55-HIV (antiretroviral) drugs

Question 1

Nucleoside Reverse Transcriptase Inhibitors

names, MOA

Answer 1

Abacavir, Lamivudine, Emtricitabine, Tenofovir, Zidovudine

mimic nucleotides that require cellular kinases to convert. These target reverse transcriptase….

Question 2

Abacavir (use, adverse)

Answer 2

NRTI for all HIV patients

Allergic reaction, HLA genetic screen required

Question 3

Lamivudine (use)

Answer 3

prevent vertical transmission, chronic HBV

Question 4

Emtricitabine (adverse)

Answer 4

oral contarindicated for pregnant women/young kids

hyperpigmentation of palms and soles

Question 5

Tenofovir disoproxil (use, adverse)

Answer 5

all HIV, chronic HBV

Renal/bone toxicity, fanconi syndrome (rare)

Question 6

Zidovudine (use, adverse)

Answer 6

all HIV, post-exposure prophylaxis

myelosuppression, nail hyperpigmenation

Question 7

Non-nucleoside Reverse Transcriptase Inhibitors

names, MOA

Answer 7

Efavirenz, Nevirapine

bind to reverse transcriptase and inhibit activity (not active site)

Question 8

Efavirenz (use, adverse)

Answer 8

all HIV, NOT pregnancy

induces CYP450 enzymes

Question 9

Nevirapine (use, adverse)

Answer 9

all HIV, prevent vertical transmission

severe hepatitis!!!, induces CYP450 enzymes

Question 10

Protease inhibitors (names, MOA)

Answer 10

Atazanavir, ritonavir

Blocks activity of HIV protease, blocks maturation of virions

Question 11

Atazanavir (Use, adverse)

Answer 11

all HIV over 6

requires acid for absorption, inhibits CYP450 enzymes

Question 12

Ritonavir (use, adverse)

Answer 12

Not sole drug. used as “booster” for other ARV drugs because POTENT inhibitor of CYP450 enzymes
paresthesias, hepatitis, lipodystrophy

Question 13

Maraviroc (MOA, use, adverse)

Answer 13

co-receptor antagonist tha binds CCR5 protein and prevents interaction with HIV protein
therapy experienced patients!–must screen for CCR5 tropism of virus (not cheap)
cough, URT infections, postural hypotension

Question 14

Enfuvirtide (MOA, use, adverse)

Answer 14

Inhibits fusion of viral envelope with cell plasma membrane
injectable for treatment experienced patients that may be resistant to other treatments
painful nodes at injection sites

Question 15

Raltegravir (MOA, use, adverse)

Answer 15

Inhibits incorporation of viral provirus DNA into host DNA (integrase inhibitor)–early administration is important
all HIV
creatine kinase elevation, myopathy, rhabdomyolysis