Antimicrobial Drug Characterisitcs Flashcards
Beta lactams and aminoglycosides are incompatible ______
In vitro
- clinicians stagger animnoglycoside and penicillin dosings to avoid high in vivo concentrations
How do beta lactams inhibit cell wall synthesis?
Bind to penicillin binding proteins to prevent cross-linkage of peptidoglycan cell wall
How does the cidal action of beta lactams occur?
Osmotic imbalance between hypertonic bacterial cytoplasm and host isotonic environment
- -> protoplasts bulge thru cell wall until cell bursts
- -> if bacteria are in an environment isotonic to their cytoplasm, a static action occurs
________ decreases the activity of beta lactams
Purulent debris
What are the 3 mechanisms of beta lactam resistance?
- degradation by bacterial enzymes
- penicillin binding site alteration
- reduced penetration (seen in gram neg structure = impaired crypticity)
What allows passage of resistance between species of bacteria and between genera?
Plasmids (between species) and transposons (between genera)
Crystalline penicillin G
IV, IM, SQ
- rapid high concentrations
- short duration of plasma concentrations
Procaine penicillin G
IM, SQ
- flip flop kinetics
- lower concentrations, but prolonged duration compared to crystalline pen-G
Benzathene penicillin G
IM
- flip flop kinetics
- extremely low concentrations with prolonged duration
- little benefit in vet med
- increases residue concerns in food animals
Penicillin G adverse reactions
Primary adverse reactions are allergic
- due to degradation product penicilloic acid
- some toxicity associated with salt (potassium pen G) or ester (procaine)
What animals should not be given beta lactams?
Guinea pigs, hamsters, rabbits
- due to hind gut floral disruption
Penicillinase resistant penicillins
Similar to pen G in structure, but not inactivated by penicillinase
- oxacillin or cefoxitin are standard for testing bacteria against drugs of this group due to their better storage stability and reliability
Which penicillinase-resistant penicillin is available for intramammary infusion in dairy cows?
Cloxacillin
Why do broad spec penicillins have better penetration of gram neg bacteria?
Increased crypticity
Which broad spec penicillin is used as an intramammary infusion?
Hetacillin
Which broad spec is absorbed twice as well orally in dogs and cats?
Amoxicillin over amipicillin
Qualitatively compare ampicillin sodium vs ampicillin trihydrate injections
Sodium ampicillin (veterinary) is injectable given by all parenteral routes
- rapid absorption and elimination (every 8 hrs)
- repository ampicillin trihydrate formulation may not be able to reach therapeutic concentrations unless organism is very susceptible (low concentration, prolonged duration)
Ampi and amoxicillin are not effective against ______, even at higher extra label doses
Enteric gram-negative bacteria
- especially true of trihydrate injectable suspensions
Adverse reactions of broad spec penicillins
- large doses of ampicillin causes diarrhea in horses via entry into the bile (type B)
- disrupts flora if given orally to ruminants (okay by injection)
- trihydrate form too irritating for use in horses –> sterile abscesses
Extended spectrum penicillins are also called _________
Anti-pseudomonal
- increased crypticity, but able to bind to altered PBP
Potentiated penicillins
Have a penicillinase inhibitor added to the formulation to release penicillin
- penicillinase inhibitor has no antibacterial properties
- clavulanic acid and sulbactam
- looses stability once hydrated, keep oral tabs in foil
- only works in bacteria resistant via penicillinase
______ are susceptible to potentiated penicillin formulations
Bacteroides fragilis
1st generation cephalosporins
Similar to narrow-spec penicillins except:
- not affected by penicillinase = good Staph activity, used in skin and bone infections!!!
- not reliable against obligate anaerobic bacteria
How does cefazolin differ from other 1st generation cephalosporins?
Is the only injectable 1st gen!!
- better activity against E. coli than other 1st gens