Ceftriaxone : Therapeutic uses, Dosage & Side Effects
Ceftriaxone is the third generation cephalosporins. Penetration into CSF is good and elimination occurs equally in urine and bile. It is used for the treatment of a number of bacterial infections including middle ear infections, endocarditis, meningitis, pneumonia, bone and joint infections, intra-abdominal infections, skin infections, urinary tract infections, gonorrhea, and pelvic inflammatory disease.
Dose : 0.5-2.0 g i.m./i.v. 8 or 12 hourly
Route : IM, IV
Onset of action : ?
Plasma Half-life : 8 hours
Duration of action : ?
Bioavailability : ?
Plasma protein binding : %
Metabolism : Negligible
Pregnancy risk category : B
Chemical formula : C18H18N8O7S3
IUPAC name : (6R,7R)-7-{[(2Z)-2-(2-amino-1,3-thiazol-4-yl)->2-(methoxyimino)acetyl]amino}-3-{[(2-methyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl)thio]methyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Trade name : Rocephin, Oframax, Monotax, Monocef, Epicephin
Antibacterial spectrum : Ceftriaxone is active against both gram positive & gram negative bacteria.
Therapeutic uses : Ceftriaxone is highly efficacious in a wide range of serious infections including bacterial meningitis (especially in children), multiresistant typhoid fever, complicated urinary tract infections, abdominal sepsis and septicaemias. A single dose of 250 mg i.m. has proven curative in gonorrhoea including PPNG, and in chancroid.
Ceftriaxone is used in following dosage for various infections :
- For skin/soft tissue/urinary infections : 1-2 g i.v. or i.m./ day.
- Meningitis : 4 g followed by 2 g i.v. (children 75-100 mg/ kg) once daily for 7-10 days.
- Typhoid : 4 g i.v. daily x 2 days followed by 2 g/day (children 75 mg/kg) till 2 days after fever subsides
Directions For Use
Intravenous Administration
- Ceftriaxone should be administered intravenously by infusion over a period of 30 minutes, except in neonates where administration over 60 minutes is recommended to reduce the risk of bilirubin encephalopathy.
Mechanism of action : Cephalosporins cause inhibition of bacterial cell wall synthesis. i.e. they have the same mechanism of action as penicillin. However, they bind to different proteins than those which bind penicillins.
Side effects : Cephalosporins are generally well tolerated, but are more toxic than penicillin. Ceftriaxone may provoke following side effects :
- Hypoprothrombinaemia, bleeding
- Haemolysis (hemolytic anemia),
- Pain at the site of injection,
- Allergic reactions,
- Eosinophilia,
- C. difficile associated diarrhea,
- Gall bladder disease,
- Elevations in liver enzymes,
- Seizures.
Drug Interactions : Ceftriaxone may interact with following drugs :
- Calcium-chloride, gluceptate, gluconate
- Cholera vaccine, live
- Edetate calcium disodium
- Intravenous electrolyte solution
- Leucovorin
- Levoleucovorin calcium
- Parenteral nutrition solution w/ electrolytes
- Pentetate calcium trisodium
Contraindications :
- Contraindicated in patients who have Anaphylaxis to Cephalosporins, Penicillins, or Other Betalactam Antibacterials.
- Contraindicated in premature neonates up to a postmenstrual age of 41 weeks (gestational age + chronological age).
- It should not be used in hyperbilirubinemic neonates, particularly those who are premature because ceftriaxone is reported to displace bilirubin from albumin binding sites, potentially causing bilirubin encephalopathy.
- Concomitant use with intravenous calcium-containing solutions/products in neonates (≤28 days) is contraindicated even if administered through different infusion lines due to rare fatal cases of calcium-ceftriaxone precipitations in neonatal lungs and kidneys.
For detailed query or in case of uncertainty, Always consult your doctor or pharmacist.
