Kapreomitsin

General characteristics. Structure:

Active ingredient: 1,0 g of a kapreomitsin of sulfate.

Polypeptide antibiotic of antitubercular action.

Pharmacological properties:

Pharmacodynamics. The polypeptide antibiotic produced by Streptomyces capreolus (MPK - 1.25-2.5 mg/l when determining in fluid medium). Suppresses synthesis of protein in a bacterial cell, has bacteriostatic action. It is effective only concerning Mycobacterium tuberculosis. At monotherapy quickly causes emergence of resistant strains, has full cross stability with Viomycinum and partial - with aminoglycosides.

Pharmacokinetics. Practically it is not soaked up in a GIT (less than 1%). Cmax in a blood plasma - through 1-2 at in oil and in 1 h at in/in and introduction in oil. Does not pass through GEB, gets through a placental barrier. It is not metabolized. It is removed generally by kidneys (during 12 h – 50-60% of a dose) in not changed look, in small amounts - with bile. It does not kumulirutsya at daily introduction in a dose of 1 g within 30 days. At a renal failure the elimination half-life increases and drug cumulation is possible.

Indications to use:

Pulmonary tuberculosis (including at inefficiency and intolerance (toxic action) of antitubercular drugs of the main row). Use in the empirical modes of chemotherapy before obtaining results of a microbiological research is possible.

Route of administration and doses:

In oil (deeply) and in/in, on 1.0 g of 1 times a day (no more than 20 mg/kg/days) within 60-120 days. The supporting course of treatment assumes introduction of a kapreomitsin in a dose of 1.0 g 2 or 3 times a week within 12-24 months in a combination with other antitubercular HP. For introduction in oil bottle contents (1.0 g) dissolve 0.9% of NaCl solution in 2 ml (it is necessary to wait 2-3 min. before full dissolution of contents). For in/in introductions solution of a kapreomitsin is diluted by 100 ml of 0.9% of NaCl solution, enter within 60 min. Patients with an impaired renal function need to carry out correction of a daily dose and frequency rate of introduction depending on clearance of creatinine. The changes of function of kidneys are more expressed, the is longer it is necessary to do breaks between injections.

Features of use:

Drug appoint with care the patient with any displays of an allergy, especially medicinal. Before purpose of drug and during treatment it is necessary to control a functional condition of kidneys once a week. To carry out an audiometriya and assessment of vestibular function. Due to a possibility of development of a hypopotassemia – it is regular to control potassium level in blood. It is not necessary to use at the same time the drugs causing nefro-and ototoksichesky action.

Side effects:

Nephrotoxicity (oliguria, renal failure). Neurotoxicity, neuromuscular blockade. Ototoxicity, vestibular disturbances. Local reactions: pain and consolidation in the place of an injection, bleeding, an aseptic necrosis. Allergic reactions: urticaria, papular rash, hyperthermia, eosinophilia.

Interaction with other medicines:

The myorelaxation effect amplifies an Aether anaesthesicus, decreases - neostigminy. Appoint in a combination with other antitubercular drugs. With care it is necessary to appoint in a combination with amikacin, gentamycin, polymyxin, Tobramycinum, Vancomycinum, Kanamycinum and Neomycinum in view of summation of ototoksichesky and nephrotoxic action.

Contraindications:

Hypersensitivity, pregnancy, lactation, age up to 12 years.

Overdose:

Symptoms: dizziness, sonitus, decrease in the general tone, neuromuscular blockade (respiratory paralysis). Hypopotassemia, hypocalcemia, hypomagnesiemia and disturbances of electrolytic balance, acute necrosis of renal tubules.

Treatment: at normal function of kidneys - hydration with maintenance of an uropoiesis at the level of 3-5 ml/h/kg; control of a water balance, level of electrolytes and KK; for elimination of neuromuscular blockade - introduction of antikholinesterazny HP, the drugs Ca2+; at the expressed renal failure - a hemodialysis.

Storage conditions:

At a temperature of 15-30 °C in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

The lyophilized powder for preparation of injection solution in glass bottles and cardboard boxes.