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antivirals
antivirals
55
Other
Not Applicable
03/30/2006

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Term
acyclovir-mechanism of action
Definition
monophosphorylated by viral thymidine kinase, futher activate host cell kinases to triphosphate. inhibits viral DNA polymerase
when incorporated into the DNA molecule, acts as a chain terminator because it lacks the equivalent of a ribosyl 3' hydroxyl group
Term
acyclovir-resistance
Definition
changes in DNA polymerase, decresed activity of TK
more than 50 percent of resistant strains completely lack TK
Term
acyclovir-clinical uses, what viruses and more about them
Definition
Herpes simplex and VZV
reduces viral shedding in genital herpes, decrease neuritis in shingles but has no effect on postherpetic neuralgia
reduces symptoms if used early in chicken pox, prophylactic in immunocompromised hosts
Term
acyclovir-administration
Definition
topical, oral and IV forms
Term
acyclovir-half life long or short
Definition
short
Term
acyclovir-side effects(which method of administration)
Definition
minor with oral use, more with IV
Crystalluria(maintain full hydration and neurotoxicity(agitation, headache, confusion-seizures in overdose)
Term
acyclovir is hematotoxic, true or false
Definition
false
Term
acyclovir-some newer drugs please
Definition
famciclovir and valacyclovir
Term
acyclovir-newer drugs, how do they differ
Definition
activity against strains resistant to acyclovir but not against 100 percent no thymidine kinasers.

longer half life than acyclovir
Term
ganciclovir-mechanism and resistance
something special
Definition
same as acyclovir,first phosphorylation is viral specific
TK in HSV, phosphotransferase(UL97) in CMV
Term
ganciclovir-spectrum of clinical use
Definition
CMV, HSV, VZV
Term
ganciclovir-mostly used in
Definition
prophylaxis and treatment of CMV especially retinitis in AIDS and transplant patients
Term
ganciclovir-side effects
Definition
fever, seizures in overdose, crystalluria, rash, mucositis
hematotoxicity(leukpenia, thrombocytopenia)
Term
foscarnet-mechanism
Definition
not an antimetabolite( whats this)
but inhibits viral RNA and DNA polymerase
Term
foscarnet-spectrum
Definition
similar as ganciclovir but increased activity against acyclovir resistant HSV
Term
foscarnet-side effects
Definition
nephrotoxicity with ATN also electrolite imbalance with hypocalcemia(tremors and seizures)
Term
foscarnet-avoid in what drug
Definition
pentamidine(used to treat pneumocytis carinii(increased nephrotoxicity and hypocalcemia)
Term
reverse transcriptase inhibitors
how many types? give thier names
Definition
2, nucleoside reverse transcriptase inhibitors, non- nucleoside reverse transcriptase inhibitors
Term
reverse transcriptase inhibitors-explain to me the meaning of nucleoside reverse transcriptase inhibitors
Definition
nucleoside antimetablites that are converted to active forms via phosphorylation
Term
NRTIs-are used together with what
Definition
Protease inhibitor
Term
NRTIs-zidovudine mechanism
Definition
antimetabolite, phosphorylated nonspecificaly to a triphosphate
compete with natural neucleotides and incorporated into viral DNA to cause chain termination
Term
NRTIs-zidovudine-resistance
Definition
mutation in the gene that codes for RT
Term
NRTIs-zidovudine-drug interactions
Definition
increased levels when combined with
probenacid, indomethacin, TMP-SMX, azole antifungals, cimetidine
decreased levels with rifampin
Term
NRTIs-zidovudine-side effects(which is dose limiting?
Definition
hematotoxicity(DL) headache, asthenia, peripheral neuropathy, myalgia, and myopathy
rare-but potentially faltal-lactic acidosis(other NRTIS also)
Term
other NRTIs-special thing about resistance
Definition
not complete cross resistance between NRTIs
Term
NRTI-didanosine(short form?) zidovudine(short form), side effect of didanosine which is dose limiting?
Definition
DDI, AZT. pancreatitis(DL), peripheral neuropahthy, hyperuricemia, liver dysfunction( imagine dida the goal keeper lying on a pancrease, so what happens? liver dysfunction gout(hyperuricemia)
Term
NRTI-lamivudine-side effects, (short form), active in treatment for another virus, what?
Definition
3TC, least toxic of NRTIs, GI deffects and neutropenia, active in hepatitis B
Term
NRTI-zalcibatine(side effects), short form
Definition
peripheral neuropathy(main)
pancreatitis, GI distress, rash neutropenia
ddc
Term
stavudine(side effects), short form
Definition
peripheral neuropathy(major), myelosupression(lesser than ZDV)
D4t
Term
NNRTIs how are they different to NRTIs
Definition
do not require metabolic activation, inhibit a diffent site from NRTIs
Term
NNRTIs names
Definition
delavirdine, nevirapine, efavirenz
Term
NNRTIs are they myelosuprresant?
Definition
no
Term
NRTI that does not need activation
Definition
adefovir
Term
PIs-2 drugs frequently used, one that is seldomly used(why?)
Definition
indinavir, ritonavir..saquinavir(not used that much, low oral bioavailability and predisposis to resistance development
Term
PIs-mechanism
Definition
PIs bind to a dipeptide on the asparatate protease inhibiting the enzyme
Term
aspartate protease is coded by what gene? what does it do
Definition
pol gene, cleaves precursor polypeptides in HIV buds to form the proteins of the mature virus core
Term
PIs-resistance, special characteristic
Definition
specific mutations of the pol gene, no complete cross resistance between different PIs
Term
side effects-indinavir
Definition
nephrolithisis, GI distress, trombocytopenia, inhibition of p450
Term
ritonavir-side effects
Definition
Gi distress, asthenia and paresthesias
Term
ritonavir major drug reactions
Definition
induces CYP1A2(which is induced by macrolides and quinolones) and inhibits major p450 isoforms leading to increased activity of dronabinol, erythromycin, ketoconazole and rifampin
Term
PIs side effects general
Definition
syndrom of disordered lipid and CHO metabolism with central adiposity and insulin resistance
Term
fusion inhibitior used to treat HIV,mechanism
Definition
enfuvirtide
binds to gp41 and inhibits the fusion of HIV1 to CD4 cells
Term
Amantidine-used to treat
Definition
influenza A. mainly prophylaxis but may reduce symptoms by 1-2 days
Term
amantadine MOa
Definition
blocks attachment, penetration and uncoating of influenza A virus
Term
amantadine-side effects
Definition
CNS-nervousness, insomnia, seizures in ovverdose. atropine like peripheral effects. livido reticularis
Term
Zanamivir and Oseltamivir-moa
Definition
inhibit neuraminidases of influenza A and B
Term
Zanamivir and Oseltamivir-what does the enzyme inhibited do
Definition
prevent clumping of virions so that more particles are available for infecting host cells
Term
Zanamivir and Oseltamivir-clinical uses
Definition
prophylaxis mainly but may reduce symptoms by 2-3days
Term
Zanamivir and Oseltamivir-SE
Definition
both nausea and vomiting
zanamivir-nasal and throat irritation(introduced via inhalation)
Term
ribavirin-mechanism
Definition
monophosphyrylated form inhibits IMP dehydrogenase
triphosphate inhibits viral RNA polymerase and end capping of viral RNA
Term
ribavirin clinical uses
Definition
respiratory syntial virus, influenza A B, Lassa fever, Hantavirus, hepatitis C(together with alpha interferon
Term
ribavirin-side effects
Definition
hematotoxic, upper airway irritation, teratogenic
Term
AIDS combinations of NRTIs to avoid, why?
Definition
DDI and DDC because of additive toxicity
D4T and AZT competition of activation
Term
HIV prophylaxis-needle stick
Definition
ZDV plus 3TC 1 month
high risk like high viral RNA copies
ZDV 3TC indinavir
Term
HIV prophylaxis pregnancy
Definition
ZDV full dose, trimester 2 and 3 plus 6 weeks to neonate, reduces vertical transmission by 80 percent

ZDV restricted to intrapartum period or nevirapine one dose at onset of delivery plus one dose to neonate
transmission decreased by 60 percent
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