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Pharmacology 2020 > Antivirals - Influenza and Hepatitis B > Flashcards

Antivirals - Influenza and Hepatitis B Flashcards

1
Q

4 antiviral drugs for influenza

A

Amantadine
Rimantadine
Oseltamivir
Zanamivir

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2
Q

Spectrum of activity of amantadine

A

Active only against Influenza A

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3
Q

Elimination of amantadine

A

Urine

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4
Q

Dose of amantadine must be reduced in what cases

A

elderly

renal insufficiency

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5
Q

Which anti-influenza agent is a synthetic tricyclic amine?

A

Amantadine

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6
Q

Which anti-influenza agent is an a-methyl derivative?

A

Rimantadine

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7
Q

Spectrum of activity of rimantadine

A

Active only against influenza A

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8
Q

Elimination of rimantadine

A

Urine

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9
Q

Dose of rimantadine must be reduced in what cases

A

elderly
renal insufficiency
hepatic insufficiency

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10
Q

MOA of amantadine and rimantadine

A

Inhibit uncoating of viral RNA

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11
Q

Which channel is blocked by rimantadine and amantadine?

A

M2 proton ion channel

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12
Q

Why are amantadine and rimantadine no longer recommended as anti-influenza drugs?

A

High rates of resistance

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13
Q

ADRs of amantadine and rimantadine

A
  • GI
  • CNS
  • birth defects
  • neurotoxicity
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14
Q

What risk is observed when amantadine and rimantadine are administered with antihistamines, anticholinergic drugs, HCTZ, and cotrimoxazole?

A

Increased neurotoxicity

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15
Q

What type of inhibitors are oseltamivir and zanamivir?

A

Neuraminidase inhibitors

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16
Q

What type of analog are oseltamivir and zanamivir?

A

Sialic acid analog

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17
Q

Oseltamivir and zanamivir selectively inhibits what enzymes

A

Influenza A and B neuraminidases

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18
Q

What particular step in viral infection is targeted by oseltamivir and zanamivir?

A

Release of progeny of influenza virus

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19
Q

Route of administration of oseltamivir

A

Oral

20
Q

Excretion of oseltamivir

A

Glomerular filtration and tubular secretion

21
Q

What is the effect on the kidney when oseltamivir is increased?

A

Decreased renal function

22
Q

What is the effect of probenicid to oseltamivir clearance?

A

Reduced renal clearance

23
Q

ADRs of oseltamivir

A
  • nausea, vomiting, headache
  • fatigue, diarrhea
  • rash (rare)
  • neuropsychiatric events (adults and adolescents)
24
Q

What ADR of oseltamivir is commonly seen in adults and adolescents?

A

Neuropsychiatric events

25
Q

Route of administration of zanamivir

A

Inhalation

26
Q

Elimination of zanamivir

A

Urine

27
Q

2 drugs for hepatitis B infection

A

Entecavir

Lamivudine

28
Q

What type of analog is entecavir

A

Guanoside nucleoside analog

29
Q

Entecavir has selective activity against _____ .

A

HBV polymerase

30
Q

MOA of entecavir

A

inhibit HBV polymerase

31
Q

Activities of HBV polymerase that are inhibited by entecavir

A
  1. base priming
  2. reverse transcription of genomic strand from the progenomic mRNA
  3. synthesis of the positive strand DNA
32
Q

Oral bioavailability of entecavir

A

100%

33
Q

Entecavir should be taken on a ____ stomach.

A

empty

34
Q

Excretion of entecavir

A

Glomerular filtration and net tubular secretion

35
Q

Clinical uses of entecavir

A
  • chronic HBV infection

- used as a weak anti-HIV drug

36
Q

What ADR is observed when entecavir is co-administered with drugs that reduce renal function?

A

Increased serum concentration of entecavir or co-administered drug

37
Q

What type of analog is lamivudine?

A

Nucleoside analog

38
Q

What is the specific activity of lamivudine?

A

Inhibit HIV reverse transcriptase and HBV DNA polymerase

39
Q

What is the active form of lamivudine?

A

Triphosphate form

40
Q

Mechanism of chain termination by lamivudine

A

Triphosphate form competes for viral DNA

41
Q

True or False: Lamivudine does not bind significantly to plasma proteins and crosses the placenta.

A

True

42
Q

Elimination of lamivudine

A

Via the urine unchanged

43
Q

Which HBV agent is recommended for pregnant women?

A

Lamivudine

44
Q

Clinical uses of lamivudine

A
  • chronic HBV infection in adults and children
  • HIV in adults
  • HIV in children greater than or equal to 3 months of age
45
Q

What ADR is expected when lamivudine is co-administered with co-trimoxazole?

A

Increased bioavailability of lamivudine

46
Q

What is the drug interaction between lamivudine and zalcitabine?

A

They inhibit the intracellular phosphorylation of each other.

Pharmacology 2020 (9 decks)

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