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Pharmacology 2020 > Antivirals- Herpes and CMV > Flashcards

Antivirals- Herpes and CMV Flashcards

1
Q

4 anti-herpes virus agents

A

Acyclovir
Valacyclovir
Famciclovir
Penciclovir

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2
Q

Acyclovir will interact with ___(enzyme)___ converting it to _____.

A

Herpes thymidine kinase

Acyclovir monophosphate

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3
Q

What active metabolite would compete with deoxyGTP for incorporation in the viral DNA?

A

Acyclovir triphosphate

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4
Q

Why would there be chain termination and abortion of elongation with acyclovir?

A

Because it lacks the 3-hydroxy group

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5
Q

What will be the effect of probenicid and cimetidine to acyclovir clearance?

A

Decrease clearance

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6
Q

Somnolence and lethargy is observed if acyclovir is administered with?

A

Zidovudine

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7
Q

MOA of acyclovir

A

Inhibit viral DNA synthesis

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8
Q

Which anti-herpes drug is widely distributed in body fluids?

A

Acyclovir

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9
Q

Mechanism of clearance of acyclovir

A

Glomerular filtration and tubular secretion

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10
Q

Oral acyclovir is indicated for?

A
  • Genital herpes

- Primary herpetic gingivostomatitis

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11
Q

IV acyclovir is indicated for?

A
  • Herpes simplex encephalitis
  • Neonatal HSV infection
  • Serious HSV and VZV infections
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12
Q

Valacyclovir is an ______ ester.

A

L-valyl ester

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13
Q

Valcyclovir is rapidly converted to acyclovir after ____ administration.

A

Oral

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14
Q

Clinical uses of valcyclovir

A

First or recurrent genital herpes

Varicella and zoster infections

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15
Q

Half-life of famciclovir and penciclovir increases with what disease

A

Renal insufficiency

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16
Q

Elimination of famciclovir and penciclovir

A

Glomerular filtration and tubular secretion

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17
Q

Famciclovir is the prodrug of?

A

Penciclovir (6-deoxypenciclovir)

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18
Q

Route of admin for famciclovir

A

Oral

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19
Q

Clinical uses of famciclovir

A

HERPES LABIALIS
First and recurrent genital herpes
Chronic daily suppression of genital herpes
Acute herpes zoster

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20
Q

Effect of probenicid to penciclovir

A

Increases levels of penciclovir

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21
Q

ADR of famciclovir

A

Headache, nausea, diarrhea
Confusion (elderly)
Hallucinations, urticaria

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22
Q

What type of analog is penciclovir?

A

Acyclic guanine nucleoside

23
Q

What are the acyclic guanine nucleoside analogs?

A

Acyclovir
Penciclovir
Ganciclovir

24
Q

MOA of penciclovir

A

Inhibitor of viral DNA synthesis

25
Q

What enzyme phosphorylates penciclovir?

A

Viral thymidine kinase

26
Q

Dosage form of penciclovir

A

Topical cream

27
Q

Clinical use of penciclovir

A

Herpes labialis

28
Q

3 agents to treat cytomegalovirus infections

A

Ganciclovir
Valganciclovir
Foscarnet

29
Q

Spectrum of activity of ganciclovir

A

All herpes viruses, especially active against CMV

30
Q

Dosage form of ganciclovir

A

IV and intravitreal injections

31
Q

Elimination of ganciclovir

A

90% eliminated unchanged by glomerular filtration and tubular secretion

32
Q

Clinical uses of ganciclovir

A 
CMV retinitis
CMV colitis
esophagitis
pneumonitis
Reduce risk of CMV infection on transplant recipients
Kaposi’s sarcoma in AIDS patients
33
Q

What enzyme facilitates the conversion of ganciclovir to ganciclovir monophosphate in CMV?

A

Protein kinase pUL97

34
Q

Mechanisms of resistance in ganciclovir

A

Mutations in viral phosphotransferase

Mutations in viral DNA polymerase

35
Q

ADRs in ganciclovir

A

MYELOSUPPRESSION
Nausea, diarrhea, fever, rash, headache, insomnia, peripheral neuropathy
Vitreous hemorrhage and retinal detachment

36
Q

Effect of trimethoprim and probenicid to ganciclovir

A

Increased ganciclovir levels

37
Q

Effect of ganciclovir to didanosine

A

Increased didanosine levels

38
Q

What type of ester prodrug is valganciclovir?

A

L-valyl ester

39
Q

Valganciclovir is rapidly hydrolyzed to ganciclovir via what enzymes

A

Esterases

40
Q

Esterases are found where?

A

Intestinal wall and liver

41
Q

Elimination of valganciclovir

A

Renal elimination - glomerular filtration and tubular secretion

42
Q

Clinical uses of valganciclovir

A

CMV retinitis

Prevention in transplant recipients

43
Q

What type of analog is foscarnet?

A

Inorganic phosphate analog

44
Q

MOA of foscarnet

A

Inhibit viral nucleic acid synthesis

45
Q

Foscarnet reversibly blocks what binding site?

A

Pyrophosphate binding site

46
Q

What specific mechanism is inhibited by foscarnet?

A

Cleavage of pyrophosphate from deoxynucleotide triphosphate

47
Q

Dosage form of foscarnet

A

IV

Intravitreal

48
Q

True or False: Foscarnet could be deposited in bone.

A

True, 30% could be deposied in bone

49
Q

Elimination of foscarnet

A

Glomerular filtration and acute tubular secretion

50
Q

Clinical uses of foscarnet

A

End organ CMV diseases (retinitis, colitis, esophagitis)
Ganciclovir-resistant diseases
Acyclovir-resistant HSV and VZV infections
CMV retinitis in AIDS patients

51
Q

ADRs of foscarnet

A

RENAL IMPAIRMENT
Hypocalcemia
Genital ulcerations

52
Q

What ADR is expected when foscarnet is co-administered with pentamidine?

A

Severe hypocalcemia

53
Q

What ADR is expected when foscarnet is co-administered with zidovudine?

A

Risk of anemia

54
Q

What ADR is expected when foscarnet is co-administered with imipenem?

A

Risk of seizures

Pharmacology 2020 (9 decks)

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