Week 6: HIV drugs

Question 1

Name Nucleoside Reverse Transcriptase Inhibitors

Answer 1

Zidovudine (AZT), Lamivudine, Abacavir, Emtricitabine

Question 2

Name NucleoTIDE Reverse Transcriptase Inhibitor

Answer 2

Tenofovir

Question 3

Name Non-nucleoside reverse transcriptase inhibitor

Answer 3

Etravirine, Efavirenz, Rilpivirine

Question 4

Name Protase Inhibitors

Answer 4

Atazanavir, Darunavir

Question 5

Name integrase inhibitor

Answer 5

Raltegravir

Question 6

Name Fusion inhibitor

Answer 6

Enfuvirtide (T-20)

Question 7

Name CCR5 antagonist

Answer 7

Maraviroc

Question 8

What is the goal of HIV treatment?

Answer 8

fully undetectable levels of virus

Question 9

What is the mechanism of NRTIs?

Answer 9

competitively inhibit reverse transcriptase and can be incorporated into viral DNA chain and cause termination

Question 10

T/F: NRTIs require phosphorylation by cellular enzymes to be active

Answer 10

True

Question 11

What are AE of NRTIs?

Answer 11

lactic acidosis with hepatic steatosis; most likely due to mitochondrial toxicity

Question 12

What are AE of zidovudine?

Answer 12

granulocytopenia and anemia in 45% of patients, CNS disturbances

Question 13

What are AE of Abacavir?

Answer 13

hypersensitivity reactions (Test for HLA-B*5701)

Question 14

What is MOA of Tenofovir (nucleotide RTI)

Answer 14

same as NRTI

Question 15

What are AE of tenofovir?

Answer 15

nausea, vomiting, diarrhea and POTENTIAL FOR RENAL FAILURE

Question 16

What is MOA of nnRTI (etravirine, efavirenz, rilpivirine)

Answer 16

bind directly to RT at a site different from NRTI, preventing enzyme from producing viral DNA

Question 17

Do NNRTIs have cross resistance with NRTIs and protease inhibitors?

Answer 17

No

Question 18

What are AE of NNRTIs?

Answer 18

varying levels of GI intolerance and skin rash, can affect cytochrome P450

Question 19

What can you not use rilpivirine?

Answer 19

patients with pretreatment viral loads of >100,000 copies/ml

Question 20

What is mechanism of protease inhibitors?

Answer 20

Prevents maturation of full assembled virus, preventing buddying of the virus and therefore preventing further infections

Question 21

What are AE of Protease inhibitors?

Answer 21

GI, hepatotoxicity, hyperglycemia and insulin resistance, dyslipidemia, CYP3A4

Question 22

What is the better use of ritonavir?

Answer 22

Inhibits CYP3A4 to increase serum levels of other drugs

Question 23

What is MOA of cobicistat?

Answer 23

pharmacokinetic enhancer that inhibits CYP3A4 and intestinal transport proteins; acts as a booster of protease inhibitors

Question 24

What is MOA of enfuvirtide (FI)

Answer 24

Prevents conformational change of gp41 upon binding of HIV particle to cell

Question 25

What is MOA of integrase inhibitors (Raltegravir)

Answer 25

Inhibits strand transfer into host DNA

Question 26

What is MOA of CCR5 antagonist (Maraviroc)

Answer 26

Blocks CCR5, a major co-receptor used by HIV-1 to gain entry into host cells

Question 27

What is AE of CCR5 antagonist?

Answer 27

pyrexia, rash, postural dizziness

Question 28

What is HAART the result of? What is it?

Answer 28

long term use of combination anti-retroviral therapies usually RTIs in combo with PI. Results in lipodystrophy (central adiposity, hyperlipidemia, insulin resistance and DM)