Drug profile on Ceftriaxone

1. DRUG PROFILE ON CEFTRIAXONE
P. RAMI REDDY MEMORIAL COLLEGE OF
PHARMACY
Presented by:
Navya Teja. O
Pharm.D 4th year

2.  Drug name: Ceftriaxone
 Brand name : Rocephin , unecef , ceftrix
 Molecular formula : C18H18N8O7S3
 Molecular weight: 576
 ATC code: j01DD04v
 Pharmacological classification: Third-generation cephalosporins
 Therapeutic classification: Antibiotics
 Pregnacy risk category : c
 Available form: Available by prescription only
- Injection = 250mg,500mg, 1g,2g,10g (bulk)
- Package infusion = 1g, 2g

3.  INDICATIONS AND DOSAGES :
 Bacteremia, septicemia, and serious respiratory, bone, joint, urinary,
gynaecologic, intra-abdominal, and skin infection from susceptible organisms
-Adults and children ages 12 and older: 1 - 2g I.M or I.V . Once daily
- should not exceed 4g
-Children under age12: 50-75 mg /kg I.M or I.V once daily
- Maximum dose: 2g
 Gonococcal meningitis , endocarditis
-adults: 1- 2g I.V q 12 hours for 10 to 14 days for meningitis
1-2g I.V q 12 hours for 3 to 4 weeks for endocarditis
-children: 50 -100 mg I.M or I.V daily or divided q 12 hours,
- 7 to 14 days for Meningitis
- 28 days for Endocarditis
 Haemophilus ducreyi infection
-Adults: 250 mg I.M as a single dose

4.  Sexually transmitted epididymitis, pelvic inflammation disease
-adults : 250 mg I.M as a single dose , follow up with other antibiotics
 Anti-infective for sexual assault victims
-adults : 125 mg I.M as a single dose in conjunction with other antibiotics
 Lyme disease
-adults: 1 or 2 g I.M or I.V q 12 hourly
 Persisting or relapsing otitis media in children
-children ages 3 months and older : 50 mg /kg I.M – O.D for 3 days
 INTRAVENOUS ADMINISTRATION :
 reconstitute the drug with sterile water or saline water or D5W or D10w or a
combination of normal saline solution and dextrose injection and other compatible
solutions for injection
 Reconstitute by adding
-2.4 ml of diluent to the 250 mg vial
- 4.8 ml to the 500 mg via
- 9.6 ml to the 1 g vial

5. -19.2 ml to the 2g vials
 All reconstituted solutions yield a concentration that averages 100 mg /ml .after
reconstitution , dilute further for intermittent infusion to desired concentration
 Infuse over 15 to 30 minutes
 MECHANISM OF ACTION :
• Ceftriaxone is more active against some beta-lactamase producing gram negative
organisms
• ceftriaxone is Primarily bactericidal , it may be bacteriostatic , activity depends on
organisms , tissue penetration and drug dosage .
• Ceftriaxone inhibit the transpeptidation process Leads to formation of imperfect
cell wall Synthesis result in osmotic drive from the outside isotonic environment of the
host cell to the inside of hypertonic bacterial cytoplasm and finally activation of the
autolysis enzymes leading to the lysis of bacteria

8.  PHARMACOKINETICS :
 Absorption: Not absorbed from the gastrointestinal tract and must be
given parenterally
 Distribution: Distributed widely into most body tissue and fluids
Including the – gall bladder, Liver, kidney, bone, sputum,
bile, pleural & synovial fluids
Ceftriaxone has good CSF penetration.
Ceftriaxone crosses the placenta
Protein binding is dose dependent
 Metabolism: partially metabolized
 Excretion: Excreted principally in urine
-Some drugs are excreted in bile by the biliary mechanism
-Small amount of drug appear in breast milk

9. Elimination half-life is 6 to 11 hours in adults with normal renal function, severe renal
disease prolongs half-life only moderately, and neither hemodialysis nor peritoneal
dialysis will remove Ceftriaxone
 CONTRAINDICATIOND AND PRECAUTIONS :
- Contraindicated in patients hypersensitivity to Ceftriaxone or other cephalosporins
- Use cautiously in breastfeeding women & in patients with penicillin allergy
 INTERACTIONS :
Drug-drug :
1. Probenecid – may increase clearance by blocking biliary secretion and displacement of
Ceftriaxone from plasma proteins, avoid use together
2. Quinolones – Invitro synergism against pneumonia
Route Onset Peak Duration
I.V Immediate Immediate Unknown
I.M Unknown 2 to hours Unknown

10.  ADVERSE REACTIONS
 CNS: headache, dizziness
 GI: pseudomembranous colitis, nausea, vomiting. Diarrhoea, urolithiasis
 GU: Genital purities, candidiasis, elevated BUN levels
 HEMATOLOGICAL: Eosinophilia. Thrombocytopenia, leukopenia
 HEPATIC: Elevated liver function test results jaundice
 SKIN: pain, induration tenderness [at junction site]. Phlebitis, rash, purities,
 OTHER: Hypersensitivity reactions, serum sickness, anaphylaxis, elevated
temperature, chills.
 OVERDOSE AND TREATMENT:
 Signs and symptoms of overdose include neuromuscular hypersensitivity
 Seizures may follow high CNS levels
 Treatment is supportive

11.  CLINICAL CONSIDERATIONS :
 Alert names of some cephalosporin's are similar, use caution when dispensing
 For patients on sodium restriction – note that Ceftriaxone injection contains 3.6
mEq of sodium um per gram of the drug
 Dosage adjustment usually isn’t needed in patients with renal insufficiency
because of partial biliary excretion
 Ceftriaxone causes false-positive results in urine glucose tests using cupric
sulfate use glucose oxide instead
 Ceftriaxone also causes false- elevations in urine creatinine levels in tests their
jaffe reaction
 Ceftriaxone may cause positive to coomb’s test results
 THERAPEUTIC MONITORING :
While patients are on large doses or prolonged therapy, advise clinicians to
monitor high risk patients for superinfection

12.  SPECIAL POPULATIONS :
 Breast-feeding patients: drugs appear in breast milk, use with caution in breast-
feeding women
 Pediatric patients: Ceftriaxone may be used in neonates and children
Use cautiously in hyper bilirubinaemia neonates because of the ability of the drug
to displace bilirubin
 PATIENT COUNSELLING :
 Inform the patient of potential adverse reactions
 Tell patients to report discomfort in the I.V site
 REFERENCE :
 American Hospital Formulary Services.
 HL Sharma – principles of pharmacology, third edition

13. Thank You