Ceftriaxone drug profile, drug club ppt

drug profile of ceftriaxone

1. DRUG CLUB DRUG PROFILE CEFTRIAXONE BY ELDHOSE BENNY III PHARM D 13Q2711

2. CEFTRIAXONE Name of the Drug: Ceftriaxone Category of the Drug: 3 rd Generation Cephalosporin Brand Name & Manufacturer: Oframax, Monocef, Monotax , Rosephin Available formulations with strength : Injectable: 0.25, 0.5, 1.0g per vials Infusion: 1g , 2g Powders : 250mg, 500mg, 1gm, 2gm, 10gm

3. Indications Bacteraemia Septicaemia Serious respiratory tract infections Gonococcal meningitis Bone Joint urinary tract Gynaecologic Intra-abdominal Skin infections caused by susceptible organisms

4. Mechanism Of Action Third generation cephalosporin with broad spectrum gram –ve activity has lower efficacy against gram positive organisms but higher efficacy against resistant organisms; highly stable in presence of B-lactamases (penicillinase and cephalosporinase) of gram –ve and gram +ve bacteria. Bactericidal activity results from inhibiting cell wall synthesis by binding to 1 or more penicillin binding proteins; exerts antimicrobial effect by interfering with synthesis of peptidoglycan (major structural component of bacterial cell wall ); bacteria eventually lyse because activity of cell wall autolytic enzymes continues while cell wall assembly is arrested.

5. P harmacokinetic Parameters Absorption: Well absorbed, administered IV & IM Distribution: distributed widely into most body tissues and fluids, including the gall bladder, liver, kidneys, bone, sputum, bile, pleural and synovial fluids; unlike most other cephalosporins, ceftriaxone has got good CSF penetration. It crosses placental barrier. Protein binding is dose dependent and decreases as serum levels rise, average is 84% to 96%.

6. Metabolism: Partially metabolized (in liver) Excretion: Excreted principally in urine; some drug is excreted in bile by biliary mechanisms and small amount appear in breast milk. Severe renal disease prolongs half life only moderately. Neither haemodialysis nor peritoneal dialysis will remove ceftriaxone. Half Life: 5 1/2 – 11 hours in adults with normal renal function.

7. Time Action Profile Onset: IV- Immediate IM-Unknown Peak: IV- Immediate IM- 1 1/2 – 4 hr. Duration: IV/IM- Unknown

8. Pharmacodynamic Parameters Dose: Adults and children aged 12 and older: 1 or 2g IM or IV once daily or in equally divided doses b.i.d . total daily dose shouldn’t exceed 4g. Children younger than age 12: total daily dose is 50 to 75 mg/kg IM/IV given in divided doses q 12 hours. Maximum daily dose is 2g.

9. ADRs: GI: pseudomembranous colitis, diarrhoea Hematologic: eosinophilia, thrombocytosis, leukopenia Skin: Pain, induration, and tenderness at injection site, rash Other: Hypersensitivity reactions (serum sickness, anaphylaxis)

10. Drug Interaction Aminoglycosides: Produces synergistic antimicrobial activity against Pseudomonas aeruginosa and some strains of Enterobacteriaceae. Monitor patient closely Probenecid: May increase clearance by blocking biliary secretion and displacement of ceftriaxone from plasma proteins. Avoid use together. Quinolones: Produce in vitro synergism against Streptococcus pneumonia. Clinical relevance unknown.

11. Contraindication Hypersensitivity to ceftriaxone or other cephalosporins. Use cautiously in breast feeding women and in patients with penicillin allergy.

12. Renal Impairment: reduce dose if eGFR less than 10ml/min/1.73m 2 (max 2gm daily ) Hepatic Impairment: reduce dose and monitor plasma if hepatic impairment is present. Pregnancy – Category B, use cautiously Lactation – Drug is found in milk, avoid using Paediatrics – may use in neonates and children, use cautiously in hyperbilirubinemic neonates because of ability of drug to replace bilirubin

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