Kapreomitsin

General characteristics. Structure:

Active ingredient: 1000 mg of a kapreomitsin (in the form of a kapreomitsin of sulfate).

Pharmacological properties:

Pharmacodynamics. An antituberculous remedy, the polypeptide antibiotic produced by Streptomyces capreolus (MPK - 1.25-2.5 mg/l when determining in fluid medium). Represents a complex from 4 microbiological active components which structure is completely not established. Mix of kapreomitsin of IA, IB, IIA and IIB has approximate percentage of 25, 67, 3 and 6%. It is applied in the form of a kapreomitsin of sulfate.

It is selectively active concerning Mycobacterium tuberculosis which are localized out of - and in a cell. Inhibits synthesis of protein in a bacterial cell, has bacteriostatic action. At monotherapy quickly causes emergence of resistant strains; cross resistance to Kanamycinum, Viomycinum and in certain cases to amikacin and Neomycinum is noted. Cross resistance was not observed between kapreomitsiny and an isoniazid, aminosalicylic acid, Cycloserinum, streptomycin, Etioniamidum and Ethambutolum.

Indications to use:

Treatment of the pulmonary forms of tuberculosis caused by Mycobacterium tuberculosis strains, sensitive to it, if antitubercular drugs of the first row (an isoniazid, Rifampinum, Ethambutolum, aminosalicylic acid, streptomycin) are inefficient, or cannot be applied because of toxic action, or presence of steady tubercular bacteria.

Route of administration and doses:

The average dose makes 1 g/days (it is not necessary to exceed a dose of 20 mg/kg/days). The drug is administered intravenously or intramusculary daily for 60 or 120 days, and then - on 1 g any of two ways 2-3 times a week. Treatment of tuberculosis should be continued within 12-24 months. If there is no opportunity to administer the drugs injektsionno, then at the patient's extract from hospital they should be replaced with peroral forms.

Features of use:

Before an initiation of treatment kapreomitsiny it is necessary to confirm existence of sensitivity to Mycobacterium tuberculosis strain kapreomitsin. Kapreomitsin is recommended to use in combination with other chemotherapeutic means, but not as monotherapy.

Side effects:

From an urinary system: nephrotoxicity — toxic nephrite, injury of kidneys with a necrosis of tubules, a dysuria, a renal failure, increase in level of an urea nitrogen in blood more 20mg/100 ml (36% of cases), and more 30mg/100 ml (10% of cases), increase in level of creatinine in blood serum, emergence of an abnormal uric deposit: cylindruria, microhematuria, leukocyturia. In an isolated case – the disturbances of electrolytic balance reminding the Barter syndrome.

From a nervous system and sense bodys: unusual fatigue or weakness, drowsiness, neuromuscular blockade, breath difficulty (owing to decrease in a tone of respiratory muscles) up to an apnoea (after bystry intravenous administration neuromuscular blockade and respiratory paralysis is possible); ototoxicity — a hearing impairment (subclinical — 11% which are clinically expressed — 3%), including irreversible, noise, a ring, buzz or feeling of "mortgaging" in ears; a vestibulotoksichnost — a lack of coordination of movements, instability of gait, dizziness.

From bodies of a GIT: nausea, vomiting, anorexia, thirst, a hepatotoxic with disturbance of functional indicators of a liver (especially against the background of liver diseases in the anamnesis).

Allergic reactions: urticaria, makulo-papular skin rash, itch, erubescence, fever.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): arrhythmia (owing to electrolytic disturbances), a leukocytosis, a leukopenia, an eosinophilia (5%), in rare instances - thrombocytopenia.

Others: disturbance of electrolytic balance, including hypopotassemia, hypocalcemia, hypomagnesiemia; mialgiya; morbidity, infiltration, development of sterile abscesses or the raised bleeding in an injection site.

Interaction with other medicines:

In a combination with other antitubercular medicines (streptomycin, Viomycinum), and also at a combination to polymyxin, colistin, amikacin, gentamycin, Tobramycinum, Vancomycinum, Kanamycinum, Neomycinum, furosemide, Acidum etacrynicum or a metoksiflurany ototoksichesko and nephrotoxic action mutually amplifies. The myorelaxation effect amplifies an Aether anaesthesicus, aminoglycosides, polymyxins, citrate preservatives of blood, decreases - neostigminy.

Contraindications:

* hypersensitivity to drug components,

* pregnancy, feeding by a breast,

* children's age (safety and efficiency of use are not defined).

Overdose:

Symptoms: a renal failure, up to an acute necrosis of tubules (the risk increases at elderly, against the background of initial dysfunction of kidneys, dehydration), damage of acoustical and vestibular departments of the VIII couple of cranial nerves, neuromuscular blockade up to an apnoea (especially at bystry in introduction), an electrolytic imbalance: a hypopotassemia, a hypocalcemia, a hypomagnesiemia, the disturbances of electrolytic balance reminding the Barter syndrome.

Treatment: at treatment of overdose of a kapreomitsin it must be kept in mind a possibility of overdose by several drugs, interactions of the combined drugs and feature of pharmacokinetics of the individual patient at once. Purpose of absorbent carbon, a gastric lavage is carried out. It is necessary to provide careful observation of the patient and maintenance of the main vital signs: breath, blood circulation, concentration of blood gases, level of electrolytes. Patients with normal function of kidneys should carry out hydration so that to support outflow of urine at the level from 3 to 5 ml/kg/h (at normal function of kidneys). It is necessary to control carefully a water balance, level of electrolytes, clearance of creatinine. At patients with the expressed renal failures it is possible to apply a hemodialysis to removal of a kapreomitsin effectively. For stopping of neuromuscular blockade, including respiratory depression and an apnoea — introduction of antikholinesterazny means, calcium drugs.

Issue conditions:

According to the recipe

Packaging:

The powder lyophilized for preparation of solution for injections of 1000 mg in bottles with a capacity of 10 ml in packaging No. 1 and No. 40.