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Antiviral Drugs

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benujiso's version from 2018-03-21 23:37

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Question Answer
Acyclovir UseHSV-1/2 (esp encephalitis); suppresses but does not cure; VZV when involves eye; prophylaxis for CMV
Acyclovir Mechanismprodrug phosphorylated by thymidine kinase; triphosphate analog inhibits HSV DNA polymerase > cx chain termination
Acyclovir Resistancemutation of HSV DNA polymerase
Acyclovir SEcrystal formation and tubular obstruction, transient renal dysfunction if dehydrated (IV); GI, headache, skin (oral)
Valacyclovir Usegenital herpes, shingles
Valacyclovir Mechanismprodrug of acyclovir; provide higher serum level than acyclovir (better oral availability than ACV)
Valacyclovir SEGI tolerance, thrombotic thrombocytopenia purpura in AIDS
Cidofovir UseCMV, adenovirus, TK deficient HSV
Cidofovir Mechanismdeoxycytidine analog; competitive chain inhibitor
Cidofovir SEhigh nephrotoxicity, causes apoptosis in proximal renal tubular cells; LAST RESORT
Ganciclovir UseTx CMV infection esp in AIDS pts (retinitis, enterocolitis)
Ganciclovir Mechlike Acyclovir but w/ inc susceptibility by host cell enzymes; also does not need virus thymidine kinase
Ganciclovir SEBM suppression!!, CNS toxicity
Foscarnet UseCMV retinitis, Ganciclovir resistant CMV, CMV prophylaxis, Acyclovir resistant HSV
Foscarnet mechinhibits viral DNA & RNA pol and RT by interacting w/ pyrophosphate binding site on enzymes
Foscarnet SENephrotoxicity, hypocalcemia, anemia, nausea, fever, hypoK, hypo and hyperP, seizures, arrhythmia
Zidovudine (AZT) useHIV-1 (NRTI drug)
Zidovudine mechprodrug - deoxythymidine analog; when phosph integrates into viral DNA cx chain termination; ALSO, binds to viral RNa-dependent DNA polymerase + inhibits
Lamivudine Mechanismdeoxycytidine
Lamivudine useHIV, HepB
Zidovudine SELeukopenia, anemia
Zidovudine + interferonenhances anti-HIV act, but also dramatically inc neutropenia & hepatotox
NRTI drugs SElactic acidosis, fatty liver (esp Zidovudine)
Emtricitabine useHIV, HepB
Emtricitabine + Lamivudinedo not use; no synergy; complete cross-resitance
Emtricitabine SEGI, skin, lactic acidosis, fatty liver, hepatomegaly
Lamivudine SEZidovudine but dec freq; PANCREATITIS, fatty liver
AbacavirNRTI w/ hypersensitivity SE1
Abacavir mechanismdeoxyguanosine analog
Abacavir SEGI, fever, rash
Tenofovir useHIV (NRTI), HepB, used in multi-drug anti-HIV regimens
Tenofovir MechnucleoSide NRT, deoxyadenosine analog; HBV polymerase inhibitor; NRTI > prodrug of AMP analog >dose 1/day and req no further phosphorylation
Tenofovir + LamivudineCross-resistance
Tenofovir SEFanconi's Syndrome (nephrotoxicity); CI: children, pregnancy
Efavirenze NNRTI; HIV
Efavirenze Mechdirectly inhibits viral RT
Efavirenze SErash, CNS effects (bad dreams, drowsiness, insomnia, dizziness, confusion)
RitonavirProtease Inhibitor for HIV (used in combo w/ other PI's to prolong their T1/2; not used alone b/c SE's unfavorable)
Ritonavir SEworst of group: met by CYP450 >> INDUCER; GI distress, HA, asthenia, fatigue, taste disturbance, paresthesia, inc CK, ALT, TGs
Ritonavir CI'sTerfenadine,anti-arrythmics, sedative/hypnotics, analgesics, etc
IndinavirPI: HIV
Indinavir + Lamivudine achieve undetectable virus levels: DRAMATIC EFFECT
Ritonavir vs. IndinavirRit has good oral availab, while Indinavir does not (take in fasting state)
EfuvirtideFusion Inhibitor: use in HIV
Efuvirtide Mechblocks confirmation change in viral coat protein gp41 > necc for viral entry; IM Only
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