RiteMED Ceftriaxone

Each vial contains: Ceftriaxone (as sodium), USP 1 g.
Each diluent ampoule contains: Sterile Water for Injection, USP 10 mL.

Pharmacology: Mechanism of Action: Ceftriaxone kills bacteria by interfering with synthesis of the bacterial cell wall. It binds with high affinity to proteins in the bacterial cell wall thus interfering with the peptidoglycan synthesis. Peptidoglycan is a heteropolymeric structure that provides the cell wall with mechanical stability.
Microbiology: Ceftriaxone is bactericidal against a broad spectrum of bacteria at easily achievable plasma concentrations.
Gram-negative Aerobes: Acinetobacter calcoaceticus, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli (including ampicillin-resistant and beta-lactamase producing strains), Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis (including beta-lactamase producing strains), Morganella morganii, Neisseria gonorrhoeae (including penicillinase- and non-penicillinase producing strains), Neisseria meningitides, Proteus mirabilis, Proteus vulgaris, Serratia marcescens.
Ceftriaxone is also active against many strains of Pseudomonas aeruginosa.
NOTE: Many strains of the above organisms that are multiply resistant to other antibiotics, e.g., penicillins, cephalosporins and aminoglycosides, are susceptible to ceftriaxone.
Gram-positive Aerobes: Staphylococcus aureus (Including penicillinase-producing strains), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Viridans group streptococci.
NOTE: Methicillin-resistant staphylococci are resistant to cephalosporins, including ceftriaxone. Most strains of Group D streptococci and enterococci, e.g., Enterococcus (Streptococcus faecalis, are resistant).
Anaerobes: Bacteroides fragilis, Clostridium species, Peptostreptococcus species.
Gram-negative Aerobes: Citrobacter diversus, Citrobacter freundii, Providencia species (including Providencia rettgeri), Salmonella species (including S. typhi), Shigella species.
Gram-positive Aerobes: Streptococcus agalactiae.
Anaerobes: Bacteroides bivius, Bacteroides melaninogenicus.
Pharmacokinetics: Ceftriaxone demonstrates nonlinear dose-dependent pharmacokinetics because of its protein binding; about 85 to 95% is bound to plasma protein depending on the concentration of ceftriaxone.
Mean peak plasma concentrations of about 40 and 80 micrograms/mL have been reported 2 hours after intramuscular injection of 0.5 and 1 g of ceftriaxone, respectively. The plasma half-life of ceftriaxone is not dependent on the dose and varies between 6 and 9 hours; it may be prolonged in neonates. The half-life does not change appreciably in patients with moderate renal impairment, but it may be prolonged in severe renal impairment especially when there is also hepatic impairment.
Ceftriaxone is widely distributed in body tissues and fluids. It crosses both inflamed and non-inflamed meninges, generally achieving therapeutic concentrations in the CSF. It crosses the placenta and low concentrations have been detected in breast milk. High concentrations are achieved in bile.
About 40 to 65% of a dose of ceftriaxone is excreted unchanged in the urine, principally by glomerular filtration, the remainder is excreted in the bile and is ultimately found in the faeces as unchanged drug and microbiologically inactive compounds.

For the treatment of lower respiratory tract infections, skin and soft tissue infections, urinary tract infections, gonorrhea, pelvic-inflammatory disease, bone and joint infections, and intra-abdominal infections caused by susceptible pathogens.

Ceftriaxone may be administered intravenously or intramuscularly.
ADULTS: Usual adult daily dose: 1 to 2 g given once a day (or in equally divided doses twice a day) depending on the type and severity of infection. The total daily dose should not exceed 4 g.
Treatment of uncomplicated gonococcal infection: 250 mg IM as a single dose.
Surgical infection prophylaxis: 1 g IV 0.5 to 2 hours before surgery.
Children: Treatment of skin and skin structure infections: 50 to 75 mg/kg once a day (or in equally divided doses twice a day). Total daily dose should not exceed 2 g.
Treatment of acute bacterial otitis media: 50 mg/kg IM as a single dose (not to exceed 1 g).
Treatment of serious miscellaneous infections (except meningitis): 50 to 75 mg/kg daily given in 2 divided doses every 12 hours. Total daily dose should not exceed 2 g.
Treatment of meningitis: Initial dose: 100 mg/kg (not to exceed 4 g). Thereafter, a total daily dose of 100 mg/kg/day (not to exceed 4 g daily) is recommended. The daily dose may be administered once a day (or in equally divided doses every 12 hours). The usual duration of therapy is 7 to 14 days.
For the prevention of secondary cases of meningococcal meningitis: A single intramuscular dose of 250 mg may be used for adults and 125 mg for children.
Usual duration of therapy is 4 to 14 days; In complicated infections, longer therapy may be required.
For infections caused by Streptococcus pyogenes, therapy should be continued for at least 10 days.
Or, as prescribed by the physician.

Ceftriaxone is contraindicated in patients with known allergy to cephalosporin class of antibiotics.

Modify dosage in patients with severe renal impairment; prolonged use may result in superinfection; use with caution in patients with a history of penicillin allergy, especially lgE-mediated reactions; may cause antibiotic associated colitis or colitis secondary to C. difficile.
Use in Pregnancy: Pregnancy category B. No adequate and well-controlled studies in pregnant women. Ceftriaxone should be used in pregnancy only if clearly needed.

Use in Pregnancy: Pregnancy category B. No adequate and well-controlled studies in pregnant women. Ceftriaxone should be used in pregnancy only if clearly needed.

The most common adverse effects are hypersensitivity reactions, including skin rashes, urticaria, eosinophilia, fever, reactions resembling serum sickness, and anaphylaxis. Transient increases in liver enzyme values have been reported. Hepatitis and cholestatic jaundice have occurred rarely. Convulsions and other signs of CNS toxicity have been associated with high doses, especially in patients with severe renal impairment. Gastrointestinal adverse effects such as nausea, vomiting, and diarrhea have been reported rarely. Prolonged use may result in overgrowth of non-susceptible organisms and pseudomembranous colitis may develop. There may be pain at the injection site following intramuscular use, and thrombophlebitis has occurred following intravenous infusion. Changes in bowel flora may be more marked because of greater biliary excretion of ceftriaxone; diarrhea may occur more often, especially in children. Biliary sludge or pseudolithiasis due to a precipitate of calcium ceftriaxone has been seen occasionally. Ceftriaxone is highly protein bound and is able to displace bilirubin from albumin binding sites causing hyperbilirubinemia. Neutropenia and rare cases of fatal hemolysis has been reported.

Ceftriaxone has an N-methylthiotriazine side-chain and may have the potential to increase the effects of anticoagulants and to cause a disulfiram-like reaction with alcohol. Unlike many cephalosporins, probenecid does not affect the renal excretion of ceftriaxone.

Directions for Reconstitution: Intravenous injection: For IV use: Add 10 mL Sterile Water for Injection to 1 g Ceftriaxone.
Administer by IV injection lasting two to four minutes.
Intramuscular Injection: For IM use: Add 4 mL Sterile Water for Injection to 1 g Ceftriaxone.
Intravenous Infusion: For IV INFUSION use: Dissolve 2 g Ceftriaxone in 40 mL of a calcium-free infusion solution: sodium chloride 0.9%, sodium chloride 0.45% + dextrose 2.5%, dextrose 5%, dextrose 10%, levulose 5%, dextran 6% in dextrose, Sterile Water for Injection.
Ceftriaxone solutions should not be mixed with or piggybacked into solutions containing other antimicrobial drugs or into diluent solutions other than those listed previously, owing to possible incompatibility.
The reconstituted solution is stable for 6 hours at temperatures not exceeding 25°C (or 24 hours at 2-8°C).

Store at temperatures not exceeding 30°C.
Protect from light.

Cephalosporins

J01DD04 - ceftriaxone ; Belongs to the class of third-generation cephalosporins. Used in the systemic treatment of infections.

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