Вилимиксин®

General characteristics. Structure:

Active ingredient: 25 mg and 50 mg of polymyxin B of sulfate (in terms of the sum of V1, V2, V3, V1-polymyxins І).

The antibiotic applied against gram-negative microorganisms, sensitive to polymyxin B.

Pharmacological properties:

Pharmacodynamics. The antibiotic produced by spore-forming bacteria of Bacillus polymixa. Activity is defined by a biological way and is expressed in PIECE; 1 mg contains 8 thousand. Pieces. Has the bactericidal effect connected with disturbance of integrity of a membrane of a microbic cell. It is absorbed on membrane phospholipids, increases its permeability, causes a lysis of bacteria.

It is active concerning gram-negative microorganisms: Pseudomonas aeruginosa, Salmonella spp., Shigella spp., Escherichia coli, Klebsiella spp., Bordetella pertussis, Haemophilus influenzae, Enterobacter. Fuzobakteriya and bacteroids (Bacteroides fragilis) are moderately sensitive.

Does not work on coccal aerobic (Staphylococcus spp., Streptococcus spp. (including Streptococcus pneumoniae), Neisseria gonorrhoeae, Neisseria meningitidis) and anaerobic microorganisms, on the majority of strains of Proteus spp., Mycobacterium tuberculosis, Corynebacterium diphtheriae and mushrooms.

Stability develops slowly; is full with colistin, polymyxin E.

Pharmacokinetics. At intake it is not soaked up and creates high concentration in a GIT. TCmax at introduction in oil is 1-2 h, Cmax - 2-7 mg/ml; at in introduction in a dose of 2-4 mg/kg of Cmax - 2-8 mg/ml. T1/2 is 3-4 h. At a heavy renal failure - 2-3 days. Communication with proteins of plasma - 50%. Badly gets through fabric barriers, does not get through GEB.

In small amounts gets through a placenta and into breast milk. It is not metabolized. It is removed by kidneys in not changed look (60% within 3-4 days) and with bile. At repeated introduction does not kumulirut.

Indications to use:

Inside: the acute infections caused by sensitive microorganisms: infectious and inflammatory gastrointestinal diseases, it is possible in combination with furasolidone;

parenterally - sepsis, meningitis, pneumonia, a generalized wound fever;

outwardly (or in a cavity), locally - infections of urinary tract (including cystitis, an urethritis), ENT organs (including otitis, antritis, sinusitis), skin (including the infected burns, abscess, phlegmon, decubituses), bones (including osteomyelitis), an eye (including a keratitis, conjunctivitis).

Route of administration and doses:

Intramusculary, intravenously, inside, outwardly.

In oil, adult - on 0.5-0.7 mg/kg 3-4 times a day. A daily dose - 200 mg. To children, irrespective of age - on 0.3-0.6 mg/kg 3-4 times a day. Before introduction powder for preparation of injection solution (25 and 50 mg) waters for injections or 0.9% of NaCl solution dissolve in 1-2 ml 0.5-1% of solution of Procainum. For in/in introductions powder dissolve 5% of solution of a dextrose in 200-300 ml and enter kapelno, with a speed of 60-80 of cap/min. For adults a daily dose - 2 mg/kg in 2 receptions with an interval of 12 h, the maximum daily dose - 150 mg. For introduction to children, dissolve 5-10% of solution of a dextrose in 30-100 ml; the same dose, as at introduction in oil.

At a renal failure the dose decreases and intervals between introductions according to KK increase.

Inside, in the form of aqueous solution. Adult - 100 mg each 6 h; to children - 4 mg/kg in 3 receptions. Treatment duration - 5-7 days.

Locally dig in in a conjunctival sac on 1-3 cap 0.1-0.25% of solution each hour.

Intratekalno - to adults and children is more senior than 2 years - 50 thousand. Piece of 1 times a day within 3-4 days, then every other day during 2 weeks; to children up to 2 years - 20 thousand. Piece/days within 3-4 days or on 25 thousand. Piece of 1 times in 2 days.

Features of use:

At the infections caused by gram-negative microorganisms (Enterobacter, Pseudomonas aeruginosa), appoint only at resistance of the activator to other less toxic HP.

At prolonged treatment it is necessary to control function of kidneys of 1 times in 2 days.

Parenterally apply only in the conditions of a hospital.

There are no data indicating influence on psychomotor reactions at management of avtomatransportny means and other meanizm.

Side effects:

From a nervous system: dizziness, ataxy, consciousness disturbance, drowsiness, paresthesias, neuromuscular blockade.

From an urinary system: albuminuria, cylindruria, azotemia, proteinuria, renal tubular necrosis.

From respiratory system: paralysis of respiratory muscles, apnoea.

From the alimentary system: epigastric pain, nausea, loss of appetite.

From sense bodys: vision disorder.

Allergic reactions: skin rash, itch, eosinophilia.

Local reactions: phlebitis, a periphlebitis, thrombophlebitis, morbidity in the place of an injection.

Others: superinfection, candidiasis, at intrathecal introduction - meningeal symptoms.

Interaction with other medicines:

It is incompatible with not depolarizing muscle relaxants.

Action synergism with chloramphenicol, karbenitsilliny, tetracycline, streptocides and Trimethoprimum concerning Pseudomonas aeruginosa, Proteus, Serratia, with ampicillin - gram-negative sticks.

Let's combine with bacitracin and nystatin.

Strengthens from - and nephrotoxicity of aminoglycosides (Kanamycinum, streptomycin, Neomycinum, gentamycin), and also the neuromuscular transmission blockade caused by them. Reduces concentration of heparin in blood (forms complexes).

Pharmaceutical incompatibility with sodium salt of ampicillin, chloramphenicol, antibiotics of group of cephalosporins, tetracycline, solutions of amino acids, heparin. Increases nephrotoxicity of Amphotericinum of Century.

Contraindications:

Hypersensitivity, HPN, myasthenia, pregnancy, lactation period. For topical administration - perforation of a tympanic membrane, for external use - extensive damages of skin.

Overdose:

Symptoms: paralysis of respiratory muscles, ototoxicity, nephrotoxicity.

The supporting and symptomatic therapy is shown.

Storage conditions:

In the place protected from light, in the distance from children at a temperature at 25 degrees Celsius.

Issue conditions:

According to the recipe

Packaging:

- 1 bottle with drug and the application instruction is placed in a pack from a cardboard.

- 1 bottle with drug and 1 ampoule with solvent is packed into a blister strip packaging. One blister strip packaging and the application instruction are put in a pack cardboard.

- 5 bottles with drug pack into blister strip packagings. One blister strip packaging and the application instruction are put in a pack cardboard.

- 5 bottles with drug complete with 5 ampoules of solvent pack into blister strip packagings. One blister strip packaging with drug, one blister strip packaging with solvent and the application instruction is put in a pack cardboard