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Pharmacology > Antivirals > Flashcards

Antivirals Flashcards

1
Q

6 classes of antiretrovirals

A

NRTI
NNRTI
Protease inhibitors
Entry inhibitors
Fusion inhibitors
Integrase inhibitors

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2
Q

Common ending to NRTIs

A

-dine (not all)

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3
Q

Common ending to protease inhibitors

A

-navir

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4
Q

ONLY NRTI that doesn’t have to be phosphorylated and why

A

Tenofovir

It is a nucleoTide

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5
Q

NRTI mechanism of action

A

Inhibit diester bond formation
—> viral DNA premature termination

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6
Q

Main side effect of all NRTIs

A

Mitochondrial toxicity
Lactic acidosis

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7
Q

Lamivudine

A

NRTI
Also used for hepatitis B
Peripheral neuropathy
One of the less toxic

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8
Q

Tenofovir uses

A

HIV
Hepatitis B

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9
Q

Zidovudine

A

NRTI
Pregnancy and breastfeeding
Infant prophylaxis

Myelosuppression
Lipodystrophy

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10
Q

Stavudine

A

NRTI
Children and adults
Peripheral neuropathy
Lipodystrophy

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11
Q

Didanosine

A

NRTI
Pancreatitis dose-dependent
Peripheral neuropathy

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12
Q

Abacavir

A

NRTI
Hypersensitivity: HLA-B57:01
—> type IV, delayed rash

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13
Q

NNRTI MOA

A

Binds allosterically —> inhibits reverse transcriptase
—> halt DNA polymerase

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14
Q

NNRTI 3 main side effects

A

Hepatic failure - life-threatening within 6 weeks

CNS: hallucinations, dizzy, ache, insomnia

Teratogenic

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15
Q

NNRTIs (inhibit/induce) P450.

A

Induce ++++

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16
Q

Nevirapine

A

NNRTI
Infants and children
Rash

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17
Q

Efavirenz

A

NNRTI
Only in combination!
Very effective and tolerable except psychiatric effects

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18
Q

NNRTIs are more effective versus HIV 1 or 2?

A

HIV 1

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19
Q

NRTIs are more effective versus HIV 1 or 2?

A

Both <3

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20
Q

Protease inhibitors are more effective versus HIV 1 or 2?

A

Both <3

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21
Q

What gene are proteases encoded by? Why are they needed?

A

POL

To create virions into mature versions

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22
Q

How do strains of HIV obtain resistance?

A

POL mutations

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23
Q

Protease inhibitors main side effects

A

METABOLIC
- Insulin resistance —>hyperglu —> diabetes
- Dyslipidemia
- Lipodystrophy

Inhibit P450

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24
Q

Indinavir

A

Protease inhibitor

Nephrolithiasis within days - give H2O
Least protein-bound

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25
Q

Ritonavir

A

Protease inhibitor

BOOSTS other drug duration by inhibiting P450
GI effects

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26
Q

Atazanavir

A

Protease inhibitor

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27
Q

Darunavir

A

Protease inhibitor
FAST

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28
Q

Fosamprenavir

A

Protease inhibitor
Long half-life

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29
Q

Tipranavir

A

Protease inhibitor
ONLY if resistant to other meds, can cause hepatotoxicity or intracranial bleeding
Given with ritonavir

30
Q

Lopinavir

A

Protease inhibitor
Pediatric with ritonavir

31
Q

Saquinavir

A

Protease inhibitor
Rarely used

32
Q

Which medication is used to boost effect duration of protease inhibitors?

A

Colbistat

Also ritonavir

33
Q

Which drug is contraindicated with protease inhibitors?

A

Rifampin!!!
(Induces P450)

34
Q

Maraviroc

A

Entry inhibitor
Binds to CCR5, can’t bind to gp120

35
Q

Gene in charge of structure proteins in HIV

A

Env gene —> gp41, gp120

36
Q

Enfuvirtide

A

Fusion inhibitor in HIV
Inhibits gp41
ONLY HIV 1
Subcutaneous

37
Q

Raltegravir

A

Integrase inhibitor in HIV
Prevents mRNA formation after DNA
Well tolerated, rare rhabdomyolysis
Both HIV 1 and 2

38
Q

Threshold for HBV treatment

A

> = 10,000 copies/mL AND high ALT

39
Q

3 possible drugs for HBV

A

Entecavir
Tenofovir TDF
IFN

40
Q

IFN can only be given if cirrhosis is (compensated/decompensated)

A

Compensated

41
Q

What is important about pegylated interferons?

A

Longer half-life
Steady concentrations
1 weekly dose

42
Q

IFN why are they not recomended?

A

Flu-like symptoms
Neurotoxicity
Myelosuppression
Lupus
Tinnitus
Retinopathy
Etc.
AND EXPENSIVE

43
Q

IFN uses

A

Hepatitis B and C
Cancers
Multiple sclerosis (beta)
Chronic granulomatous disease (gamma)

44
Q

Treatment of choice for decompensated cirrhosis by hepatitis virus

A

Nucleoside analogues

45
Q

Which is the cheapest anti-hepatitis? Why isn’t it given as monotherapy?

A

Lamivudine

High resistance, 71% mutation

46
Q

First line treatment for HBV

A

ENTECAVIR

47
Q

TDF —> tenofovir

A

TDF is prodrug, cleaved by esterases

48
Q

Entecavir side effects

A

Nausea, fatigue, headache
Lactic acidosis
Hepatomegaly

49
Q

Entecavir

A

Guanosine analogue
FIRST line for HBV

50
Q

Adefovir

A

Adenosine monophosphate analogue for HBV
Inhibits viral DNA polymerase

51
Q

Why is entecavir preferred over adefovir?

A

Adefovir —> resistance and NEPHROTOXICITY

52
Q

Lamivudine

A

Nucleoside analogue for HBV
High resistance, add tenofovir or adefovir

53
Q

HCV genotypes and most common one

A

6 total
1 is the most common, followed by 3

54
Q

NS5B enzyme

A

RNA-polymerase inhibitors for HCV
In ALL GENOTYPES

Ex. Sobosfuvir

55
Q

NS3/4A

A

Protease inhibitors for HCV
Inhibit P450

Ex. Simeprevir for genotype 1 or 4

56
Q

Ribavirin

A

Nucleoside analogue
Inhibits RNA polymerase of HCV

Given with PEG-IFN

57
Q

Ribavirin main side effects (2)

A

Hemolytic anemia dose-dependent 20%
Teratogenic category X

58
Q

First-line treatment for HCV

A

Ribavirin + PEG-IFN

59
Q

HSV first line treatment

A

Acyclovir

60
Q

Acyclovir

A

Guanosine nucleoside for HSV
1. +P by VIRAL thymidine-kinase
2. +2p by cellular enzymes

Triphosphate —| DNA synthesis

61
Q

Acyclovir indications

A

HSV encephalitis
Neonatal

62
Q

Acyclovir side effects

A

Interstitial nephritis
Crystalline nephropathy
Can be avoided by drinking H2O

63
Q

Ganciclovir

A

Guanosine nucleoside for HSV
1. +P by VIRAL thymidine-kinase
2. +2p by cellular enzymes

Triphosphate —| DNA polymerase

64
Q

Valganciclovir

A

Ganciclovir prodrug
More bioavailability

65
Q

(Val)ganciclovir side effect

A

Myelosuppression —> possible leukemia

66
Q

Oseltamivir

A

Sialic acid analogue
Inhibits neuraminidases in influenza
—> no virion release
GI effects

67
Q

First line of treatment for influenza

A

Oseltamivir

68
Q

Zanamivir

A

Neuraminidase inhibitor

69
Q

Why is oseltamivir preferred over zanamivir?

What other difference is there between both?

A

Zanamivir can cause severe side effects if there is a pre-existent airway disease.

Oseltamivir: oral
Zanamivir: inhaled

70
Q

First line treatment for CMV

A

(Val)ganciclovir

71
Q

Safest antiretroviral

A

Lamivudine

72
Q

NRTIs = La Zebra Anda TENsa, Es Season De VIH

A

Lamivudine
Zidovudine
Abacavir
Tenofovir
Emcitrabine
Stavudine
Didanosine

Pharmacology (13 decks)

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