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Pencillins (beta lactam antimicrobials) - Coggle Diagram
Pencillins (beta lactam antimicrobials)
Mechanism of Action
Bactericidal
4-member core beta-lactam ring + 5-member side ring
binds to transpeptidatse (PBP) and prevent cross-link formation ---> inhibits cell wall synthesis ---> cell death
Examples
Natural Penicillins
Pencillin G
ADME
IV/IM
Pencillin V
ADME
Oral
Beta-lactamase resistant Penicillins
Flucloxacillin
ADME
Oral/IV
Methicillin
Cloxacillin
Nafcillin
Aminopenicillins
Ampicillin
Amoxicillin
ADME
Oral
Carboxypenicillins
Temocillin
Ticarcillin
Ureidopenicillins
Piperacillin
AMDE
IV
Penicillin + beta-lactamase inhibitor combinations
Amoxicillin/Clavulanate
Piperacillin/Tazobactam
Ampicillin/Sulbactam
Ticarcillin/Clavulanate
Side Effects
GI
Nausea
Vomiting
Diarrhea
C. difficile
infection
Skin
Rash
Phlebitis
Try to give a in a larger vein
Haematological
Neutropenia (low WBCs)
Platelet dysfunction
CNS
Seizures
Encephalopathy
Nephrotoxicity
Acute interstitial nephritis
Hepatic
Hepatitis
May get abnormal LFTs
Choleostasis
Usually see with Flucloxacillin and Co-Amoxiclav
Hypokalemia
Hypersensitivity type 1 and 4 reactions
Activity/Use
PencillinV/G
(narrow spectrum)
Streptococci
Pharyngitis
Skin/soft tissue infections
Pneumonia
Bone/joint infections
Endocarditis
Neisseria meningitidis
Meningococcal Meningitis
Treponema pallidum
Syphilis
Clostridia
Diphtheria
Flucloxacillin
Staph. aureus
Skin/soft tissue infections
Bone/joint infections
Endocarditis
Amoxicillin
(broader spectrum than Penicillin V/G)
Streptococci
Enterococci
UTI
Endocarditis
E. coli
UTI
Intra-abdominal infections
Listeria
Co-amoxiclav
(broad spectrum)
Gram - bacilli
Streptococci
Pneumonia
Enterococci
Intra-abdominal infections
Staph. aureus
Anaerobes
Anaerobic infections
Piptazobactam
(broad spectrum)
Gram - bacilli
Hospital-acquired pneumonia
Pseudomonas aeruginosa
Neutropenic sepsis
Streptococci
Enterococci
Intra-abdominal infections
Staph. aureus
Anaerobes
Anaerobic infections
Not so much used for community-acquired infections
ADME
Administration
Time-dependent action
Given multiple times a day
Excretion/Metabolism
Renal excretion: tubular secretion >> glomerular filtration
Probenecid inhibits tubular secretion
Dose reduction required in renal impairment
Nafcillin 80% hepatic metabolism
Distribution
Most tissues/fluids
Crosses placenta
Crosses (inflamed) BBB
Absorption
Reduced with food and pH
Amoxicillin > Penicillin V