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Pharmacology > Protein Synthesis inhibitors > Flashcards

Protein Synthesis inhibitors Flashcards

1
Q

Which protein synthesis inhibitors are cidal and which are static?

A
  • Aminoglycosides are cidal
  • Tetracyclinies, Chloramphenicol, Macrolides, Lincosamides are static
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2
Q

Name a specific chloramphenicol drug. Why is this drug different from other chloramphenicols?

A

Florfenicol
* Not susceptible to acetyltransferase inactivation
* Does not cause irreversible aplastic anemia (may cause reversible anemia after prolonged usage)

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3
Q

Are aminoglycosides time or concentration dependent?

A

Concentration dependent

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4
Q

What is the mechanism of action of aminoglycosides?

A

Binds 30S ribosomal subunit and interferes with protein synthesis

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5
Q

What are the 3 types of toxicity associated with aminoglycosides?

A

Nephrotoxicity, Ototoxicity, Neuromuscular blockade

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6
Q

What is the spectrum of activity of aminoglycosides?

A

Mostly aerobic gram negatives

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7
Q

How does the microenvironment affect the efficacy of aminoglycosides?

A
  • Inactive in acidic environment
  • Most active in alkaline environment
  • Bound by sediment in pus and inactivated
  • Inactive in low O2 tension environment
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8
Q

What length of PAE do aminoglycosides have?

A

Long (concentration dependent)

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9
Q

What are the mechanisms of toxicity of aminoglycoside?

(3)

A

Drug preferentially accumlates in kidney tubules and chochlea (have the same membrane lipids), lysosome dysfunction. In neuromuscular blockade, effects of acetylcholine are reduced at neuromuscular junction.

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10
Q

Are toxicities from aminoglycosides reversible?

A

Kidney: YES Renal tubular cells can regenerate
Cochlea: NO
Neuromuscular: YES

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11
Q

How do you prevent aminoglycoside toxicity?

A
  • Maintain hydration
  • Ensure appropriate blood flow to the kidney
  • Ensure maximum time below the trough conc
  • Appropriate dosage and frequency
  • Avoid other nephrotoxic agents
  • Use combination therapies
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12
Q

What factors determine how you dose aminoglycosides?

A
  • Age, Kidney health-> may need higher dose with longer spacing to reduce toxicity.
  • Cotraindicated if animal needs anesthesia or other neuromuscular blockade agents
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13
Q

How do you monitor dosing of aminoglycosides?

A

Monitoring urinalysis for kidney function

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14
Q

Which bacteriostatic drug can also be cidal? Under what conditions?

A

Macrolides are bacteriostatic, but can be slowly bactericidal (time dependent action like blactams)

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15
Q

What is the mechanism of action of tetracyclines?

A

Binds 30S ribosomal subunit to inhibit protein synthesis

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16
Q

What is the “bonus effect” of tetracyclines?

A

Anti-inflammatory action

17
Q

What is the mechanism of action of Chloramphenicols?

A

Inhibits 50S ribosomal subunit to disrupt protein synthesis

18
Q

What are dosing restrictions of chloramphenicol?

A

BANNED IN FOOD
ANIMALS!!!!

19
Q

What is the mechanism of action of Macrolides?

A

Inhibits 50S ribosomal subunit to disrupt protein synthesis

20
Q

What is the mechanism of action of Lincosamides?

A

Inhibits 50S ribosomal subunit to disrupt protein synthesis

21
Q

What sort of spectrum of activity do tetracyclines have? In general are there many resistant organisms?

A
  • Wide spectrum of activity
  • Many organisms have developed resistance
22
Q

Which bacteriostatic protein synthesis drugs can/can’t you use together?

A

Don’t want to use 50S drugs together (Macrolides, Lincosamides, Chloramphenicol)

23
Q

How do bacteria develop resistance to tetracyclines?

A
  • Acquisition of efflux pump
  • Ribosome protection proteins
  • Enzyme inactivation
24
Q

How do bacteria develop resistance to chloramphenicol?

A

Acquisition of a plasmid that encodes an enzyme (acetyltransferase) which inactivates chloramphenicol

25
Q

How do bacteria develop resistance to Macrolides?

A
  • Target modification (ribosome change)
  • Production of methylase to decrease dug binding
  • Enzymatic inactivation of drug
26
Q

How do bacteria develop resistance to Lincosamides?

A

Same as macrolides
* Target modification (ribosome change)
* Production of methylase to decrease dug binding
* Enzymatic inactivation of drug

27
Q

What are the important side effects of Tetracyclines?

A

Life threatening antibiotic induced colitis in horses!, Renal and hepatic toxicity at high doses, permanent tooth discoloration in young animals

28
Q

What are the important side effects of Chloramphenicol?

A

Aplastic anemia in humans (banned in food animals)

29
Q

What are the important side effects of Macrolides?

A

Life threatening colitis in adult horses, hyperthermia/respiratory distess in foals, Cardiovascular toxicosis except in cattle

30
Q

What are the important side effects of Lincosamides?

A

GI ISSUES Life threatening colitis in hindgut fermenters (HOrses + SA), C. diff in humans, diarrhea in swine and cattle

31
Q

What type of drug is Erythromycin? What is a specific side effect of Erythromycin?

A

Macrolide (static P S inhibitor)
GI upset due to prokinetic activity of Erythromycin on motilin receptors

32
Q

What type of drug is Tilmicosin? What is a unique side effect of Tilmicosin?

A

Macrolide (50S P S inhibitor)
Accidental self injection of tilmicosin CAN BE FATAL!!!

33
Q

What is the spectrum of activity of each bacteriostatic protein synthesis inhibitor drug? Are some better than others for certain bacteria?

A

Tetracyclines: wide spectrum, lots of resistance
Chloramphenicol: wide spectrum
Macrolides: Mostly Gram (+), Mycoplasma
Lincosamides: Mostly Gram (+), Mycoplasma, Toxoplasma

Macrolides accumulate in LUNGS
Lincosamides good for anaerobes
Tetracyclines rickettsia, spirochetes, protozoa, mycobacteria, anaerobic + aerobic

34
Q

Distinguish unique pharmacokinetic properties of each bacteriostatic protein synthesis inhibitor drug

A

Tetracyclines: accumulate in bone and teeth
Chloramphenicol: Destroyed by rumen, accumulates in brain, cats long half life
Macrolides: accumulates in WBCs
Lincosamides: accumulates in WBCs
Erythromycin and tilmicosin: accumulate in lungs

35
Q

Should you be cautious as the person administering any drugs? Why?

A
  • Chloramphenicols: aplastic anemia in humans
  • Tilmicosin Accidental self injection of tilmicosin CAN BE FATAL
36
Q

What drugs bind the 30S ribosomal subunit?

A

Tetracyclines, Aminoglycosides

37
Q

What drugs bind the 50S ribosomal subunit?

A

Macrolides (Erythromycin, Tilmicosin), Chloramphenicols (Florfenicol), Lincosamides

38
Q

What type of drug is Tilmicosin? What is a unique use of Tilmicosin?

A

Macrolide (50S P S inhibitor)
Bovine and ovine respiratory disease

Pharmacology (9 decks)

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