HIV Pharm

Question 1

zidovudine (AZT)

Answer 1

• Nucleotide RT inhibitor
• Blocks thymidine addition
• Effective against HIV and HTLV
• risk of lactic acidosis syndrome, bone marrow suppression, myopathy, hepatic steatosis

Question 2

stavudine

Answer 2

• Like AZT
• Nucleotide RT inhibitor
• Blocks thymidine addition
• Only effective against HIV
• risk of lactic acidosis syndrome, peripheral neuropathy, fat wasting, hepatic steatosis

Question 3

emtricitabine

Answer 3

• Nucleotide RT inhibitor
• Blocks cytosine addition
• Effective against HIV and HBV
• long half life, and excreted unchanged in urine
• leads to hyperpigmentation

Question 4

lamivudine

Answer 4

• Nucleotide RT inhibitor
• Blocks cytodine addition
• Effective against HIV and HBV
• dual treatment with doltegravir is used for treatment naïve patients
• long half life, and excreted unchanged in urine

Question 5

abacavir

Answer 5

• Nucleotide RT inhibitor
• Blocks guanosine addition
• patient can’t have HLA-B*5701 genotype due to toxicity
• not a CYP substrate
• risk of hyperlipidemia and cardiac events

Question 6

didanosine

Answer 6

• Nucleotide RT inhibitor
• Blocks adenosine addition
• can be toxic: peripheral neuropathy, pancreatitis, hepatic steatosis

Question 7

tenofovir disoproxil fumarate

Answer 7

• Nucleotide RT inhibitor
• Blocks adenosine addition
• Effective against HIV and HBV
• can cause renal tubular necrosis and Fanconi syndrome, and decreased bone mineral density.

Question 8

tenofavir alafenamide

Answer 8

• -Nucleotide RT inhibitor
• Blocks adenosine addition
• Effective against HIV and HBV
• distributes differently than TDF (lower [plasma], higher [IC])
• less renal and bone toxicity

Question 9

raltegravir

Answer 9

• Integrase Strand Transfer Inhibitors
• blocks covalent bond formation in viral & host DNA (strand transfer)
• rare skin and immune hypersensitivity rxns

Question 10

elvitegravir (/c or /r)

Answer 10

• Integrase Strand Transfer Inhibitors
• blocks covalent bond formation in viral & host DNA (strand transfer)
• metabolozed by CYP3A4 so it needs to be boosted

Question 11

dolutegravir

Answer 11

• Integrase Strand Transfer Inhibitors
• blocks covalent bond formation in viral & host DNA (strand transfer)
• high genetic barrier to resistance
• avoid in pregnancy due to neural tube defects

Question 12

bictegravir

Answer 12

• Integrase Strand Transfer Inhibitors
• blocks covalent bond formation in viral & host DNA (strand transfer)
• high genetic barrier to resistance
• only available in tablet bictegravir/emtricitabine/TAF

Question 13

enfuvirtide

Answer 13

• 36 aa peptide derived from viral gp41 part that fuses with cell membrane
• inhibits membrane fusion
• ONLY effective against HIV-1
• only parenteral administration

Question 14

saquinavir

Answer 14

• protease inhibitor, prevents maturation of HIV particle
• not often used due to pill burden
• GI distress and fat wasting

Question 15

lopinavir /r

Answer 15

• protease inhibitor, prevents maturation of HIV capsid
• often works after other PIs fail
• GI distress, hyperlipidemia

Question 16

azatanavir /c

Answer 16

• protease inhibitor, prevents maturation of HIV capsid
• treatment-naïve patients
• unconjugated hyperbilirubinemia not associated with hepatitis
• GI distress, fat wasting

Question 17

darunavir /c

Answer 17

• non-peptide protease inhibitor, prevents maturation of capsid
• sulfa drug, can cause allergy
• GI distress, fat wasting

Question 18

nevirapine

Answer 18

• Non-Nucleoside Reverse Transcriptase Inhibitors
• ONLY for HIV-1
• induces CYP3A4, reduces level of birth control
• rash/itching

Question 19

efavirenz

Answer 19

• Non-Nucleoside Reverse Transcriptase Inhibitors
• ONLY for HIV-1
• given as efavirenz/emtricitabine/tenofovir
• induces CYP3A4
• psychiatric effects, potentially teratogenic

Question 20

etravirine

Answer 20

• Non-Nucleoside Reverse Transcriptase Inhibitors
• ONLY for HIV-1
• Still works after mutations that disable other NNRTIs
• induces CYP3A4
• can cause fat redistribution and Stevens-Johnson Syndrome

Question 21

rilpivirine

Answer 21

• Non-Nucleoside Reverse Transcriptase Inhibitors
• ONLY for HIV-1
• not affected by mutations that inhibit efavirenz and nevirapine
• metabolized by CYP3A4
• depression, decreased cortisol, fat redistribution, immune reconstitution syndrome

Question 22

doravirine

Answer 22

• Non-Nucleoside Reverse Transcriptase Inhibitors
• ONLY for treatment-naïve patients with HIV-1
• novel resistance unlike others in class
• metabolized by CYP3A4
• immune reconstitution syndrome

Question 23

maraviroc

Answer 23

• chemokine receptor antagonist, blocks binding of GP120 to CCR5 co-receptor
• resistance develops by shift tot CXCR4 or mutation in V3 loop in GP120
• expensive tropism test req’d before use
• CYP3A4 substrate
• minor rxn, and hepatic toxicity

Question 24

/r = ritonavir

Answer 24

• protease inhibitor that blocks CYP3A4

- used to boost levels of protein inhibitors

Question 25

/c = cobicistat

Answer 25

• CYP3A4 inhibitor

- used to boost levels of protein inhibitors

Question 26

indinavir

Answer 26

• protease inhibitor, prevents maturation of HIV particle

- can cause crystaluria or renal stones