antiretroviral drugs

Question 1

clinical efficacy of antiretroviral drugs measured by

Answer 1

plasma hiv-rna assays, cd4 counts

Question 2

t cells (cmi) lost when

Answer 2

cd4 cells less than 200 cells/microl

Question 3

antiHIV targets

Answer 3

reverse transcriptase
Integrase
protease
chemokine co receptors, ccr5
fusion (gp and cd4 receptors)

Question 4

drugs

Answer 4

protease inhibitors

reverse transcriptase - nucleoside and non nucleoside inhibitor

Question 5

nucleoside rti

Answer 5

requires phosphorylation - triphosphate forms of these drugs are formed

Question 6

zidovudine

Answer 6

nucleoside reverse transcriptase inhibitor

Question 7

zidovudine

Answer 7

thymidine analogue

Question 8

protease

Answer 8

fractionation of polyprotein

Question 9

polyprotein

Answer 9

formed by incorporated viral dna - structural and regulatory viral proteins

Question 10

resistance to azido thymidine

Answer 10

alteration in reverse transcriptase

Question 11

absorption

Answer 11

oral rapid

bioavailability - 65%

Question 12

azido thymidine

Answer 12

hepatic glucuronic conjugate -half life 1 hr
excretion urine
50% csf
plasma protein bound 30%

Question 13

azido thymidine dose

Answer 13

200mg bd adult

Question 14

azido thymidine adverse effects

Answer 14

mitochondrial dna polymerase inhibition
anemia, neutropenia
nausea
anorexia
insomnia

Question 15

interactions azido thymidine

Answer 15

paracetamol and anitfungal azoles - increase toxicity

antagonism - stavudine

Question 16

use azido thymidine

Answer 16

increase cd4
decrease hiv rna
decrease mortality
reduce neuro complications
reduce new Kaposi sarcoma lesions

Question 17

didanosine

Answer 17

purine analogue

high toxicity

Question 18

didanosine side effects

Answer 18

neuropathy

a

Question 19

stavudine

Answer 19

thymidine analogue
use thymidine kinase

peripheral neuropathy

dose 30 mg BD