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PENICILLIN by Mind Map: PENICILLIN

1. -It is similar to ampicillin except, •Oral absorption is better, food does not interefere •Incidence of diarrhea decreased.

2. 1) PENICILLIN G (benzyl penicillin)

2.1. Pharmacokinetics

2.2. Adverse effects

2.3. Uses

3. Mechanism of action

3.1. Drug impermeable

4. In Gram -ve, Porin channels •lost •altered

5. Penicillin binding protein (PBP) | PnG + PBP = inhibition of transpeptidation | Production of Cell Wall Deficient forms (CWD) | Swelling and bursting (hyperosmotic pressure) | Bactericidal effect

6. Cocci 1) Highly sensitive - Pneumococci 2) Resistant - Staphylococcus aureus

7. Antibacterial spectrum

8. 3. Sulbactam Semi synthetic 2-3 times less potent than clavulanic acid Progressive inhibitor Combination - Ampicillin

8.1. Uses : Skin and soft tissue infections Urinary, biliary and respiratory tract infections Gonorrhea

8.2. Adverse effects : Thrombophlebitis, rash, diarrhea

9. 1) Acid labile 2) CSF penetration - low 3) I. M. site - Sod. PnG absorption is rapid and complete 4) t1/2 : Healthy adults- 30 mins Neonates- longer 5) Rapid excretion •Glomerular filtration (10%) •Tubular secretion= Slow, blocked by Probenecid

10. Antibacterial spectrum: Active against - S. aureus, E. coli, H. influenzae

11. 1) Streptococcal infections 2) Pneumococcal infections 3) Meningococcal infections 4) Gonorrhea 5) Syphilis, tetanus, gas gangrene, trench mouth (ulceration) 6) Diphtheria 7) Actinomycosis 8) Prophylactic use: Agranulocytosis, rheumatic fever, bactericidal endocarditis

11.1. Bacilli (gram +ve) 1) Highly sensitive - B. anthrasis, Clostridia, Cornybacterium diphtheria 2) Resistant - Bacteroides fragilis

12. Mechanism of resistance

12.1. Drug destroying

12.1.1. Production of penicillinase Gram +ve = more Gram -ve = comparatively less

12.2. Drug tolerant

12.2.1. PBP and transpeptidase enzyme | Low affinity towards PnG

13. 1) Local irritancy and direct toxicity • Pain (i.m) , nausea •Thrombophlebitis •Toxicity to brain : mental confusion, muscular twitching, convulsion 2) Hypersensitivity (major problem) •Frequent : rash, itching, urticaria, fever •Less common : wheezing, serum sickness, angioneurotic edema •More common : parenteral administration •Most allergic : Procaine penicillin

14. Adverse effects : GI tolerance is poor Rashes, hepatic injury rare

15. Examples: 1) METHICILLIN- -It is not acid resistant. -Resistant - Staphylococcus aureus -Altered PBP's , do not bind to penicillins. -A/E: Haematuria, Albuminuria

16. B-Lactamase Inhibitors Eg. 1. Clavulanic acid 2. Coamoxiclav 3. Sulbactam 4. Tazobactam

16.1. 1. Clavulanic Acid

16.2. MOA : •Progessive inhibitor - Binding with B- lactamase is reversible than covalent. •Suicidal inhibitor - After binding to enzyme gets inactivated. •Inhibits B-Lactamase by permeating the cell wall.

16.3. 8 times more active against pseudomonas than carbenicillin. Uses- Immunocomprised and neutropenic patients.

16.3.1. P'kinetics: -BA- 60% -t1/2- 1 hr - elimination by glomerular filtration.

16.4. 2. Coamoxiclav Amoxicillin + Clavulanic acid

16.5. 4. Tazobactam Combination - Piperacillin

16.5.1. P'kinetics : Oral absorption inconsistent Given parenterally

16.5.2. Uses : Severe infections - peritonitis, pelvic / urinary / respiratory infections

17. Semi synthetic 1) Procaine penicillin 2) Benzathine penicillin

17.1. A) Acid-resistant alternative to PnG Eg. Phenoxymethyl penicillin (PnV)

17.1.1. •Side chain in structure will protect B- lactam ring. •Penicillinase producing Bacteria- very effective •Non penicillinase producing Bacteria- less effective

17.2. B) Penicillinase Resistant Eg. Methicillin & Cloxacillin

17.2.1. 2) CLOXACILLIN- -It is acid resistant -Resistant : less active against PnG sensitive organism -More active than methicillin

17.3. C) Extended Spectrum Eg.1) Aminopenicillin 2) Carboxypenicillin 3) Ureidopenicillin

17.3.1. 1. Ampicillin •Antibacterial spectrum : -Less active against gram +ve -More active against Streptococcus viridans.

17.3.1.1. P'kinetics: Incomplete oral absorption. t1/2: 1hr

17.3.1.2. Uses: •Cholesystitis ( painful inflammation of gallbladder's wall) •Typhoid fever: rarely used •Bacillary Dysentary

17.3.1.3. A/E: Diarrhea , Rashes

17.3.1.3.1. •Acid stable & better oral absorption. •More active against Gram -ve bacteria. •Antibacterial Spectrum- similar to PnG

17.3.1.4. 2.Amoxicillin

17.3.2. 1) AMINOPENICILLINS Eg. Ampicillin Amoxicillin

17.3.2.1. Uses: Bronchitis UTI Gonorrhea

17.3.3. 2) CARBOXYPENICILLINS Eg. Carbenicillin

17.3.3.1. P'kinetics - -Neither penicillinase nor acid resistant

17.3.3.2. Adverse effects : •C/I patients with renal & cardiac problem. •High doses- bleeding by interfering with platelet function

17.3.3.3. Uses : -UTI -Burns

17.4. 3) UREIDOPENICILLIN Eg. Piperacillin

17.4.1. Antibaterial Spectrum: • Susceptible : Proteus • Less susceptible :E.coli • Resistant :Gram +ve cocci

18. Naturally occurring