Beta Lactamase Inhibitors
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The document discusses beta-lactamase inhibitors such as clavulanic acid and sulbactam, which are used to combat bacterial resistance to beta-lactam antibiotics. Clavulanic acid is a 'suicide inhibitor' that irreversibly binds to beta-lactamases, improving the efficacy of amoxicillin against resistant bacterial strains, while sulbactam is less potent but can be used with ampicillin. The document outlines their pharmacokinetics, clinical uses, and potential adverse effects.
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Beta Lactamase Inhibitors
- 1. BETA- LACTAMASE INHIBITORS Anusha Shaji, B.Pharm, M.Pharm Assistant Professor Department of Pharmacology Nirmala College of Pharmacy, Muvattupuzha, Ernakulam
- 2. Contents Introduction Clavulanic acid Pharmacokinetics Clinical uses Adverse effects Sulbactam Pharmacokinetics Adverse effects
- 3. Beta- Lactamase Inhibitors Eg. Clavulanic acid, Sulbactam, Tazobactam A family of enzymes produced by many gram positive and gram negative bacteria That inactivate beta lactam antibiotics by opening the beta lactam ring Clavulanic acid Source: Obtained from Streptomyces clavuligerus It has beta lactam ring- but no antibacterial activity of its own Also called suicide inhibitor → because it gets inactivated after binding to the enzyme It permeates the outer layers of the cell wall of gram negative bacteria → inhibits the periplasmically located beta lactamase
- 4. It is a progressive inhibitor Binding with beta lactamse is reversible initially ↓ Later it becomes covalent → inhibition increases with time Pharmacokinetics Rapid oral absorption Bioavailability- 60% Elimination half life- 1 hour Elimination by glomerular filtration Tissue distribution matches amoxicillin, with which it is combined called coamoxiclav It is largely hydrolysed and decarboxylated before excretion
- 5. Uses Addition of clavulanic acid re-establishes the activity of amoxicillin against beta lactamase producing Staph. aureus, H. influenzae, E.coli, Proteus, Klebsiella and Salmonella. Coamoxiclav is indicated for; Skin and soft tissue infections Respiratory tract infections Adverse effects Candida stomatitis/vaginitis Rashes, diarrhea, vomiting etc g.i tolerance is poorer- especially in children
- 6. Sulbactam Semisynthetic beta lactamse inhibitor Progressive inhibitor On weight basis, it is 2-3 times less potent than clavulanic acid At higher concentration- same level inhibition Does not induce chromosomal beta lactamases, while clavulanic acid can induce some of them Pharmacokinetics Oral absorption of sulbactum is inconsistent. Preferably given parenterally It has been combined with ampicillin for use against beta-lactamase producing resistant strains.
- 7. Sultamicillin tosylate Complex salt of sulbactam & ampicillin Absorption is better Given orally Adverse effects Pain at site of injection Thrombophlebitis of injected vein Rash Diarrhoae