Adult: 1-2 g as a single dose. Child: ≤12 years weighing <50 kg: 50 mg/kg as a single dose; >12 years weighing ≥50kg: Same as adult dose.
Parenteral Syphilis
Adult: 0.5-1 g once daily, increased to 2 g once daily for neurosyphilis for 10-14 days, given via slow IV inj over 5 minutes, or infused over at least 30 minutes, or deep IM inj. Child: <15 days 50 mg/kg daily via IV infusion over 60 minutes; 15 days to 12 years weighing <50 kg: 75-100 mg/kg daily via IV infusion over at least 30 minutes for 10-14 days. Max: 4 g once daily; >12 years weighing ≥50 kg: Same as adult dose.
Parenteral Susceptible infections
Adult: 1-2 g daily, increased to 4 g daily in severe infections, given once or in 2 divided doses via slow IV inj over 5 minutes, or infused over at least 30 minutes, or deep IM inj. Dose >2 g is given via IV inj or infusion. Child: <15 days 20-50 mg/kg once daily via IV infusion over 60 minutes; 15 days to 12 years weighing <50 kg: 50-80 mg/kg daily, may be increased to 100 mg/kg for severe infections via IV infusion over at least 30 minutes. Max: 4 g daily; >12 years weighing ≥50 kg: Same as adult dose.
Parenteral Lyme disease
Adult: 2 g once daily for 14-21 days, given via slow IV inj over 5 minutes, or infused over at least 30 minutes, or deep IM inj. Child: 15 days to 12 years weighing <50 kg: 50-80 mg/kg once daily for 14-21 days given via IV infusion over at least 30 minutes; >12 years weighing ≥50kg: Same as adult dose.
Parenteral Prophylaxis of surgical infections
Adult: 1-2 g as a single dose given 0.5-2 hours before surgery via slow IV inj over 5 minutes, or infused over at least 30 minutes, or deep IM inj. Child: <15 days 20-50 mg/kg as single pre-operative dose via IV infusion over 60 minutes; 15 days to 12 years weighing <50 kg: 50-80 mg/kg as a single pre-operative dose via IV infusion over at least 30 minutes; >12 years weighing ≥50kg: Same as adult dose.
Renal Impairment
CrCl (mL/min)
Dosage
<10
Max: 2 g daily.
Reconstitution
IM inj: Add 0.9 mL, 1.8 mL, 3.6 mL or 7.2 mL of compatible diluent to vials labelled as containing 250 mg, 500 mg, 1 g and 2 g, respectively, to provide a solution containing approx 250 mg/mL. Alternatively, add 1 mL, 2.1 mL or 4.2 mL of compatible diluent to vials labelled as containing 500 mg, 1 g and 2 g, respectively, to provide a solution containing approx 350 mg/mL. IV inj or infusion: Add 2.4 mL, 4.8 mL, 9.6 mL or 19.2 mL of compatible diluent to vials labelled as containing 250 mg, 500 mg, 1 g and 2 g, respectively, to provide a solution containing approx 100 mg/mL. Further dilute with compatible IV diluent to yield solution containing 10-40 mg/mL.
Incompatibility
Incompatible with Ca-containing solutions or preparations via Y-site (e.g. Ringer’s or Hartmann’s solution, TPN). Physically incompatible in admixtures with vancomycin, amsacrine, aminoglycosides and fluconazole.
Contraindications
Hypersensitivity to cephalosporins or history of severe hypersensitivity to other type of β-lactam antibiotic (e.g. penicillins, monobactams, carbapenems). Premature neonates up to a postmenstrual age of 41 weeks (gestational age and chronological age), full-term neonates (up to 28 days of age) with hyperbilirubinaemia, jaundice, hypoalbuminaemia, or acidosis requiring IV Ca treatment, or Ca containing infusions.
Special Precautions
Patient with history of allergy to penicillins or any drug, gastrointestinal disease (e.g. colitis), renal lithiasis; hypercalciuria, impaired vit K synthesis or low vit K stores. Severe renal and hepatic impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: Stevens-Johnson syndrome, toxic epidermal necrolysis (TEN)/Lyell’s syndrome, hypersensitivity, renal and gallbladder precipitation, pancreatitis secondary to biliary obstruction, renal lithiasis, superinfection. Blood and lymphatic system disorders: Eosinophilia, leucopenia, thrombocytopenia. Gastrointestinal disorders: Diarrhoea, oral candidiasis. General disorders and admin site conditions: Diaphoresis. Injury, poisoning and procedural complications: Pain, induration and tenderness at inj site (IM). Investigations: Increased hepatic enzymes, BUN and serum creatinine; sonographic abnormalities in the gallbladder. Nervous system disorders: Headache, dizziness. Reproductive system and breast disorders: Candidal vaginitis. Skin and subcutaneous tissue disorders: Rash. Vascular disorders: Flushing. Potentially Fatal: Severe haemolytic anaemia, Clostridium difficile-associated diarrhoea (CDAD).
This drug may cause dizziness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor prothrombin time/INR. Monitor signs and symptoms of hypersensitivity.
Overdosage
Symptoms: Diarrhoea, nausea and vomiting. Management: Symptomatic treatment.
Drug Interactions
May increase anticoagulant effect of vit K antagonists (e.g. warfarin). May increase nephrotoxicity of aminoglycosides. May diminish therapeutic effect of BCG, typhoid vaccine, Na picosulfate. Potentially Fatal: Admin with Ca-containing IV solution may cause precipitation of a crystalline material in the lungs and kidneys.
Lab Interference
May lead to false-positive results to Coomb’s test; false-positive urinary glucose test using non-enzymatic methods; false-positive galactosemia test.
Action
Description: Ceftriaxone is a 3rd generation cephalosporin antibiotic. It binds to 1 or more penicillin-binding proteins (PBPs) inhibiting the final transpeptidation step of peptidoglycan synthesis in bacterial cell wall, leading to bacterial cell lysis and death. Pharmacokinetics: Absorption: Well absorbed (IM). Time to peak plasma concentration: 2-3 hours (IM). Distribution: Widely distributed in body including gallbladder, lungs, bone, bile, CSF. Crosses the placenta and enters breast milk (low concentration). Volume of distribution: Approx 6-14 L. Plasma protein binding: Approx 85-95%. Excretion: Via urine (approx 40-65% as unchanged drug); faeces (as unchanged drug). Elimination half-life: 6-9 hours.
Chemical Structure
Ceftriaxone Source: National Center for Biotechnology Information. PubChem Database. Ceftriaxone, CID=5479530, https://pubchem.ncbi.nlm.nih.gov/compound/Ceftriaxone (accessed on Jan. 21, 2020)
J01DD63 - ceftriaxone and beta-lactamase inhibitor ; Belongs to the class of third-generation cephalosporins. Used in the systemic treatment of infections.
References
Anon. Ceftriaxone. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 05/03/2019.Anon. Ceftriaxone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/03/2019.Buckingham R (ed). Ceftriaxone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/03/2019.Ceftriaxone (Fresenius Kabi USA, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2019.Ceftriaxone for Injection and Dextrose Injection. U.S. FDA. https://www.fda.gov/. Accessed 10/11/2014.Ceftriaxone Sodium Injection, Powder for Solution (Baxter Healthcare Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 10/11/2014.Joint Formulary Committee. Ceftriaxone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/11/2014.
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