HIV Therapy

Question 1

Protease Inhibitors

Answer 1

“Navir tease a protease”- all protease inhibitors end in “Navir”

• Inhibit HIV-1 protease (pol gene), which is needed to cleave HIV mRNA into functional parts, preventing maturation of new viruses
• SE: Hyperglycemia, GI intolerance, Lipodystrophy, Inhibit P450 (PICK EGS)

Question 2

Lopinavir

Answer 2

Protease inhibitor

*GI intolerance, inhibits P450

Question 3

Atazanavir

Answer 3

Protease inhibitor

*GI intolerance, inhibits P450

Question 4

Darunavir

Answer 4

Protease inhibitor

*GI intolerance, inhibits P450

Question 5

Fosamprenavir

Answer 5

Protease inhibitor

*GI intolerance, inhibits P450

Question 6

Saquinavir

Answer 6

Protease inhibitor

*GI intolerance, inhibits P450, lipodystrophy, hyperglycemia

Question 7

Ritonavir

Answer 7

Protease inhibitor

*GI intolerance, inhibits P450, pancreatitis

Question 8

Indinavir

Answer 8

Protease inhibitor

*GI intolerance, inhibits P450, lypodystrophy, hyperglycemia, nephrolithiasis/nephropathy, hematuria

Question 9

Protease inhibitor SE

Answer 9

• Hyperglycemia, GI intolerance, Lipodystrophy
• Hyperglycemia and Lipodystrophy especially in Indinavir, Saquinavir, Amprenavir
• Pancreatitis in Ritonavir
• Nephrolithiasis, Nephropathy, Hematuria in Indinavir

Question 10

Protease Inhibitor that especially causes hyperglycemia and lipodystrophy

Answer 10

ISA: Indinar (also renal), Saquinavir, Amprenavir

Question 11

Protease Inhibitor that especially causes pancreatitis

Answer 11

Ritonavir

Question 12

Protease Inhibitor that especially causes nephrolithiasis, nephropathy, hematuria

Answer 12

Indinavir (also hyperglycemia and lipodystrophy)

Question 13

NRTIs

Answer 13

Competitively inhibit nucleotide binding to RT and terminate the DNA chain (lack 3’OH):
“STEAL Zidane’s Didanosine”
*All but Tenofovir must be phosphorylated
*Zidovudine is used for general prophylaxis and during pregnancy
*SE: BM suppression, peripheral neuropathy, lactic acidosis, rash (hypersensitivity)

Question 14

Stavudine

Answer 14

NRTI, must be phosphorylated

*BM suppression, lactic acidosis, rash, pancreatitis, peripheral neuropathy, hepatic steatosis

Question 15

Tenofovir

Answer 15

NRTI, does not need to be phosphorylated

*BM suppression, lactic acidosis, rash

Question 16

Emtricitabine

Answer 16

NRTI, must be phosphorylated

*BM suppression, lactic acidosis, rash

Question 17

Abacavir

Answer 17

NRTI, must be phosphorylated

*BM suppression, lactic acidosis, RASH (hypersensitivity reactions)

Question 18

Lamivudine

Answer 18

NRTI, must be phosphorylated

*BM suppression, lactic acidosis, rash

Question 19

Zidovudine

Answer 19

NRTI, must be phosphorylated

• BM suppression, lactic acidosis, rash, ANEMIA
• Used for general prophylaxis and during pregnancy

Question 20

Didanosine

Answer 20

NRTI, must be phosphorylated

*BM suppression, lactic acidosis, rash, pancreatitis, peripheral neuropathy, hepatic steatosis

Question 21

NRTI that especially causes pancreatitis, peripheral neuropathy, hepatic steatosis

Answer 21

Stavudine, Didanosine

Question 22

NRTI that especially causes hypersensitivity reaction

Answer 22

Abacavir

Question 23

HIV drug that especially causes anemia

Answer 23

Zidovudine (NRTI): also used for prophylaxis and pregnancy

Question 24

HIV drug used for prophylaxis and pregnancy

Answer 24

Zidovudine (NRTI): also causes anemia

Question 25

NRTI that does not need to be phosphorylated

Answer 25

Tenofovir

Question 26

NNRTIs

Answer 26

* Noncompetitively bind RT at different site from nucleotide * Do not need phosphorylation * Same SE as NRTIs: BM suppression, rash * NED: Nevirapine, Efavirenz, Delavirdine

Question 27

Nevirapine

Answer 27

NNRTI, does not need phosphorylation | *BM suppression, rash

Question 28

Efavirenz

Answer 28

NNRTI, does not need phosphorylation * BM suppression, rash * False-positive cannabinoid test, Confusion

Question 29

Delavirdine

Answer 29

NNRTI, does not need phosphyrlation | *BM suppression, rash

Question 30

HIV drug that causes false-positive cannabinoid test and confusion

Answer 30

Efavirenz (NNRTI)

Question 31

HIV drug class that must be phosphorylated, and causes BM suppression, peripheral neuropathy, lactic acidosis, rash (hypersensitivity)

Answer 31

NRTIs (STEAL Zidane's Didanosine)

Question 32

HIV drug class that inhibits pol gene products

Answer 32

Protease Inhibitors (-Navir): also inhibit P450

Question 33

HIV drug class that inhibit P450

Answer 33

Protease Inhibitors (PICK EGS)

Question 34

HIV drug class that causes hyperglycemia, GI intolerance, lipodystrophy

Answer 34

Protease Inhibitors (-Navir): also inhibit P450

Question 35

Integrase inhibitors

Answer 35

Raltegravir: reversibly inhibits HIV integrase | *SE: hypercholesterolemia

Question 36

HIV drug that causes hypercholesterolemia

Answer 36

Raltegravir (integrase inhibitor)

Question 37

HIV drug only used for R5 strains

Answer 37

Maraviroc (CCR5 antagonist)

Question 38

Maraviroc

Answer 38

CCR5 antagonist, only used for R5 strains

Question 39

Raltegravir

Answer 39

Integrase inhibitor | *SE: hypercholesterolemia