Polymibaxa-APH (Lyophilisate) Instructions for Use

Marketing Authorization Holder

Alpharma, LLC (Russia)

Manufactured By

Belarusian-Dutch Joint Venture "FARMLAND", LLC (Republic of Belarus)

ATC Code

J01XB02 (Polymyxin B)

Active Substance

Polymyxin B

Polymyxin B (Rec.INN registered by WHO)

Dosage Forms

	Polymibaxa-APH	Lyophilisate for preparation of solution for injections 25 mg
		Lyophilisate for preparation of solution for injections 50 mg

Dosage Form, Packaging, and Composition

Lyophilisate for preparation of solution for injections

50 mg – vials – carton packs – By prescription

Lyophilisate for preparation of solution for injections

50 mg – vials – carton packs – By prescription

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, leading 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 show resistance 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 poorly penetrates 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 infection, infections in burn patients.

ICD codes

Dosage Regimen

Administer Polymyxin B by intravenous infusion, intramuscular injection, or intrathecal route.

Determine the exact dose, route, and duration of therapy individually based on the infection’s severity, causative pathogen susceptibility, and patient’s renal function.

For intravenous administration, reconstitute the lyophilisate with Sterile Water for Injection. Further dilute the resulting solution in 300-500 mL of 5% Dextrose Injection for infusion.

For intramuscular administration, dissolve the contents of the vial in 2 mL of Sterile Water for Injection or 0.9% Sodium Chloride Injection.

The typical adult and pediatric daily dose is 15,000-25,000 IU/kg (approximately 1.5-2.5 mg/kg), administered in divided doses every 12 hours.

In patients with renal impairment, reduce the dose or extend the dosing interval based on creatinine clearance. Monitor serum drug concentrations to guide dosing.

For intrathecal administration in cases of meningitis, the adult dose is 50,000 IU (5 mg) once daily for 3-4 days, then 50,000 IU every other day. For children over 2 years, use 20,000 IU (2 mg) daily for 3-4 days or every other day. For infants, use 20,000 IU (2 mg) once daily for 3-4 days.

The total daily dose for all routes should generally not exceed 25,000 IU/kg (2.5 mg/kg).

Continue therapy for at least 48-72 hours after symptoms disappear and bacterial eradication is confirmed.

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

Use in children is possible according to indications, in doses and regimens recommended for the respective age. It is necessary to strictly follow the instructions in the polymyxin B drug labels regarding the dosing regimen for children of different ages.

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.

For parenteral use, it is used only in a hospital setting.

During 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 can be used as part of 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, antibiotics of the cephalosporin group, 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.