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: 3rd 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. Pharmacokinetic 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: 51/2 – 11 hours in adults with normal renal
function.

7. Time Action Profile
• Onset: IV- Immediate
IM-Unknown
• Peak: IV- Immediate
IM- 11/2 – 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/1.73m2 (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

13. THANK YOU