HIV drugs

Question 1

HAART: consists of

Answer 1

3 drugs to prevent resistance:

2 NTRIs + 1 of the following: NNRTI, protease inhibitor, integrase inhibitor

Question 2

Protease inhibitors:

Answer 2

Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Ritonavir, Saquinavir
All end in “navir”
“Navir tease a protease”

Question 3

Protease inhibitors: mech

Answer 3

Assembly of virions depends on HIV-1 protease (pol gene), which cleaves the polypeptide products of HIV mRNA into their functional parts. Thus, protease inhibitors PREVENT MATURATION OF NEW VIRUSES.

Question 4

Ritonavir:

Answer 4

Can “boost” other drug conc’s by inhibiting cytochrome P-450

Question 5

Protease inhibitor tox:

Answer 5

Hyperglycemia, GI intolerance (N/D), lipodystrophy.
Nephropathy, hematuria (Indinavir)
Rifampin (potent CYP/UGT inducer) contraindicated with protease inhibitors because it can decrease protease inhibitor concentration. (Use Rifabutin instead)

Question 6

NRTIs:

Answer 6

Abacavir (ABC), Didanosine (ddl), Emtricitabine (FTC), Lamivudine (3TC), Stavudine (d4T), Tenofovir (TDF), Zidovudine (ZDV, formerly AZT)

Question 7

NRTIs: mech

Answer 7

Competitively inhibit nucleotide binding reverse transcriptase and terminate the DNA chain (lack a 3’OH group).
Tenofovir is a nucleoTide; the others are nucleoSides and need to be phosphorylated to be active.
ZDV: general prophylaxis and during pregnancy to decrease risk of fetal transmission
Have you dined (vudine) with my nuclear (nucleosides) family?

Question 8

NRTI: tox

Answer 8

Bone marrow suppression (can be reversed with granulocyte colony-stimulating factor [G-CSF] and erythropoietin), peripheral neuropathy, lactic acidosis (nucleosides), rash (non-nucleosides), anemia (ZDV), pancreatitis (didanosine)

Question 9

NNRTIs:

Answer 9

Evafirenz, Nevirapine, Delavirdine

Question 10

NNRTIs: mech

Answer 10

Bind to reverse transcriptase at site DIFFERENT from NTRIs. Do not require phosphorylation to be active or compete with nucleotides.

Question 11

NNRTIs: tox

Answer 11

Rash and hepatotoxicity are common to all NNRTIs. Vivid dreams and CNS symptoms are common with Efavirenz. Delavirdine and efavirenz are CONTRAindicated in pregnancy.

Question 12

Integrase Inhibitors:

Answer 12

Raltegravir

Question 13

Raltegravir: mech

Answer 13

Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase.

Question 14

Raltegravir: tox

Answer 14

Increase creatine kinase

Question 15

Fusion Inhibitors:

Answer 15

Enfuvirtide, Maraviroc

Question 16

Enfuvirtide: mech

Answer 16

Fusion inhibitor

Binds gp41, inhibiting viral entry

Question 17

Enfuvirtide: tox

Answer 17

Skin rxn at injection site

Question 18

Maraviroc: mech

Answer 18

Fusion inhibitor

Binds CCR-5 on surface of T cells/monocytes, inhibiting interaction with gp120