Anti-Viral Agents Flashcards

1
Q

Drugs used for chemoprophylaxis influenza

A

Amantadine

Rimantadine

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2
Q

Amantadine (Symmetrel) is used for tx of Parkinson’s disease and excreted largely unchanged in urine,

A

True

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3
Q

4-10x more active than amantadine and it has fewer side-effects due to extensive biotransformation

A

Rimantadine (Flumadine)

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4
Q

Mechanism of action of Amantadine and Rimantadine.

A
  • Inhibit viral uncoating
  • Interferes with hemagglutinin processing which inhibits viral assembly
  • Interferes with M2 protein
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5
Q

Uses of drugs for chemoprophylaxis influenza

A

Tx of influenza type A
Seasonal tx with 70-90% protection against Type a
Not effective to type B

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6
Q

Drugs acts as Neuraminidase Inhibitors

A

Oseltamivir, Zanamivir

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7
Q

MOA of Neuraminidase Inhibitor Drugs

A

Inhibits neuraminidase which prevents enhancing of penetration of viruses to host cells = the viruses tend to aggregate and migration of viruses to host cells are inhibited

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8
Q

Uses of Neuraminidase Inhibitor Drugs

A

Effective against Influenza types A and B

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9
Q

Effective for pre and post exposure to Influenza virus and used as a dry powder for oral inhalation.

A

Zanamivir

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10
Q

A prodrug in ethyl ester form and the first effective drug against influenza types A and B

A

Oseltamivir

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11
Q

These are extremely potent cytokines with antiviral, immunomodulating and antiproliferative actions which is synthesized by infected cells in response to inducers which elicit antiviral state or natural killer cell response

A

Interferons

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12
Q

Two interferons drugs

A
Interferon alfa
Interferon beta (Betaseron)
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13
Q

Use of Interferons

A

With broad spectrum anti-viral activity against DNA and RNA viruses

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14
Q

Interferons are not orally available, thus given IM/SC/topical or nasal spray.

T or F

A

True

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15
Q

Nucleoside Antimetabolites are inhibitors of DNA Polymerase

A

True

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16
Q

Nucleoside antimetabolite introduced for treatment of herpes simplex keratitis in 1963.

A

Idoxuridine

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17
Q

MOA of Idoxuridine

A

Inhibits replication of DNA viruses such as herpesvirus, poxvirus

Phosphorylated to triphosphate form which inhibits viral DNA synthesis by inhibiting viral DNA polymerase and leads to strand breakage and faulty transcription

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18
Q

Iodinated analog of thymidine

A

Idoxuridine

19
Q

Pyrimidine nucleoside, related to Idoxuridine used for the treatment of shingles, herpetic keratitis, Idoxuridine resistant-viral infections.

A

Cytarabine

20
Q

MOA of cytarabine

A

Phosphorylated to triphosphate form which blocks DNA polymerase and blocks cellular utilization of deoxycytidine which inhibits viral DNA replication

21
Q

Trifluorinated pyrimidine nucleoside with inhibitory action against HSV-1 and HSV-2, CMV, vaccinia, adenovirus.

A

Trifluridine

22
Q

The following statements are NOT true about Trifluridine, EXCEPT:

I. Has brand name Viroptic
II. Tx of primary keratoconjunctivitis, recurrent epithelial keratitis by HSV 1 and 2
III. For Acyclovir-resistant HSV infections

a. III only
b. I only
c. I, II, III
d. NOTA

A

c. I, II, III

23
Q

MOA of Trifluridine

A

Triphosphate form inhibits thymidine triphosphate incorporation into DNA by DNA polymerase = fragile, poorly functioning viral DNA

24
Q

Obtained from Streptomyces antibioticus and is used an alternative to Idoxuridie for tx of HSV keratitis and encephalitis.

A

Vidarabine

25
Q

MOA of Vidarabine

A

Activity confined to DNA viruses – triphosphate form competes with deoxyadenosine triphosphate for viral DNA polymerase

26
Q

L-valyl ester of acyclovir and increases BA by increasing lipophilicity.

A

Valacyclovir

27
Q

T or F

Valacyclovir is used as tx of shingles in immunocompromised patient.

A

True

28
Q

Nucleoside antimetabolite that is administered orally and parenterally which is used for the treatment of herpesvirus infections.

A

Acyclovir

29
Q

Acyclovir is most active against HSV-1, 2x less active to HSV-2, 10x less potent to VZV.

Uninfected human cells are unaffected by acyclovir.

a. First statement is correct.
b. Second statement is correct.
c. Both statements are correct.
d. Both statements are incorrect.

A

C.

30
Q

Orally active prodrug for chronic form of Hepatitis B

A

Adefovir

31
Q

Its diphosphate form inhibits Hepatitis B Virus DNA polymerase

A

Dipivoxil

32
Q

Analog of acyclovir and used against Herpes simplex viruses, Varicella-Zoster Virus (VZV), and Cytomegalovirus.

A

Ganciclovir

33
Q

MOA of Ganciclovir

A

Triphosphate form inhibits DNA polymerase and is incorporated into viral DNA leading to strand breakage and cessation of elongation

34
Q

The use Ganciclovir is limited because it causes myelosuppression such as neutropenia, thrombocytopenia, anemia.

T or F

A

True

35
Q

100-fold less potent than acyclovir and tx for HSV I and 2

A

Penciclovir

36
Q

The triphosphate form of this drug is a competitive inhibitor of viral DNA polymerase

A

Penciclovir

37
Q

Diacetyl inactive prodrug thus lacks antiviral activity

A

Famciclovir

38
Q

A nucleoside antimetabolite with high therapeutic index against Cytomegalovirus (CMV)

A

Cidofovir

39
Q

MOA of Cidofovir

A

Diphosphate form is a competitive inhibitor of viral DNA polymerase and is incorporated into growing viral DNA strand causing DNA chain termination

40
Q

Cidofovir has dose-limiting toxicity that can lead renal impairment, so it must be given with rehydration and probenecid.

T or F

A

True

41
Q

A nucleoside antimetabolite with synergistic activity with Zidovudine and Didanosine.

A

Foscarnet sodium

42
Q

Second line for CMV in AIDS patient

A

Foscarnet sodium

43
Q

MOA of Foscarnet sodium

A

No significant intracellular metabolism – reversible non competitive inhibitor of pyrophosphate binding site of