Block II Drugs

Question 1

ritonavir

Answer 1

antiretroviral therapy (ART)– HIV

protease inhibitor (blocks the cleavage of gag/pol, inhibiting the maturation of the virus)

*used as “booster” for other drugs, to allow more PIs to remain in blood (inhibit cytochrome P450)

Question 2

efavirenz

Answer 2

antiretroviral therapy (ART)– HIV

NNRTI: non nucleoside reverse transcriptase inhibitor

-binds & inhibits reverse transcriptase

*very long half life (can stick around for weeks after d/c)

*most frequent transmitted resistance seen is to NNRTIs

Question 3

atripla

Answer 3

-antiretroviral therapy (ART)– HIV

combination of efavirenz (NNRTI) & truvada (tenofovir + emtricitabine, NRTIs)

Question 4

raltegravir

Answer 4

antiretroviral therapy (ART)– HIV

integrase inhibitor (intereferes with incorporating DNA transcript of viral genome into cellular DNA)

Question 5

acyclovir

Answer 5

antiviral; inhibits herpes simplex DNA polymerase (crossing cell membrane); reduces severity of diseases associated with productive infections

• low toxicity
• ineffective for CMV because CMV doesn’t have thymidine kinase
• used for EBV too

Question 6

oseltamivir (tamiflu)

Answer 6

• NA (neuramidase) inhibitor
• oral antiviral for influenza virus(target NA protein, acting as analogue of scialic acid, where NA usually cleaves, to inhibit NA & prevent influenza release from host cell)
• equally effective against influenza A and B

Question 7

emtricitabine

Answer 7

antiretroviral therapy (ART)– HIV

NRTI: nucleoside analogue reverse transcriptase inhibitor (blocks reverse transcriptase)

Question 8

ganciclovir

Answer 8

antivrial used for CMV; drug is activated by UL97 protein of CMV; inhibits viral & host DNA polymerase

-higher toxicity than acyclovir; effective for active EBV infections