Rophin

Each vial contains Ceftriaxone sodium equivalent to ceftriaxone 1 g.

Pharmacology: Pharmacokinetics: Ceftriaxone demonstrates nonlinear dose-dependent pharmacokinetics because of its protein binding; about 85 to 95% is bound to plasma proteins 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 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.

Ceftriaxone is used for the treatment of susceptible infections such as chancroid, endocarditis, gastroenteritis (invasive salmonellosis; shigellosis), gonorrhoea, Lyme disease, meningitis (including meningococcal meningitis prophylaxis), pneumonia, septicaemia, syphilis, typhoid fever, and Whipple's disease. It is also used for surgical infection prophylaxis.

Ceftriaxone is given as the sodium salt by slow intravenous injection over at least 2 to 4 minutes, by intermittent intravenous infusion over at least 30 minutes, or by deep intramuscular injection. If more than 1 g is to be injected intramuscularly then the dose should be divided between more than one site.
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 may be given.
Doses for infants and children (under 50 kg) are 20 to 50 mg/kg once daily; for severe infections up to 80 mg/kg daily may be given.
In neonates, the maximum dose should not exceed 50 mg/kg daily; intravenous doses in neonates should be given over 60 minutes.
Doses above 50 mg/kg should be given by intravenous infusion only.
For the treatment of uncomplicated gonorrhoea, a single intramuscular dose of 250 mg is recommended.
For surgical infection prophylaxis, a single dose of 1 g may be given 0.5 to 2 hours before surgery; a 2-g dose is suggested before colorectal surgery.
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.

In the case of overdose nausea, vomiting, diarrhea can occur.
Treatment of Intoxication: 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.

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

Deposition of the calcium salt has occurred rarely in the urine. Isolated cases of death in term or premature neonates have been associated with precipitation of calcium ceftriaxone in lungs and kidneys, and in some of these cases a calcium-containing product has been given by a different route or line, or at a different time. US licensed product information therefore contraindicates the use of ceftriaxone within 48 hours of products or solutions containing calcium, particularly in neonates. Ceftriaxone is highly protein bound and is able to displace bilirubin from albumin binding sites, causing hyperbilirubinaemia; its use should be avoided in jaundiced neonates.

The most common side effects were systemic (gastro intestinal and hematological changes) like loose stools/diarrhea, nausea, vomiting, allergic dermatitis, pruritus, urticaria, oedema and local like inflammatory reactions in the vein wall after IV administration may occur.
Ceftriaxone for injection should not be used in neonates (especially prematures) at risk of developing bilirubin encephalopathy.
Changes in bowel flora may be more marked than with cefotaxime because of the greater biliary excretion of ceftriaxone; diarrhoea may occur more often, especially in children. Biliary sludge or pseudolithiasis due to a precipitate of calcium ceftriaxone has been seen occasionally in patients given ceftriaxone.
Neutropenia has been reported with most cephalosporins; a complex mechanism has been attributed to that associated with ceftriaxone. There have been rare reports of fatal haemolysis associated with ceftriaxone.
Although ceftriaxone has a N-methylthiotriazine ring rather than a N-methylthiotetrazole side-chain, it might still have the potential to cause hypoprothrombinaemia.

Ceftriaxone has a 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.

Method of Reconstitution: For Intramuscular injection: Reconstitute with 3.6 mL of sterile water for injection.
For Intermittent Intravenous infusion: Reconstitute with 10 mL of sterile water for injection.
For single use, only. Discard any unused contents.

Store at temperature not exceeding 30°C.
Reconstituted solution: Store at temperatures between 2°C to 8°C and use within 24 hours.

Cephalosporins

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

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