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26 Cards in this Set

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acyclovir (Zovirix)
Herpes drug
guanosine derivative
phosphorylated to acyclovir triphosphate by thymidine kinase
competitive substrate of viral DNA polymerase...irreversible complex. chain termination
cross resistant: valcyclovir, famciclovir, ganciclovir
ADE: nausea, nephrotoxicity, neurotoxicity
valacyclovir (Valtrex)
Herpes drug
prodrug of Acyclovir
oral dosage has better bioavailability than acyclovir
no IV dosage form
famciclovir (Famvir)
Herpes drug
guanosine alnalog
prodrug of penciclovir
better bioavailability than acyclovir
but lower affinity for viral dna pol
oral only
penciclovir
herpes drug
guanosine analog
topical use only
must be used every 2 hrs to shorten duration of lesions by 1/2 day
ganciclovir (Cytovene)
for CMV
acyclic guanosine analog
phosphorylated by phosphotransfersase
inhibits viral DNA pol and causes termination of viral DNA elongation
ADE's: myelosuppression, carcinogenic, embryotoxic
oral, IV
valganciclovir (Valcyte)
CMV
prodrug of ganciclovir
only oral
Cidofovir
CMV drug
cytosine nucleotide analog
phosphorylation does not require viral enzymes
inhibits viral DNA polymerase
very long half life
IV formulation only
ADE: 25% of people get nephrotoxicity
ganciclovir resistant CMV may be cross-resistant to cidofovir
Foscarnet
for HSV and CMV
inorganic pyrophosphate
inhibits DNA polymerase, RNA polymerase, HIV reverse transcriptase directly
does not require phosphorylation
active against acyclovir and ganciclovir resistant strains
Tenofovir (Viread)
nucleoTide reverse transcriptase inhibitor
does not require phosphorylation
Lamivudine (Epivir)
NRTI (HIV and HBV)
structural analog of purine and pyrimidine base...competitively inhibit HIV-1 reverse transcriptase
incorporated in viral DNA chain and causes termination
ADE: lactic acidemia, hepatomegaly, steatosis
Zidovudine (Retrovir, AZT)
NRTI
adverse class drug effects: lactic acidemia, hepatomegaly, steatosis

IDE - bone marrow suppression
Emtricitabine
NRTI

ACDE: lactic acidemia, hepatomegaly, steatosis
abacavir
NRTI

ACDE: lactic acidemia, hepatomegaly, steatosis

IDE: hypersensitivity rxn...can progress to multi-organ failure
efavirenz (Sustiva)
NNRTI

ACDE: hypersensitivity rxns, Stevens-Johnson
tipranavir
PIs

ACDE: metabolic syndrome (lipodystrophy, hyperlipidemia, hyperglycemia)

IDE: 14 reports of fatal and non-fatal intracranial hemorrhage
lopinavir/ritonavir
PI's are metabolized by CYP3A4...so dosed together with ritonavir b/c it is the most potent inhibitor of CYP3A4...concurrent admin results in increased plasma levels
atazanavir
PI
ACDE: metabolic syndrome (lipodystrophy, hyperlipdemia, hyperglycemia)
enfuvirtide
Fusion inhibitor
binds to gp41 and prevents conformational changes required for fusion of viral and cell membranes
no cross resistance
ADE: injection site rxns, eosinophilia
for treatment experienced
maraviroc
entry inhibitors
binds to CCR5 receptor and CD4 cells preventing HIV from binding to this receptor
ADE: cough URI, rash, abdominal pain, musculoskeletal, dizziness
warning regarding hepatoxicity
caution in patients on anti-hypertensive therapy (postural hypertension is dose limiting ADR)
raltegravir
Integrase Inhibitors
inhibit insertion of HIV DNA into human DNA by integrase enzyme
ADE: diarrhea, nausea, headache, Creatine kinase elevations noted, myopathy, rhabdomylosis
for treatment experienced
adefovir
HBV drug
nucleoTide analag of adenosine
competitively inhibits HBV DNA pol resulting in chain termination

active in lamivudine resistant strains
ADE: reversible nephrotoxicity
entecavir
HBV drug
guanosine nucleoside analog
competes with natural substrate of HBV polymerase to inhibit DNA synthesis
more potent anti-viral activity than lamivudine
resistance rare
ADE: lactic acidosis,hepatomegaly w/ steatosis
ribavirin
HCV drug
guanosine analog
undergoes phosphorylation
interferes w/ synthesis of guanosine triphosphate and inhibits viral RNA polymerase

use w/ interferon alpha 2b
ADE: hemolytic anemia
amantidine and rimantidine
anti-influenza A drug
inhibit uncoating of viral RNA of influenza A and prevent replication
target protein is M2
rimantidine >>>> amantidine
70-90% protective in prevention of influenza A
begun w/in 1-2 days of symptoms reduces duration 1-2 days
oseltamivir
neuraminidase inhibitor...viral protein needed for viral replication and release from infected cells

release of viral progeny inhibited and spread to neighboring cells, result is virus "sticking" to host cell

oral prodrug
zanamivir
neuraminidase inhibitor...viral protein needed for viral replication and release from infected cells

release of viral progeny inhibited and spread to neighboring cells, result is virus "sticking" to host cell

oral inhaler