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BETA-LACTAMASE INHIBITOR, BETA-LACTAMASE INHIBITOR, Obtain from…
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BETA-LACTAMASE INHIBITOR
Clavulanic acid
MOA
- Progressive inhibit B-lactamase
- Bind reversibly with B-lactamase, later covalently
- Covalent binding increase inhibition time
- 'Suicide' inhibitor - becomes inactivates after binding
- Permeates the outer layer of cell wall of Gram-ve bac, inhibits periplasmically located B-lactamase
Pharmacokinetics
- Rapid oral absorption
- Bioavailability: 60%
- Available for injection
- Half-life: 1hr
- Eliminated thru kidney; hydrolysed and decarboxylated before excretion
- Elimination not affected by probenecid
Adverse effects
- Poor GI tolerance in children
- Candida stomatitis
- Candida vaginitis
- Rashes
- Hepatic injury
Uses
- Re-establish the activity of Amoxicillin
- B-lactamase producing resistant Staph. aureus
- Peptococcus
- H. influenza
- N. gonorrhoeae
- [single dose Amoxicillin 3g + Clavulanic acid 0.5g + Probenecid 1g]
- E. coli
- Proteus
- Klebsiella
- Salmonella
- Shigella
- Bacteria fragilis
- Skin & soft tissues infections
- Intra-abdominal & gynaecological sepsis
- Urinary, Bilary, Respiratory tract infections
- Not effective for:
- MRSA - have altered PBPs
- Amoxicillin sensitive strains
Sulbactam
Indications
- Penicillinase-producing N. gonorrhea (PPNG)
- Mixed anaerobic infections
- Tooth abscess
- Intra-abdominal infections
- Gynecological infection
- Surgical infection
- Skin and Soft tissues infection
Adverse effects
- Pain at site of injection
- Thrombophlebitis of injected site
- Rash
- Diarrhea
Pharmacokinetics
- Oral absorption is inconsistent
- Complex salts with Ampicillin // Sultamicillin tosylate has better absorption
- Preferred parentaral administration
- Combined with Ampicillin
- Obtain from Streptomyces clavuligerus
- Has B-lactam ring
- No antibacterial activity
- semi-synthetic
- Highly active against Class II-IV B-lactamase
- Poor active to Class I
- Does not induce chromosomal B-lactamases
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