Antiretrovirals

Question 1

what are the 5 nucleoside reverse transcriptase inhibitors

Answer 1

zidovudine, emtricitabine, tenofovir, lamivudine, abacavir

Question 2

MOA of NRTIS

Answer 2

requires phosphorlyation x 3, incorporated into viral DNA and inhibits viral reverse transcriptase

Question 3

zidovudine, good for what patients?

Answer 3

AIDS dementia (CNS penetration) and safe in pregnancy

Question 4

zidovudine toxicity

Answer 4

CNS, lactic acidosis, hepatoxicity, myelosuppresion

Question 5

first line NRTS for HIV

Answer 5

tenofovir and emtricitabine

Question 6

side effects of tenofovir and emtricitabine

Answer 6

flatulence

Question 7

toxicity of abacavir

Answer 7

serious hypersensitivity, SJS so screen for HLA-B-5701, cannot restart drug if every go off, is usually fatal

Question 8

what are the two NNRTIs

Answer 8

efavirenz and rilpivirine

Question 9

MOA for NNRTIs

Answer 9

binds directly to inhibit viral reverse transcriptase

Question 10

toxicities of efavirenz

Answer 10

drug interactions (CYP3A4), teratogenic so avoid in pregnancy

Question 11

DOC for NNRTIs

Answer 11

efavirenz, use rilpivirine if pregnant

Question 12

protease inhibitors

Answer 12

all end in ivir, except abacavir which is an NRTIs

Question 13

protease inhibitors MOA

Answer 13

bind to proteases inhibiting their function (digestion of long polypeptides into smaller mature ones)

Question 14

must give a protease inhibitor with what other drug

Answer 14

NRTIs, due to mutations and resistance if given alone

Question 15

common toxicities of protease inhibitors

Answer 15

altered body fat distribution, insulin resistance, elevated serum cholesterol, spontaneous bleeding

Question 16

drug interactions of PIs

Answer 16

metabolized by CYP3A4 so often given with ritonavir to increase blood levels and decrease dosing, do not give with drugs that induce CYP3A4 because it will decrease levels (aka RIFAMPIN, St. John’s wort)

Question 17

toxicities of ritonavir

Answer 17

do not combine with saquinavir, QT

contains ethanol, do not give with disulfiram, flagyl, cephalosporins

Question 18

PI DOC

Answer 18

darunavir

Question 19

limits to darunavir and tipranavir

Answer 19

contains a sulfa moiety, do not use in patients with an allergy to sulfa

Question 20

PI drug of second choice

Answer 20

atazenavir

Question 21

side effects of atazenavir

Answer 21

diarrhea, rash, nausea is common, may cause an increase in bilirubin

Question 22

what drug is lopinavir given with

Answer 22

ritonavir, increases bioavailability

Question 23

why do we not give indinavir often

Answer 23

cross resistance with ritonavir, nephrolithiasis, hyperbilirubienia

Question 24

who should be given tipranavir

Answer 24

treatment experienced pateints

Question 25

what are the two fusion inhibitors

Answer 25

enfuvirtide, maraviroc

Question 26

MOA of enfuvirtide

Answer 26

binds to gp41 subunit and prevents conformational change

Question 27

enfuvirtide

Answer 27

only for treatment experienced patients, SQ only, increases chance of bacterial pneumonia

Question 28

maravoic MOA

Answer 28

CCR5 binding to inhibit fusion

Question 29

MOA for dolutegravir

Answer 29

integrase inhibitor