Antibiotics I Flashcards

1
Q

What does penicillin inhibit?

A

Cell wall peptidoglycan synthesis

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2
Q

What happens when disruption of the peptidoglycan wall occurs?

A

Osmotic lysis of the bacterium

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3
Q

What causes ‘Hotspot’ in dogs?

A

Staphylococcus

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4
Q

Beta lactam antibiotics …

A

Contain a beta lactam ring in their molecular structures. Inhibits cell wall biosynthesis in the bacterial organism.

Beta lactams are hydrophilic, they do not like crossing membranes.

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5
Q

Targeting bacterial peptidoglycan is an example of what?

A

Selective Toxicity

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6
Q

What is the most commonly used beta-lactamase inhibitor?

A

Clavulanic acid eg amoxycillin

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7
Q

Beta-Lactam Antibiotics

What are natrual penicillins predominatly active against?

A

Gram +ves and anaerobes, but some very important gram -ves also

incl pasteurella, streptococcus, and clostridia

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8
Q

Beta-Lactam Antibiotics

What are aminopenicillins active against?

A

predom G+ve & anaerones, some important G-ve’s

Same as penicillin, but with better penetration (pKA related) into tissues/bacteria. eg amoxycillin.

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9
Q

Beta-lactam Antibiotics

What are first gen cephalosporons active against?

A

Gram +ive, successive generations have increased activity against Gram-negative bacteria.

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10
Q

Beta-Lactam Antibiotics

Why does first gen cephalosporins have excellent activity against staphylococcus

/

A

B-lactam ring is structually resistant to B lactamase.

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11
Q

Beta-Lactam Antibiotics

Third gen cephalosporins active against?

A

Further improved gram neg but reduced gram pos activity.

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12
Q

What is the t1/2 of B-lactams?

A

approx 1hr

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13
Q

How safe is B-lactamans in regards to toxicity and what can it be used in?

A

Verysafe.

Geriatrics, juveniles, pregnancy and during lactation.

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14
Q

What are the side effects of B-lactams and how do they come about?

A

Usually come about through a dysbiosis

  • killing good bacteria
  • recolonisation by a monomorphic population
  • toxins
  • GIT signs

Diarrhoahea, vomitting most common side effects

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15
Q

A bit about Procaine Penicillin?

A
  • Kills streptococcus, clostridia and pasteurella
  • Excellent anaerobic efficacy
  • Does not work against b-lactamase producing bacteria
  • Convient dosing (sid)
  • Never IV
  • Low LD50 esp in horses
  • Prescribed commonly
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16
Q

What is the procaine used for in penicillin?

A

An insoluble salt

17
Q

What can procaine do to a horse’s brain?

A

Inhibits neural conduction in inhibitory inter-neurons

18
Q

A bit about amoxicillin - clavulanic acid

A
  • excellent anaerobic efficiacy
  • works against b-lactamase producing bacteria
  • convient dosing (sid or bid)
  • good distribution to most tissues
  • not good for abcesses, pneumonia and mastitis
  • Never IV
19
Q

What happens if you give a small animal oral beta lactam?

A

Destroys normal gut flora, overgrowth of clostridum difficile, toxin production.

20
Q

Give a summary of Aminoglycosides

A
  • 30S ribosome target
  • Gram neg mostly
  • Doesnt kill anaerobes
  • SID dosing
  • Synergy with b-lactams
  • Poor oral absorption
  • Vestibular ototoxicity
  • Nephrotoxicity
21
Q

What is one of, if not the most commonly used antibiotic classes for production animals?

A

Tetracyclines

22
Q

What is the mechanism of action of the ocytetracycline?

A

Binds to ribosomes and inhibits protein synthesis

23
Q

A bit about tetracyclines?

A
  • broad spectrum
  • long t1/2 (12hrs)
  • excellent distribution
  • 50:50 hepatic: renal metabolism
  • out of date solutions are toxic
  • large animal use mostly
24
Q

Name the two classes of beta lactams

A
  1. penicillins
  2. cephalosporins (more resistant to breakage)
25
Q

Who is more susceptible to beta lactams and why?

gram +ve or gram -ve?

A
  • gram +ve more susceptible as more peptidoglycan and not as well protected
  • Gram -ve has more membrane so better protected.
    cell wall double lipid membrane structure, porins less permeable to BL.
26
Q

What do beta lactamases do?

(enzymes present in resistant bacteria)

A

hydrolyse beta-lactam ring (except cephalosporins)

27
Q

How do beta-lactamase inhibitors work?
MOA

A
  • Use a second beta-lactam that will bind (preferrentially as greater affinity for enzyme) to the beta-lactamase
  • and therefore spare the first (and more clinically efficacious) beta-lactam
28
Q

Describe the pharmacokinetics of b-lactams

A
  • hydrophilic
  • weak acids
  • good distribution except in pneumonic lung and absceses (abscess due to acidic enviro)
  • renal elimination