Antivirals and other Antimicrobials Flashcards
Class: zidovudine
Nucleoside RTI
Side effect: zidovudine
CNS disturbances: confusion, seizures
Class: lamivudine
Nucleoside RTI
Side effect: lamivudine
None. Has activity against hepatitis B
Class: emtricitabine
Nucleoside RTI
Side effect: emtricitabine
None. Has activity against hepatitis B
Class: didanosine
Nucleoside RTI
Side effect: didanosine
Pancreatitis
Class: zalcitabine
Nucleoside RTI
Side effect: zalcitabine
Pancreatitis (uncommon), oral ulcers
Class: stavudine
Nucleoside RTI
Side effect: stavudine
Increased hepatic transaminases, lipoatrophy, hyperlipidemia, lactic acidosis
Class: abacavir
Nucleoside RTI
Side effect: abacavir
Hypersensitivity reactions in HLA-B5701 (requires screening)
Class: tenofovir
NucleoTide RTI
Side effect: tenofovir
Renal impairment with hypophosphotemia. Also has activity against hepatitis B.
Nonspecific side effects of NRTI class
Peripheral neuropathy, lactic acidosis, fat redistribution (lipodystrophy)
Class: nevirapine
NNRTI
Side effect: nevirapine
Rash (SJS), elevated LFTs/liver failure
CYP450 inducer–induces it’s own metabolism!
Class: delavirdine
NNRTI
Side effect: delavirdine
Rash, elevated LFTs
CYP450 INHIBITOR–increases levels of drugs metabolized by CYP450. Inhibits it’s own metabolism!
Class: efavirenz
NNRTI
Side effect: efavirenz
CNS disturbances (abnormal dreams, impaired concentration, somnolence) CYP450 inducer
Class: etravirine
NNRTI–effective in persons with resistance to other NNRTIs
Side effect: etravirine
Rash (mild)
CYP450 inducer
Class: rilpivirine
NNRTI–effective in persons with resistance to other NNRTIs
Side effect: rilpivirine
Depression, insomnia, headache, rash
CYP450 inducer
Problem with resistance to NNRTI’s?
Resistance against one drug of this class confers resistance to the majority of them. Etravirine and rilpivirine remain effective in strains with prior NNRTI resistance.
General side effects of protease inhibitors?
Dyslipidemia, insulin resistance, lipodystrophy
Class: saquinavir
Protease inhibitor
Side effect: saquinavir
Poorly absorbed –> GI effects (diarrhea, nausea, dyspepsia, vomiting)
Reformulated as fortovase which has enhanced bioavailability
Class: indinavir
Protease inhibitor
Side effect: indinavir
Kidney stones, GI upset (but absorbed well in fasting state)
Class: ritonavir
Protease inhibitor
Side effect: ritonavir
GI side effects
Potent CYP450 inhibitor (used to “boost” levels of other drugs which allows less frequent dosing)
Class: nelfinavir
Protease inhibitor
Side effect: nelfinavir
Diarrhea
Class: amprenavir/fosamprenavir
Protease inhibitor
Side effect: amprenavir/fosamprenavir
GI upset, rash, paresthesias
Class: lopinavir
Protase inhibitor. Coformulated with ritonavir as combivir.
Side effect: lopinavir/combivir
Mild GI. Well tolerated.
Used during pregnancy.
Class: atazanavir
Protease inhibitor
Side effect: atazanavir
Indirect bilirubinemia without jaundice. Less impact on lipids. Cannot be taken with PPIs.
Class: tipranavir
Protease inhibitor
Side effect: tipranavir
GI upset. Coadministered with ritonavir for boosting.
Class: darunavir
Protease inhibitor–effective in patients with resistance to other PI’s
Side effect: darunavir
GI upset. Once daily dosing.
Class: enfuvirtide
Fusion inhibitor (binds p41 of envelope)
Side effect: enfuvirtide
Injection site reactions, neutropenia
“Salvage regimen”
Class: maraviroc
CCR5 inhibitor
Side effect: maraviroc
Well tolerated
Class: raltegravir
Integrase inhibitor
Side effect: raltegravir
Diarrhea, nausea, fatigue
Class: elvitegravir
Integrase inhibitor
Side effect: elvitegravir
Diarrhea, nausea, proteinuria
Administered in combination with emtricitabine, tenofovir, and cobicistat (CYP450 inhibitor), called Stribild
MOA: amantadine, rimantadine
Inhibits viral genome uncoating of influenza A only
Class: oseltamivir, zanamivir, peramivir
Neuraminidase inhibitors
Clinical use of ribavirin?
RSV in infants, Lassa fever (arenaviridae), hantavirus pulmonary syndrome, HCV (in combination with interferon)
Clinical use of interferon?
Treatment of chronic hepatitis B and hepatitis C in combination with ribavirin
MOA: boceprevir/telaprevir
Hepatitis C protease NS3-4A inhibitors.
Used in combination with interferon and ribavirin
Class: acyclovir/famciclovir/valacyclovir
Guanosine analogue, requires phosphorylation by HERPES thymidine kinase
Class: ganciclovir
Guanosine analogue, requires phosphorylation by HUMAN thymidine kinase
Class: cidofovir
Cytosine analogue, requires phosphorylation by HUMAN cellular kinases
Class: foscarnet
Pyrophosphate analogue which inhibit viral DNA polymerase/reverse transcriptase