Broad Spectrum Penicillin Properties of ampicillin: Exists in the form of a zwitterion; polar protein binding in serum is low (20%) Active against G - ve bacteria β- Lactam antibiotic should reach the inner part of cell wall to kill the bacteria Acid stable: orally active It is not absorbead orally as a drug, rather it is absorbed as an amino acid -Preference in absorption is for phenylalanine followed by ampicillin
Broad Spectrum Penicillin Antimicrbial Spectrum & Indications: 1-Effective against same organisms as pen G 2-Gram – ve: Haemophilus influenzea E.Coli - Salmonella typhi - Proteus mirabilis - Helicobacter pylori - -Adverse ettects : 1- Diarrhea 2- Pseudomembraneous Colitis 3- Ampicillin Rash ” 4- Effect on the efficacy of birth control pills
Broad Spectrum Penicillin Bacampicillin is inactive as such and by the action of blood esterases, can be cenverted back to ampicillin Cyclacillin doesn ’ t cause “ ampicillin Rash ” WHY? A moxicillin is absorbed orally through the same active transport system that normally absorbs the amino acid tyrosine The transport system cannot differentiate between them It has a longer t 1/2. WHY?
Broad Spectrum Penicillin Amoxicillin+ clavulanic acid “ augmentin ® ” CA is considered a suicide enzyme inhibitor Amoxicillin and CA have the same pharmacokinetic properties Ampicillin + sulbactam “ unasyn ® ” Sulbactam posses a weak antibacterial activity of its own It inhibits irreversibly the β- lactamase enzyme Daily dosage should not exceed 4g of sulbactam