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PENICILLINS, having side chain that protect B-lactam ring Treat…

- - - - Not penicillinase resistant
        
        Not acid resistant
        
        Inactive orally
        
        Excrete rapidly in urine
        
        Half-life: 1hr
        
        Used as sodium salt - Sodium for fluid retention in CHF patients
        
        Dose: 1-2g im // 1-5g iv every 4-6 hrs
        
        High doses cause bleeding - interfere platelets function
        
        Indications: often combine with Gentamicin
        
        Serious infections: Pseudonomas, Proteus
        
        Burns
        
        Urinary tract infection
        
        Septicaemia
        
        Orodental infections
        
        Active against: P. aeruginosa, Indole+ve proteus
        
        Less active: Salmonella, E. coli, Enterobacter
        
        Not active: Klebsiella, Gram+ve cocci
    - - More potent than Carbenicillin against Pseudomonas
  - - - Anti-pseudomonal penicillin
        
        8x more active than Carbenicillin
        
        Active against: Klebsiella
        
        Used in neutropenic/immuno-compromised associated Gram-ve infections & burns
        
        Elimination/Half-life: 1hr
        
        Concurrent use with Gentamicin or Tobramycin is advised
        
        Dose: 100-150mg/kg/day TID im/iv
        
        Max. dose: 16g/day
        
        IV route is preferred when >2g to be administered
    - - Active against: Pseudonomas & Klebsiella
        
        Parenteral administration for Enterib bacilli infections
- - - - Acid-resistant alternative to PnG
        
        Differ to PnG: acid stability
        
        Better oral absorption
        
        Peak conc. reached in 1 hour
        
        Half-life: 30-60mins
        
        Activity against:
        1) Neisseria
        2) Gram-ve bacteria
        3) Anaerobes
        4) Streptococcal pharyngitis
        5) Sinusis
        6) Otitis media
        7) Minor pneumococcal infections
        8) Prophylaxis of Rheumatic fever
        
        Doses: 250-500mg; Children: 125-250mg QID
  - - - Ester of Ampicillin
        
        A prodrug
        
        Nearly complete absorption in GIT
        
        Largely hydrolysed during absorption
        
        Does not disturb intestinal ecology
        
        Higher plasma levels
        
        Better tissues penetration
        
        Dose: 400-800mg BD
    - - Close congener of Ampicillins
        
        not a prodrug
        
        Better oral absorption
        
        Food does not interfere absorption
        
        Higher and more sustained blood levels
        
        Less diarrhea incident
        
        More preferred for:
        
        Typhoid
        
        Bronchitis
        
        Urinary tract infections
        
        SABE
        
        Gonorrhea
        
        Dental infections - 250-500mg TDS 5days
        
        Dose: 0.25-1g TDS oral/im
    - - Amino substitution in the side chain
        
        some are prodrugs
        
        Not resistant to penicillinase
        
        Not resistant to other B-lactamases
        
        Active against all organisms sensitive to PnG
        
        Active against Gram-ve bacilli:
        
        H. influenza
        
        E. coli
        
        Proteus
        
        Salmonella
        
        Shigella
        
        More active than PnG to: Strep. viridans & Enterococci
        
        Equally active to: Pneumococci, Gonococci, Meningococci
        
        Less active to: Gram+ve cocci
        
        Not affected to:
        
        Penicillinase-producing Staph.
        
        Gram-ve bacilli: Pseudonomas, Kelbsiella, Indole positive Proteus
        
        Anaerobes: Bacteroides fragilis
    - - Hydrocortisone - inactivates Ampicillin
        
        Probenecid - retards renal excretion
        
        Failure of oral contraceptive
        
        Ampicillins interfere enterohepatic cycling,
        
        inhibiting colonic flora
    - - Urinary tract infections
        
        Respiratory tract infections: Bronchitis, Sinusitis, Otitis media
        
        Meningitis
        
        Non-penicillinase producing N. gonorrhoea - single dose 3.5g + 1g Probeneceid
        
        Bacillary dysentery due to Shingella
        
        Typhoid fever
        
        Cholecystitis
        
        Subacute bacterial endocarditis
        
        Septicaemias - in combination with Gentamicin or 3rd generation Cephalosporin
        
        Dental infections
    - - Diarrhea
        
        Irritates lower intestine, alter bacterial flora - incomplete absorption
        
        Rashes
        
        high incident (10%)
        
        specially to low immunity: AIDS, herpes virus infections, lymphatic leukemia
        
        may not be allergic but toxic
        
        Hypersensitivity to PnG should not be given Ampicillin
    - - 0.5-2g oral/iv/im QID - severity dependent
        
        Children: 25-50mg/kg/day
    - - Not degraded by gastric acid
        
        Oral absorption - incomplete but adequate
        
        Food interferes absorption
        
        Enterohepatic circulation occurs
        
        Elimination via kidney
        
        Half-life: 1 hour