Polaksin B (Lyophilisate) Instructions for Use

Marketing Authorization Holder

Bharat Serums & Vaccines, Ltd. (India)

ATC Code

J01XB02 (Polymyxin B)

Active Substance

Polymyxin B

Polymyxin B (Rec.INN registered by WHO)

Dosage Forms

	Polaksin B	Lyophilisate for preparation of solution for injections 25 mg: 5 ml vial, 1 pc.
		Lyophilisate for preparation of solution for injections 50 mg: 5 ml vial, 1 pc.

Dosage Form, Packaging, and Composition

Lyophilisate for preparation of solution for injections is a white or almost white porous mass, compacted into a tablet or an amorphous porous mass. The reconstituted solution is a liquid from colorless to yellowish-brown.

25 mg – 5 ml vials (1) – cardboard packs.

Lyophilisate for preparation of solution for injections is a white or almost white porous mass, compacted into a tablet or an amorphous porous mass. The reconstituted solution is a liquid from colorless to yellowish-brown.

50 mg – 5 ml vials (1) – cardboard packs.

Clinical-Pharmacological Group

Antibiotic of the polypeptide group

Pharmacotherapeutic Group

Antibiotic-cyclic polypeptide

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 mostly 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 has cross-resistance with colistin.

Pharmacokinetics

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

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

ICD codes

Dosage Regimen

Administer intravenously, intramuscularly, or intrathecally. Determine the dose, route, and duration of therapy individually based on the infection severity, pathogen susceptibility, and patient renal function.

For intravenous infusion, reconstitute the 25 mg (250,000 IU) or 50 mg (500,000 IU) vial with Sterile Water for Injection. Further dilute the reconstituted solution in 300-500 mL of 5% Dextrose Injection. Infuse over 60-90 minutes.

For intramuscular injection, reconstitute the vial with 2 mL of Sterile Water for Injection or 0.9% Sodium Chloride Injection. Divide the total daily dose into 2-4 equal administrations.

For intrathecal administration, use a solution containing 5 mg/mL (50,000 IU/mL). The typical adult dose is 5 mg once daily for 3-4 days, then 5 mg every other day. Continue therapy until cerebrospinal fluid cultures are negative for at least two weeks.

The usual adult and pediatric daily dose is 15,000-25,000 IU/kg/day. Do not exceed 25,000 IU/kg/day. For patients with renal impairment, reduce the dosage based on the degree of impairment. Monitor serum drug concentrations to guide dosing.

In life-threatening infections caused by *Pseudomonas aeruginosa*, the daily dose may be increased up to 30,000 IU/kg/day, but only with extreme caution and close monitoring for 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 chronic renal failure.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy.

If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided.

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 doses and regimens recommended for the respective age. One should strictly follow the instructions in the polymyxin B drug labels regarding the dosage 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.

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

During long-term treatment, kidney 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 simultaneously, 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.