test 6 cell wall inhibitors Flashcards
Cell Wall Inhibitors: Penicillins & Cephalosporins
› β- lactam antibiotics
› Selectively interfere with the synthesis of the bacterial cell wall
– Prevent peptidoglycan cross-linking in presence of antibiotics
– Newly produced cell walls are weak and the bacteria fall apart
› Require actively proliferating microorganisms
› Bactericidal
β- lactam antibiotics Classified by
– Spectrum of activity (what they are able to target or not)
› Penicillin spectrum determined by “R group” attachment
– Resistance to β-lactamase
› An enzyme produced by bacteria that attacks the β- lactam ring
β- lactamase is a significant source of antibiotic resistance among microbes
Penicillins
- interfere with the cross-linking
- bactericidal
› Derived from Penicillium mold
› First generation penicillins are effective against gram-positive and gram-negative organisms - most widely effective and least toxic of all the antibiotics
– BUT, resistance levels are high!
- so use is becoming limited
Penicillin Categories
- Natural
- Antistaphylococcal
- Broad spectrum
- Antipseudomonal
Natural Penicillins
› Penicillin G
Penicillin G uses
- pneumococcal pneumonia
- bacterial pneumonia - gonorrhea
- syphilis
Antistaphylococcal Penicillins
› Developed in response to growing resistance to staph
› Used specifically for penicillinase-producing staphylococci (including MSSA)
› Minimal activity against gram-negative infections
Staphylococcus Aureus
› Gram-positive
› Non-pathogenic & pathogenic strains
- hospital inquired infection
- Non-pathogenic
› Skin, Nostrils, Female reproductive tract
- Pathogenic
› Pimples, Impetigo, Boils, Cellulites, Abscesses, Pneumonia, Meningitis, Endocarditis, Sepsis
Broad Spectrum Penicillins
› Spectrum similar to Penicillin G, but more effective against gram-negative bacilli
› Resistance now a major clinical problem
› Ampicillin
› Amoxicillin
– D.O.C for dental prophylaxis to prevent bacterial endocarditis
Pseudomonas aeruginosa
– Very problematic – Very pathogenic – Gram negative – Readily develops resistance to antibiotics – Notorious for causing blue/green pus
Antipseudomonal Penicillins
› Treates Pseudomonas aeruginosa › Also effective against other gram negative bacilli › Parenteral only (not effective orally) › Piperacillin (most potent) › Ticarcillin
Clavulanic Acid
› Also has a β-lactam ring but no antimicrobial activity
› Suicide inhibitor of bacterial β-lactamase
– Attaches to and permanently deactivates the enzyme by letting it attack it instead of the antibiotic
› Used in combination with
– amoxicillin (Augmentin)
– ticarcillin (Timentin)
Penicillin Pharmacokinetics
› Administration
– Varies-oral, IV, IM
› Absorption
– Incompletely absorbed after oral administration
› Reach intestines and affect intestinal flora= diarrhea!
– Food increases gastric emptying time and acids destroy drug
– Take on empty stomach
› Distribution
– Do not penetrate bone or BBB unless inflamed!
› Excretion
– Kidneys
Penicillin Adverse Reactions
› Hypersensitivity
– 5% of patients
– Range from rash to mouth swelling to anaphylaxis
– Patient history regarding severity of previous rxn is essential
– Cross-allergies occur among β-lactams
› Diarrhea
› Nephritis
› Neurotoxicity
› Hematologic toxicities
Cephalosporins
› β-lactam antibiotics › More resistant to certain β-lactamases than penicillins › Classified based on their resistance to β- lactamases and their spectrum – 1st Generation – 2nd Generation – 3rd Generation – 4th Generation – Advanced Generation -VERY COMMONLY USED IN THE CPB PRIME