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Pharma 2nd semester > C.6. Antiretroviral agents > Flashcards

C.6. Antiretroviral agents Flashcards

1
Q

what do NRTI’s stand for?

A

Nucleoside/Nucleotide reverse transcriptase inhibitors

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2
Q

what is the mechanism of action of NRTI’s?

A

competitively inhibit the binding of natural nucleotides to reverse transcriptase (RNA- dependent DNA polymerase enzyme)
act as a DNA chain terminator, binding with no 3’ OH group

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3
Q

What are NRTI’s?

A

prodrugs, converted by host cell kinases to triphosphates

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4
Q

when does Resistance happen when giving NRTI’s or NNRTI’s?

A

when using a single agent, via mutations in the Pol Gene

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5
Q

side effects of NRTI’s

A 
GI distress 
headache, fatigue 
hepatotoxicity 
lactic acidosis 
mitochondrial toxicity
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6
Q

list the NRTI’S

A 
Abacavir (ABC)
Emtricitabine (FTC)
Lamivudine (3TC)
Zidovudine (ZDV)
*have you dined (vudine) with my nuclear (nucleosides) family 
Tenofovir (TDF)
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7
Q

which NRTI is a nucleotide?

A

Tenofovir

all the others are nucleosides, require more phosphorylation steps for activation

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8
Q

which NRTI’s are used for hepatitis B infection?

A

Lamivudine

Tenofovir

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9
Q

which NRTI’s is a Guanosine analogue?

A

Abacavir

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10
Q

which NRTI is used during pregnancy and lactation?

A

Zidovudine

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11
Q

what are the contraindications for giving Emtricitabine?

A

pregnancy, children, renal or hepatic dysfunction

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12
Q

which NRTI is the least potent and least toxic agent?

A

Lamivudine

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13
Q

which NRTI is the most toxic?

A

zidovudine

bone marrow suppression–> may need blood transfusions

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14
Q

which metabolism does Zidovudine have?

A

hepatic+ renal elimination

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15
Q

which NRTI is a more potent agent of Lamivudine?

A

Emtricitabine

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16
Q

which type of toxicity does Tenofovir cause?

A

Nephrotoxicity

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17
Q

what are the SE’s of Abacavir treatment?

A

allergy

associated with HLA-B *57:01 allele

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18
Q

what is the SE of Emtricitabine?

A

GI distress

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19
Q

what does Lamivudine cause?

A

peripheral neuropathy (mild)

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20
Q

what are NNRTI’s

A

Non- nucleoside reverse transcriptase inhibitors

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21
Q

NNRTI’s are not active against..?

A

HIV-2 strains

22
Q

what is the mechanism of NNRTI’s?

A

bind to a site on reverse transcriptase different from the binding site of NRTI’s

23
Q

a synergistic effect is achieved when NNRTI’s is used with..

A

NRTI’s and/or PI’s

24
Q

is there cross-resistance of NNRTI’s with NRTI’s?

A

no

25
Q

what is Etravirine?

A

the newest NNRTI approved for HIV treatment (2nd gen’)

maybe effective against strains resistant to other NNRTI’s

26
Q

side effects of Etravirine

A

rash, nausea, diarrhea

27
Q

is Etravirine an inducer or inhibitor of CYP450 enzymes

A

both

extensive drug-drug interactions

28
Q

what is Elvitegravir?

A

Integrase inhibitor

29
Q

what is the mechanism of action of Elvitegravir (tegra)

A

pyrimidine derivative that binds integrase

inhibits the integration of transcribed viral DNA into host cell chromosomes

30
Q

is Elvitegravir safe during pregnancy?

A

yes

31
Q

how do we give Elvitegravir?

A

orally

32
Q

what are the SE of Elvitegravir

A

↑ CK, myopathy, rhabdomyolysis

nausea, headache, dizziness

33
Q

list the protease inhibitors

A

Ritonavir
Darunavir
Lopinavir

“Navir (Never) tease a protease”

34
Q

which proton inhibitor is the most commonly used?

A

Ritonavir

35
Q

which PI is used in combination with Ritonavir in patients resistant to other PI’s?

A

Darunavir

36
Q

mechanism of action of Protease inhibitors

A

inhibits Aspartate protease (encoded by Pol gene)

37
Q

what is the mechanism of resistance of PI’s?

A

specific point mutations in the Pol gene

38
Q

are all the PI’s substrates and inhibitors of cytochrome P450 enzymes?

A

yes,

extensive drug-drug interactions

39
Q

the fact the PI’s inhibits lipid-regulating proteins has led to the development of..

A

metabolic disorder

40
Q

which PI is used in combination with subtherapeutic dose of Ritonavir?

A

Lopinavir

ritonavir inhibits lopinavir metabolism –> enhances it’s activity

41
Q

which PI is the most potent inhibitor of P450 enzymes?

A

ritonavir

boost other drug concentrations

42
Q

what are the SE of ritonavir

A

Gi distress, bitter taste

hepatotoxicity

43
Q

what are the SE of Darunavir

A

GI distress, skin rash

sulfonamide hypersensitivity reaction

44
Q

what is Maraviroc?

A

CCR5 receptor inhibitor –> prevent interaction between viral gp120 and CD4 on the target cell

45
Q

is Maraviroc given with other antiretroviral agents?

A

yes

46
Q

how is Maraviroc given?

A

oral

47
Q

what are the SE of Maraviroc

A

cough
diarrhea
muscle and joint pain
↑ liver enzymes

48
Q

what is the approach for HAART? give examples

A

initiation of 3 antiretroviral drugs (‘2+1 role’), before symptoms appear (if possible)
Tenofovir+Emtricatbine+ Etravirine (NNRTI)
Tenofovir+Emtricatbine+ Ritonavir (PO)
Tenofovir+Emtricatbine+ Elvitegravir (Integrase inhibitor)

49
Q

what is PrEP?

A

pre-exposure prophylaxis

Tenofovir +Emtricitabine

50
Q

what is PEP?

A

post-exposure prophylaxis

Tenofovir +Emtricitabine +/- Reltegravir

51
Q

what do we give for pregnancy antiretroviral prophylaxis?

A

2+1 regimen +zidovudine

prevent vertical transmission

Pharma 2nd semester (49 decks)

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