Polymyxin B (Lyophilisate, Powder) Instructions for Use

ATC Code

J01XB02 (Polymyxin B)

Active Substance

Polymyxin B

Polymyxin B (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antibiotic of the polypeptide group

Pharmacotherapeutic Group

Systemic antibacterial agents; other antibacterial agents; polymyxins

Pharmacological Action

An antibiotic of polypeptide structure.

The mechanism of action is mainly due to the blockade of the permeability of the cytoplasmic membrane of bacterial cells, which leads to their destruction.

It is active against most gram-negative bacteria: Escherichia coli, Enterobacter spp., Klebsiella spp., Haemophilus influenzae, Bordetella pertussis, Salmonella spp., Shigella spp.; it is especially active against Pseudomonas aeruginosa.

Vibrio cholerae (except for Vibrio cholerae eltor) and Coccidioides immitis are also sensitive to polymyxin B, but most fungi are resistant to this antibiotic.

Serratia marcescens, Providencia spp., Bacteroides fragilis are usually resistant. It is not active against Proteus spp., Neisseria spp., obligate anaerobic and gram-positive bacteria.

It exhibits cross-resistance with colistin.

Pharmacokinetics

After intramuscular administration, the maximum plasma concentration (C_max) is reached within 2 hours. Plasma protein binding is 50%.

It penetrates poorly through tissue barriers and does not cross the blood-brain barrier.

It crosses the placenta in small amounts and is excreted in breast milk.

It is not metabolized.

It is excreted by the kidneys unchanged (60% within 3-4 days) and through the intestines.

The elimination half-life (T_1/2) is 3-4 hours; in severe renal failure, it is 2-3 days.

It does not accumulate upon repeated administration.

Indications

Severe infectious and inflammatory diseases caused by gram-negative microorganisms sensitive to polymyxin B with multiple resistance to other antibiotics: sepsis, meningitis, pneumonia, skin and soft tissue infections, including wound infections, infections in burn patients.

ICD codes

Dosage Regimen

Administer intravenously, intramuscularly, or intrathecally based on infection severity and pathogen susceptibility.

For intravenous infusion, reconstitute lyophilisate with Sterile Water for Injection. Further dilute in 300-500 mL of 5% Dextrose Injection. Infuse over 60-90 minutes.

For intramuscular injection, administer deep into a large muscle mass. Rotate injection sites to minimize local reactions.

For intrathecal administration, use solutions prepared with 0.9% Sodium Chloride Injection without preservatives. Strictly adhere to aseptic technique.

The adult and pediatric daily intravenous or intramuscular dose is 15,000-25,000 units/kg/day. Divide the total daily dose and administer every 12 hours. The maximum total daily dose must not exceed 2,000,000 units (200 mg).

For adult meningitis requiring intrathecal therapy, administer 50,000 units once daily for 3-4 days, then 50,000 units every other day. Continue for at least 2 weeks after obtaining negative cerebrospinal fluid cultures.

For pediatric meningitis (age 2 years and older), the intrathecal dose is 20,000 units once daily for 3-4 days or 25,000 units every other day. For infants under 2 years, the intrathecal dose is 20,000 units once daily for 3-4 days or 25,000 units every other day.

Adjust dosage in renal impairment. Reduce the dose or extend the dosing interval based on the degree of renal dysfunction. Monitor serum drug concentrations to guide therapy.

The duration of therapy is typically 7-14 days but depends on the clinical response. Do not exceed the recommended dosage or duration due to the risk of nephrotoxicity and neurotoxicity.

Adverse Reactions

Nervous system disorders: dizziness, ataxia, impaired consciousness, drowsiness, paresthesia, neuromuscular blockade.

Urinary system disorders: albuminuria, cylindruria, azotemia, proteinuria, renal tubular necrosis.

Respiratory system disorders: paralysis of respiratory muscles, apnea.

Digestive system disorders: epigastric pain, nausea, decreased appetite, pseudomembranous colitis.

Allergic reactions: skin rash, itching, eosinophilia.

Local reactions: phlebitis, periphlebitis, thrombophlebitis, pain at the intramuscular injection site.

Other: visual disturbances, superinfection, candidiasis; with intrathecal administration – meningeal symptoms.

Contraindications

Hypersensitivity to polymyxin B; myasthenia gravis.

With caution in chronic renal failure.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy.

If use during lactation is necessary, the issue of discontinuing breastfeeding should be considered.

Use in Renal Impairment

Polymyxin B should be used with caution in chronic renal failure.

Pediatric Use

It can be used in children according to indications, in age-appropriate recommended doses and regimens. The instructions for polymyxin B drugs regarding the dosing regimen for children of different ages should be strictly followed.

Special Precautions

For infections caused by gram-negative microorganisms (Enterobacter, Pseudomonas aeruginosa, etc.), polymyxin B is prescribed only when the pathogen is resistant to other less toxic antimicrobial drugs.

Parenteral use is only permitted in a hospital setting.

With parenteral use, monitoring of the plasma concentration of polymyxin B is necessary.

During long-term treatment, renal function should be monitored every 2 days.

Polymyxin B may be used in combination drugs with neomycin, bacitracin, nystatin, trimethoprim, as well as with dexamethasone.

Drug Interactions

Polymyxin B is incompatible with non-depolarizing muscle relaxants (risk of respiratory muscle paralysis).

When used concomitantly, a synergistic effect is observed with chloramphenicol, carbenicillin, tetracycline, sulfonamides, and trimethoprim against Pseudomonas aeruginosa, Proteus spp., Serratia spp.; with ampicillin – against most gram-negative bacteria.

It is compatible with bacitracin and nystatin.

When combined with aminoglycosides (kanamycin, streptomycin, neomycin, gentamicin), the risk of ototoxicity and nephrotoxicity, as well as neuromuscular blockade, increases.

It increases the nephrotoxicity of amphotericin B.

Pharmaceutical incompatibility with the sodium salt of ampicillin, chloramphenicol, cephalosporin antibiotics, tetracycline, amino acid solutions, heparin; they should not be mixed in the same syringe or infusion medium.

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.