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Each vial contains: Ceftriaxone (as sodium) 1 g.
Ceftriaxone for injection, USP is a sterile, semisynthetic, broad-spectrum cephalosporin antibiotic for intravenous or intramuscular administration. Ceftriaxone sodium is (6R, 7R)-7-[2-(2-Amino-4-thiazolyl)glyoxylamido]-8-oxo3-[[(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-2carboxylic acid, 72-(Z)-(O-methyloxime), disodium salt, sesquaterhydrate. The chemical formula of ceftriaxone sodium is C₁₈H₁₆N₈Na₂O₇S₃·3.5H₂O. It has a calculated molecular weight of 661.60.
Ceftriaxone sodium is a white to yellowish crystalline powder which is readily soluble in water, sparingly soluble in methanol and very slightly soluble in ethanol. The pH of a 1% aqueous solution is approximately 6.7. The color of ceftriaxone sodium solutions ranges from light yellow to amber, depending on the length of storage, concentration and diluent used. Each vial contains ceftriaxone sodium equivalent to 1 gram of ceftriaxone activity. Ceftriaxone sodium contains approximately 83 mg (3.6 mEq) of sodium per gram of ceftriaxone activity.

Antibacterial (Cephalosporin).
Pharmacology: Pharmacodynamics: Ceftriaxone is a cephalosporin/cephamycin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. Ceftriaxone has in vitro activity against gram-positive aerobic, gram-negative aerobic, and anaerobic bacteria. The bactericidal activity of ceftriaxone results from the inhibition of cell wall synthesis and is mediated through ceftriaxone binding to penicillin-binding proteins (PBPs). Ceftriaxone is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended-spectrum beta-lactamases. However, resistance to ceftriaxone usually occurs through beta-lactamase hydrolysis, altered PBPs, or reduced bacterial cell permeability. Ceftriaxone should not be mixed with or giving in the same IV line as diluents/products containing calcium as they may cause ceftriaxone to precipitate. Ceftriaxone use may also cause biliary sludge or gallbladder pseudolithiasis.
Pharmacokinetics: Pharmacokinetics in the Middle Ear Fluid: In one study, total ceftriaxone concentrations (bound and unbound) were measured in middle ear fluid obtained during the insertion of tympanostomy tubes in 42 pediatric patients with otitis media. Sampling times were from 1 to 50 hours after a single intramuscular injection of 50 mg/kg of ceftriaxone. Mean (±SD) ceftriaxone levels in the middle ear reached a peak of 35 (±12) μg/mL at 24 hours, and remained at 19 (±7) μg/mL at 48 hours. Based on middle ear fluid ceftriaxone concentrations in the 23 to 25 hour and the 46 to 50 hour sampling time intervals, a half-life of 25 hours was calculated. Ceftriaxone is highly bound to plasma proteins. The extent of binding to proteins in the middle ear fluid is unknown.

Ceftriaxone is susceptible the following organisms: Staphylococcus aureus (including beta-lactamase producing strains), Streptococcus pneumoniae, Staphylococcus epidermidis, Haemophilus influenzae, Haemophilus parainfluenzae, Escherichia coli, Proteus mirabilis, Pseudomonas aeruginosa, Proteus vulgaris, Proteus morganii, Neisseria gonorrhoeae, including both penicillinase - and nonpenicillinase-producing strains, Klebsiella pneumoniae. Streptococcus pyogenes, Clostridium species (excepting C. difficile), Serratia species, Salmonella species (including Salmonella typhi), Enterobacter species, Shigella species, Moraxella species. Group B streptococcus (Streptococcus agalactiae), Viridans group streptococci, Peptostreptococcus Haemophilus ducreyi, Neisseria meningitidis, Treponema pallidum, Fusobacterium, Bacteroides fragilis, Yersinia (including Yersinia enterocolitica), Providencia, Citrobacter, Alcaligenes, Aeromonas, Plesiomonas shigelloide.
Ceftriaxone is indicated for the treatment of the following infections: Lower Respiratory Tract Infections; Acute Bacterial Otitis Media; Skin and Skin Structure Infections; Urinary Tract Infections (complicated and uncomplicated); Uncomplicated Gonorrhea (cervical/urethral and rectal); Pelvic Inflammatory Disease caused by Neisseria gonorrhoeae; Bone and Joint Infections; Intra-Abdominal Infections; Meningitis, Septicemia.

Injection: ADULTS: The usual adult daily dose is given 1 to 2 grams by IM or IV 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 grams.
NEONATES (under 14 days from birth): The recommended dose of is 20 to 50 mg/kg/day once a day and the dose should not exceed 50 mg/kg/day.
INFANTS & CHILDREN UNDER 12 YEARS OLD: The recommended dose is 20 to 80 mg/kg/day once a day. When the dose was given over 50 mg/kg, it should be administered intravenously by infusion over a period of 30 minutes.
ELDERLY PEOPLE: The usual dose is same with for adults.
In the treatment of meningitis, it is recommended that the initial therapeutic dose be 100 mg/kg (not to exceed 4 grams). Thereafter, a total daily dose of 100 mg/kg/day (not to exceed 4 grams daily) is recommended. The daily dose may be administered once a day (or in equally divided doses every 12 hours).
Effective duration of therapy: See Table 1.

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For the treatment of uncomplicated gonococcal infections, a single intramuscular dose of 250 mg is recommended.
For preoperative use (surgical prophylaxis), a single dose of 1-2 grams administered intravenously to 2 hours before surgery is recommended.
No dosage adjustment is necessary for patients with impairment of renal or hepatic function, however, blood levels should be monitored in patients with severe renal impairment (eg, dialysis patients) and in patients with both renal and hepatic dysfunctions. In patients with estimated creatinine clearance of less than 10 mL/min, total daily dose should not exceed 2 grams.
Duration of therapy: Generally, ceftriaxone therapy should be continued for at least 48-72 hours after the signs and symptoms of infection have disappeared.

Ceftriaxone overdosage has been reported in patients with severe renal impairment. Reactions have included neurological outcomes, including encephalopathy, seizures, myoclonus, and non-convulsive status epilepticus. In the event of overdosage, discontinue ceftriaxone for injection therapy and provide general supportive treatment. In the case of overdosage, drug concentration would not be reduced by hemodialysis or peritoneal dialysis. There is no specific antidote. Treatment of overdosage should be symptomatic.

In patients who have shown allergy to the ceftriaxone; In patients with known allergy to the cephalosporin class of antibiotics; In patients with known allergy to the penicillin class of antibiotics; In patients with known allergy to the adrenalin class of local anesthetic (ex: lidocaine) - only Intramuscular Administration.

Before therapy with ceftriaxone is instituted, careful inquiry should be made to determine whether the patient has had previous hypersensitivity reactions to cephalosporins, penicillins or other drugs. 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.
Patients with renal failure and hepatic dysfunction normally require no adjustment in dosage when usual doses of ceftriaxone are administered but concentrations of drug in the serum should be monitored periodically.
There have been reports of sonographic abnormalities in the gallbladder of patients treated with ceftriaxone, some of these patients also had symptoms of gallbladder disease. These abnormalities appear on sonography as an echo without acoustical shadowing suggesting sludge or as an echo with acoustical shadowing which may be misinterpreted as gallstones. The chemical nature of the sonographically detected material has been determined to be predominantly a ceftriaxone-calcium salt. The condition appears to be transient and reversible upon discontinuation of ceftriaxone and institution of conservative management. Therefore, ceftriaxone should be discontinued in patients who develop signs and symptoms suggestive of gallbladder disease and/or the sonographic findings described previously.
Interference with Laboratory Tests: A positive Coombs' test may be seen during treatment with cephalosporins. A false-positive reaction to glucose may occur with reducing substances but not with the use of specific glucose oxidase methods.
A false-positive galactosemia test may occur like other antibiotics.

Pregnancy: Consequently, ceftriaxone should not be administered during pregnancy especially during the first trimester, without carefully weighing the expected benefits against the possible risks.
Lactation: Ceftriaxone is excreted in human milk in low concentrations. Caution should be exercised when the drug is administered to nursing mothers.

Shock: Less frequently reported were shock.
Hypersensitivity: Rash. Less frequently reported were pruritus, fever or chills.
Hematologic: Eosinophilia, thrombocytosis and leukopenia. Less frequently reported were anemia, hemolytic anemia, neutropenia, lymphopenia, thrombocytopenia and prolongation of the prothrombin time.
Hepatic: Elevations of SGOT or SGPT. Less frequently reported were elevations of alkaline phosphatase and bilirubin.
Renal: Elevations of the BUN. Less frequently reported were elevations of creatinine and the presence of casts in the urine.
Gastrointestinal: Diarrhea. Less frequently reported were nausea or vomiting, and dysgeusia. The onset of pseudomembranous colitis symptoms may occur during or after antibacterial treatment.
Respiratory system: In case taking with other cephalosporin antibiotics, PIE syndrome may occur.
Genitourinary: Moniliasis or vaginitis were reported occasionally.
Vitamin deficiency: Vitamin K deficiency, vitamin B deficiency rarely occur.
Miscellaneous: Other rarely observed reactions include leukocytosis, lymphocytosis, monocytosis, basophilia, a decrease in the colitis, flatulence, dyspepsia, palpitations and epistaxis.

Cephalosporin antibiotics at high dosage should be given with caution to patients receiving aminoglycoside antibiotics or potent diuretics such as furosemide as these combinations are thought to have an adverse effect on renal function.
There is no possibility of an accidental disulfiram-alcohol reaction.
Probenecid has no effect on elimination of Ceftriaxone.

Directions for Reconstitution: Intramuscular Administration: Dissolve ceftriaxone in 1 % lidocaine solution using more than 2 mL for 0.25 g, 0.5 g or 3.5 mL for 1 g. Prepared solution should be injected well within the body of a relatively large muscle such as the upper outer quadrant of the buttock. 1% lidocaine solution (4 mL for 1 g) may be used to avoid a pain I.M. injection. But, this solution should not be administered into a blood vessel.
Intravenous Administration: After reconstitution, each 1 mL solution contains approximately 100 mg equivalent of ceftriaxone. Ceftriaxone should be administered intravenously by infusion over a period of 30 minutes. Ceftriaxone may be mixed with these solutions (not containing calcium): 0.9% sodium chloride solution, 0.45% sodium chloride solution +2.5% dextrose, 5% dextrose, 10% dextrose, 5% dextrose with 6% dextran solution, 6-10% hydoxyethyl dextran solution, sterile water.
Ceftriaxone solutions should not be physically mixed with or piggybacked into solutions containing other antimicrobial drugs or into diluent solutions other than those previously mentioned, due to possible incompatibility. The ceftriaxone diluent solutions are stable at room temperature (25°C) for 6 hours or at 5°C for 24 hours. After reconstitution, protection from normal light is not necessary.
The color of solutions ranges from light yellow to amber, depending on the length of storage, concentration and diluent used.
Reconstitution with Water for Injection: Intramuscular Administration: Reconstitute Ceftriaxone with Water for Injection. (See Table 2.)

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After reconstitution, each 1 mL of solution contains approximately 250 mg or 350 mg equivalent of ceftriaxone according to the amount of diluent. Indicated as follows. If required, more dilute solutions could be utilized.
A 350 mg/mL concentration is not recommended for the 250 mg vial since it may not be possible to withdraw the entire contents. As with all intramuscular preparations, Ceftriaxone should be injected well within the body of a relatively large muscle; aspiration helps to avoid unintentional injection into a blood vessel.
Intravenous Administration: Ceftriaxone should be administered intravenously by infusion over a period of 30 minutes. Concentrations between 10 mg/mL and 40 mg/mL are recommended; however, lower concentrations may be used if desired. Reconstitute vials with an appropriate IV diluents. (See Table 3.)

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After reconstitution, each 1 mL solution contains approximately 100 mg equivalent of ceftriaxone. Withdraw entire contents and dilute to the desired concentration with the appropriate IV diluent.
Compatibility of Reconstituted Solution: Ceftriaxone sterile powder should be stored at temperatures not exceeding 30°C and protected from light. After reconstitution, protection from normal light is not necessary. The color of solutions ranges from light yellow to amber, depending on the length of storage, concentration and diluents used.
Ceftriaxone solutions remain stable (loss of potency less than 10%) for the following time periods: See Table 4.

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Frozen solutions should be thawed at room temperature before use. After thawing, unused portions should be discarded. DO NOT REFREEZE.
Pharmaceutical Precautions: It is preferable to use only freshly prepared solutions for both intravenous and intramuscular injection.

Store at temperatures not exceeding 30°C.

Cephalosporins

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

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