(7) Antimicrobials: Antivirals HIV (6.1-6.4) Flashcards

1
Q

How are NRTIs different from endogenous molecules?

A

Lack 3’ hydroxyl

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2
Q

MOA: NRTIs: NRTIs

A

Incorporation into viral DNA ⇒ Premature chain termination

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3
Q

How are nucleoside NRTIs activated?

A

Phosphorylation

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4
Q

Adverse Effects (2) : All NRTIs

A

(1) Mitochondrial toxicity
(2) ⇒ Lactic acidosis

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5
Q

Suffix: NRTIs

A

“-dine”

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6
Q

Which NRTIs are used to treat Hepatitis B?

A

(1) Lamivudine
(2) Tenofovir

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7
Q

Is Tenofovir a nucleoside or nucleotide?

A

Tenofovir = Nucleotide

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8
Q

Which NRTI is first-line during pregnancy and breastfeeding?

A

Zidovudine

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9
Q

Adverse Effect: Zidovudine

A

Myelosuppression

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10
Q

Which NRTIs are associated with lipodystrophy?

A

(1) Zidovudine
(2) Stavudine

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11
Q

Which NRTI is associated with pancreatitis?

A

Didanosine

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12
Q

Which NRTI is most associated with hypersensitivity reactions?

A

Abacavir

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13
Q

Which HLA allele has an association with hypersensitivity reactions with Abacavir?

A

HLA-B 57:01

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14
Q

What type of hypersensitivity reaction is associated with Abacavir?

A

Type IV

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15
Q

Which NRTI is associated with hyperpigmentation of palms and soles?

A

Emtricitabine

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16
Q

Do NNRTIs require phosphorylation to be active?

A

No

17
Q

MOA: NNRTIs

A

Directly bind reverse transcriptase and inhibit enzyme

18
Q

Adverse Effects (2) : NNRTIs

A

(1) Liver failure
(2) Stevens-Johnson syndrome

19
Q

Which NNRTI is most associated with CNS side effects?

A

Efavirenz

20
Q

Which class of HIV drugs should be avoided in pregnancy?

A

NNRTIs

(Nevirapine is not contraindicated)

21
Q

What effect do NNRTIs have on CYP450 system?

A

Varying – some induce and others inhibit

22
Q

Which NNRTI is NOT contraindicated in pregnancy?

A

Nevirapine

(N in Nevirapine stands for No contraindication)

23
Q

Suffix: Protease inhibitors

A

“-navir”

24
Q

What HIV gene codes for proteases?

A

pol

25
Q

Adverse Effects - Metabolic (3) : Protease inhibitors

A

(1) Insulin resistance
(2) Dyslipidemia
(3) Central adiposity

26
Q

What drug used to treat HIV is associated with nephrolithiasis?

A

Indinavir

27
Q

What protease inhibitor is the strongest inhibitor of the CYP450 system?

A

Ritonavir

28
Q

What tuberculosis drug is contraindicated in people taking protease inhibitors?

A

Rifampin

29
Q

MOA: HIV Protease inhibitors

A

Inhibits cleavage of precursor protein into active units

30
Q

What does the HIV gag gene code for?

A

The STRUCTURAL proteins,

(1) p24
(2) p7

31
Q

What does the HIV env gene code for?

A

The ENVELOPE proteins,

(1) gp41
(2) gp120

32
Q

What HIV protein binds host CD4/CCR5?

A

gp120

33
Q

MOA: Maraviroc

A

Binds CCR5 ⇒ Inhibits interaction with gp120

(Note: This is likely more effective during early infection when CCR5 receptor is preferred over CXCR4)

34
Q

What HIV protein is responsible for fusion?

A

gp41

35
Q

MOA: Enfuvirtide

A

Binds gp41 ⇒ Inhibits fusion

36
Q

What does HIV pol gene code for?

A

(1) Protease
(2) Reverse transcriptase
(3) Integrase

37
Q

MOA: Raltegravir

A

HIV integrase inhibitor

38
Q

Adverse Effect: Integrase inhibitors

A

Rhabdomyolysis