Ceftriaxone for injection USP
Each vial contains ceftriaxone sodium (Sterile) equivalent to ceftriaxone 1g.
Each diluent ampoule contains 10mI sterile water for injection.
MECHANISM OF ACTION
Ceftriaxone is a third generation cephalosporin that exerts its action by blocking the cross linking of the peptidoglycan component of the bacterial cell wall necessary for its synthesis. It is bactericidal in action. It has considerable stability against degradation by most bacterial beta-lactamases.
SPECTRUM OF ACTIVITY
Ceftriaxone has activity on both gram positive and gram negative organisms. Its spectrum of activity includes both aerobic and anaerobic species. This includes: Staphylococcus aureus; Staphylococcus epidermidis; (Only Methiclilin susceptible strains of Staphylococci are sensitive to ceftriaxone); Neisseria gonorrhoeae, Escherichia coli; Proteus mirabilis; Proteus vulgaris; Streptococcus pneumoniae; Streptococcus pyrogenes (Group A); Streptococcus agalactiae (Group B); Haemophilus influenza; Haemophilus parainfluenza; and klebsiella pneumoniae; Clostridium spp. (except C. Difficile); Fusobacterium spp. (except F mortfierum and F varium); Peptococcus spp.
Lyntriaxone is indicated in the following conditions when caused by susceptible organisms: lower respiratory tract infections (pneumonia, bronchitis); septicaemia; meningitis; bone, skin and soft tissue infections; gonorrhoea; perioperative prophylaxis of infections associated with surgery; renal and urinary tract infections; pelvic inflammatory disease; abdominal infection (peritonitis, infections of the biliary tract).
DOSAGE AND ADMINISTRATION
The usual adult (and children over l2 years of age) dose is 1g once daily. In severe infections, the dose can be increased to 2-4g daily. For children less than l2 years of age the standard dose is 20-50mg / kg body weight / day given once daily. In severe infections doses up to 80mg / kg body weight / day can be given through slow intravenous infusion over a period of at least 30 minutes. The duration of therapy varies with the course of the disease. Usually Lyntriaxone should be continued for at least 48 hours after the eradication of the bacteria is observed.
Lyntriaxone can be given both through slow intravenous injection, slow intravenous infusion, or by deep intramuscular injection.
For intravenous injection, 1g of Lyntriaxone should be mixed with 10ml sterile water for injection and administered slowly over 2-4 minutes directly into the vein.
The injection should be given freshly prepared.
For intravenous infusion, 1-2g of Lyntriaxone should be dissolved in 40ml of calcium free solution which may include 5 or 10% dextrose in water or normal saline. The infusion should be given over a period of at least 30 minutes. Solutions containing Lyntriaxone should not be mixed with solutions containing other substances especially calcium containing substances like Hartmann’s and Ringer’s solutions.
For intramuscular injection, 1g of Lyntriaxone should be dissolved in 3.5m1 of 1% lignocaine hydrochloride BP The injection should be given by deep intramuscular injection. Lyntriaxone in lignocaine solution should not be given intravenously. If more than 1g is to be given, the dosage should be divided and be given on more than one site.
Mean plasma concentration after 1g intravenous dose administration is about 200mg/l. When 2g infusion is given over 30 minutes, mean concentration of 250mg /l is achieved.
About 60% of Lyntriaxone dose is excreted unchanged in the urine and the rest through biliary and intestinal tracts. The mean plasma half life is 8 hours.
CONTRA-INDICATIONS, PRECAUTIONS, SIDE EFFECTS, WARNINGS, ETC
Precautions and contra-indications: Lyntriaxone should not be given to patients with known hypersensitivity to cephalosporins and penicillins. In rare cases of anaphylactic reactions, counter measures like the use of adrenalin followed by corticosteroid therapy should immediately be administered. The stated dosage should not be exceeded. Lyntriaxone is contraindicated in pre-mature infants and in full term infants below 2 months of age. It should not be given to neonates due to possible displacement of bilirubin from serum albumin.
In the case of concomitant presence of renal and hepatic impairment, the plasma concentration of Lyntriaxone should be monitored and the dose adjusted accordingly. No dose adjustment is necessary if only one of the above stated impairments is present.
However in severe renal failure (creatinine clearance less than 10ml per minute) the possible maximum daily dose should be 2g.
Drug Interactions: Alcohol, anticoagulants.
Side effects and adverse reactions: Lyntriaxone is usually well tolerated with side effects mild and transient. The most commonly complained of are:
Gastro-intestinal tract disorders
Headache, dizziness and drug fever
Super infections such as Clostridium difficile pseudo membranous colitis could, though rarely occur
Pain and discomfort may be experienced at the site of intramuscular injection.
Treatment of overdose: There is no specific antidote. Treatment should be symptomatic.
Packaging: Lyntriaxone is packed as 1g vial with l ampoule l0ml sterile water for injection per pack.
Storage: Lyntriaxone should be stored below 25 degrees Celsius away from light and moisture. Avoid freezing and keep away from children.
Giant Pharmaceutical Ltd
CSPC Zhongnuo Pharmaceutical
No. 188 Gongnong Road, Shijiazhuang City, China
Lyn-edge Pharmaceuticals Ltd
113 Old Aba Road Part Harcourt, Nigeria