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Penicillins PowerPoint Presentation

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Description : Penicillins:-antibiotics

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Published on : Sep 10, 2021 | Views : 2449 | Downloads : 1

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Slide 1-

Penicillins:- History:- Chemistry:- A = Thiazolidine ring B = β – lactam ring R = Side chain A+B= 6-aminopenicillanic acid nucleus 1
Slide 2-

Classification of Penicillins:- (a). Natural:- Benzyl penicillin (Pen – G) ---- Phenoxymethyl penicillin (Pen-V) – Procaine Penicillin ---- Benzathine Penicillin ---- 2
Slide 3-

(b). Semi synth Penicillins:- (i). Penicillinase resistant penicillins (resistant to staphylococcal B-lactamases):- (Anti-staphylococcal penicillins) Methicillin ----- Isoxazolyl Penicillins ---- Oxacillin Cloxacillin Dicloxacillin Flucloxacillin Nafcillin ---- 3
Slide 4-

(ii). Extended spectrum Penicillins:- Amino – Penicillins:- ---- Ampicillin Amoxicillin Esters of ampicillin (iii). Antipseudomonal Penicillins:- Carboxy Pen:- Carbenecillin ----- Ticarcillin ----- Carfecillin ------ Ureido – Penicillins: ------ Azlocillin Mezlocillin Piperacillin 4
Slide 5-

Mechanism of action of Penicillins:- Inhibit bacterial cell wall synthesis by inhibiting trasnpeptidation process through interfering the penicillin binding protein (PBP an enzyme), Halting peptidoglycan synthesis and the cell dies. 5
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Slide 7-

Resistance to Penicillins:- Production of Beta – lacatamases (Many 100 types) Reduced permeability of drug Modification of penicillin binding proteins. (PBP) Efflux pump 7
Slide 8-

Anti – bacterial spectrum of Penicillins:- (i). Pen. G & Pen. V:- G +ve bacteria (Cocci & Bacilli) except BLP staph aureus. G –ve Cocci (Neisseria species) NBLP G –ve anaerobes (Except B. fragilis). Spirochetes Not active against G –ve rods & enteric organisms. 8
Slide 9-

(ii). BLM resistant penicillins:- (Anti-staphylococcal Pen):- Resistant to Staph Beta – Lactamases Highly active against BLP staph. aureus Much less active against other G +ve bact Not active → Enterococci, Anaerobes & G –ve Cocci & rods 9
Slide 10-

Extended spectrum penicillins:- (i). Aminopenicillins:- G +ve organisms More activity against group – D streptococci Haemophilus sp. Listeria G –ve enteric org → E. Coli, proteus, salmonella & shigella Amoxicillin + clavulanic acid → BLP enteric org. 10
Slide 11-

(ii). Anti- pesudomonal penicillins:- Pseudomonas, Enterobacter & other G –ve m.o Less active for G +ve org. (iii). Reserved spectrum penicillins:- G –ve organisms 11
Slide 12-

b- Lactamase inhibitors:- Clavulanic acid Sulbactam Trazobactam 12
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Amoxycillin Plus Clavulanic Acid:- Spectrum:- Most active against plasmid encoded Beta - latamases produced by otherwise sensitive m.o. Staph aureus H– influenzae N. Gonorrhoe E – coli Salmonella Shigella Kl. Pneumonae 13
Slide 14-

Pharmacokinetics of Penicillins:- (a). Absorption:- Oral adm Parentral adm: 14
Slide 15-

(b). Distribution:- Plasma protein binding: 20 % → Ampicillin & Amoxicillin More than 90 % → Nafcillin & Isoxazolyl penicillins Being polar comp Poor penetration into BBB, Eye & Prostate More penetration of BBB in inflam Well distrib → body fluids & spaces t ½ = 15 min – 1.3 hrs → ↑10 -- 20 hrs → in anuric pts. 15
Slide 16-

Metabolism & Exc:- No significant metabolism Exc – kidney ---- 90 % tub. Sec & 10 % Gl. Fil Renal Clearance less efficient in Newborn Primarily Hepatic (Bile) → Nafcillin Both Renal & Hepatic → Oxa , Cloxa & Dicloxacillin Milk & Sputum 3 – 15 % Renal exc → ↓↓ by probenicid 16