Ceftriaxone
- Atc Codes:J01DD04
- CAS Codes:104376-79-6#73384-59-5
- PHARMGKB ID:104376-79-6#73384-59-5
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Genes that may be involved
- Inhibits
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Cefotrix, Ceftriaxon, Rocephin, Tercefon; Belgium: Ceftriaxone, Rocephine; Bulgaria: Ceftriaxon, Ceftriaxone, Ceftrin, Medaxone, Tercef; Cyprus: Antibacin, Ceftrix, Medaxonum, Rocephin, Veracol; Czech Republic: Ceftriaxon, Lendacin, Samixon; Denmark: Cefotrix, Ceftriaxon, Rocephalin; Estonia: Ceftriaxone, Medaxone, Tercef; Finland: Ceftriaxon, Ceftriaxone, Rocephalin; France: Ceftriaxone, Rocephine, Triacefan; Germany: Ceftriaxon; Greece: Antibacin, Azatyl, Bresec, Ceftriaxone, Ceftrixon, Ceriaxon, Farcef, Glorixone, Infeflox, Labilex, Medaxone, Riaxon, Rolisporin, Travilan, Ugotrex, Veracol; Hungary: Ceftriaxon, Lendacin, Megion, Rocephin; Ireland: Ceftriaxone, Rocephin; Italy: Axobat, Bixon, Cefoxair, Cefrag, Ceftriaxone, Claxon, Davixon, Daytrix, Deixim, Diaxone, Eftry, Eraxitron, Fidato, Frineg, Kocefan, Monoxar, Nilson, Panatrix, Pantoxon, Pokecef, Ragex, Rocefin, Setriox, Sirtap, Valexime; Latvia: Ceftriaxone, Ciplacef, Mesporin, Oframax, Rocephin; Lithuania: Biotrakson, Medaxone, Oframax, Tercef; Luxembourg: Rocephine; Malta: Ceftriaxone, Fidato, Medaxonum, Rocephin, Travilan, Veracol; Netherlands: Ceftriaxon, Exogran, Rocephin; Poland: Biotrakson, Ceftriaxon, Ceftriaxone, Lendacin, Mesporin, Oframax, Rocephin, Tartriakson; Portugal: Betasporina, Ceftriaxona, Ceriax, Kemudin, Rocephin; Romania: Cefort, Medaxone, Novosef, Oframax, Rocephin, Seftrion; Slovakia: Ceftriaxon, Lendacin, Tercef; Slovenia: Lendacin, Olicef; Spain: Ceftriaxona, Rocefalín; Sweden: Ceftriaxon, Rocephalin; UK: Ceftriaxone, Rocephin.
North America
Canada: Ceftriaxone, Rocephin; USA: Ceftriaxone, Rocephin.
Latin America
Argentina: Acantex, Cefomax, Ceftriaxona, Exempla, Rivacefin, Soltrimox; Brazil: Ceftriax, Ceftriaxona, Glicocef, Keftron, Mesporan, Prodoxin, Rocefin, Triaxon, Triaxton, Trioxina; Mexico: Amcef, Asepzona, Aurofox, Axtar, Benaxona, Cefaxona, Cefraden, Ceftrex, Ceftriaxona, Ceftrilem, Centrifal, Limiprol, Megion, Oframax, Primotox, Rocephin, Tacex, Terbac, Tindortec, Triaken, Triox, Xonatil.
Asia
Japan: Ceftriaxone, Cefxone, Ceroneed, Rocemerck, Rocephin, Rozeclart, Sefirom.
Drug combinations
Chemistry
Ceftriaxone Sodium: C~18~H~16~N~8~Na~2~O~7~S~3~ 3½H~2~O. Mw: 661.60. (1) 5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 7-[[(2-amino-4-thiazolyl)(methoxyimino)acetyl]amino]-8-oxo-3-[[(1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl)thio]methyl]-, disodium salt, [6R-[6α,7β(Z)]]-, hydrate (2:7); (2)(6R,7R)-7-[2-(2-Amino-4-thiazolyl)glyoxylamido]-8-oxo-3-[[(1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-as-triazin-3-yl)thio]methyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 7^2^-(Z)-(O-methyloxime), disodium salt, sesquaterhydrate. CAS-104376-79-6; CAS-73384-59-5 (ceftriaxone)(1981).
Pharmacologic Category
Antibacterials; Third Generation Cephalosporins. (ATC-Code: J01DD04).
Mechanism of action
Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins. Active in vitro and in clinical infections against Gram-positive aerobic bacteria, such as Streptococcus pneumoniae, S. pyogenes (group A β-hemolytic streptococci), Staphylococcus aureus (including penicillinase-producing strains), S. epidermidis, and viridans streptococci. Also active in vitro against S. agalactiae (group B streptococci). Active in vitro and in clinical infections against Gram-negative aerobic bacteria such as Acinetobacter calcoaceticus, Enterobacter (including E. aerogenes, E. cloacae), Escherichia coli, Haemophilus influenzae (including ampicillin-resistant and β-lactamase-producing strains), H. parainfluenzae, Klebsiella pneumoniae, K. oxytoca, Moraxella catarrhalis (including β-lactamase-producing strains), Morganella morganii, Neisseria gonorrhoeae, N. meningitidis, Proteus mirabilis, P. vulgaris, Pseudomonas aeruginosa, and Serratia marcescens. Also active in vitro against Capnocytophaga, Citrobacter, Providencia, Salmonella, and Shigella. Less active than ceftazidime against Ps. aeruginosa. Active in vitro and in clinical infections against Bacteroides fragilis, Clostridium (except C. difficile), and Peptostreptococus. Also active in vitro against Prevotella bivius and Porphyromonas melaninogenicus. Inactive against Chlamydia, fungi, and viruses.
Therapeutic use
Lower respiratory tract infections, acute bacterial otitis media, skin and skin structure infections, bone and joint infections, intra-abdominal and urinary tract infections, pelvic inflammatory disease, uncomplicated gonorrhea, bacterial septicemia, and meningitis. Used in surgical prophylaxis. Alternative antibiotic for prevention of infective endocarditis when parenteral administration is needed.
Pregnancy and lactiation implications
Teratogenic effects not observed in animal studies. The pharmacokinetics of ceftriaxone in the third trimester is similar to that of nonpregnant patients (possible lower peak concentrations during labor). Crosses the placenta and distributes to amniotic fluid. Recommended for use in pregnant women for the treatment of gonococcal infections. Enters breast milk (use caution).
Unlabeled use
Chancroid, complicated gonococcal infections, epididymitis. Sexually-transmitted diseases. Periorbital or buccal cellulitis. Salmonellosis or shigellosis. Atypical community-acquired pneumonia. Epiglottitis, Lyme disease. Chemoprophylaxis for high-risk contacts and persons with invasive meningococcal disease, sexual assault, typhoid fever, Whipple’s disease.
Contraindications
Hypersensitivity to ceftriaxone sodium, any component of the formulation, or other cephalosporins. Avoid use in hyperbilirubinemic neonates, particularly those who are premature (ceftriaxone displaces bilirubin from albumin binding sites). Concomitant use with intravenous calcium-containing solutions/products in neonates (≤28 days).
Warnings and precautions
May be associated with increased INR, especially in nutritionally-deficient patients, prolonged treatment, hepatic or renal disease. Use with caution in history of penicillin allergy, especially IgE-mediated reactions (e.g. anaphylaxis, angioedema, urticaria). Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea and pseudomembranous colitis. Use with caution in history of gastrointestinal disease, especially colitis. Abnormal gallbladder sonograms reported, possibly due to ceftriaxone-calcium precipitates. Pancreatitis reported secondary to biliary obstruction. Contraindicated in hyperbilirubinemic neonates. Fatal precipitation reactions in neonates due to co-administration of calcium-containing solutions reported (concurrent use in neonates is contraindicated). Risk of «gasping syndrome» (potentially fatal) in neonates due to consumption of benzoic acid. May cause positive direct Coombs’ test, false-positive urinary glucose test using cupric sulfate, false-positive serum or urine creatinine with Jaffé reaction.