Penicillins Flashcards
What is the general structure of Penicillins?
B-Lactam Ring with a Thiazolidine ring and an acyl side chain
What is the MoA of penicillins?
Inhibit bacterial cell wall synthesis by blocking the crosslinking of adjacent peptidoglycan strands
Results in lysis
What is the target of B-lactam antibiotics?
Penicillin-binding proteins
Transpeptidases, transglycolases and D-alanine carboxykinase
What are the resistance mechanisms to penicillins?
B-lactamase production
Alterations in penicillin binding proteins
Decreased penetration to site of action
What is the primary route of elimination of penicillins?
Renal excretion
Must adjust dose for renal insufficiency
What is the Cockroft-Gault equation?
(140-age) x weight(kg) / (SerumCreatinine) x (72)
Can be used for majority of renally excreted drugs
When do most penicillins achieve peak levels?
1-2 hours after ingestion
What three penicillins does food not affect absorption for?
Amoxicillin, Pen V, and Carbenicillin
Penicillins don’t distribute well to what locations?
Brain
CSF
Prostate
What is the most common adverse effect of penicillins?
Hypersensitivity reactions
Hypersensitivity to one means probably to all
What are other major adverse effects of penicillins?
Eosinophilia
Interstitial Nephritis (Methicillin)
Pseudomembranous Colitis
What are the penicillinase resistant penicillins?
IV - Methicillin, Oxacillin, Nafcillin
PO- Cloxacillin, Dicloxacillin
What are the aminopenicillins?
Ampicillin (QID) and Amoxicillin (TID)
Amino group allows for penetration into gram negative cell wall
What is the spectrum for aminopenicillins?
Streptococcus and Enterococcus
Haemophilus
Salmonella/Shigella
Proteus, E. coli, Klebiella
What are the adverse effects of aminopenicillins?
Hypersensitvity
Diarrhea - take with food to decrease sx