Each vial contains: Ceftriaxone (as sodium) 1 g.
Ceftriaxone (TRIAVEX 1) is a third generation cephalosporin antibiotic with a broad spectrum antimicrobial activity. It is stable against degradation and inactivation by beta-lactamase. Ceftriaxone is administered parenterally as the sodium salt.
Pharmacology: Pharmacodynamics: Mechanism of Action: Sterile Ceftriaxone Sodium is bactericidal. Like other beta lactams, Sterile Ceftriaxone Sodium kills bacteria by preventing their cell wall synthesis.
Pharmacokinetics: Sterile Ceftriaxone Sodium is completely absorbed following intramuscular administration with peak plasma concentration occurring 2-3 hours after the dose. When Sterile Ceftriaxone Sodium is given by IV infusion, plasma levels were substantially higher after single IM doses of 0.5 and 1.0 g mean plasma were, at 30 minutes 30 and 40 mcg/mL, at 2 hours 43 and 76 mcg/mL, at 4 hours, 39 and 68 mcg/mL and at 12 hours 16 and 29 mcg/mL. The plasma half-life of Sterile Ceftriaxone Sodium is not dependent on the dose and carries between 6 and 9 hours. 85 to 95% of Sterile Ceftriaxone sodium is reversibly bound to plasma proteins. Sterile Ceftriaxone Sodium is penetrates well into most tissues and body fluids including CSF (with inflamed and non-inflamed meninges). High concentrations are rich in bile.
Sterile Ceftriaxone Sodium is metabolized in the body. 33 to 67% of the dose is excreted unchanged in the urine. The rest is excreted is unchanged in the bile and is ultimately excreted in the feces as inactive compounds.
Elimination half-life is only minimally altered in the elderly or in patients with renal or hepatic dysfunction. However, it is decreased in neonates.
Microbiology: Antimicrobial Activity: Sterile Ceftriaxone Sodium is highly stable against beta lactamases including both penicillinases and cephalosporinase produced by Gram negative and Gram positive organisms. Sterile Ceftriaxone Sodium is active against most Gram positive and Gram negative aerobes and some anaerobes.
Gram positive bacteria: Sterile Ceftriaxone Sodium is very active against S. Pneumoniae and Streptococci groups A and B. Other gram positive organisms susceptible to Sterile Ceftriaxone Sodium include Staphylococcus aureus including penicillinase producing strains and Staph. Epidermidis.
Gram negative bacteria: Sensitive Organisms include E. coli, Citrobacter freundii, C. diversus, Klebsiella spp., K. pneumoniae, Enterobacter spp., E. aerogenes, E. cloacae, Serratia spp., and Shigella spp., Morganella morganii and P. vulgaris, Neisseria are sensitive to Sterile Ceftriaxone Sodium. These include both penicillinase producing and non producing gonococci and N. meningitidis. Haemophilus influenzae including ampicillin resistant strains are sensitive.
Anaerobic organisms: Sterile Ceftriaxone Sodium is active against Bacteroides fragilis, B. melaninogenicus, B. Bivius, Clostridium spp., and Peptostreptococcus. Sterile Ceftriaxone Sodium is active against Treponema to a similar extent as benzyl penicillin and highly active against Borrelia burgdorferi.
Ceftriaxone is used in the treatment of lower respiratory tract infections and pneumonia, serious bacterial infections with or without bacteremia or septicemia, pelvic inflammatory disease, urinary tract infections, skin and soft tissue infections, bacterial meningitis, surgical prophylaxis, sexually transmitted disease, bone and joint infections.
Sterile Ceftriaxone Sodium can be given IM or IV, in the seriously ill patient the IV route is preferred. The usual duration of therapy is 4 to 14 days; in complicated infections, longer therapy may be required.
Children: The usual dosage of Sterile Ceftriaxone for the serious infections in children and other than CNS infections (meningitis) caused by susceptible organisms is 50-75 mg/kg (not to exceed 2 g) daily in equally divided doses every 12 hours or in single daily doses.
For the treatment of CNS infections, the usual dosage is 100 mg/kg given in equally divided doses every 12 hours or 75 mg/kg loading dose of a drug maybe used to initiate therapy.
Dosage in renal and hepatic impairment: Sterile Ceftriaxone Sodium is executed via both biliary and renal excretion. Therefore, patients with renal failure normally require no adjustment in dosage when usual doses of Sterile Ceftriaxone Sodium are administered, but concentrations of drug in serum should be monitored periodically. Dosage adjustments should not be necessary in patients with hepatic dysfunction; however in patients with both hepatic dysfunction and significant renal diseases, Sterile Ceftriaxone Sodium should not exceed 2 g daily.
Adults: The usual adult dose is 1 to 2 g daily as a single dose or in two divided doses. In severe infections up to 4 g daily. For the treatment of gonorrhea, a single intramuscular dose of 250 mg is recommended. For surgical infection prophylaxis in adults, a single dose of 1 g is administered 0.5 to 2 hours prior to surgery or as directed by a physician.
Sterile Ceftriaxone Sodium is contraindicated to patients with known hypersensitivity to cephalosporins.
Prothrombin has been altered in patients receiving Sterile Ceftriaxone Sodium.
Hypersensitivity to Cephalosporins and/or penicillins should be looked before starting Sterile Ceftriaxone Sodium.
Sterile Ceftriaxone Sodium should be given with caution in patients with gastrointestinal disease especially colitis.
The drug should be discontinued in patients showing evidence of gall bladder disease or sonographic abnormalities.
Carcinogenicity: Specific studies to determine the carcinogenic potential of Sterile Ceftriaxone Sodium have not been performed to date and animal toxicity studies have been performed to a maximum duration of 6 months.
There are no adequate or controlled studies using Sterile Ceftriaxone Sodium in pregnant women and the drug should be used during pregnancy only when clearly needed.
Because Sterile Ceftriaxone Sodium is distributed into milk, the drug should be used with caution in nursing women.
Sterile Ceftriaxone Sodium is generally well tolerated. Adverse reactions are usually mild and transient and drug discontinuation has been required only in about 1% of patients.
Common side effects are diarrhea, occasional nausea/vomiting, glossitis or stomatitis. Hypersensitivity reactions such as rash, pruritus, urticaria and oedema, transient pain at site of IM injection and local phlebitis have also been reported.
Alcohol: A possible disulfiram reaction may occur with alcohol.
Directions for Use: Intramuscular Injection: IM injections of Sterile Ceftriaxone Sodium are prepared by adding 0.9, 1.8, 3.6 mL of sterile water for injection, 0.9% sodium chloride injection, 5% dextrose injection, bacteriostatic water for injection containing 0.9% benzyl alcohol or 1% lidocaine hydrochloride to vials labeled containing 250 mg, 500 mg, 1 g of Sterile Ceftriaxone Sodium respectively to provide solutions containing 250 mg/mL. More dilute solutions of the drug maybe used for IM injection if required.
Intermittent IV infusion: For intermittent IV infusion, vials labeled as containing 250 mg, 500 mg or 1 g of Sterile Ceftriaxone Sodium should be reconstituted with 3.5 (not less than 2.4), 4.8 or 9.6 mL respectively to provide solutions containing approximately 100 mg/mL. Reconstituted solutions of the drug should then be further diluted in compatible IV solution, generally to a concentration of 10-40 mg/mL, although lower concentrations may be used if desired.
Direction for Reconstitution: With 10 mL diluent. Add 3 mL for IM and 10 mL for IV use of Sterile Water for injection.
Store at temperatures not exceeding 30°C. Protect from light.
J01DD04 - ceftriaxone ; Belongs to the class of third-generation cephalosporins. Used in the systemic treatment of infections.
Powd for inj (vial + 10 mL diluent) 1 g x 1's.