Antivirals (lecture)

Question 1

What is the first line Rx for Herpes and its MoA?

Answer 1

Acyclovir: DNA chain termination because it is a guanosine analog

Question 2

How does Acyclovir specifically target HSV?

Answer 2

It is a prodrug that is metabolized by viral thymidine kinase?

Question 3

Azifothymidine is a part of what class of drugs? What is the MoA of that class?

Answer 3

Nucleoside Reverse Transcriptase Inhibitor: They work as chain terminators of reverse transcriptase

Question 4

What is the underlying reason for AZT toxicities?

Answer 4

It is a prodrug that is not only broken down by viral enzymes, but is ALSO broken down by the HOST’s healthy cells.

Question 5

What are the three big side effects of NRTIs?

Answer 5

Macrocytic anemia, neutropenia, lactic acidosis (the big one)

Question 6

Zidovudine, Emtricitabine, Abacavir, and Lamivudine are all examples of ______ (class of drug).

Answer 6

NRTIs hit RT with ZEAL

Question 7

What two NRTIs are used with co infection of HIV and HVB?

Answer 7

Emtricitabine and Lamivudine

Question 8

Abacavir will cause hepatomegaly in what specific population?

Answer 8

People with HLA-B*5701 genotype

Question 9

Tenovir is a _______ (class of drug) and differs from NRTIs in its activity how?

Answer 9

NucleoTIDE analog RT inhibitor, so it is active in resting cells

Question 10

Nevirapine, Rilpivirine, Etravirine, delavirdine, and Efacvirenz are all examples of what class of Rx?

Answer 10

Non-nucleoside reverse transcriptase inhibitors

Question 11

What NNRTI is used prophylactically for vertical transmission?

Answer 11

Nevirapine

Question 12

What NNRTI is contraindicated in pregnancy?

Answer 12

Efavirenz

Question 13

What is the last line NNRTI?

Answer 13

Etravirine

Question 14

Which NNRTI is known to cause Stevens Johnson Syndrome?

Answer 14

Nevirapine

Question 15

What is the MoA of Lamivudine and tenofovir? How are they used in the context of HIV infection?

Answer 15

DNA polymerase inhibitors first used for HBV, but are also effective in HIV treatment (co-infection).

Question 16

What is the MoA of Maraviroc?

Answer 16

Inhibition of gp 120 (HIV receptor) and CCR5 (T cell receptor) binding. This inhibits binding of HIV with T cells. WILL NOT WORK IF SWITCH TO CXCR5 (of the T cell).

Question 17

What is the MoA of Enfuvirtide?

Answer 17

Lock gp 41 (HIV co receptor) in its extended conformation, inhibiting cell fusion.

Question 18

What is the MoA of Raltegravir?

Answer 18

HIV integrase inhibitor.

‘-teg’ –> inTEGrate

Question 19

Protease inhibitors all end in ______.

Answer 19

-navir

Question 20

What is the first line protease inhibitor in pregnant patients?

Answer 20

Ritonavir - this also increases the activity of other protease inhibitors

Question 21

As a general rule, is there cross resistance of drugs within a class?

Answer 21

NO. If one drug in a class doesn’t work, trying another of the same class is commonplace.

Question 22

Ribavirin is used in what two viral infections?

Answer 22

HCV and RSV (aerosolized)

Question 23

HCV protease inhibitors have the suffix ______.

Answer 23

-previr

Question 24

What is the MoA and use of Sofosbuvir?

Answer 24

HCV RNA synthase inhibitor.