Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
24 Cards in this Set
- Front
- Back
|
amantadine
|
blocks viral uncoating by interfering w/influenza A M2 protein (an ion channel)
|
|
|
oseltamivir
|
prodrug converted to oseltamivir carboxylate (active) which competitively inhibits influenza neuraminidase; interferes w/ viral release from infected cells and viral penetration into resp epithelium; virus b/cms more susceptible to inactivation by respiratory mucus
|
|
|
trifluridine
|
thymidine analog; competitively interferes w/ DNA synthesis
|
|
|
acyclovir
|
guanosine derivative; inhibits DNA Pol; phosphorylated form produced 40-100X faster in infected cells by herpes thymidine kinase (specificity for HSV infected cells); inhibits herpes DNA Pol 10-30X more than host cell DNA Pol; competitive inhibitor of dGTP for DNA pol and terminates DNA chain
|
|
|
famciclovir
|
mech similar to acyclovir; prodrug converted to penciclovir then triphosphorylated (active) to inhibit viral DNA pol
|
|
|
penciclovir
|
similar to acyclovir
|
|
|
ganciclovir
|
similar to acyclovir but monophophorylation step catalyzed by CMV protein kinase, Host Ezs convert it to triP form; virustatic; competitively inhibits DNA synthesis & terminates DNA elongation
|
|
|
foscarnet
|
selectively inhibits CMV DNA Pol by binding to its pyrophosphate-binding site therefore blocking viral DNA synth; (inhibits CMV Pol 100x more than Host Pol) does NOT require conversion to triphosphate form to be active
|
|
|
fomivirsen
|
antisense nucleic acid that inhibits gene expression a/o CMV replication; [binds major immediate early region of CMV]
|
|
|
adefovir
|
prodrug converted to triP active form; acyclic dATP analog inhibits HepB DNA pol by competing for dATP incorporation and causing DNA chain termination when incorporated into DNA
|
|
|
lamivudine (3TC)
|
nucleoside analog inhibitor of reverse transcriptase [domain of the HepB DNA Pol] (activated by phosphorylation by Host Ezs); blocks RNA intermediate to DNA
|
|
|
tenofovir
|
adenosine monophosphate nucleotide prodrug that is hydrolyzed to tenofovir phosphonate, which is further phosphorylated by cell Ezs to active form that inhibits RT by competing w/ dATP for incorporation into DNA, resulting in chain termination
|
|
|
ribavirin
|
interferes w/ viral mRNA synthesis; mono-P form inhibits inosine-5'-P DH and thus GTP synthesis; tri-P form inhibits GTP-dependent capping of viral mRNA; (nucleoside analog phosphorylated by Host Ezs)
|
|
|
interferon
|
exerts nonspecific antiviral activities; induce host cells to produce Ezs that block translation of viral mRNA; induces protein kinase (phosphorylates elongation factor), oligoisoadenylate synthetase (activates RNase that degrades viral mRNA), PDE (degrades terminal nucleotides of tRNA)
|
|
|
zidovudine (AZT)
|
thymidine analog phosphorylated by cellular kinases to tri-P active form; blocks nucleic acid synthesis by competitively inhibiting RT; also acts as DNA chain terminator
|
|
|
lamivudine (3TC)
|
nucleoside analog inhibitor of RT, phosphorylated by cell enzymes to active Rx
|
|
|
tenofovir
|
see above
|
|
|
emtricitabine
|
Flourinated analog of 3TC, inhibits RT via competing with dCTP- get chain term.
|
|
|
efavirenz
|
non-competitive inhibitor of RT that does NOT require phosphorylation for activity [binds at different site than NRTIs to cause a conformn'l change so acitve site is no longer available]
|
|
|
lopinavir
|
prevents viral protease from cleaving gag-pol polypeptide into separate fxnl proteins; fits into protease active site and acts as a competitive inhibitor; results in non-infectious viral particles
|
|
|
ritonavir
|
same but too toxic to be used at levels high enough for PI
|
|
|
enfuvirtide
|
inhibits fusion of viral (HIV-1) and cellular (CD4+) membranes to block initial entry; binds gp41 subunit of HIV glycoprotein blocking conformn'l changes required for membrane fusion
|
|
|
maraviroc
|
antagonist of chemokine co-R (CCR5), blocks entry of HIV into cells
|
|
|
raltegravir
|
inhibits HIV-1 integrase activity, preventing integration of HIV-1 DNA into genome
|
