA
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Neuraminidase inhibitor
Prevent viral release & spread - Idoxuirdine MOA
-
causes DNA breakage- historical drug (or topical) only
very toxic - Acycloguanosine Use
- HSV, EBV, Shingles
- Acycloguanosine MOA
-
interferes with DNA replication
(chain terminator)
relys on thymidine kinase - Ganciclovir MOA
-
competitive inhibitor of dGTP- chain terminator
lacks specificity of Acyclovir - Treatment for CMV
- Ganciclovir
- Ribavirin MOA
- labilizes viral mRNA by reducing 5' cap formation
- Ribavirin Toxicities
- BM depression, GI, CNS, Teratogenic, mutagenic, carcinogenic
- Treatment for RSV, Hep C or Hanta
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Ribavirin
Hep C use ribavirin + IFN a - 5 (or 6) first line drugs for TB
- Isoniazid, Rifampicin, Pyrazinamide, Ethambutol, Streptomycin (ciprofloxacin)
- Isoniazid MOA
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Bacteriacidal: inhibition of mycolic acid synthesis-
forms inhibitory complex w/MB acyl carrier protein - Isoniazid SEs
-
Slow acetylators- Neuorpathy b/c loss of pyridoxine- (tx w/pyroxidine NOT benzos or barbits)
Fast acetylators- hepatotoxicity
Lupus like syndrome (like hydralazine & procainamide- gives positive ANA) - Rifampicin MOA
-
Blocks RNA synthesis
(inhibits DNA dependend RNA polymerase) - Rifampicin SEs
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Drug Interactions!!
oral contraceptives, hormones, coumadin (& theophyline- like Cipro & Zileutin), others
(colors body fluids orange/red) - Ethambutol MOA
- inhibits mycolic acid synthesis
- Ethambutol SEs
-
inability to perceive green
optic neuritis
relatively non-toxic - Pyrazinamide MOA
- inhibits mycolic acid synthesis- inhibits fatty acid synthetase I (FASI)
- Pryazinamide SEs
-
flushing, arthralgia, hepatotoxicity (monitor enzymes)
synergistic w/isoniazide - Classes of treatment for HIV
-
NRTIs
NNRTIs
PI
Entry Inhibitor - 6 NRTIs
-
Azidothymidine (zidovudine)- BM
Stavudine- P & PN
Lamivudine (3-thiacytidine)- P & PN
Dideoxyinosine- P & PN
Abacavir- allergies
Tenofovir- (SEs like PIs) - Azidothymidine MOA
- RTI & chain terminator- cell becomes deficient in thymidine
- Azidothymidine SEs
-
Severe:
BM, granulocytopenia, anemia, neurotoxic, NVHA, insomnia, myalgia
25% of patients can't tolerate - Stavudine MOA
- RTI & chain terminator
- Stavudine SEs
-
interferes w/mitochondrial DNA
contraindicated w/AZT
pancreatitis - Lamivudine MOA
-
less active & less toxic than AZT
Prevents resistance to AZT - Lamivudine SEs
-
less severe than AZT
no BM, no neuro
resistance quickly w/cross resistance to ddI, ddC & abacavir - 3TC
- Lamivudine
- d4T
- Stavudine
- Prevents resistance to AZT
- Lamivudine
- Dideoxyinosine MOA
- RTI
- Dideoxyinosine SEs
- pancreatitis & mitochondrial
- Abacavir MOA
- guanosine analog, RTI
- Abacavir SEs
- allergies, fever, rash, respiratory
- Tenofovir MOA
- RTI-
- Tenofovir SEs
- Unique- GI, glycosuria, hyperglycemia & triglyceridemia, renal, neutropenia
- 3 NNRTIs
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Nevirapine
Delavirdine
efavirenz - NNRTIs MOA
- RTI not nucleoside analog
- NNRTIs SEs
-
fever, nausea, CNS, hepatotoxicity
rash to Stevens-Johnson - Protease Inhibitors Names
-
saquin-
indin-
riton-
melfin-
ampren-
lopin- avir - PIs MOA
- prevent cleavage of HIV protein precursors
- PIs SE
- diabetes & diabetic like syndrome, cholesterol & TGs increased, fat wasting, asthenia,
- Treatment guidelines for HIV
-
2 NRTIs & a PI
2 NRTIs & a NNRTI
1 NRTI & 1 NNRTI & 2 PIs - Enfuvirtide MOA
-
entry inhibitor
prevents HIV binding to CD4