Viatrex

Each vial contains: Ceftriaxone (as sodium) 1 g.

Pharmacology: Pharmacokinetics: Ceftriaxone demonstrates non-linear 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. 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 the 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.

Susceptible strains: Staphylococcus aureus (including penicillinase-producing strains), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus group A (Streptococcus pyogenes), Streptococcus group B (Streptococcus agalactiae), Streptococcus viridans, Streptococcus bovis, Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis, Citrobacter spp., Enterobacter spp. (some strains are resistant), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae (including Ampicillin resistant strains). Haemophilus parainfluenzae, Klebsiella spp. (K. pneumoniae), Moraxella spp., Proteus morganii, Proteus mirabilis, Proteus vulgaris, Providencia spp., Neisseria gonorrhoeae (including penicillinase-producing strains), Neisseria meningitidis, Plesiomonas shigelloides, Pseudomonas aeruginosa (some strains are resistant), Salmonella spp. (including S. typhi), Serratia spp. (including S. marcescens), Shigella spp., Yersinia spp. (including Y. Enterocolitica), Treponema pallidum, Bacteroides spp. (including some strains of B. Fragilis), Clostridium spp. (except C. difficile), Fusobacterium (except F. mortiferum and F. varium), Peptococcus, Peptostreptococcus.
Main indications: For the treatment of susceptible infections such as chancroid, endocarditis, gastro-enteritis (invasive salmonellosis; shigellosis), gonorrhea, Lyme disease, meningitis (including meningococcal meningitis prophylaxis), septicaemia, surgical infection (prophylaxis), syphilis, typhoid fever and Whipple's disease.

It is administered as the sodium salt by intermittent intravenous infusion over 30 minutes or by deep intramuscular injection. Doses are expressed in terms of the equivalent amount of ceftriaxone. It is usually given to adults in a dose of 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. Children may be given 50 to 75 mg per kg body-weight daily in two divided doses; the total daily dose should not exceed 2 g. For the treatment of meningitis in children, ceftriaxone may be given in a dose of 100 mg per kg daily in two divided doses, sometimes with a loading dose of 75 mg per kg; the total daily dose should not exceed 4 g.
A single intramuscular dose of 250 mg is recommended for the treatment of gonorrhea in adult. For surgical infection prophylaxis in adults, a single dose of 1 g is administered 0.5 to 2 hours prior to surgery.
A reduction in dosage may be necessary in patients with severe renal failure and in those with both impaired renal and hepatic function; plasma concentrations should be monitored in such patients.

Ceftriaxone injection is contraindicated in patients with known hypersensitivity to the cephalosporins class of antibiotics. Hyperbilirubinemic neonates, particularly those who are premature. Neonates less than 28 days old if they are receiving calcium containing IV products.

Patients with history of hypersensitivity to ceftriaxone or Cephalosporin antibiotics.
Should be given cautiously in the following cases: Patients with history of penicillin allergy.
Patient with severe renal disorder (as the plasma concentration maintained for a long period of time. Decreased dosage or increased interval between treatments are required).
Patient with poor oral ingestion or parenteral nutrition patients and elderly patients (cautious monitoring is required since Vitamin K deficiency may occur).
Use with caution in patients with gallbladder, biliary tract, liver or pancreatic disease.
Super infections may occur with prolonged or repeated therapy.
Use in Pregnancy: Since safety use in pregnancy has not been established, ceftriaxone should be used during pregnancy only when the expected benefits clearly outweigh the potential risks.
Use in Lactation: Small amount of the drug has been distributed in human milk. Therefore the administration to nursing mothers should be avoided since it may displace bilirubin and cause kernicterus.

Use in Pregnancy: Since safety use in pregnancy has not been established, ceftriaxone should be used during pregnancy only when the expected benefits clearly outweigh the potential risks.
Use in Lactation: Small amount of the drug has been distributed in human milk. Therefore the administration to nursing mothers should be avoided since it may displace bilirubin and cause kernicterus.

Shock: As shock may rarely occur, cautious monitoring is required, and in case that unpleasantness, stridor, dizziness, tenesmus, tinnitus, perspiration, etc., occur, further administration should be discontinued and appropriate measure should be taken.
Hypersensitivity: In case of exanthema, urticaria, erythema, flare, pruritus, shivering, fever, allergic dermatitis, edema, erythema multiforme, anaphylactic or anaphylactic like reaction occur, further administration should be discontinued and appropriate measure should be taken.
Blood: Occasionally granulocytopenia, eosinophilia, thrombocytosis, leukopenia, rarely anemia, hemolytic anemia, thrombocytopenia, prothrombin abnormality may occur.
Liver: Occasionally elevation of GOT, AL-P and symptomatic precipitation of ceftriaxone calcium salt in gall bladder rarely elevation of bilirubin, γ-GTP may occur.
Kidney: As severe renal disorder such as acute renal insufficiency is reported rarely, caution monitoring is required and if abnormality is acknowledged further administration should be discontinued and appropriate measures should be taken.
GI System: Rarely severe enterocolitis such as pseudomembranous enterocolitis may occur. If abdominal pain and frequent diarrhea occur, appropriate measures such as immediate discontinuation of Ceftriaxone should be taken.
Occasionally nausea, vomiting, loose stools, diarrhea or rarely abdominal pain, anorexia, etc. have occurred.
Respiratory System: In administration of other cephalosporin series antibiotics, interstitial pneumonia accompanied with flush, cough, dyspnea, disorder of chest X-ray, eosinophilia, and PIE syndrome may occur rarely. If those symptoms occur the administration should be discontinued and/or appropriate therapy including the administration of adrenocortical hormone should be instituted.
Superinfection: Rarely stomatitis, candidiasis may occur.
Avitaminosis: Rarely, avitaminosis K (e.g. hypoprothrombinemia, bleeding tendency) and vitamin B deficiency (e.g. Glossitis, stomatitis, anorexia, neuritis, etc.) may occur.
Others: Occasionally headache and rarely dizziness, edema, precipitation in gallbladder, ventricular extrasystole, elevated creatinine of blood, genital mycosis may occur.

Direction for Reconstitution: Intramuscular Administration: For 1 g vial, inject 1% Lidocaine solution (3.5 mL) into the vial and shake vial thoroughly to form solution. Do not inject intravenously if reconstituted with Lidocaine.
Intravenous Administration: Ceftriaxone injection should be administered intravenously by infusion over a period of 30 minutes. Inject Sterile Water for Injection (10 mL) into vial, shake vial thoroughly to form solution. 2 g may be dissolved in 40 mL of the following calcium-free solution. A saline solution, 0.45% NaCl and 2.5% Glucose solution, 5% Glucose solution, 10% Glucose solution, 5% Glucose solution containing 6% Dextrin solution, Hydroxyethyl starch or Water for Injection. Ceftriaxone injection should not be physically mixed with solutions containing other antimicrobial drugs into diluent solutions other than those mentioned previously, due to possible incompatibility.
Reconstituted solutions retain their physical and chemical stability for six hours or 24 hours at 25°C. As a general rule, however, the solution should be used immediately after preparation.
They range in color from pale yellow to amber, depending on the concentration and the length of storage. This characteristic of the active ingredient is of no significance for the efficacy or tolerance of the drug.

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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