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Beta-lactam Antibiot
Drugs and their effects
| Question | Answer |
|---|---|
| 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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