Each vial contains Sterile Ceftriaxone Sodium equivalent to Ceftriaxone 1.0 g.
The bactericidal activity of ceftriaxone results from inhibition of bacterial cell wall synthesis. Ceftriaxone exerts in-vitro activity against a wide range of gram-negative and gram-positive microorganisms. Ceftriaxone is highly stable to most β-lactamases, both penicillinases and cephalosporinases, of gram-positive and gram-negative bacteria. Ceftriaxone is usually active
against the following microorganisms in-vitro and in clinical infections.
Aerobes gram-positive: Staphylococci, Streptococci, beta-hemolytic, Streptococcus pneumoniae, Streptococcus pyogenes.
Aerobes gram-negative: Acinetobacter sp., Citrobacter sp., Enterobacter sp., Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella sp., Morganella (Proteus) morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Providencia sp., Providencia rettgeri, Pseudomonas aeruginosa, Salmonella sp., Salmonella typhi, Serratia sp., Shigella sp.
Anaerobes: Bacteroides sp., Bacteroides fragilis, Clostridium sp., Eubacterium sp., Fusobacterium sp., Peptococcus sp., Peptostreptococcus sp.
PHARMACOKINETICS: Ceftriaxone exhibits nonlinear dose-dependent pharmacokinetics. All basic pharmacokinetics parameters (except elimination half-life) are dose dependent if based on total drug concentrations. Following IM administration of a single ceftriaxone dose of 0.5 - 1 g in healthy adults, the drug appears to be completely absorbed, and peak serum concentrations are attained 1.5 - 4 hours after the dose.
The volume of distribution of ceftriaxone is dose-dependent and ranges from 5.8 - 13.5 L in healthy adults. The volume of distribution of ceftriaxone is 0.497 - 0.608 L/kg in neonates 1 - 45 days of age and 0.26 - 0.54 L/kg in children 1.5 months to 16 years of age following a single ceftriaxone dose of 50 - 100 mg/kg.
Following IM administration, ceftriaxone is widely distributed into body tissues and fluids including the gallbladder, lungs, bone, heart, bile, prostate adenoma tissue, uterine tissue, atrial appendage, sputum, tears, middle ear fluid and synovial fluids. Ceftriaxone generally diffuses into CSF following IM administration of the drug. The degree of protein binding of ceftriaxone is concentration dependent and decreases nonlinearly with increasing concentrations of the drug. Ceftriaxone binds mainly to albumin. Protein binding of ceftriaxone is lower in neonates and children than in adults because of decreased plasma albumin concentrations in this age group.
In adults with normal renal and hepatic function, the distribution half-life of ceftriaxone is 0.12 - 0.7 hours and the elimination half-life is 5.4 - 10.9 hours. Ceftriaxone is excreted both by renal and nonrenal mechanisms. The drug is excreted principally in urine by glomerular filtration and also is excreted in feces via bile. Following IM administration of a single dose of ceftriaxone in adults with normal renal and hepatic function, 33 - 67% of the dose is excreted in urine as unchanged drug and the remainder of the dose is excreted in feces as unchanged drug.
Serum clearance of ceftriaxone is dose-dependent and ranges from 9.7 - 25 mL/minute in healthy adults. The serum half - life of ceftriaxone is longer in neonates than in older children and adults. The elimination half-life of ceftriaxone is only slightly prolonged in patients with moderately impaired renal function. Studies in patients with hepatic impairment indicate that the pharmacokinetics of ceftriaxone are not generally altered in these patients. Ceftriaxone is not removed by hemodialysis or peritoneal dialysis.
CEFTREX is used for the treatment of infections caused by pathogens sensitive to ceftriaxone e.g.: lower respiratory tract infections; skin and skin structure infections; bone and joint infections; intra-abdominal infections; urinary tract infections; meningitis, septicemia and gonorrhea caused by susceptible organisms.
Intramuscular injection: CEFTREX 1 g is dissolved in 3.5 ml of 1% lidocaine solution and administered by deep intragluteal injection. It is recommended that not more than 1 g be injected on either side. *The lidocaine solution must never be administered intravenously.
Standard dosage: Adults and children over 12 years: Administered 1 - 2 g once daily (every 24 hours) in
severe cases the dosage may be raised to a maximum dose of 4 g administered once daily.
Infants and children (three weeks to 12 years): 20 - 80 mg/kg body weight administered once daily.
Neonates (up to two weeks): 20 - 50 mg/kg body weight, administered once daily (not to exceed 50 mg/kg/day).
Dosage in renal and hepatic impairment: Modification of the usual dosage of ceftriaxone generally in unnecessary in patients with impaired renal or hepatic function alone; however, serum concentrations of the drug should be monitored when ceftriaxone is used in patients with severe renal impairment and in patients with both hepatic and substantial renal impairment. If evidence of accumulation of the drug occurs, dosage should be decreased accordingly. Dosage in adults with both hepatic and substantial renal impairment should not exceed 2 g daily unless serum concentrations of the drug are monitored closely.
Because ceftriaxone is not removed by hemodialysis, supplemental doses of the drug are unnecessary during or after dialysis.
Duration: Generally, ceftriaxone therapy should be continued for at least 2 days after the signs and symptoms of infection have disappeared. The usual duration of therapy is 4 to 14 days; in complicated infection, longer therapy may be required.
Special dosage: In bacterial meningitis in infants and children, treatment begins with doses of 100 mg/kg body weight (not to exceed 4 g) once daily. The duration of therapy is as the following: Neisseria meningitidis 4 days, Streptococcus pneumoniae 7 days, Haemophilus influenzae 6 days.
For the treatment of Gonorrhea: A single IM dose of 250 mg is advised.
Direction for use: Reconstituted solutions retain their physical and chemical stability for six hours at room temperature (or 24 hours at 5°C). As a general rule; however, the solutions should be used immediately after preparation. They range in color from pale yellow to amber, depending on the concentration and the length of storage. This characteristic of the active ingredient is of no significance for the efficacy or tolerance of the drug.
Inappropriately large doses may cause seizures, particularly in renal impairment. Reduce dosage when renal function is impaired. If seizures occur, promptly discontinue the drug, administer anticonvulsants if clinically indicated. Ceftriaxone is not removed by hemodialysis or peritoneal dialysis, and these procedures would be ineffective in reducing ceftriaxone concentrations following overdosage. There is no specific antidote. If acute overdosage of ceftriaxone occurs, supportive and symptomatic treatment should be initiated.
Hypersensitivity to the cephalosporin or related antibiotics.
1. Administer cautiously to penicillin-sensitive patients.
2. Ceftriaxone may be associated with a fall in prothrombin activity. Monitor prothrombin time for patients at risk and administer exogenous vitamin K as indicated. Vitamin K administration may be necessary if the prothrombin time is prolonged before therapy.
3. Pseudomembranous colitis may occur and consider this diagnosis in patients who develop
diarrhea with antibiotic use. A toxin produced by Clostridium difficile is a primary cause of antibiotic-associated colitis. Colitis may range in severity from mild to life-threatening. Mild case of colitis may respond to drug discontinuation alone. When the colitis is not relieved by drug discontinuation, or when it is severe, oral vancomycin is treatment of choice.
4. Inject IM preparations deep into musculature.
5. Since ceftriaxone can precipitate in the gallbladder, some clinicians recommend that ceftriaxone be used with caution in patients with preexisting disease of the gallbladder, biliary tract, liver, or
pancreas.
Use in Children: Because the drug can displace bilirubin from serum albumin, ceftriaxone should not be administered to hyperbilirubinemic neonates, particularly those who are premature.
PREGNANCY: Category B. Safety for use during pregnancy is not established. Use only when potential benefits outweigh potential hazards to the fetus. Cephalosporins appear safe for pregnant patients, but relatively few controlled studies exist.
LACTATION: Because ceftriaxone is distributed into milk, the drug should be used with caution in nursing women.
Hematologic effects: Hematologic effects are among the most frequent adverse effects reported with ceftriaxone such as eosinophilia, thrombocytosis, leukopenia, anemia, neutropenia, thrombocytopenia, hypoprothrombinemia or prolongation of prothrombin time (PT).
GI effects: Diarrhea, nausea, vomiting, dysgeusia, colitis, abdominal pain, flatulence, dyspepsia, gallbladder sludge and biliary lithiasis.
Dermatologic and sensitivity reactions: Rash, pruritus, fever, chills.
Hepatic effects: Increased serum concentrations of AST, ALT, alkaline phosphatase and bilirubin.
Renal effects: Increased concentrations of BUN, serum creatinine, presence of casts in urine.
Local effects: Pain and tenderness at the infection site from IM injection. Local reactions occur less frequently and are less intense when IM injections of ceftriaxone are reconstituted with 1% lidocaine hydrochloride.
Others: Flushing, headache, dizziness, oral candidiasis, candidal vaginitis, palpitation and epistaxis.
Probenecid: Concomitant administration of oral probenecid (500 mg daily) does not appear to affect the pharmacokinetics of ceftriaxone.
Aminoglycosides: In vitro studies indicate that the antibacterial activity of ceftriaxone and aminoglycosides may be additive or synergistic against some strains of Enterobacteriaceae and some strains of Pseudomonas aeruginosa.
Alcohol: A disulfiram-like reaction may occur. However, this effect
generally has been reported only with β-lactam antibiotics that contain an N-methylthiotetrazole (NMTT) side chain. That ceftriaxone does not contain these side chain.
Loop diuretics: Use CEFTREX with caution in patients receiving potent diuretics (e.g. loop diuretics). The risk of nephrotoxicity may be increased. Monitor renal function.
Drug/Lab test interaction: Immunohematology test: A false-positive direct Coombs' test has occurred in some patients receiving ceftriaxone, in hematologic studies, in transfusion cross-matching procedure.
Test for urinary glucose: Like most cephalosporins, ceftriaxone interferes with urinary glucose determinations using cupric sulfate (e.g. Benedict's solution, Clinitest). A false-positive reaction may occur but not with enzyme-based tests such as clinistix.
J01DD04 - ceftriaxone ; Belongs to the class of third-generation cephalosporins. Used in the systemic treatment of infections.
Ceftrex powd for inj 1 g
1's;20 × 1's
Sign Out
