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Pharmacology > Antiviral Drugs > Flashcards

Antiviral Drugs Flashcards

1
Q

What Herpes viruses is acyclovir indicated for? Which is it not?

A

Indicated for Herpes family (1&2), Varicella

Not indicated for Epstein Bar

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2
Q

What is the MOA for Acyclovir?

A

Prodrug converted to acyclo-guanidine triphosphate by viral thymidine kinase. Sequentially phosphorylated by cellular enzymes to acyclo-GTP
Inhibits viral DNA polymerase and is incorporated into DNA resulting in chain termination

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3
Q

Does Acyclovir (Acyclo-GTP) target human DNA polymerases?

A

It is more selective for viral DNA polymerases but can have some effect

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4
Q

What type of inhibitor is Acyclo-GTP for viral DNA polymerase?

A

Competitive

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5
Q

What does Acyclo-GTP lack that results in chain termination?

A

The 3’ hydroxyl group

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6
Q

What is the mechanism of drug resistance to acyclovir?

A

1) Decreased viral expression of thymidine kinase
2) Mutation of thymidine kinase, selection of viruses that do not activate acyclovir
3) Mutation and selection for viral DNA polymerases that are not inhibited as well by acyclo-GTP

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7
Q

What two routes are tolerated well by acyclovir? What are adverse effects of each?

A

Topical - burning sensation

Oral - nausea, diarrhea, headache, vertigo

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8
Q

What are adverse effect of acyclovir when given for shingles? When given IV?

A

Shingles - tiredness

IV - reversible renal damage

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9
Q

Have can renal damage be avoided when giving acyclovir intravenously?

A

Avoiding rapid infusion

Adequate hydration

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10
Q

What is the major contraindication for Acyclovir?

A

Avoid other IV nephratoxic drugs

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11
Q

What two other drugs could be used to treat Herpes? What features make them better and/or worse?

A

Valacyclovir - prodrug of acyclovir, better oral availability
Famiciclovir - prodrug of penciclovir (topical only drug), better oral availability

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12
Q

What are 5 topical drugs for ocular herpes?

A

Ganciclovir or Acyclovir
Trifluridine
Brivudine
Vidarabine

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13
Q

What is the indication, MOA, and adverse effects for Trifluridine?

A

Indication: Ocular infections with HSV 1 or 2
MOA: inhibits viral DNA synthesis
Adverse Effects: burning and stinging, edema of eyelid, not absorbed systemically

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14
Q

What is the indication, MOA, and adverse effects of Vidarabine?

A

Indication: Acute keratoconjunctivitis or recurrent epithelial keratitis caused by HSV 1 or 2
MOA: Inhibits DNA syntheis
Adverse effects: Burning and stinging

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15
Q

What is the primary indication for ganciclovir? Why would it be used prophylactically? What are two methods of availability?

A

Indication: CMV infections
Prophylactic use in organ transplant patients
Availability: Oral and IV

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16
Q

What is a contraindication for ganciclovir?

A

Pregnancy

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17
Q

What viral enzyme works on ganciclovir instead of viral thymidine kinase?

A

Viral deoxyguanosine kinase

18
Q

What enzymes are expressed at high levels in CMV and HSV infections that catalyze the formation of ganciclovir diphosphate and ganciclovir triphosphate?

A

Cellular kinases

19
Q

What is the method of action for GCV-5’ triphosphate?

A

Inhibits viral DNA polymerase

Chain termination

20
Q

What are the adverse effects of ganciclovir? What is the contraindication?

A

Granulocytopenia and Thrombocytopenia

Contraindicated with zidovudine

21
Q

What three other drugs are approved for CMV?

A

Valganciclovir (prodrug of ganciclovir)
Cidofovir
Foscarnet

22
Q

What is the second line drug used for CMV retinitis that also was the first anti-sense drug?

A

Fomivirsen

23
Q

What is the adverse effect that makes Fomivirsen a second line drug for CMV retinitis? What drug interaction can suppress this reaction?

A

Ocular inflammation

Can be suppressed with glucocorticoids

24
Q

Which two Hepititis viruses have vaccines? Which two are there drugs for?

A

Vaccines for A and B

Drugs for B and C

25
Q

What are the 4 hepatitis antivirals indicated for hepatitis B? Which two are more effective? Which two are less effective? What do they all inhibit?

A

More effective: Entecavir and Tenofovir
Less effective: Lamivudine and Adefovir
Hepatitis B reverse transcriptase

26
Q

What is the MOA for entecavir?

A

A prodrug converted to entecavir tri-phosphate, inhibiting Hep B reverse transcriptase
Incorporation into viral DNA by reverse transcriptase results in DNA chain termination

27
Q

Which Hep B drug is also used for HIV? Which disease requires a lower dose?

A

Tenofovir

Hep B

28
Q

What are two reasons to use combination drug treatment?

A

Better blocking of viral replication

Drug resistance is less likely to arise

29
Q

What are the 5 classes of drugs for Hep C?

A 
Viral protease inhibitors (Simeprevir)
Viral RNA polymerase inhibitors (chain termination) (Sofosbuvir)
NS5A protein inhibitor (Ledipasvir)
Pegylated Interferon
Ribavirin
30
Q

What drug inhibits HCV NS3/4A protease?

A

Simeprevir

31
Q

What does the triphosphate derivative of Sofosbuvir mimic so it can be incorporated into the elongating RNA primer by HCV RNA polymerase, resulting in chain termination?

A

Cellular uridine

32
Q

Is sofosbuvis a pro-drug? What is it a substrate for?

A

Yes, substrate for RNA polymerase

33
Q

NS5A protein plays a vital role in what part of Hep C viral activity? What two drugs act as inhibitors?

A

Viral replication, assembly, and secretion

Lepipasvir and Ombitasvir

34
Q

What adverse symptoms make pegylated interferon a less desired drug for Hep C?

A

Flu like symptoms

Thus, it rarely is used anymore

35
Q

What drug for Hep C can cause hemolytic anemia and is not effective when used alone?

A

Ribavarin

36
Q

Which three drugs are most widely used in combination to treat Hep C?

A

Simeprevir, Sofosbuvir, Ledipasvir

37
Q

People over what age should get a flu vaccine?

A

6 months

38
Q

What two classes of drugs treat the flu? Do they work well?

A

Adamantanes and Neuraminidase inhibitors

No, they usually only reduce hospital time or symptom time

39
Q

Which drugs treat influenza A and not influenza B? MOA? Availability? Adverse effects?

A

Amantadine and Rimantadine (Adamantanes)
Inhibit viral M2 protein channels which inhibits proton influx and uncoating of virus
Oral
CNS effects, dizziness, nervousness, insomnia

40
Q

Which two neuraminidase inhibitors treat the flu? Which should not be used in asthma patients?

A

Oseltamivir and Zanamivir

Zanamivir - not to use in asthma patients

41
Q

When must oseltamivir and Zanamivir be given in order to improve outcome?

A

Within 2 days of symptoms

42
Q

What is the MOA of neuraminidase inhibitors?

A

Cleaves sialic acid residues on host cells which are required for release of the virus progeny. Promotes clumping.

Pharmacology (7 decks)

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