Капремабол®

General characteristics. Structure:

Active ingredient: 1 g of a kapreomitsin of sulfate (in terms of капреомицин).

Antibiotic polypeptide with the directed action against Mycobacterium tuberculosis

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.

Has teratogenic effect (anomalies of a skeletogeny in experiments on rats).

Pharmacokinetics. Practically it is not soaked up in a GIT (less than 1%). TCmax in plasma - in 1-2 h after introduction in oil 1 g and its size makes 20-47 mg/l; after 10 h - 4 mg/l. Later in/in 1 h infusion in a dose of 1 g of Cmax makes 30-50 mg/l. AUC at in/in and introduction in oil is identical. 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) by glomerular filtering in not changed look, in small amounts - with bile.

Does not kumulirut at daily introduction in a dose 1 g within 30 days. At a renal failure of T1/2 the tendency to cumulation increases and appears.

Indications to use:

Pulmonary tuberculosis (including at inefficiency and intolerance of HP of the I row).

Route of administration and doses:

In oil (deeply) and in/in, on 1 g of 1 times a day (no more than 20 mg/kg/days) within 60-120 days, further on 1 g 2 or 3 times a week within 12-24 months, in a combination with other antitubercular HP.

Patients with renal failures should reduce a dose according to KK: at an anury a daily dose - 1.29 mg/kg, during 48 h - 2.58 mg/kg, 72 h - 3.87 mg/kg;

at KK of 10 ml/min. for 24 h - 2.43 mg/kg, 48 h - 4.87 mg/kg, 72 h - 7.3 mg/kg;
at KK of 20 ml/min. for 24 h - 3.58 mg/kg, 48 h - 7.16 mg/kg, 72 h - 10.7 mg/kg;
at KK of 30 ml/min. for 24 h - 4.72 mg/kg, 48 h - 9.45 mg/kg, 72 h - 14.2 mg/kg;
at KK of 40 ml/min. for 24 h - 5.87 mg/kg, 48 h - 11.7 mg/kg;
at KK of 50 ml/min. for 24 h - 7.01 mg/kg, 48 h - 14 mg/kg;
at KK of 60 ml/min. for 24 h - 8.16 mg/kg;
at KK of 80 ml/min. for 24 h - 10.4 mg/kg;
at KK of 100 ml/min. for 24 h - 12.7 mg/kg;
at KK of 110 ml/min. for 24 h - 13.9 mg/kg.

For introduction in oil bottle contents (1 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.

Features of use:

The research of function of kidneys should be conducted before treatment and once a week during treatment.

Prior to treatment it is necessary to carry out an audiometriya and assessment of vestibular function. During treatment control hematologic indicators and function of a liver.

At introduction it is necessary to use all contents of a bottle.

It is always appointed in combination with other antitubercular HP.

In time and after surgical intervention with care use against the background of the HP causing neuromuscular blockade (especially at high probability of its incomplete termination in the postoperative period).

During treatment it is necessary to control constantly the mode and schemes of dosing, correctness and a regularity of performance of appointments. In case of the admission of an injection enter as soon as possible, only if there did not come time of introduction of the following dose; doses do not double.

In the absence of improvement of a state during 2-3 weeks or at emergence of new symptoms of a disease consultation of the specialist is necessary.

Side effects:

From an urinary system: nephrotoxicity (increase in an urea nitrogen in a blood plasma, decrease in removal of a fenolsulfonftalein and emergence of an abnormal uric deposit (cylinders, erythrocytes, leukocytes)), toxic nephrite.

From bodies of a hemopoiesis: the eosinophilia (passing at a dose decline up to 2-3 g a day), a leukocytosis, a leukopenia, thrombocytopenia.

From a nervous system: neurotoxicity, neuromuscular blockade.

From sense bodys: ototoxicity - deafness (subclinical and clinically expressed, including irreversible), a sonitus, dizziness.

From the alimentary system: an abnormal liver function (at use in a combination with other gepatotoksichny antitubercular HP) which communication with reception of a kapreomitsin is not found out.

Local reactions: pain and consolidation in the place of an injection, aseptic abscess.
Allergic reactions: urticaria, makulopapulezny rash, fever.

Interaction with other medicines:

The myorelaxation effect amplifies ether diethyl, other aminoglycosides, polymyxins, citrate preservatives of blood, decreases - a neostigmina methyl sulfate.

In a combination with other antitubercular HP (streptomycin, Viomycinum), and also at a combination to polymyxins, including colistin, amikacin, gentamycin, Tobramycinum, Vancomycinum, Kanamycinum, Neomycinum, furosemide, Acidum etacrynicum or a metoksiflurany ototoksichesko and nephrotoxic action mutually amplifies.

Contraindications:

Hypersensitivity, pregnancy, the lactation period, children's age (safety and efficiency of use are not established).

With care. Renal failure, hearing disorder, dehydration, gravis myasthenia, parkinsonism, advanced age.

Overdose:

Symptoms: dizziness, sonitus, вертиго (defeat of acoustical and vestibular departments of the VIII pair of cranial nerves), 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 of 3-5 ml/h/kg; control of a water balance, concentration of electrolytes and KK; for elimination of neuromuscular blockade - administration of inhibitors of cholinesterase, the drugs Ca2+; at the expressed renal failure - a hemodialysis.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 degrees Celsius. To store out of access for children.

Issue conditions:

According to the recipe

Packaging:

1 g of powder in glass bottles of 10 ml. 1 bottle in cardboard packaging. Or 1 bottle and 1 ampoule with solvent in a blister strip packaging from PVC and aluminum foil and a cardboard box. Or 5 bottles from drugs in a blister strip packaging from PVC and aluminum foil and in a cardboard box. Or 5 bottles and 5 ampoules of solvent in a blister strip packaging from PVC and aluminum foil in a cardboard box.