Macfin Ceftriazone Injection

MACFIN® INJECTION
Ceftriazone Injection 1g

 
Composition

Each vial contains:
Ceftriaxone Sodium BP
Equivalent to Anhydrous Ceftriaxone lg

 
Clinical Pharmacology

Ceftriaxone is a third generation cephalosporin antibacterial used for the treatment of susceptible infections. Ceftriaxone is a representative third-generation cephalosporin antibiotic.

The bactericidal activity of ceftriaxone results from inhibition of cell wall synthesis. Ceftriaxone has a high degree of stability in the presence of betalactamases, both penicillinases and cephalosporinases, of gram-negative and gram- positive bacteria. Ceftriaxone has been shown to be active against most strains of the micro-organisms, both in-vitro and in clinical infections.

 

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 lg 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 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 (cerebro spinal fluid). 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.

 
Indications and Usage

MACFIN is used for the treatment of susceptible infections and serious infections due to sensitive bacteria. They include chancroid, endocarditis, gastro-enteritis (invasive salmonellosis; shigellosis), gonorrhea, Lyme disease, meningitis (including meningococcal meningitis prophylaxis), pneumonia, septicaemia, syphilis, typhoid fever, and Whipple’s disease.

It is also used for surgical infection prophylaxis.

 
Administration and Dosage

MACFIN is given 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 1g is to be injected intramuscularly then the dose should be divided between more than one site.

The usual adult dose is 1 to 2g daily as a single dose or in two divided doses; in severe infections up to 4g daily may be given.

Doses for infants and children (under 50kg) are 20 to 50mg/kg once daily; for severe infections up to 80mg/kg daily may be given.

In neonates, the maximum dose should not exceed 50mg/kg daily; intravenous doses in neonates should be given over 60 minutes. Doses above 50mg/kg should be given by intravenous infusion only.

A single intramuscular dose of 250mg is recommended for the treatment of uncomplicated gonorrhea in adults.

For surgical infection prophylaxis in adults, a single dose of 1g may be given 0.5 to 2 hours before surgery; a 2g dose is suggested before colorectal
surgery.

For the prevention of secondary cases of meningococcal meningitis, a single intramuscular dose of 250mg may be used for adults and 125mg for children.

 
Reconstitution and Administration

For intravenous (I.V.) use: Reconstitute with 10ml water for injection.

For intramuscular (I.M.) use: Reconstitute with 3.5ml diluent containing 1% Lidocaine Hydrochloride.

 
Advice

When reconstituted with Lidocaine Hydrochloride, the solution must never be administered intravenously.

– Intramuscular doses over 1g should be divided between more than one site.

– Administer by intravenous infusion over 60 minutes in neonates.

– Once the solution is made use immediately.

 
Contraindications

Cefalosporin hypersensitivity; porphyria; neonates with jaundice, hypoalbuminaemia, acidosis or impaired bilurubin binding.

 
Precautions

Sensitivity to beta-lactam antibacterials (avoid if history of immediate hypersensitivity reaction); severe renal impairment; hepatic impairment if accompanied by renal impairment; premature neonates; may displace bilurubin from serum albumin; treatment longer than 14 days, renal failure, dehydration, pregnancy and breastfeeding; false positive urinary glucose (if tested for reducing substances) and false positive Coombs’ test.

 
Adverse Effects

Diarrhoea, nausea and vomiting, abdominal discomfort, headache; antibiotic associated colitis (particularly with higher doses); allergic reactions including rashes, pruritus, urticaria, serum sickness – like reaction, fever and arthralgia, and anaphylaxis; transient hepatitis and cholestatic jaundice; eosinophillia and blood disorders (including thrombocytopenia, leukopenia, agranulocytosis, applastic anaemia, and haemolytic anaemia); reversible interstitial nephrititis, hyperactivity, nervousness, sleep disturbances, confusion, hypertonia and dizziness, calcium ceftriaxone precipitates in urine (particularly in very young, dehydrated), or those who are immobilized or in gall bladder – consider discontinuation if symptomatic; rarely prolongation of prothrombin time, pancreatitis.

 
Warnings

The Lidocaine solution must never be administered intravenously.

 
Administration in hepatic and renal impairment

A reduction in dosage of ceftriaxone may be necessary in patients with severe renal impairment, in whom the daily dose should not exceed 2g, and in those with both renal and hepatic impairment; plasma concentrations should be monitored in such patients.

 
Pregnancy

Not known to be harmful.

 
Breastfeeding

Excreted in low concentrations; safe in usual dosage; monitor infants.

 
Drug Interactions

– Contraceptives, Oral: Contraceptive effect of estrogens is possibly reduced (risk is probably small).

– Warfarin: Possibly enhancing anticoagulant effect

– Disulfiram-like reaction: Ceftriaxone may lead to a disulfiram – like reaction when administered in some patients drinking wine or taking drugs containing alcohol. In that, drinking wine or taking drugs containing alcohol should be avoided when using this product and several days after the use.

 
Overdose and Antidote

In the case of over-dosage, drug concentration would not be reduced by haemodialysis or peritoneal dialysis. There is no specific antidote. Treatment of over-dosage should be symptomatic.

 
Presentation

MACFIN: Each pack contains one vial ceftriaxone 1g; two diluent ampoules 10ml water for injection and 3.5ml 1% Lidocaine Hydrochloride for injection.

 
Storage

Store below 25oC. Protect from light. Do not freeze.
Keep out of the reach of children.

 
Manufactured by

Reyoung Pharmaceutical Co. Ltd.

No. 6, Erlangshan Road, Yiyuan,

Shandong, P.R. China.

 

Marketed by

Pacmai Int’l Ltd.

No. 8, Alhaji Yusuf Adebayo Street,

Olodi-Apapa, Lagos, Nigeria.

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