Professional Documents
Culture Documents
Antivirals
Antivirals
Antivirals
MOA
Major Drugs
Block viral Amantadine penetration/ uncoating Rimantadine Inhibit viral DNA Acyclovir, Ganciclovir, polymerase Foscarnet Inhibit viral RNA Foscarnet, Ribavirin polymerase Inhibit viral RT AZT, DDI, DDC, d4T, 3TC Inhibit viral aspartate Indinavir, Ritonavir, protease Saquinavir Inhibit viral Zanamivir, Oseltamivir neuramidase
Acyclovir
MOA: ACV ACV monoPO4 ACV triPO4 DNA polymerase (DNA chain termination) USE: HSV & VZV Form: Topical, PO, IV AE: IV (Crsytalluria & Neurotoxic) Resistance: due to change in DNA polymerase / dec. activity of TK
TK Host cellsTK
Ganciclovir
MOA: same as ACV (not DNA chain termination) USE: HSV, VZV, CMV (prop & Tx) Form: PO, IV, retinal implant AE: Dose limiting hematotoxicity, mucositis, fever, rash, crystalluria, Seizures in OD Resistance: same as ACV
Foscarnet
MOA: Not an antimetabolite, but still (-) DNA & RNA polymerases USE: Identical to GCV, but > activity versus resistant strains of HSV Form: IV AE: Dose limiting nephrotoxicity w/ ATN, electrolyte imbalance dec. Ca+2 tremors & seizures
Ribavirin
MOA: RBV monoPO4 IMP DH RBV triPO4 viral RNA polymerase & end-capping of viral RNA USE: RSV, Inf A & B, Lassa fever, Hantavirus, adjunts to alpha-intf in Hepa C Form: Aerosol, Topical, PO, IV AE:Hematotoxic, upper airway irritation, Teratogenic
NRTIs
Components of most combination drug regimens used in HIV infection Used 2 NRTIs w/ PI Use in HAART ( dec viral RNA, inc CD4 cells, dec opportunistic infxn)
Nonnucleoside RTIs
Resistance emerges if used individually Additive/ Synergistic against HIV E.g: Nevirapine, Delaviridine
MOA: ZDV RT (Viral chain termination) USE: HIV infected w/ dec CD4 ct; Pregnant HIV dec transmission to baby Form: PO; IV AE: Dose limiting hematotoxicity, HA, Asthenia, myalgia, myopathy, peripheral neuropathy, LA Resistance: Mutation in the gene that codes RT
Other NRTIs
MOA: Same as AZT USE: Same as AZT Form: PO AE: Different
Pancreatitis
Peripheral neuropathy
Peripheral neuropathy
Lamivudine (2Least toxic of NRTIs, but deoxy-3thiacytidine, some GI effects & 3TC) neutropenia
PIs
MOA: Aspartate protease is a viral enzyme that cleaves precursor polypeptides in HIV buds to form the CHONs of the mature virion core. USE: In combination w/ 2 NRTIs AE: Indinavir (GI distress, asthenia, paresthenia) Saquinavir (one of the least toxic, has very low oral bioavailability) Resistance: Mutation of protease