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

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
Route of administration of zanamivir
Inhalation
26
Elimination of zanamivir
Urine
27
2 drugs for hepatitis B infection
Entecavir | Lamivudine
28
What type of analog is entecavir
Guanoside nucleoside analog
29
Entecavir has selective activity against _____ .
HBV polymerase
30
MOA of entecavir
inhibit HBV polymerase
31
Activities of HBV polymerase that are inhibited by entecavir
1. base priming 2. reverse transcription of genomic strand from the progenomic mRNA 3. synthesis of the positive strand DNA
32
Oral bioavailability of entecavir
100%
33
Entecavir should be taken on a ____ stomach.
empty
34
Excretion of entecavir
Glomerular filtration and net tubular secretion
35
Clinical uses of entecavir
- chronic HBV infection | - used as a weak anti-HIV drug
36
What ADR is observed when entecavir is co-administered with drugs that reduce renal function?
Increased serum concentration of entecavir or co-administered drug
37
What type of analog is lamivudine?
Nucleoside analog
38
What is the specific activity of lamivudine?
Inhibit HIV reverse transcriptase and HBV DNA polymerase
39
What is the active form of lamivudine?
Triphosphate form
40
Mechanism of chain termination by lamivudine
Triphosphate form competes for viral DNA
41
True or False: Lamivudine does not bind significantly to plasma proteins and crosses the placenta.
True
42
Elimination of lamivudine
Via the urine unchanged
43
Which HBV agent is recommended for pregnant women?
Lamivudine
44
Clinical uses of lamivudine
- chronic HBV infection in adults and children - HIV in adults - HIV in children greater than or equal to 3 months of age
45
What ADR is expected when lamivudine is co-administered with co-trimoxazole?
Increased bioavailability of lamivudine
46
What is the drug interaction between lamivudine and zalcitabine?
They inhibit the intracellular phosphorylation of each other.