Rezibelacta (Powder) Instructions for Use

Marketing Authorization Holder

Laboratorios Atral, S.A. (Portugal)

ATC Code

J01DD01 (Cefotaxime)

Active Substance

Cefotaxime (Rec.INN registered by WHO)

Dosage Form

Rezibelacta

Powder for solution for intravenous and intramuscular administration 1 g: vial. 1 pc.

Dosage Form, Packaging, and Composition

1 g – 10 ml vials (1) – cardboard packs.
1 g – 10 ml vials (50) – cardboard boxes.

Clinical-Pharmacological Group

Third generation cephalosporin

Pharmacotherapeutic Group

Antibiotic-cephalosporin

Pharmacological Action

Cefotaxime is a broad-spectrum third-generation cephalosporin antibiotic. It exerts a bactericidal effect by inhibiting the synthesis of the bacterial cell wall.

The mechanism of action is due to the acetylation of membrane-bound transpeptidases and disruption of the cross-linking of peptidoglycans, which is necessary to ensure the strength and rigidity of the cell wall.

It is highly active against gram-negative bacteria (resistant to other antibiotics): Escherichia coli, Citrobacter spp., Proteus mirabilis, Providencia spp., Klebsiella spp., Serratia spp., some strains of Pseudomonas spp., Haemophilus influenzae.

It is less active against Streptococcus spp. (including Streptococcus pneumoniae), Staphylococcus spp., Neisseria meningitidis, Neisseria gonorrhoeae, Bacteroides spp.

It is resistant to the action of most beta-lactamases.

Pharmacokinetics

It is rapidly absorbed from the injection site. Plasma protein binding is 40%.

It is widely distributed in body tissues and fluids. It reaches therapeutic concentrations in the cerebrospinal fluid, especially in meningitis.

It crosses the placental barrier and is excreted in breast milk in low concentrations. It is partially metabolized in the liver.

40-60% of the dose is excreted unchanged in the urine within 24 hours, 20% is excreted as metabolites.

Indications

Severe infectious and inflammatory diseases caused by microorganisms sensitive to cefotaxime, including peritonitis, sepsis, abdominal infections and pelvic infections, lower respiratory tract infections, urinary tract infections, bone and joint infections, skin and soft tissue infections, infected wounds and burns, gonorrhea, meningitis, Lyme disease.

Prevention of infections after surgery.

ICD codes

Dosage Regimen

Administer the intravenous or intramuscular route. Adjust the dosage based on infection severity, causative organism, and patient renal function.

For adults and children weighing over 50 kg, the usual dose is 1 g to 2 g every 4 to 12 hours. For severe infections, such as sepsis or meningitis, increase the dose and frequency.

For children weighing less than 50 kg, administer 50 mg/kg to 180 mg/kg per day in 2 to 6 divided doses. For meningitis, use the higher end of the dosage range.

Do not exceed the maximum daily dose of 12 g for adults. Do not exceed the maximum daily dose of 180 mg/kg for children under 50 kg.

In patients with severe renal impairment (creatinine clearance less than 20 mL/min), reduce the dose by half after an initial standard loading dose.

For surgical prophylaxis, administer a single 1 g dose intravenously 30 to 90 minutes before the procedure.

For uncomplicated gonorrhea, administer a single 1 g dose intramuscularly.

Adverse Reactions

From the digestive system: nausea, vomiting, diarrhea, transient increase in the activity of hepatic transaminases, cholestatic jaundice, hepatitis, pseudomembranous colitis.

Allergic reactions: skin rash, itching, eosinophilia; rarely – angioedema.

From the hematopoietic system: with prolonged use in high doses, changes in the peripheral blood picture are possible (leukopenia, neutropenia, thrombocytopenia, hemolytic anemia).

From the blood coagulation system: hypoprothrombinemia.

From the urinary system: interstitial nephritis.

Effects due to chemotherapeutic action: candidiasis.

Local reactions: phlebitis (with intravenous administration), pain at the injection site (with intramuscular administration).

Contraindications

Hypersensitivity to cefotaxime and other cephalosporins.

Use in Pregnancy and Lactation

The use of cefotaxime is not recommended in the first trimester of pregnancy.

Use in the second and third trimesters of pregnancy and during lactation is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus or breastfed infant.

It should be borne in mind that after intravenous administration of cefotaxime at a dose of 1 g, the maximum concentration of the active substance in breast milk after 2-3 hours averages 0.32±0.09 µg/ml. At this concentration, a negative effect on the oropharyngeal flora of the child is possible.

In experimental studies on animals, no teratogenic or embryotoxic effects of cefotaxime were found.

Use in Renal Impairment

Cefotaxime should be used with caution in renal impairment.

Pediatric Use

Cefotaxime should be used with caution in newborns.

Special Precautions

Cefotaxime should be used with caution in renal impairment, history of colitis, and in newborns.

In patients with hypersensitivity to penicillins, allergic reactions to cephalosporin antibiotics are possible.

During treatment, a positive direct Coombs test and a false-positive urine glucose reaction are possible.

It should be used with caution concomitantly with “loop” diuretics.

Drug Interactions

Cefotaxime, by suppressing the intestinal flora, interferes with the synthesis of vitamin K. Therefore, with simultaneous use with drugs that reduce platelet aggregation (NSAIDs, salicylates, sulfinpyrazone), the risk of bleeding increases.

For the same reason, when used concomitantly with anticoagulants, an enhancement of the anticoagulant effect is noted.

With simultaneous use with aminoglycosides, polymyxin B and “loop” diuretics, the risk of kidney damage increases.

With simultaneous use with drugs that reduce tubular secretion, the concentration of cefotaxime in the blood plasma increases.

Probenecid slows down the excretion of cefotaxime by reducing its tubular secretion.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.