Pharmacology S5 Flashcards

1
Q

Infections treated with antiviral agents

DNA viruses

A

– Herpes simplex I

– Herpes simplex II

– Varicella-zoster

– Cytomegalovirus

– Epstein Barr Virus

– Human Herpes-virus 8

Hepatitis B

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2
Q

Infections treated with antiviral agents

RNA viruses

A

Influenza

– Human Immunodeficiency Virus

– Hepatitis C

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3
Q

Amantadanes: M2 ion channel inhibitors

Give E

A

Amantadine and Rimantadine

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4
Q

Amantadanes mechanism of action

A

M2 ion channel blocker

Tricyclic primary amines block M2 channel to inhibit viral uncoating Active against influenza A including non-human subtypes

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5
Q

M2 inhibitors reduce symptoms but have clinical limitations

A

Spectrum: influenza A only

Side effects: Central Nervous System Renal excretion (amantadine)

Single point mutation in M2 gene: S31N

– High-level, rapid emergence resistance

– Transmissible

– H5N1 isolates 2003-present: resistant

– H3N2 (>60% Asia 2003-4, >90% US 2005-6)

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6
Q

Novel antiviral target: neuraminidase

Features

A

Human and non-human influenza A

– Influenza B

– M2 resistant viruses

– Avian strains including H5N1

– Reconstructed 1918 pandemic H1N1

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7
Q

Time to treatment benefit of neuraminidase

A

Patients aged 12-70 yrs

– within 48 h of sudden onset of symptoms

Oseltamivir 75 mg bd for 5 days

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8
Q

neuraminidase drugs give E

A

Oseltamivir

Zanamavir

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9
Q

Pharmacokinetics of oseltamivir

Zanamivir

A

Zanamavir

Oseltamivir

– low bioavailability

– dry powder aerosol

– Remains detectable in sputum up to 24 hours post dosing

– Renally excreted

Oseltamivir

– Prodrug

– 80% bioavailability

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10
Q

Influenza virus life cycle

A
Absorption 
Endocytosis 
Endosomal vesicle 
Viral uncoating 
RNA replication 
New RNA 
Assembly 
Budding
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11
Q

Adverse events of neuramindase inhibitor

A

– Vomiting (15.0% vs 9.3%);

– abdominal pain (4.7% vs 3.9%)

– epistaxis (3.1% vs 2.5%)

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12
Q

Chloramphenicol inhibit protein synthesis by which mechanism

A

Binds to 50 S portion and inhibits formation of peptide bond

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13
Q

Erythromycin inhibit protein synthesis by which mechanism

A

Binds to 50S portion prevents translocation - movement of ribosome along mRNA

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14
Q

Tetracyclines inhibit protein synthesis by which mechanism

A

Interfere with attachment of tRNA to mRNA - ribosome complex

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15
Q

Streptomycin inhibit protein synthesis by which mechanism

A

Change shape of 30 S portion causes code on mRNA to read incorrectly

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16
Q

The two reasons for antibiotics

A

Prophylaxis of bacterial infections

Therapy of significant bacterial

infections

17
Q

What is the likely cause of infection?

A

Duration of illness

Likely organism

Anatomical site

Personal background

Past medical history

Occupational history

Travel history

Age

Time of year

18
Q

Which antibiotic is the best choice? (safety)

A

Age

Toxicity

Efficacy

Cost

Safety

Drug interactions

Administration route

Allergies

Organ function

Pregnancy, breast feeding

19
Q

Antibiotic adverse events

A

Toxicities

• Allergic reactions

• Idiosyncratic reactions
Antibiotic associated diarrhea

20
Q

Pharmacodynamics

  • Time dependent killing
  • Concentration dependent killing
A

Time dependent killing

• Concentration dependent killing

– Succesful treatment requires prolonged antibiotic presence at site of infection

– But not high concentration

– Succesful treatment requires high antibiotic concentration at site of infection

– But not for long

21
Q

Chloramphenicol inhibit protein synthesis by which mechanism

A

Binds to 50 S portion and inhibits formation of peptide bond

22
Q

Erythromycin inhibit protein synthesis by which mechanism

A

Binds to 50S portion prevents translocation - movement of ribosome along mRNA

23
Q

Tetracyclines inhibit protein synthesis by which mechanism

A

Interfere with attachment of tRNA to mRNA - ribosome complex

24
Q

Streptomycin inhibit protein synthesis by which mechanism

A

Change shape of 30 S portion causes code on mRNA to read incorrectly