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Antivirals (comprehensive)
Creighton University School of Medicine
113
Medical
Professional
08/24/2013

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Cards

Term
Term
Definition
Definition
Term
Acyclovir (viruses)
Definition
HSV-1, HSV-2, VZV
Term
Acyclovir (MOA)
Definition
Chain terminates viral DNA, and the chain inactivates viral-DNA polymerase
Term
Acyclovir (indications)
Definition
HSV encephalitis, HSV/VZV for IC, genital HSV
Term
Acyclovir (adverse effects)
Definition
Headache, N/V, rash, RENAL TOXICITY
Term
Valacyclovir (advantages to acyclovir)
Definition
Only need 2x/day dosing, high bioavailability
Term
Valacyclovir (adverse effects)
Definition
Thrombotic microangiopathy in IC patients when used at high doses
Term
Famciclovir (indications)
Definition
HSV and VZV infections
Term
Famciclovir (adverse effects)
Definition
Headache and nausea
Term
Famciclovir (MOA)
Definition
Inhibits DNA polymerase but does not chain terminate
Term
Penciclovir (indications)
Definition
Topical for herpes lip lesions, low oral bioavailability
Term
Trifluridine (MOA)
Definition
Inhibits Herpes simplex viral DNA synthesis
Term
Trifluridine (indications)
Definition
HSV-1, HSV-2, keratoconjunctivitis, topical application only, possible for acyclovir resistance
Term
Trifluridine (adverse effects)
Definition
Teratogenic
Term
Docosanol (MOA)
Definition
Long chain saturated alcohol which inhibits fusion between plasma membrane and viral HSV envelope
Term
Docosanol (indications)
Definition
Herpes labialis--Cold sores and fever blisters, offers only moderate relief
Term
Docosanol (adverse effects)
Definition
Rash and pruritus
Term
Ganciclovir (MOA)
Definition
Chain terminates viral DNA, and the chain inactivates viral-DNA polymerase
Term
Ganciclovir (activation)
Definition
Activated intracellularly by phosphorylation by CMV viral enzyme
Term
Ganciclovir (viral selectivity)
Definition
More active against CMV, equal activity towards HSV-1, HSV-2, VZV, EBV
Term
Ganciclovir (adverse effects)
Definition
More toxic than acyclovir, teratogenic, bone marrow suppression -> neutropenia
Term
Ganciclovir (indications)
Definition
Intraocular implants and by IV only for life/sight threatening CMV illness
Term
Valganciclovir (indications)
Definition
CMV retinitis treatment with oral dose versus IV dose with ganciclovir
Term
Cidofovir (MOA)
Definition
Activated by intracellular phosphoyrlation and inhibits CMV DNA polymerase
Term
Cidofovir (indications)
Definition
CMV retinitis by IV
Term
Cidofovir (adverse affects)
Definition
Neutropenia, nephrotoxicity (protected by probenecid)
Term
Foscarnet (MOA)
Definition
Pyrophosphate analog that inhibits viral DNA polymerase
Term
Foscarnet (viral selectivity)
Definition
CMV, HSV, VZV (esp. resistant strains)
Term
Foscarnet (indications)
Definition
CMV retinitis, HSV acyclovir/pencyclovir resistant strains
Term
Foscarnet (adverse effects)
Definition
Renal (major), N/V, CNS, electrolyte imbalance
Term
Adamantine (MOA)
Definition
block uncoating of myxoviruses (Influenza A), via inhibition of hydrogen ion channels which normally allow the acidification and resultant uncoating of this virus
Term
Adamantine (viral selectivity)
Definition
Only for Influenza A
Term
Amantadine (adverse effects)
Definition
No Liver, CNS, renal, GI, teratogenic
Term
Rimantadine (adverse effects)
Definition
Liver, no CNS, no Renal, GI, teratogenic
Term
Oseltamivir (indications)
Definition
Influenza A and B
Term
Zanamivir (indications)
Definition
Influenza A and B
Term
Oseltamivir (MOA)
Definition
Bind neuraminidase
Term
Oseltamivir (phamacokinetics)
Definition
Oral prodrug with good bioavilability, only need once/twice per day
Term
Oseltamivir (adverse effects)
Definition
Hypersensitivity, nausea, vomiting, headache
Term
Zanamivir (pharmacokinetics)
Definition
Poor bioavailability, but really good lung distribution
Term
Zanamivir (adverse effects)
Definition
Nasal/throat discomfort, headach, cough, bronchospasm, NOT FOR ASTHMATICS OR NURSING MOTHERS
Term
Ribavirin (MOA)
Definition
Purine analog that inhibits Influenza A and B, and RSV, and somewhat Hep-C
Term
Ribavirin (viral selectivity)
Definition
RSV in children, Hep-C when combined with IFN-alpha-2b
Term
Ribavirin (adverse effects)
Definition
HEMOLYTIC ANEMIA, TERATOGEN, IRRITATES RESPIRATORY TRACT
Term
Palivizumab (MOA)
Definition
Monoclonal antibody used to prevent RSV in high-risk infants and children with respiratory disease
Term
NRTIs (properties)
Definition
lactic acidosis
hepatic steatosis
peripheral neuropathy
bone marrow suppression
Term
zidovudine (MOA/class)
Definition
NRTI
Term
zidovudine (adverese effects)
Definition
lactic acidosis
lipodystrophy
bone marrow depression
Term
Zidovudine (drug-drug interactions)
Definition
Ganciclovir (synergistic neutropenia)
Trimethoprim (decreases reneal excretion
Probenecid (uric acid excreted in place of Zidovudine)
Stavudine (competes with zidovudine for phosphoyrlation resulting in antagonism)
Term
Zidovudine (indications)
Definition
reduces freq. of neonatal HIV infections; oral administration
Term
didanosine (MOA/class)
Definition
NRTI
Term
didanosine (indications/adverse effects)
Definition
limited use/poor bioavailability; lactic acidosis, pancreatitis (MAJOR)
Term
stavudine (MOA/class)
Definition
NRTI
Term
stavudine (adverse effects)
Definition
lactic acidosis
lipodystrophy
Term
Hepatitis B rebound effect drugs?
Definition
lamivudine, emitricitabine, tenofovir
Term
Drugs used to block neonate transmission
Definition
Zidovudine, Emtricitabine, Lamivudine, Nevirapine, Nelfinavir, Lopinavir/ritonavir
Term
lamivudine (MOA/class)
Definition
NRTI
Term
lamivudine (non-HIV indication)
Definition
treats Hep B
Term
lamivudine (adverse effects)
Definition
lactic acidosis (but decreased relative to other NRTIs)
Term
emtricitabine (MOA/class)
Definition
NRTI
Term
emtricitabine (non-HIV indication)
Definition
treats Hep B
Term
emitricitabine (dosing)
Definition
once a day, due to increased half-life from fluorination
Term
emtricitabine (adverse effects)
Definition
lactic acidosis (but decreased relative to other NRTIs), hyperpigmentation of the palms and soles, headache
Term
abacavir (MOA/class)
Definition
NRTI
Term
abacavir (adverse effects)
Definition
lactic acidosis (but decreased relative to other NRTIs)
hypersensitivity (HLAB*5701 gene -> if present, susc. to hypersensitivity)
Term
tenofovir (MOA/class)
Definition
NRTI
Term
tenofovir (indications)
Definition
pre-exposure prophylaxis (w/ emtricitabine), HIV infections (obvi...lol)
Term
tenofovir (adverse effects)
Definition
nephrotoxicity, bone loss
Term
tenofovir (non-HIV indication)
Definition
treats Hep B
Term
tenofovir (adverse effects)
Definition
lactic acidosis (but decreased relative to other NRTIs)
Term
nevirapine (MOA/class)
Definition
NNRTI
Term
nevirapine (adverse effects)
Definition
rash (Steven-Johnson Syndrome)
**Hepatoxicity
Term
NNRTIs (properties)
Definition
-cause rash
-increased transaminase levels
-metabolized by CYP450 enzymes (act as a substrate)
-D-D interactions -> Rifampin induces CYP3A4, thus drug conc. Decreases
Term
teratogenic anti-viral drugs?
Definition
efavirenz, ribavirin, ganciclovir, valganciclovir, trifluoridine, amantidine, rimantidine
Term
delavirdine (MOA/class)
Definition
NNRTI
Term
efavirenz (indication)
Definition
preferred NNRTI
Term
efavirenz (indication)
Definition
CNS (depression), vivid dreams
Term
etravirine (MOA/class)
Definition
NNRTI
Term
etravirine (adverse effects)
Definition
GI(rare among NNRTIs), rash; potential D-D interactions -> major CYP inducer
Term
rilpivarine (pharmacokinetics)
Definition
doesn't induce or inhibit, only a substrate for CYP3A4 enzymes
Term
rilpivirine (MOA/class)
Definition
NNRTI
Term
Protease Inhibitors (properties)
Definition
-all PIs inhibit P450
-D-D interaction -> rifampin decreases PI levels -> don't use rifampin, use rifabutin
-at low doses, ritonavir specifically enhances other PI levels
Term
Protease Inhibitors (adverse effects -> all)
Definition
-fat redistribution
-hyperlipidemia
-hyperglycemia
-bone loss
-elevation of serum transaminases
-CORONARY ARTERY DISEASE
Term
ritonavir (MOA/class)
Definition
PI (boosting agent for other PIs)
Term
saquinavir (hard gelatin capsul)/ritonavir (MOA/class)
Definition
PI
Term
nelfinavir (MOA/class)
Definition
PI
Term
nelfinavir (pharmacokinetics)
Definition
no boosting w/ ritonavir
Term
nelfinavir (add'l adverse effects)
Definition
GI: diarrhea (MAJOR)
Term
atazanavir/ritonavir (MOA/class)
Definition
PI
Term
atazanavir/ritonavir (adverse effects)
Definition
less severe hyperlipidemia than other PIs; use caution w/ pts w/ cardiac abnormality
Term
lopinavir/ritonavir (MOA/class)
Definition
PI
Term
lopinavir/ritonavir (adverse effects)
Definition
few additional side effects
Term
fosamprenavir/ritonavir (MOA/class)
Definition
PI
Term
fosamprenavir/ritonavir (adverse effects)
Definition
contains sulfonamide, thus rash/allergy potential, kidney stones
Term
darunavir/ritonavir (MOA/class)
Definition
PI
Term
darunavir/ritonavir (add'l adverse effects)
Definition
contains sulfonamide, thus rash/allergy potential
Term
tipranavir (MOA/class)
Definition
PI
Term
tipranavir (add'l adverse effects)
Definition
-contains sulfonamide, thus rash/allergy potential
-intracranial hemorrhaging
Term
enfuvirtide (MOA/class)
Definition
fusion inhibitor; interferes w/ HIV binding to host cell membrane via HIV gp41
Term
enfuvirtide (indications)
Definition
ART resistant HIV infections; use in combo
Term
maraviroc (MOA/class)
Definition
CCR5 co-receptor antagonist; blocks HIV entry receptor CCR5 (that interacts with HIV gp120)
Term
maraviroc (indications)
Definition
initial HIV Tx and when HIV resistant to other regimes
Term
raltegravir (MOA/class)
Definition
integrase strand transfer inhibitor; inhibits final step in integration catalyzed by integrase
Term
raltegravir (indications)
Definition
first line HIV Tx; well tolerated
Term
elvitagravir (MOA/class)
Definition
integrase strand transfer inhibitor; inhibits final step in integration catalyzed by integrase
Term
elvitagravir (indications)
Definition
first line therapy for HIV
Term
elvitagravir (formulation)
Definition
-one pill combo w/: elvitegravir/cobicistat/emtricitabine/tenofovir
-cobicistat -> boosting agent that inhibits CYP3A4 metabolism
-emtricitabine -> rebound effect w/ Hep. B
Term
Drugs to treat Hep B
Definition
-interferons -> peginterferon alpha-2b and 2a

-nucleoside/tide analogues -> tenofovir and entecavir (1st line); lamivudine and emtricitabine (often resistance to these); adefovir and telbivudine;
Term
Drugs to treat Hep C
Definition
-interferons -> peginterferon alpha-2b and 2a

- nucleoside analog -> ribavirin

-protease inhibitors (blocks protease that converts HCV polypeptide into mature viral particles) -> telaprevir and boceprevir

**telaprevir or boceprevir are used in combo w/ ribavirn and an IFN
Term
Drugs that cause neutropenia
Definition
ganciclovir, cidofovir, zidovudine
Term
Drugs that cause nephrotoxicity
Definition
tenofovir, cidofovir, foscarnet, zidovudine, amantadine, acycolovir
Term
Drugs that cause hemolytic anemia
Definition
ribavirin
Term
Drugs that cause bone marrow suppression
Definition
ganciclovir, zidovudine
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