Antiretrovirals

Question 1

NRTIs

Answer 1

Abacavir-lamivudine
Tenofovir-emtricitabine

Question 2

NNRTIs

Answer 2

Efavirenz

Question 3

Protease inhibitors

Answer 3

Danrunavir

Question 4

fusion/attachment inhibitors

Answer 4

Enfuviritide
Maraviroc
Fostemsavir

Question 5

Integrase inhibitors

Answer 5

Dolutegravir

Question 6

Boosting agents

Answer 6

Cobicistat
Ritonavir

Question 7

Antivirals are

Answer 7

Virustatic
Nucleuc acid analogs that inhibit replication of viral DNA/RNA

Question 8

Antiviral agents are ineffective against

Answer 8

Latent viruses

Question 9

HIV treatment

Answer 9

3 drug regamin (ART
2 NRTIs plus a third agent (INSTI, PI, NNRTI)

Question 10

A two drug regamin for treatment of naive patients

Answer 10

Lamivudine-dolutegravir

Question 11

PrEP

Answer 11

Tenofovir-emtricitabine (2 NRTIs)
Reduces HIV transmission risk
Used in high-risk HIV negative patients

Question 12

Probilibilty of HIV resistence is directly proportional to

Answer 12

The viral load in the presence of a partially suppressive drug

Question 13

Consequencers of long term HIV therapy

Answer 13

Lipodistrophy
Drug interactions due to inhibition of CYP3A4
Immune reconstitution inflammatory syndrome

Question 14

Targets of HIV therapy

Answer 14

Blockade of viral attachment fusion or entry (GP41/GP120 Spike complex)
Inhibition of reverse transcriptase a viral RNA to DNA (reverse transcriptase)
Inhibition of genomic integration of viral DNA (integrase)
Inhibition of Viron assembly release in maturation (protease) 

Question 15

Only NRTI prodrug

Answer 15

tenofovir

Question 16

NRTI mechanism of action

Answer 16

Converted to active try phosphatases by host cell kinase that inhibit HIV reverse transcriptase and cause retroviral DNA chain termination

Question 17

Tenofovir, lamivudine, emtricitabine are also active against

Answer 17

Hepatitis B virus

Question 18

NRTI resistance

Answer 18

Do to monotherapy so drugs must be paired
Tenofoxir-emtricitabine
Abacavir-lamivudine

Question 19

NRTI adverse effects

Answer 19

Mitochondrial toxicity-Myelosuppression neuropathy pancreatitis lipoatrophy hepatic stenosis
Black box warning for exacerbation of hepatitis B and cough active patients who discontinue HBV treatment

Question 20

Tenofovir adverse effect

Answer 20

Decreased bone mineral density (suppliment calcium-vitamin D)
Renal toxicity (avoid NSAIDs)

Question 21

Abacavir adverse effect

Answer 21

Black box warning for fatal hypersensitivity
Contraindicated in HLA-B*5701 allele-positive patients

Question 22

NNRTIs mechanism

Answer 22

Allosteric inhibition of HIV-1

Question 23

Efavirenz resistance

Answer 23

Due to use as a single agent
Leads to mutations in binding site that reduce affinity

Question 24

NNRTI pharmacokinetics

Answer 24

Clearned by CYP3A4

Question 25

NNRTI adverse effects

Answer 25

Neurologic and psychiatric (Vivid dreams dizziness headache insomnia) Rash Hyperlipidemia Prolonged QT interval

Question 26

Protease inhibitors mechansim

Answer 26

Competitive inhibition of HIV protease Prevents cleavage of gag and poor poly proteins so virus fails to mature and remains non-infective

Question 27

Resistance to protease inhibitors

Answer 27

High barrier to resistance

Question 28

Protease inhibitor metabolism

Answer 28

CYP3A4

Question 29

Protease inhibitors are commonly admisitered with

Answer 29

Boosting agents: Ritonair- a PI that inhibits CYP3A4 Cobicistat- inhibits CYP3A4, but has no anti-retroviral activity, used to boost PIs and INSTI elvitegravir

Question 30

Protease inhibitor adverse effects

Answer 30

Gi intollerance Hyperlipidemia Hyperglycemia Drug interactions: CYP inhibitors such as azoles (require dose reduction) CYP inducers such as rifampin (dose escalation)

Question 31

enfuvirtide is a

Answer 31

Meptide mimic of HIV gp41 protein

Question 32

enfuvirtide mechanism

Answer 32

Binds gp41 tp prevent HIV envelope from fusing with T cell membrane

Question 33

enfuvirtide must be given

Answer 33

Parenternally (only when first-line agents fail)

Question 34

enfuvirtide adverse effects

Answer 34

Injection site reactions Elevated risk of bacterial pneumonia

Question 35

Maraviroc mechanism

Answer 35

Blocks CCR5 co-receotir to prevent entry (only antiretroviral that targets host protein)

Question 36

Maraviroc adverse rection

Answer 36

Black box warning for hepatotoxicity

Question 37

Fostemsavir mechanism

Answer 37

Prodrug that binds to gp120 and prevents attachment (only when first line agents fail)

Question 38

Fostemsavir side effects

Answer 38

Hepatotoxicity prolionged QT interival

Question 39

INSTI (dolutegravir) mechanism

Answer 39

Inhibits HIV integrase to prevent insetion of viral DNA (resistance uncomon)

Question 40

NSTI adverse effects

Answer 40

Weight gain Neural tube defects (should be used with birth control)