Intrataxime (Powder) Instructions for Use

Marketing Authorization Holder

LDP – Laboratorios Torlan (Spain)

Contact Information

TORLAN Laboratory (France)

ATC Code

J01DD01 (Cefotaxime)

Active Substance

Cefotaxime (Rec.INN registered by WHO)

Dosage Form

Intrataxime

Powder for solution for intravenous and intramuscular injection 1 g: vial 1, 10 or 100 pcs.

Dosage Form, Packaging, and Composition

Powder for preparation of solution for intravenous and intramuscular injection white or white with a yellowish tint, crystalline.

Vials (1) – cardboard packs.
Vials (10) – cardboard boxes.
Vials (100) – cardboard boxes.

Clinical-Pharmacological Group

Third generation cephalosporin

Pharmacotherapeutic Group

Antibiotic-cephalosporin

Pharmacological Action

Cephalosporin antibiotic of the third generation for parenteral administration. It acts bactericidally by disrupting the synthesis of the microbial cell wall. It has a broad spectrum of action.

Active against gram-positive and gram-negative microorganisms resistant to other antibiotics Acinetobacter spp., Aeromonas hydrophila, Bacillus subtilis, Bacteroides spp. (including some strains of Bacteroides fragilis), Bordetella pertussis, Borrelia burgdorferi, Citrobacter spp., Clostridium spp. (including Clostridium perfringens), Corynebacterium diphtheriae, Enterobacter spp., Enterococcus spp., Erysipelothrix insidiosa, Erysipelothrix rhusiopathiae, Escherichia coli, Eubacterium spp., Fusobacterium spp. (including Fusobacterium nucleatum), Haemophilus influenzae (including penicillinase-producing strains), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis, Morganella morganii, Neisseria gonorrhoeae (including penicillinase-producing strains). Neisseria meningitidis, Peptococcus spp., Peptostreptococcus spp., Propionibacterium spp., Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri), Pseudomonas aeruginosa, Salmonella spp., Serratia spp., some strains of Pseudomonas aeruginosa, Shigella spp., Staphylococcus epidermidis (except for methicillin-resistant Staphylococcus epidermidis and Staphylococcus aureus), Staphylococcus spp. (including Staphylococcus aureus, including penicillinase-producing strains), Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Veillonella spp., Yersinia spp. Most strains of Clostridium difficile are resistant.

Resistant to most β-lactamases of gram-positive and gram-negative microorganisms.

Pharmacokinetics

After a single intravenous administration in doses of 1 and 2 g, T_max is 30 min, C_max is 101.7 and 214 µg/ml, respectively. After intramuscular administration of a 1 g dose, T_max is 30 min and C_max is 21 µg/ml, respectively. Plasma protein binding is 30-50%. Bioavailability is 90-95%.

It creates therapeutic concentrations in most tissues (myocardium, bone tissue, skin, soft tissues) and body fluids (cerebrospinal, synovial, pericardial, pleural, sputum, bile, urine). It penetrates the blood-brain barrier. V_d is 0.25-0.39 l/kg.

T_1/2 is 1 h with intravenous administration and 1-1.5 h with intramuscular administration. It is excreted by the kidneys – 20-36% unchanged, the rest as metabolites (15-25% as the pharmacologically active desacetylcefotaxime and 20-25% as two inactive metabolites – M2 and M3).

Bactericidal concentration in the blood persists for more than 12 hours.

In chronic renal failure and in elderly individuals, T_1/2 increases by 2 times. T_1/2 in newborns is 0.75-1.5 h, in premature infants (body weight less than 1500 g) it increases to 4.6 h; in children with body weight over 1500 g it is 3.4 h. With repeated intravenous administrations of 1 g every 6 h for 14 days, no accumulation is observed. It penetrates into breast milk.

Indications

Severe bacterial infections caused by susceptible microorganisms:

• Infections of the respiratory tract and ENT organs;
• Urinary tract infections;
• Septicemia, bacteremia, sepsis;
• Endocarditis;
• Intra-abdominal infections (including peritonitis);
• CNS infections (meningitis);
• Infections of the skin and soft tissues, bones, joints;
• Pelvic organ infections;
• Chlamydia;
• Gonorrhea;
• Infected wounds and burns;
• Lyme disease (borreliosis);
• Salmonellosis;
• Infections against the background of immunodeficiency;
• Prevention of infections after surgical operations (including urological, obstetric-gynecological, gastrointestinal).

ICD codes

Dosage Regimen

Intramuscularly and intravenously.

For intramuscular administration, dissolve 1 g of Intrataxime in 4 ml of sterile water for injections, administer deep into the gluteal muscle. A 1% lidocaine solution (4 ml per 1 g) is also used as a solvent for intramuscular administration.

For intravenous administration, dissolve 1 g of Intrataxime in 4 ml of sterile water for injections. Administer slowly over 3-5 minutes.

For drip infusion (over 50-60 minutes), dissolve 2 g of the drug in 100 ml of 0.9% sodium chloride solution or 5% dextrose solution, Ringer’s solution, sodium lactate, dextrans with molecular weights of 50-70 kDa and 30-40 kDa.

For the purpose of preventing the development of infections before surgery, administer a single dose of 1 g during induction of general anesthesia. If necessary, the administration is repeated after 6-12 hours.

For cesarean section – at the moment of clamping the umbilical vein – intravenously 1 g, then after 6 and 12 hours after the first dose – an additional 1 g each.

In case of creatinine clearance (CrCl) of 20 ml/min/1.73 m² or less, the daily dose is reduced by half.

Adults and children with body weight of 50 kg and more: for uncomplicated infections, as well as for urinary tract infections – intramuscularly or intravenously 1 g every 8-12 hours; for uncomplicated acute gonorrhea – intramuscularly 1 g as a single dose; for moderate infections – intramuscularly or intravenously 1-2 g every 12 hours; for severe infections, such as meningitis – intravenously 2 g every 4-8 hours, maximum daily dose – 12 g. The duration of treatment is determined individually.

Children with body weight under 50 kg – 50-180 mg/kg body weight/day.

For premature and newborn infants up to 1 week – intravenously 50 mg/kg every 12 hours; at age 1-4 weeks – intravenously 50 mg/kg every 8 hours.

Adverse Reactions

Allergic reactions: urticaria, chills or fever, rash, skin itching; rarely – eosinophilia, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), angioedema, anaphylactic shock.

From the nervous system: headache, dizziness.

Local reactions: phlebitis, pain along the vein, pain and infiltrate at the intramuscular injection site.

From the urinary system: impaired renal function, oliguria, interstitial nephritis.

From the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbacteriosis, impaired liver function; rarely – stomatitis, glossitis, pseudomembranous colitis, increased activity of hepatic transaminases and alkaline phosphatase, hyperbilirubinemia.

From the hematopoietic organs: hemolytic anemia, leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hypocoagulation.

Laboratory parameters: azotemia, increased blood urea concentration, hypercreatininemia, positive Coombs test.

Other: superinfection (in particular, candidal vaginitis).

Contraindications

• In children under 2.5 years, intramuscular administration of the drug should not be used;
• Hypersensitivity (including to penicillins, cephalosporins, carbapenems).

With caution

Impaired renal and liver function, neonatal period (for intravenous administration), gastrointestinal diseases, especially colitis, ulcerative colitis (including in history).

Use in Pregnancy and Lactation

The use of the drug during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.

It is excreted in breast milk in low concentrations, therefore, if it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.

Use in Renal Impairment

In case of creatinine clearance (CrCl) of 20 ml/min/1.73 m² or less, the daily dose is reduced by half.

Pediatric Use

Children with body weight under 50 kg – 50-180 mg/kg body weight/day.

For premature and newborn infants up to 1 week – intravenously 50 mg/kg every 12 hours; at age 1-4 weeks – intravenously 50 mg/kg every 8 hours.

Special Precautions

Before prescribing the drug, it is necessary to collect an allergic history, especially regarding beta-lactam antibiotics. Cross-allergy between penicillins and cephalosporins is known. In individuals with a history of allergic reactions to penicillin, the drug should be used with extreme caution.

If hypersensitivity reactions occur (which can be severe and even fatal), the drug should be discontinued.

If the duration of treatment with the drug exceeds 18 days, it is necessary to monitor the peripheral blood picture.

A false-positive Coombs test is possible.

When determining glucose in urine by a non-enzymatic method (e.g., Benedict’s method), false-positive results are possible.

Overdose

Symptoms: convulsions, encephalopathy (in case of administration of large doses, especially in patients with renal failure), tremor, increased neuromuscular excitability.

Treatment: symptomatic.

Drug Interactions

Increases the risk of bleeding when combined with antiplatelet agents, NSAIDs.

The likelihood of kidney damage increases with simultaneous use of aminoglycosides, polymyxin B and “loop” diuretics.

Drugs that block tubular secretion increase plasma concentrations of Intrataxime and slow its excretion.

Pharmaceutically incompatible with solutions of other antibiotics in the same syringe or dropper.

Storage Conditions

List B. Store in places inaccessible to children, in a light-protected place at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years.

For intramuscular injections: the sterile powder of Intrataxime after dilution in water or lidocaine solution is chemically stable for 8 hours (at room temperature not exceeding 25°C (77°F)) or for 24 hours (at temperature from 2°C (35.6°F) to 8°C (46.4°F), in a light-protected place).

For injections or infusions when dissolved in water for injections: for 12 hours (at room temperature not exceeding 25°C (77°F)) or for 24 hours (at temperature from 2°C (35.6°F) to 8°C (46.4°F), in a light-protected place). A pale yellow tint of the solution does not mean a decrease in antibiotic activity.

For infusions in infusion solutions: the sterile powder of Intrataxime is chemically stable for 8 hours after dilution in Haemaccel solution, Ionosteril and for 6 hours after dilution in 10% dextrose solution, dextrans with molecular weights of 50-70 kDa and 30-40 kDa.

Note: it is necessary to ensure aseptic conditions when diluting the drug and preparing solutions (especially if the diluted Intrataxime is not administered immediately).

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.