III - Antibacterial Agents Flashcards
What are the four classes of antibacterial agents based on mechanism of action?
- Cell wall synthesis inhibitors
- Protein synthesis inhibitors
- Antimetabolites
- Nucleic acid synthesis inhibitors
List the cell wall synthesis inhibitors (4 broad categories)
Penicillins
Cephalosporins
Other beta lactams
Glycopeptides
What are the five families of penicillins?
- Natural penicillins
- Aminopenicillins
- Anti-staph penicillins
- Anti-pseudomonal penicillins
- Beta lactamase inhibitor combinations
2 natural penicillins
Penicillin V
Penicillin G
2 aminopenicillins
Amoxicillin
Ampicillin
4 anti-staph penicillins
Methicillin
Cloxacillin
Dicloxacillin
Oxacillin
3 anti-pseudomonal penicillins
Ticarcillin
Piperacillin
Carbenicillin
1 beta lactamase inhibitor combination
Amoxicillin clavulanate
How are cephalosporins categorized?
1st, 2nd, 3rd generation
List 4 1st generation cephalosporin drugs
Cefadroxil
Cephalothin
Cephalexin
Cefazolin
List two second generation cephalosporin drugs
Cefaclor
Cefoxitin
List four 3rd generation cephalosporins
Ceftiofur
Cefpodoxime
Cefovecin
Ceftriaxone
Name one beta lactam
Imipenem-cilastatin
One example of a glycopeptide
vancomycin
Five categories of protein synthesis inhibitors
- Tetracyclines
- Aminoglycosides
- Amphenicols
- Macrolides
- Lincosamides
Name three tetracyclines
Tetracycline
Oxytetracycline
Doxycycline
Name four aminoglycosides
Gentamicin
Amikacin
Tobramycin (ophthalmic)
Neomycin (topical)
Name three amphenicols
Chloramphenicol
Florfenicol
Thiamphenicol
Name five macrolides
Erythromycin
Tilmicosin
Azithromycin
Tylosin
Tulathromycin
Name two Lincosamides
Lincomycin
Clindamycin
Three categories of Antimetabolites (inhibitors of intermediate metabolism)
- Sulfonamides
- Folate reduction inhibitors
- Potentiates sulfonamides
Name two sulfonamides
Sulfadiazine
Sulfasalazine
Name three folate reduction inhibitors
Trimethoprim
Ormetoprim
Pyrimethamine
Name two Potentiates sulfonamides
Trimethoprim-sulfa
Ormetoprim-sulfadimethoxine
List the Nucleic Acid Synthesis Inhibitors
- Fluoroquinolones
- Rifampin
- Metronidazole
Name seven Fluoroquinolones
Enroflaxin
Orbifloxacin
Difloxacin
Barbofloxacin
Danofloxacin
Ciprofloxacin
Pradofloxacin
All beta lactams are considered _____.
Bactericidal
Beta lactams bind the ________ enzymes.
Bacterial transpeptidase
Aka penicillin binding proteins
This drug binds precursors of peptidoglycans interfering with bacterial cell wall synthesis.
Vancomycin
Beta lactams - what are the two most important mechanisms of resistance to penicillins?
- Enzymatic destruction by beta-lactamases produced by bacteria (cephalosporin lactam ring is more resistant)
- Altered target (altered penicillin binding protein)
________ and _________ are NOT effective against Pseudomonas and Styaphylococcus.
Natural penicillins - penicillin V and G
Amino penicillins - amoxicillin, ampicillin
(Susceptible to beta lactamase)
Spectrum of Activity: Penicillins
Gram + aerobic
Natural P
Aminopenicillins
Antipseudomonal
Spectrum of Activity: Penicillins
Gram - aerobic
Natural P (limited)
Aminopenicillins (better than NP)
Antipseudomonal
Spectrum of Activity: Penicillins
Gram + anaerobic
Natural P
Aminopenicillins (slightly less than NP)
Antipseudomonal
Spectrum of Activity: Penicillins
Gram - anaerobic
Natural P (limited effect)
Aminopenicillins (slightly less than NP)
Antipseudomonal
Spectrum of activity: cephalosporins
Gram + aerobic
1G - cefadroxil, cephalothin, cephalexin, cefazolin
2G (weak) - cefactor, cefotoxin, cefotetan
3G - ceftiofur, cefpodoxime, cefovecin, ceftazidime, cefotaxime extended gram negative (Antipseudomonal)
Spectrum of Activity: Cephalosporins
Gram -
1G - (fair)
2G - greater than 1G
3G - slightly increased resistance to beta lactamases
3G - Antipseudomonal
Spectrum of activity: cephalosporins
Gram + and - anaerobes
2nd generation - just these two
Cefoxitin
Cefotetan
Spectrum of activity: other beta lactams
Aerobic, gram +/-
Imipenem
Vancomycin
Spectrum of activity: other beta lactams
Anaerobic gram +/-
Imipenem
These two drugs are often reserved for very resistant organisms in human patients, so veterinary use should be limited.
Vancomycin
Imipenem
Imipenem-cilastatin-bactericidal
?????
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Beta lactams, in general, are very safe, but the most common adverse reaction is ____________.
Hypersensitivity - which can be life threatening
Some of the cephalosporins have been associated with _________ (very rare).
Renal failure
Any antibiotic can potentially alter ________, resulting in ____.
Normal flora of the GI tract
Resulting in diarrhea
Any drug can potentially irritate the ___, causing ___.
Stomach and small intestine
Vomiting / inappetence
Procaine penicillin G can cause a _______ reaction for up to _____ after injection.
Positive procaine test
Two weeks
The glycopeptide vancomycin is only available in ____ form.
Injectable / IV
Rapid IV administration of Vancomycin causes ______.
A hypersensitivity type reaction (histamine release)
Vancomycin has occasionally been associated with what four types of toxicity?
Renal toxicity
Ototoxicity
Reversible thrombocytopenia and neutropenia
Is vancomycin approved for use in food animals?
NO - it is prohibited.
Sodium and potassium salts of penicillin are commonly used in ____ but have to be administered ___ /day.
Foals
4x/day
Procaine penicillin G is commonly used in:
Horses and cattle
Indications for benzathine penicillin G
Shipping fever complex:
Strep, Staph aureus, Arcanobacterium pyogenes
Blackleg:
Clostridium chauvoei
Anti Staph penicillins are commonly used to treat:
Mastitis in dairy cattle
How are antipseudomonal penicillins used?
Ticarcillin IV to treat serious gram - infections in dogs
Intrauterine in mares
Amino-penicillins are used to treat:
Horses (IV ONLY)
Cattle (intramammary amoxicillin)
Dogs
Cats
The most commonly used first generation cephalosporins (2)
Cefadroxil
Cephalexin
Oral bioavailability in horses for these two cephalosporin drugs is very low.
Cefadroxil and cephalexin - first generation
This first generation cephalosporin is formulated for dairy cattle.
Cephapirin
This first generation cephalosporin is used in dogs, cats, and horses, especially with orthopedic surgeries.
Cefazolin - penetrates bone; used prophylactically
These two second generation cephalosporins are used for abdominal surgical prophylaxis in dogs and cats.
Cefoxitin
Cefotetan
Because of their activity against gram- and some anaerobic organisms.
Ceftiofur, a third generation cephalosporin is labeled for treating:
UTI in cats and dogs (SQ)
Respiratory infections in horses, cattle, and pigs
Cefovecin (Convenia) is a ___ generation cephalosporin used to treat:
3rd
Skin infections in dogs and cats
One-time injectable
This 3rd generation cephalosporin is administered daily to treat skin infections in dogs.
Cefpodoxime
These 3rd generation cephalosporins are not labeled for use in veterinary medicine but are occasionally used in dogs, cats, and foals for severe, resistant infections.
Carbapenems
Vancomycin is not labeled for use in veterinary medicine, and is illegal to use in food animals, but is occasionally used for:
Resistant Staphylococcal (MRSA) and/or Enterococcus infections in dogs, cats, and horses.
What are the five categories of protein synthesis inhibitors?
Tetracyclines
Aminoglycosides
Amphenicols
Macrolides
Lincosamides
Which protein synthesis inhibitors are bacteriostatic?
Tetracyclines
Amphenicols
Macrolides
Lincosamides
Which protein synthesis inhibitors are bacteriocidal?
Aminoglycosides
Name three tetracyclines
Tetracycline
Oxytetracycline
Doxycycline
Name four aminoglycosides.
Gentamicin
Amikacin
Tobramycin (ophthalmic)
Neomycin (topical)
Name three amphenicols
chloramphenicol
Florfenicol
Thiamphenicol
Name five macrolides
Erythromycin
Tilmicosin
Azithromycin
Tylosin
Tulathromycin
Name two Lincosamides
Lincomycin
Clindamycin
Resistance to Lincosamides, macrolides, and amphenicols
Inactivation/degradation by bacterial enzymes
Resistance to tetracyclines
EFFLEX PUMP that transports the drug out of the bacterial cell; drug fails to reach its target; plasma encoded
Resistance to one tetracycline produces cross resistance to others.
Resistance to aminoglycosides
Inactivation/degradation by bacterial enzymes
Failure to reach target because of decreased porin size occurs in some gram - organisms.
These protein synthesis inhibitors are active against rickettsiaceae, mycoplasma anaplasmataceae, and chlamydia
Tetracyclines and amphenicols
Staph, Pseudomonas and E. Coli should be considered resistant to which protein synthesis inhibitors until proven otherwise?
Tetracyclines
GI side effects of protein synthesis inhibitor tetracycline
Anorexia
Vomiting
Diarrhea
In horses, IV administration of this tetracycline can be fatal.
Doxycycline
Permanent brown discoloration of teeth can occur if this protein synthesis inhibitor is administered during tooth development.
Tetracyclines
Rapid IV administration of _____ in many species has resulted in collapse possibly due to calcium chelation.
Tetracyclines
In addition to GI side effects, tetracycline can cause these four issues.
Drug-induced fever
Renal toxicity
Hepatotoxicity
Allergic reactions
Cats are particularly prone to _______ caused by tetracyclines. Any dose should be followed by water.
Esophageal lesions (fibrosis and stricture)
Aminoglycosides have three main adverse effects:
Nephrotoxicity
Ototoxicity
Neuromuscular blockade
_____ concentrations are 50X greater in renal tissue than in plasma.
Aminoglycoside
Three ways to decrease nephrotoxicity with aminoglycosides.
- Use least toxic - Amikacin
- Do not use in hypovolemic patients
- Avoid concurrent use of other nephrotoxic drugs (furosemide, NSAIDs)
Aminoglycoside Ototoxicity is ____.
irreversible
Aminoglycoside Ototoxicity can occur with ____ administration.
Topical or systemic
Optic administration of aminoglycosides should be avoided in patients with __.
A ruptured tympanic membrane