Term
| acyclovir-mechanism of action |
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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 |
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Term
|
Definition
changes in DNA polymerase, decresed activity of TK
more than 50 percent of resistant strains completely lack TK |
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Term
| acyclovir-clinical uses, what viruses and more about them |
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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 |
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Term
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Definition
| topical, oral and IV forms |
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Term
| acyclovir-half life long or short |
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Definition
|
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Term
| acyclovir-side effects(which method of administration) |
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Definition
minor with oral use, more with IV
Crystalluria(maintain full hydration and neurotoxicity(agitation, headache, confusion-seizures in overdose) |
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Term
| acyclovir is hematotoxic, true or false |
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Definition
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Term
| acyclovir-some newer drugs please |
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Definition
| famciclovir and valacyclovir |
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Term
| acyclovir-newer drugs, how do they differ |
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Definition
activity against strains resistant to acyclovir but not against 100 percent no thymidine kinasers.
longer half life than acyclovir |
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Term
ganciclovir-mechanism and resistance
something special |
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Definition
same as acyclovir,first phosphorylation is viral specific
TK in HSV, phosphotransferase(UL97) in CMV |
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Term
| ganciclovir-spectrum of clinical use |
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Definition
|
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Term
| ganciclovir-mostly used in |
|
Definition
| prophylaxis and treatment of CMV especially retinitis in AIDS and transplant patients |
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Term
|
Definition
fever, seizures in overdose, crystalluria, rash, mucositis
hematotoxicity(leukpenia, thrombocytopenia) |
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Term
|
Definition
not an antimetabolite( whats this)
but inhibits viral RNA and DNA polymerase |
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Term
|
Definition
| similar as ganciclovir but increased activity against acyclovir resistant HSV |
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Term
|
Definition
| nephrotoxicity with ATN also electrolite imbalance with hypocalcemia(tremors and seizures) |
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Term
| foscarnet-avoid in what drug |
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Definition
| pentamidine(used to treat pneumocytis carinii(increased nephrotoxicity and hypocalcemia) |
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|
Term
reverse transcriptase inhibitors
how many types? give thier names |
|
Definition
| 2, nucleoside reverse transcriptase inhibitors, non- nucleoside reverse transcriptase inhibitors |
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Term
| reverse transcriptase inhibitors-explain to me the meaning of nucleoside reverse transcriptase inhibitors |
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Definition
| nucleoside antimetablites that are converted to active forms via phosphorylation |
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|
Term
| NRTIs-are used together with what |
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Definition
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Term
| NRTIs-zidovudine mechanism |
|
Definition
antimetabolite, phosphorylated nonspecificaly to a triphosphate
compete with natural neucleotides and incorporated into viral DNA to cause chain termination |
|
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Term
| NRTIs-zidovudine-resistance |
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Definition
| mutation in the gene that codes for RT |
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|
Term
| NRTIs-zidovudine-drug interactions |
|
Definition
increased levels when combined with
probenacid, indomethacin, TMP-SMX, azole antifungals, cimetidine
decreased levels with rifampin |
|
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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) |
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Term
| other NRTIs-special thing about resistance |
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Definition
| not complete cross resistance between NRTIs |
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Term
| NRTI-didanosine(short form?) zidovudine(short form), side effect of didanosine which is dose limiting? |
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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) |
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Term
| NRTI-lamivudine-side effects, (short form), active in treatment for another virus, what? |
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Definition
| 3TC, least toxic of NRTIs, GI deffects and neutropenia, active in hepatitis B |
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Term
| NRTI-zalcibatine(side effects), short form |
|
Definition
peripheral neuropathy(main)
pancreatitis, GI distress, rash neutropenia
ddc |
|
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Term
| stavudine(side effects), short form |
|
Definition
peripheral neuropathy(major), myelosupression(lesser than ZDV)
D4t |
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|
Term
| NNRTIs how are they different to NRTIs |
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Definition
| do not require metabolic activation, inhibit a diffent site from NRTIs |
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Term
|
Definition
| delavirdine, nevirapine, efavirenz |
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|
Term
| NNRTIs are they myelosuprresant? |
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Definition
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|
Term
| NRTI that does not need activation |
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Definition
|
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Term
| PIs-2 drugs frequently used, one that is seldomly used(why?) |
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Definition
| indinavir, ritonavir..saquinavir(not used that much, low oral bioavailability and predisposis to resistance development |
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Term
|
Definition
| PIs bind to a dipeptide on the asparatate protease inhibiting the enzyme |
|
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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 |
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Term
| PIs-resistance, special characteristic |
|
Definition
| specific mutations of the pol gene, no complete cross resistance between different PIs |
|
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Term
|
Definition
| nephrolithisis, GI distress, trombocytopenia, inhibition of p450 |
|
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Term
|
Definition
| Gi distress, asthenia and paresthesias |
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|
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 |
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Term
|
Definition
| syndrom of disordered lipid and CHO metabolism with central adiposity and insulin resistance |
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Term
| fusion inhibitior used to treat HIV,mechanism |
|
Definition
enfuvirtide
binds to gp41 and inhibits the fusion of HIV1 to CD4 cells |
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Term
|
Definition
| influenza A. mainly prophylaxis but may reduce symptoms by 1-2 days |
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Term
|
Definition
| blocks attachment, penetration and uncoating of influenza A virus |
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Term
|
Definition
| CNS-nervousness, insomnia, seizures in ovverdose. atropine like peripheral effects. livido reticularis |
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Term
| Zanamivir and Oseltamivir-moa |
|
Definition
| inhibit neuraminidases of influenza A and B |
|
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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 |
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Term
| Zanamivir and Oseltamivir-clinical uses |
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Definition
| prophylaxis mainly but may reduce symptoms by 2-3days |
|
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Term
| Zanamivir and Oseltamivir-SE |
|
Definition
both nausea and vomiting
zanamivir-nasal and throat irritation(introduced via inhalation) |
|
|
Term
|
Definition
monophosphyrylated form inhibits IMP dehydrogenase
triphosphate inhibits viral RNA polymerase and end capping of viral RNA |
|
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Term
|
Definition
| respiratory syntial virus, influenza A B, Lassa fever, Hantavirus, hepatitis C(together with alpha interferon |
|
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Term
|
Definition
| hematotoxic, upper airway irritation, teratogenic |
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Term
| AIDS combinations of NRTIs to avoid, why? |
|
Definition
DDI and DDC because of additive toxicity
D4T and AZT competition of activation |
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Term
| HIV prophylaxis-needle stick |
|
Definition
ZDV plus 3TC 1 month
high risk like high viral RNA copies
ZDV 3TC indinavir |
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|
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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