Antimicrobials Flashcards

1
Q

Beta Lactam (B-Lactam) Members of the Family

A
  • Penicillins, (Ampicillin, Amoxicilling, Ticracillin)
  • Cephalosporins (1st, 2nd, 3rd, 4th Generations)
  • Sublactams
  • Carbapenems (Imipenem)
  • Monobactams (Aztreonam)
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2
Q
Beta Lactam (B-Lactam)
Mechanism of action
A

Inhibit Cell wall synthesis (peptidoglycan synthesis).

Stimulate autolysins which degrade peptidoglycan

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3
Q

Beta Lactam (B-Lactam)

A
  • All have a B-Lactam Ring
  • Differ in teir spectrum of activities
  • Some are effective against both Gram Negatives and Gram Positives
  • Some are effective against only Gram Negative than Gram positives or vice versa
  • Vary in their absorption, toxicity, and their ability to penetrate tissues or the BBB
  • Bactericidal antimicrobials
  • Excretion through kidneys
  • Time dependant killing
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4
Q

Beta Lactam (B-Lactam) Resistance mechanisms

A
  • B-Lactamase (enzyme which cleaves B lactam ring) production
  • Extended spectrum B lactamase
  • Alteration in penicillin binding proteins
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5
Q

Beta Lactam (B-Lactam) Synergism

A
  • Use in combination with Beta Lactamase inhibitors such as Clavulinic acid, sublactam, Tazobactam
  • Aminoglycoside + B lactams facilitates entry in to bacterial cells
  • Do not mix aminoglycosides with penicillin in the same syringe
  • Ticarcillin + quinolones in pseudomonas infections
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6
Q

Beta Lactam (B-Lactam) Antagonism

A
  • Tetracycline and chloramphenicol
  • Anaphylactic reaction (type I hypersensitivity)
  • Penicillin can act as a hapten
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7
Q

Tetracyclines

A
  • A broad spectrum antibiotic (active against Gram Positive, Gram negative, Mycoplasma, Chlamydia, Ehrlichia, Rickettsia, Anaplasma, Mycobacterium and protozoan parasites)
  • Widely used in ruminants and swine
  • Inhibit protein synthesis (bind to 30s ribo)
  • Bacteriostatic
  • Time dependant antimicrobials
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8
Q

Tetracyclines Members of the Family

A

Oxytetracycline, Chlortetracycline, Doxycycline, Minocycline

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9
Q

Tetracyclines Resistance mechanisms

A
  • Energy dependant efflux
  • Ribosomal protection
  • Chemical modification and catalysis by enzymes
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10
Q

Tetracycline Notable Facts

A
  • Chelating agents
  • Cross placental barrier
  • Secreted in milk
  • Anti-inflammatory, Neuroprotective and immunomodulant effects
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11
Q

Tetracycline Toxicity and adverse effects

A
  • Irritant
  • Cardiovascular effects
  • Tooth discoloration
  • Alternation of intestinal flora and enterocolitis (Horses)
  • Intravenous administration of Doxycycline in horses; cardiovascular collapse
  • Nephrotoxicosis
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12
Q

Aminoglycosides Members of the Family

A

-Gentamicin, Tobramycin, Streptomycin, Kanamycin, Neomycin, Spectinomycin, Amikacin

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13
Q

Aminoglycosides Mechanism of Action

A
  • Inhibit protein synthesis (30s ribosome)
  • Bactericidal
  • Concentration dependant antimicrobial
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14
Q

Aminoglycosides

A
  • Oxygen dependant uptake by th emicrobes
  • Purulent debris inactive aminoglycosides
  • Prolonged post antibiotic effect
  • Need parenteral administration
  • Renal excretion
  • Does not penetrate BBB
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15
Q

Aminoglycosides Synergism

A

With Beta-lactams but physically incompatible with B-lactams

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16
Q

Aminoglycosides Toxicity

A
  • Nephrotoxicity (acute tubular necrosis)
  • Calcium supplementation and high protein diet
  • Ototoxicity/Cranial nerve VIII toxicity/vestibular or cochlear damage (cats more susceptible)
17
Q

Aminoglycosides Resistance Mechanisms

A

Are by plasmid mediated enzymes which inactivate aminoglycosides

18
Q

Fluoroquinolones

A
  • Synthetic anitmicrobial agents
  • Entrofloxacin, Ciprofloxacin
  • Inhibit DNA gyrase (DNA replication)
  • Oral absorption, extended half-life
  • Concentration dependant killing
  • High intracellular concentration in phagocytes
  • Bactericidal
  • Prolonged Post antibiotic effect
  • Excreted through urine
  • Rapid resistance development
19
Q

Fluoroquinolones Resistance

A
  • Not very effective against anaerobes

- By modification or protection of target, decreased permeability, efflux pump

20
Q

Fluoroquinolones Synergism

A

With beta-lactams, amionglycosides

21
Q

Fluoroquinolones Toxicity

A
  • Generally safe
  • Articular cartilage degeneration in juvenile dogs, retinal degeneration in cats (high enrofloxacin dose)
  • Neurotoxic effect, tendon rupture (humans)
  • Canine toxic shock syndrome; S. canis infection and Fluoroquinolone monotherapy (bacteriophage induced lysis of S. canis)
22
Q

Sulfa or Potentiated Sulfa Drugs Members of the Family

A
  • Sulfonamide
  • Sulfamethoxazole
  • Sulfadiazine etc.
23
Q

Sulfa or Potentiated Sulfa Drugs

A
  • Oral absorption - good
  • Excreted through bile feces, urine
  • Broad spectrum antimicrobial agent (bacteria and protozoa)
24
Q

Sulfa or Potentiated Sulfa Drugs Synergism

A

Synergistic with diaminopyrimidines (Trimethoprim, Pyrimethamine)

25
Q

Sulfa or Potentiated Sulfa Drugs Toxicity

A

Allergic reactions in dogs (Doberman Pinschers)

26
Q

Sulfa or Potentiated Sulfa Drugs Resistance

A

By impaired drug penetration, altered enzymes

27
Q

Macrolides, Azalides, Ketolides Members or Groups

A

-Erythromycin, Azithromycin, Clarithromycin, (Tulathromycin, Tilmicosin, Tylosin)

28
Q

Macrolides, Azalides, Ketolides

A

Intracellular accumulation in phagocytes

29
Q

Macrolides, Azalides, Ketolides

A
  • Intracellular accumulation in phagocytes
  • Inhibit protein synthesis
  • Bacteriostatic
  • Immunomodulatory effect
30
Q

Macrolides, Azalides, Ketolides Resistance

A

Target site modification, active efflux, enzymatic inactivation

31
Q

Macrolides, Azalides, Ketolides - Chloramphenicol

A
  • Cloramphenicol, Thaimphenicol, florfenicol
  • Inhibit protein synthesis
  • Bacteriostatic
32
Q

Macrolides, Azalides, Ketolides - Lincosamides

A
  • Clindamycin, Lincomycin
  • Inhibit protein synthesis
  • Do not combine with macrolides
  • Bacteristatic
33
Q

Macrolides, Azalides, Ketolides - Rifampin

A
  • Inhibit RNA polymerase

- Bactericidal against intracellular and extracellular bacteria

34
Q

Macrolides, Azalides, Ketolides - Peptide Antibiotics

A

Glycopeptides (Vancomycin), Polymyxins, Bacitracin