Traxone

Traxone

ceftriaxone

Manufacturer:

Pacific Pharma (Korea)

Distributor:

AA Medical
Full Prescribing Info
Contents
Ceftriaxone.
Description
Each vial contains Sterile Ceftriaxone sodium USP equivalent to ceftriaxone 250 mg, 500 mg, 1 g.
Action
Pharmacology: The bactericidal activity of Ceftriaxone results from inhibition of cell wall synthesis. Ceftriaxone has a high degree of stability in the presence of beta-lactamase, both penicllinases, of gram-negative and gram-positive bacteria.
Average plasma concentrations of ceftriaxone following a single 30-minute intravenous (I.V.) infusion or a 0.5, 1 or 2 g dose and intramuscular (I.M.) administration of a single 0.5 (250 mg/ml or 350 mg/ml concentrations) or 1 g dose in healthy subjects are presented in Table 1.

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Ceftriaxone was completely absorbed following I.M. administration with mean maximum plasma concentrations occurring between 2 and 3 hours postdating. Multiple I.V. or I.M. doses ranging from 0.5 to 2 g at 12- to 24-hour intervals resulted in 15% to 36% accumulation of ceftriaxone above single dose values.
Ceftriaxone concentrations in urine are high, as shown in Table 2.

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Thirty-three percent to 67% of a ceftriaxone dose was excreted in the urine as unchanged drug and the remainder was secreted in the bile and ultimately found in the feces as microbiologically inactive compounds. After a 1 g I.V. dose, average concentrations of ceftriaxone, determined from 1 to 3 hours after dosing, were 581 mcg/g in the gallbladder wall and 62.1 mcg/ml in the concurrent plasma.
Over a 0.15 to 3 g dose range in healthy adult subjects, the values of elimination half-life ranged from 5.8 to 8.7 hour: apparent volume of distribution from 5.78 to 13.5 L plasma clearance from 0.58 to 1.45 L/hour; and renal clearance from 0.32 to 0.73 L/hour. Ceftriaxone is reversibly bound to human plasma proteins, and the binding decreased from a value of 95% bound at plasma concentrations of <25 mcg/ml to a value of 85% bound at 300 mcg/ml.
The average values of maximum plasma concentration, elimination half-life, plasma clearance and volume of distribution after a 50 mg/kg I.V. dose and after a 75 mg/kg I.V. dose in pediatric patients suffering from bacterial meninges are shown in Table 3. Ceftriaxone penetrated the inflamed meninges of infants and children; CSF concentrations after a 50 mg/kg I.V. dose and after a 75mg/kg I.V. dose are also shown in Table 3.

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Compared to that in healthy adult subjects, the pharmacokinetics of ceftriaxone were only minimally altered in elderly subjects and in patients with renal impairment of hepatic dysfunction therefore, dosage adjustments are not necessary for these patients with ceftriaxone dosages up to 2 g per day. Ceftriaxone was not removed to any significant extent from the plasma by hemodialysis. In 6 of 26 dialysis patients, the elimination rate of ceftriaxone was markedly reduced, suggesting that plasma concentrations of ceftriaxone should be monitored in these patients to determine if dosage adjustments are necessary.
TRAXONE Inj. is bactericidal and acts by inhibition of cell wall synthesis. It has a high degree of stability in the presence of β-lactamases (both penicillinases and cephalosporinases) of gram-positive and gram-negative bacteria. The basic method of action is the interruption of the transpeptidation process that links the individual peptidoglycan components of the bacteria, cell wall to each other.
Microbiology: TRAXONE Inj. is usually active against the following microorganisms in vitro: Gram-Positive Aerobes: Staphylococcus aureus (including penicillinase-producing strains), Staphylococcus epidermidis, Streptococcus pneumonia, Streptococcus group A (Streptococcus pyogenes), Streptococcus group B (Streptococcus agalactiae), Streptococcus viridans, Streptococcus bovis.
Note: Methicillin-resistant Staphylococcus sp are resistant to cephalosporins, including ceftriaxone. Most strains of Enterococci (eg. Streptococcus faecalis) are resistant. Gram-Negative Aerobes: Aeromonas sp, Alcaligenes sp, Branhamella catarrhalis (β-lactamase negative and positive), Citrobacter sp, Enterobacter sp (some strains are resistant), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae (including penicillinase-producing strains), Haemophilus parainfluenzae, Klebsiella sp (including K. pneumonia), Moraxella sp, Morganella morganii, Neisseria gonorrhoeae (including penicillinase-producing strains), Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia sp, Pseudomonas aeruginosa (some strains are resistant), Salmonella sp (including S. typhi), Serratia sp (including S. marcescens), Shigella sp, Vibrio sp (including V. cholerae), Yersinia sp (including Y. enterocolitica).
Note: Many strains of the previously-mentioned organisms that are multiple-resistant to other antibiotics, eg penicillins, older cephalosporins and aminoglycosides, are susceptible to ceftriaxone. Treponema pallidum is sensitive in vitro and in animal experiments. Clinical investigations indicate that primary and secondary syphilis respond well to ceftriaxone therapy.
Anaerobic Organisms: Bacteroides (including some strains of B. fragilis). Clostridium (except C. difficile), Fusobacterium, Peptococcus and Peptostreptococcus spp.
Note: Many strains of β-lactamase-producing Bacteroides sp (notably B. fragilis) are resistant.
Indications/Uses
Infections caused by pathogens sensitive to TRAXONE Inj. eg. sepsis; meningitis; abdominal infections (peritonitis, infections of the biliary and gastrointestinal tracts); infections of the bones, joints, soft tissue and skin, and of wounds; perioperative prophylaxis of infections; infections in patients with impaired defense mechanisms; renal and urinary tract infections, respiratory tract infections, particularly pneumonia, and ear, nose and throat infections, including gonorrhea.
Dosage/Direction for Use
Standard dosage: Adults and children over twelve years: The usual dosage is 1-2 g of TRAXONE Inj. administered once daily (every 24 hours). In severe cases or in infections caused by moderately sensitive organisms, the dosage may be raised to 4 g, administered once daily.
Neonates, Infants and Children up to 12 years: The following dosage schedules are recommended for once daily administration:  Infants and Children (3 weeks up to 12 years): A daily dose of 20-80 mg/kg body weight. For Children with body weights of 50 kg or more, the usual adult dosage should be used, doses of 50 mg/kg body weight or more should be administered as a slow IV infusion over at least 30 min.
Neonates (up to 2 weeks): A daily dose of 20-50 mg/kg body weight, not to exceed 50 mg/kg, on account of the immaturity of the infant's enzyme systems. It is not necessary to differentiate between premature and infants born at term.
Elderly Patients: The dosages recommended for adults require no modification in the case of geriatric patients.
Duration of Therapy: The duration of therapy varies according to the course of the disease. As with antibiotic therapy in general, administration of TRAXONE Inj. should be continued for a minimum of 48-72 hours after the patient has become afebrile or evidence of bacterial eradication has been obtained.
Combination therapy: Synergy between TRAXONE Inj. and aminoglycosides has been demonstrated with many gram negative bacilli under experimental conditions. Although enhanced activity of such combinations is not always predictable, it should be considered in severe, life-threatening infections due to organisms, eg Pseudomonas aeruginosa. Because of physical incompatibility, the 2 drugs must be administered separately at the recommended dosages.
Special Dosage Instructions: Meningitis: In bacterial meningitis in infants and children, treatment begins with doses of 100 mg/kg (not to exceed 4 g) once daily. As soon as the causative organism has been identified and its sensitivity determined, the dosage can be reduced accordingly. The best results have been found with the following duration of therapy: See Table 4.

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Gonorrhea: For the treatment of gonorrhea (penicillinase-producing and nonpenicillinase-producing strains), a single 250 mg I.M. dose is recommended.
Preoperative Prophylaxis: To prevent postoperative infection in contaminated or potentially contaminated surgery, the recommended approach, depending on the risk of infection, is a single 1 to 2 g dose of TRAXONE Inj. administered 30-90 min prior to surgery. In colorectal surgery, concurrent (but separate) administration of TRAXONE Inj. and 5-nitroimidazole eg ornidazole, has proven effective.
Impaired Renal and Hepatic Function: In patients with impaired renal function, there is no need to reduce the dosage of TRAXONE Inj. provided that hepatic function is intact. Only in cases of preterminal renal failure (creatinine clearance <10 ml/min) should the TRAXONE Inj. dosage not exceed 2 g daily. In patients with liver damage, there is no need for the dosage to be reduced provided that renal function is intact. In cases of severe concomitant renal and hepatic dysfunction, the plasma concentrations of TRAXONE Inj. should be determined at regular intervals. In patients undergoing dialysis, no additional supplementary dosing is required following the dialysis. Serum concentrations should be monitored, however, to determine whether dosage adjustments are necessary, since the elimination rate in these patients may be reduced.
Overdosage
Treatment of Overdosage: In the case of overdosage, Traxone concentrations would not be reduced by haemodialysis or peritoneal dialysis. There is no specific antidote. Treatment should be symptomatic.
Contraindications
Patients with known hypersensitivity to the cephalosporin class of antibiotics. In patients hypersensitive to penicillin, the possibility of allergic cross-reactions should be borne in mind.
Warnings
Before therapy with TRAXONE Inj. is instituted, careful inquiry should be made to determine whether the patient has had previous history of hypersensitivity reactions to cephalosporins, penicillins or other drugs. This product should be given cautiously to penicillin-sensitive patients. Antibiotics should be administered with caution to any patient who has demonstrated some form of allergy, particularly to drugs. Serious acute hypersensitivity reactions may require the use of subcutaneous epinephrine and other emergency measures. In vitro studies have shown that Ceftriaxone, like some other cephalosporins can displace bilirubin from serum albumin. Caution should be exercised when considering use of TRAXONE Inj. for hyperbilirubinemic neonates, especially prematures.
Special Precautions
As with other cephalosporins, anaphylactic shock cannot be ruled out even if a thorough patient history is taken. Anaphylactic shock requires immediate countermeasures, eg I.V. epinephrine (adrenaline) followed by a glucocorticoid.
In rare cases, shadows suggesting sludge have been detected by sonograms of the gallbladder. This condition was reversible on discontinuation or completion of TRAXONE Inj. therapy. Even if such findings are associated with pain, conservative, nonsurgical management is recommended. In vitro studies have shown that ceftriaxone, like some other cephalosporins, can displace bilirubin from serum albumin. Caution should be exercised when considering TRAXONE Inj. for hyperbilirubinemic neonates especially prematures. During prolonged treatment, the blood cell count should be checked regularly.
Use In Pregnancy & Lactation
Use in pregnancy: Although the relevant preclinical investigations revealed neither mutagenic nor teratogenic effects, TRAXONE Inj. should not be used in pregnancy (particularly in the 1st trimester) unless absolutely indicated.
Side Effects
TRAXONE Inj. is generally well tolerated. During the use of TRAXONE Inj. the following side effects, which were reversible either spontaneously or after withdrawal of the drug, have been observed.
Systemic Side Effects: Gastrointestinal Complaints (about 2% of cases): Loose stools or diarrhea, nausea, vomiting, stomatitis and glossitis.
Hematological Changes (about 2%): Eosinophilia, leucopenia, granulocytopenia, hemolytic anemia, thrombocytopenia.
Skin Reactions (about 1 %): Exanthema, allergic dermatitis, pruritus, urticaria, edema and erythema multiforme. Other rare side effects were headache and dizziness, increase in liver enzymes, gallbladder sludge, oliguria, increase in serum creatinine, mycosis of the genital tract, shivering and anaphylactic or anaphylactoid reactions. Pseudomembranous enterocolitis and coagulation disorders have been reported as very rare side effects.
Local Side Effects: In rare cases, phlebitis reactions occurred after I.V administration. These may be prevented by slow (2-4 min) injection of the substance, I.M. Injection without lidocaine solution is painful.
Drug Interactions
No impairment of renal function has so far been observed after concurrent administration of large doses of TRAXONE Inj. and potent diuretics (eg, furosemide) at high doses. There is no evidence that TRAXONE Inj. increases the renal toxicity of aminoglycosides. No effect similar to that of disulfiram has been demonstrated after ingestion of alcohol subsequent to the administration of TRAXONE Inj. Ceftriaxone does not contain an N-methylthiotetrazole moiety associated with possible ethanol intolerance and bleeding problems of certain other cephalosporins. The elimination of TRAXONE Inj. is not altered by probenecid.
Caution For Usage
Directions for Use: I.M. Injection: TRAXONE Inj. 0.25 or 0.5 g is dissolved in 2 ml, and TRAXONE Inj. 1 g 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 I.V.
I.V. Injection: TRAXONE Inj. 0.25 or 0.5 g is dissolved in 5 mL, and TRAXONE Inj. 1 g in 10 mL of water for injection and then administered by direct I.V. Injection lasting 2-4 min.
I.V. Infusion: the infusion should last at least 30 minutes. For I.V. infusion, 2 g of TRAXONE Inj. are dissolved in 40 mL of one of the following calcium-free infusion solutions: sodium chloride 0.9%, sodium chloride 0.45% + dextrose 2. 5%, dextrose 5%, dextrose 10%, levulose 5%, dextran 6% in dextrose, sterile water for injections. TRAXONE solution should not be mixed with or piggybacked into solutions containing other antimicrobial drugs or into diluent solutions other than those listed above, owing to possible incompatibility.
Storage
Protect from light and store below 25°C.
MIMS Class
ATC Classification
J01DD04 - ceftriaxone ; Belongs to the class of third-generation cephalosporins. Used in the systemic treatment of infections.
Presentation/Packing
Powd for inj [white to yellowish crystalline powder (vial) + 10 mL water (amp)] 250 mg x 1's. 500 mg x 1's. 1 g x 1's.
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