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Beta-lactam Antibiot

Drugs and their effects

QuestionAnswer
What is the function of beta-lactam antibiotics? Cell wall synthesis inhibition
What are the 4 groups of beta-lactam antibiotics? Penicillins, Cephalosporins, Monobactams, Carbapenam
What is the mechanism of action for Penicillin? Inhibit transpeptidase (PBPs*) required for cross linkages between peptidoglycans. Activate autolysins Thus, antibacterial effect of Penicillin is the result of both- inhibition of cell wall synthesis & destruction of existing cell wall by autolysins.
What are some natural Penicillins? Na Penicillin G / Benzyl penicillin, Potassium Penicillin G (oral), Repository penicillin G
ANTIBACTERIAL SPECTRUM: (PENICILLIN G/ BENZYL PENICILLIN) Gram positive infections Restricted currently due to resistance Most Beta-hemolytic Streptococcus aureus resistant Useful in treating Syphilis
SEMI-SYNTHETIC PENCILLINS ↑oral efficacy ↓ Lactamase (penicillinase) sensitivity Broaden the spectrum of activity
Acid resistant semi-synthetic Penicillins Penicillin V Clocacillin Ampicillin, Amoxycillin
Penicillinases resistant ( anti-staphylococcal) semi-synthetic Penicillin Methicillin Cloxacillin
Extended spectrum semi-synthetic Penecillin Ampicillin, Amoxycillin Anti-psuedomonas:Piperacillin Carbenicillin
What is Penicillin V used for? Oral infections due to Streptococcus Trench mouth (Ulcerative Gingivitis)
AMINOPENICILLINS ( Amoicillin and amoxycillin) Acid stable Penicillinase sensitive Used with β- Lactamase inhibitors (e.g. Clavulanic acid)
Amoxicillin Therapeutically:Most used antibiotic Prophylactically: Endocardial defects & Artificial valve pts. prevent infective endocarditis, Diabetics, Surgical procedures Principles of prophylactic use: Use appropriatedose, Use for appropriate duration
Amoxycillin vs Ampicillin Amoxicillin is more rapidly and completely absorbed and food does not interfere with absorption where Ampicillin is the opposite. Less diarrhea, superinfection and skin rashes with Amoxicillin.
Amoxycillin vs Ampicillin bacterial effectivness. Amoxycillin is more effective for S. typhi , H. pylori. Ampicillin is more effective for Shigella, H.influenzae
Adverse effect of Penicillin (hypersensitivity reaction) Rash, Bronchospasm , Vasculitis, Serum sickness Stevens-Johnson syndrome Angioedema and anaphylaxis
Adverse effect of Penicillin (Local irritancy) IM: Pain, I.V.: Thrombophlebitis Oral: nausea, Diarrhea
Adverse effect of Penicillin (Superinfection) Bowel, Resp. and Skin infections
Adverse effect of Penicillin (Neuro-toxicity) Confusion Seizures
Adverse effect of Penicillin (Hematologic toxicity) Bleeding : Pen. G, Carbenicillin
Beta Lactamase inhibitors Inhibit beta lactamase enzyme->No inactivation of Penicillins->Broaden spectrum of antibiotic
Beta Lactamase inhibitors examples Clavulanic acid, sulbactam. Clavulanic acid + amoxycillin is frequently used. Most effective against: Staphylococci H. influenzae
Cephalosporins Contain beta lactam ring Classified into four generation according to order of invention
Cephalosporins classification First: Cephalexin, Cefazolin Second: Cefaclor, Cefuroxime Third: Cefixime, Ceftriaxone Fourth: Cefipime
Cephalosporins mechanism of action Bactericidal for sensitive strains. Inhibition of cell wall synthesis: Like Penicilins. Inhibit PBP: different than those binding penicillins.
Cephalosporins adverse reaction (Hypersensitivity) Skin rashes, anaphylactic shock Cross reactivity with anaphylaxis to penicillin
Cephalosporins adverse reaction (Bleeding) ↓Platelets Treatment : Vit. K
Cephalosporins adverse reaction (Nephrotoxicity) When used along with aminoglycosides
Created by: David wiid
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