Ceftriaxone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular, Intravenous
Syphilis
Adult: Usual dose: 0.5-1 g once daily, increased to 2 g once daily for neurosyphilis for 10-14 days. Doses are given via slow IV inj over 5 minutes, IV infusion over at least 30 minutes, or deep IM inj. For IM doses, not more than 1 g must be administered at one site. Consideration must be given to local treatment guidelines.
Child: <15 days 50 mg/kg daily via IV infusion over 60 minutes or deep IM inj for 10-14 days; 15 days to 12 years weighing <50 kg: 75-100 mg/kg once daily via IV infusion over at least 30 minutes or deep IM inj for 10-14 days. Max: 4 g once daily; >12 years weighing ≥50 kg: Same as adult dose. Doses >2 g must be given via IV. For IM doses, not more than 1 g must be administered at one site. Consideration must be given to local treatment guidelines.

Intramuscular, Intravenous
Lyme disease
Adult: For early (stage II) and late (stage III) stage cases: 2 g once daily for 14-21 days. Doses are given via slow IV inj over 5 minutes, IV infusion over at least 30 minutes, or deep IM inj. For IM doses, not more than 1 g must be administered at one site. Treatment duration may vary based on the course of the disease. Consideration must be given to local treatment guidelines.
Child: 15 days to 12 years weighing <50 kg: 50-80 mg/kg once daily via IV infusion over at least 30 minutes or deep IM inj for 14-21 days; >12 years weighing ≥50kg: Same as adult dose. Doses >2 g must be given via IV. For IM doses, not more than 1 g must be administered at one site. Treatment duration may vary based on the course of the disease. Consideration must be given to local treatment guidelines.

Intramuscular, Intravenous
Bacterial meningitis
Adult: Usual dose: 2-4 g once daily or in 2 divided doses via slow IV inj over 5 minutes, IV infusion over at least 30 minutes, or deep IM inj. Doses >2 g must be given via IV inj or infusion. For IM doses, not more than 1 g must be administered at one site. Treatment duration may vary based on the course of the disease. Consideration must be given to local treatment guidelines.
Child: <15 days 50 mg/kg once daily or in 2 divided doses via IV infusion over 60 minutes or deep IM inj; 15 days to 12 years weighing <50 kg: 80-100 mg/kg once daily or in 2 divided doses via IV infusion over at least 30 minutes or deep IM inj, up to Max of 4 g daily; >12 years weighing ≥50 kg: Same as adult dose. Doses >2 g must be given via IV. For IM doses, not more than 1 g must be administered at one site. Treatment duration may vary based on the course of the disease. Consideration must be given to local treatment guidelines.

Intramuscular, Intravenous
Bone and joint infections, Community-acquired pneumonia, Intra-abdominal infections, Lower respiratory tract infections, Septicaemia, Skin and soft tissue infections, Urinary tract infections
Adult: Usual dose: 1-2 g daily, increased to 4 g daily in severe infections, to be given once daily or in 2 divided doses via slow IV inj over 5 minutes, IV infusion over at least 30 minutes, or deep IM inj. Doses >2 g must be given via IV inj or infusion. For IM doses, not more than 1 g must be administered at one site. Treatment duration may vary based on the course of the disease. Consideration must be given to local treatment guidelines.
Child: <15 days 20-50 mg/kg once daily via IV infusion over 60 minutes or deep IM inj. Max: 50 mg/kg daily; 15 days to 12 years weighing <50 kg: 50-80 mg/kg once daily or in 2 divided doses via IV infusion over at least 30 minutes or deep IM inj, may be increased to 100 mg/kg daily in severe infections up to Max of 4 g daily; >12 years weighing ≥50 kg: Same as adult dose. Doses >2 g must be given via IV. For IM doses, not more than 1 g must be administered at one site. Treatment duration may vary based on the course of the disease. Consideration must be given to local treatment guidelines.

Intramuscular, Intravenous
Prophylaxis of surgical infections
Adult: 1-2 g as a single dose given 30 minutes to 2 hours before surgery via slow IV inj over 5 minutes, IV infusion over at least 30 minutes, or deep IM inj. For IM doses, not more than 1 g must be administered at one site. Consideration must be given to local treatment guidelines.
Child: <15 days 20-50 mg/kg as single pre-operative dose via IV infusion over 60 minutes or deep IM inj; 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 or deep IM inj; >12 years weighing ≥50kg: Same as adult dose. Doses to be given 30-90 minutes before surgery. Doses >2 g must be given via IV. For IM doses, not more than 1 g must be administered at one site. Consideration must be given to local treatment guidelines.

Intramuscular
Acute otitis media
Adult: 1-2 g as a single dose. Consideration must be given to local treatment guidelines.
Child: ≤12 years weighing <50 kg: 50 mg/kg as a single dose; >12 years weighing ≥50kg: Same as adult dose.

Intramuscular
Uncomplicated gonorrhoea
Adult: In patients with penicillinase-producing and non-penicillinase-producing Neisseria gonorrhoeae strains: 0.25-0.5 g as a single dose. Consideration must be given to local treatment guidelines.
Suy thận
CrCl (mL/min) Dosage
<10 Max: 2 g daily.
Hướng dẫn pha thuốc
IM inj: Reconstitute a vial labelled as containing 250 mg or 500 mg with 2 mL and a 1 g vial with 3.5 mL of 1% lidocaine hydrochloride solution. IV inj: Reconstitute a vial labelled as containing 250 mg or 500 mg with 5 mL and a 1 g vial with 10 mL sterile water for inj. IV infusion: Reconstitute with the appropriate volume of compatible IV diluents (e.g. sterile water for inj, 0.9% NaCl inj, dextrose 5% inj, dextrose 10% inj). Further dilute the reconstituted solution with compatible IV fluids to prepare the desired concentration. Do not use Ca-containing diluents (e.g. Ringer's solution, Hartmann's solution). Recommendations for reconstitution may vary among individual products or between countries (refer to specific product guidelines).
Tương kỵ
Incompatible with Ca-containing solutions or preparations via Y-site (e.g. Ringer's or Hartmann's solution, TPN) due to the formation of ceftriaxone-Ca precipitates. Incompatible with vancomycin, amsacrine, aminoglycosides, labetalol, and fluconazole.
Chống chỉ định
Hypersensitivity to ceftriaxone, other cephalosporins, or history of severe hypersensitivity reaction to any 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, and if they require IV Ca treatment or Ca-containing infusions. IV administration of ceftriaxone solutions containing lidocaine.
Thận trọng
Patient with history of non-severe hypersensitivity to other β-lactam agents, history of gastrointestinal disease (particularly colitis) or renal lithiasis; hypercalciuria, impaired vitamin K synthesis or low vitamin K stores (e.g. malnutrition, chronic hepatic disease); risk factors for biliary stasis and sludge (e.g. preceding major therapy, severe illness and TPN). Severe renal and hepatic impairment. Neonates and children. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Biliary lithiasis, gallbladder sludge, pseudolithiasis, pancreatitis (possibly secondary to biliary obstruction), renal lithiasis (reversible), urolithiasis, acute renal failure; Jarisch-Herxheimer reaction, encephalopathy, kernicterus in neonates; fungal or bacterial superinfection (prolonged use). Rarely, increased INR (particularly during prolonged use, or in patients with nutritional deficiency, renal and hepatic impairment).
Blood and lymphatic system disorders: Eosinophilia, leucopenia, thrombocytopenia, granulocytopenia, neutropenia, anaemia, coagulopathy.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, loose stools, dysgeusia.
General disorders and administration site conditions: Inj site pain or tenderness (IV/IM); inj site induration, warm sensation, and skin tightness (IM); chills, pyrexia.
Infections and infestations: Candidiasis.
Investigations: Increased ALT, AST, alkaline phosphatase, serum bilirubin, BUN, and serum creatinine.
Nervous system disorders: Dizziness, headache.
Reproductive system and breast disorders: Vaginitis.
Skin and subcutaneous tissue disorders: Rash, pruritus, diaphoresis.
Vascular disorders: Flushing; phlebitis (IV).
Potentially Fatal: Hypersensitivity reactions, including anaphylaxis and anaphylactic shock; severe cutaneous adverse reactions (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms [DRESS], acute generalised exanthematous pustulosis), severe haemolytic anaemia; Clostridioides difficile-associated diarrhoea, pseudomembranous colitis; ceftriaxone-Ca precipitation in the lungs and kidneys (particularly in premature and term neonates).
IM/IV/Parenteral: B
Chỉ số theo dõi
Perform culture and susceptibility tests; consult local institutional recommendations before treatment initiation due to antibiotic resistance risks. Monitor prothrombin time/INR, renal function tests, and LFTs; CBC regularly during prolonged use. Assess for signs and symptoms of hypersensitivity reactions (especially anaphylaxis) during the 1st dose, haemolytic anaemia, and pancreatitis.
Quá liều
Symptoms: Diarrhoea, nausea and vomiting. Management: Symptomatic treatment.
Tương tác
May increase the risk of bleeding with vitamin K antagonists (e.g. warfarin). May increase the nephrotoxicity of aminoglycosides. May diminish the therapeutic effects of BCG, typhoid vaccine, and Na picosulfate.
Potentially Fatal: May cause precipitation of ceftriaxone-Ca in the lungs, kidneys or gallbladder when administered simultaneously with Ca-containing IV solutions or infusions (e.g. Ringer's solution, Hartmann's solution, TPN) even at different infusion lines or sites.
Ảnh hưởng đến kết quả xét nghiệm
May lead to false-positive Coomb's test, false-positive urinary glucose test using non-enzymatic methods, and false-positive galactosaemia test results.
Tác dụng
Description:
Mechanism of Action: Ceftriaxone is a 3rd generation broad-spectrum cephalosporin antibiotic. It binds to 1 or more penicillin-binding proteins (PBPs) inhibiting the final transpeptidation step of peptidoglycan synthesis in the bacterial cell walls, 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 the body including gallbladder, lungs, bone, bile, and CSF (higher concentrations when the meninges are inflamed). Crosses the placenta; enters breast milk (low concentrations). Volume of distribution: Approx 6-14 L. Plasma protein binding: Approx 85-95%.
Excretion: Via urine (approx 40-65% as unchanged drug); faeces (as inactive drug). Elimination half-life: Approx 5-9 hours.
Đặc tính

Chemical Structure Image
Ceftriaxone

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5479530, Ceftriaxone. https://pubchem.ncbi.nlm.nih.gov/compound/5479530. Accessed Aug. 25, 2022.

Bảo quản
Store intact vials between 20-25°C. Protect from light. Reconstituted solutions are stable for 6 hours below 25°C and 24 hours between 2-8°C. Storage and stability recommendations may vary among individual products or between countries. Refer to specific product guidelines.
Phân loại MIMS
Cephalosporin
Phân loại ATC
J01DD04 - ceftriaxone ; Belongs to the class of third-generation cephalosporins. Used in the systemic treatment of infections.
Tài liệu tham khảo
Anon. Ceftriaxone. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 15/08/2022.

Anon. Ceftriaxone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/08/2022.

Buckingham R (ed). Ceftriaxone Sodium. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/08/2022.

Ceftriaxone 1 g Powder for Solution for Injection or Infusion (Istituto Biochimico Italiano G. Lorenzini SpA). MHRA. https://products.mhra.gov.uk. Accessed 01/08/2022.

Ceftriaxone Sodium Injection, Powder for Solution (Sagent Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/08/2022.

Devatis Limited. Ceftriaxone 0.5 g & 1 g Powder for Injection & Ceftriaxone 2 g Powder for Infusion data sheet August 2021. Medsafe. http://www.medsafe.govt.nz. Accessed 01/08/2022.

Joint Formulary Committee. Ceftriaxone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/08/2022.

Rocephin (Roche [Malaysia] Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 01/08/2022.

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