Vilimiksin^® (Powder) Instructions for Use

Marketing Authorization Holder

PFC Prebend, LLC (Russia)

ATC Code

J01XB02 (Polymyxin B)

Active Substance

Polymyxin B

Polymyxin B (Rec.INN registered by WHO)

Dosage Forms

	Vilimiksin®	Powder for preparation of injection solution 25 mg: vial 1 or 5 pcs.
		Powder for preparation of injection solution 50 mg: vial 1 or 5 pcs.

Dosage Form, Packaging, and Composition

Powder for preparation of injection solution white or almost white, odorless or almost odorless.

25 mg – glass vials (1) – cardboard packs.
25 mg – glass vials (1) with solvent “Water for injections” (amp. 5 ml 1 pc.) – cardboard packs.
25 mg – glass vials (5) – contour cell packs (1) – cardboard packs.
25 mg – glass vials (5) – contour cell packs (1) with solvent “Water for injections” (amp. 5 ml 5 pcs. in a contour cell pack) – cardboard packs.

Powder for preparation of injection solution white or almost white, odorless or almost odorless.

50 mg – vials (1) – cardboard packs.
50 mg – vials (1) + 1 amp. with solvent – cardboard packs.
50 mg – vials (5) – contour cell packs (1) – cardboard packs.
50 mg – vials (5) + 5 amp. with solvent – contour cell packs (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 fungi are generally 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 has cross-resistance with colistin.

Pharmacokinetics

After intramuscular administration, C_max in blood plasma is reached after 2 hours. Plasma protein binding is 50%. It penetrates tissue barriers poorly 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. T_1/2 is 3-4 hours, in severe renal failure – 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 Vilimiksin^® intravenously, intramuscularly, or intrathecally. Determine the exact dose, route, and duration of therapy individually based on the infection severity, pathogen susceptibility, and patient’s renal function.

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

For intramuscular injection, dissolve the contents of one vial in 2-5 mL of Sterile Water for Injection or 1% Procaine Hydrochloride Solution. Administer the injection deeply into a large muscle mass. Rotate injection sites to minimize local irritation.

For intrathecal administration, use a solution prepared with 0.9% Sodium Chloride Injection without preservatives. The typical intrathecal dose for adults is 5 mg once daily for 3-4 days, then 5 mg every other day. Continue treatment until cerebrospinal fluid cultures are negative.

The recommended daily dose for adults and children with normal renal function is 15,000-25,000 IU/kg/day (1.5-2.5 mg/kg/day). Do not exceed a total daily dose of 25,000 IU/kg (2.5 mg/kg). In life-threatening infections, a higher initial dose may be used under strict medical supervision.

Divide the total daily dose for intravenous or intramuscular routes into two equal administrations, given every 12 hours.

Adjust the dosage mandatorily in patients with renal impairment. Base the adjustment on the patient’s creatinine clearance and regularly monitor serum drug concentrations. In severe renal failure, significantly reduce the dose or extend the dosing interval.

Monitor renal function (serum creatinine, BUN) before initiation and every two days during therapy. Discontinue the drug at the first sign of renal toxicity.

Monitor for signs of neurotoxicity and neuromuscular blockade, particularly when used concomitantly with other neurotoxic or nephrotoxic drugs, or with muscle relaxants.

Use this medication only in a hospital setting under close clinical and laboratory supervision.

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 use during lactation is necessary, 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. Strict adherence to the instructions in the polymyxin B drug labels regarding the dosing regimen for children of different ages is necessary.

Special Precautions

For infections caused by gram-negative microorganisms ( Enterobacter, Pseudomonas aeruginosa and others), 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 concentration of polymyxin B in blood plasma 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).

With simultaneous use, 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 oto- 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 30°C (86°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.