Pharm/Antiretrovirals

Question 1

Enfuvirtide

Answer 1

fusion inhibitor

Question 2

Fusion inhibitors adverse effects

Answer 2

Injection site reactions

Risk of bacterial pneumonia

Question 3

Maraviroc class

Answer 3

fusion inhibitor

Question 4

Maraviroc MoA

Answer 4

Chemokine receptor 5 antagonist prevents virus from entering host cell

Question 5

Enfuvirtide MoA

Answer 5

synthetic peptide that binds gp41 of viral envelope and prevents conformational change needed for viral fusion

Question 6

Maraviroc adverse effects

Answer 6

Cough, pyrexia, rash, M/S, CYP3A interactions

Question 7

What do the pyrimidine nucleoside analogs end in?

Answer 7

-udine or -abine

Question 8

MOA for NRTIs?

Answer 8

two-fold
Competitive inhibitor of v-RT
DNA chain termination

Question 9

NRTIs indication

Answer 9

Prevent acute infection of susceptible cells

Little effect on those already infected

Question 10

What drug is used when an HIV+ mother gives birth

Answer 10

Zidovudine

Question 11

Which 2 drugs are primarily metabolized by glucuronidation?

Answer 11

Zidovudine and raltegravir

Question 12

What 2 NRTI drugs should be taken without food?

Answer 12

Zidovudine and didanosine

Question 13

NRTI metabolism

Answer 13

does not use P450 system, excreted unchanged in urine with some exceptions

Question 14

How is abacavir metabolized?

Answer 14

By alcohol dehydrogenase

Question 15

Common toxicities of NRTIs

Answer 15

GI distress

Lactic acidosis due to mito DNA damage

Question 16

Which drug has the worst incidence of lactic acidosis?

Answer 16

Stavudine

Question 17

Zidovudine important toxicities

Answer 17

myelosuppression

Question 18

Didanosine important toxicities

Answer 18

pancreatitis; peripheral neuropathy

Question 19

Stavudine side effects

Answer 19

pancreatitis; peripheral neuropathy

Question 20

Don’t drink and ____

Answer 20

take abacavir

Question 21

WHy is tenofovir special?

Answer 21

NucleoTide RT inhibitor

Only needs 2 P events for activation

Question 22

Why are nucleotide RT inhibitors more rapid than nucleoside RT inhibitors?

Answer 22

2 P vs 3 P events

Question 23

Tenofovir MOA

Answer 23

inhibit v-RT

Question 24

What is truvada and what is it used for?

Answer 24

Tenofovir + emtricitabine

useful for chemoprophylaxis

Question 25

What are the NNRTIs?

Answer 25

Delavirdine
Nevirapine
Efavirenz

NED never nods

Question 26

NNRTIs MOA

Answer 26

Binds RT causing conform change to block activity; doesn’t need +P

Question 27

What is the best NNRTI?

Answer 27

Efavirenz…it’s “favirable”

Question 28

Which NNRTI is a CYP3A inhibitor?

Answer 28

Delavirdine; the other two are inducers

Question 29

How are NNRTIs metabolized?

Answer 29

P450

Question 30

What are the common adverse effects of NNRTIs?

Answer 30

Maculopapular rashes on trunk and extremities

Question 31

What is the one integrase inhibitor?

Answer 31

Raltegravir

Question 32

Raltegravir MOA

Answer 32

Inhibits integrase

Question 33

Raltegravir metabolism?

Answer 33

glucuronidation in liver; no P450 stuff

Question 34

How are the protease inhibitors named?

Answer 34

end in -avir (except Abacavir)

Question 35

What is the indication for protease inhibitors?

Answer 35

Most effective ART

Effective for both acute and chronic infections

Effective for both monocytes and macrophages

Question 36

How are PIs metabolized?

Answer 36

P450

Question 37

PIs and drug interactions?

Answer 37

Potent inhibitor of P3A4

Question 38

Which PI is the strongest P3A4 inhibitor?

Answer 38

Ritonavir

Question 39

What are some cons about ritonavir?

Answer 39

P3A4 inhibition
Autoinduction of metabolism
hepatotoxic at high doses

Question 40

Common adverse effects of PIs?

Answer 40

Lipodystrophy - buffalo hump neck

Question 41

Unique side effect of indinavir

Answer 41

Kidney stones

Question 42

Unique side effect of atazanavir

Answer 42

hyperbilirubinemia