Kapreomitsin

General characteristics. Structure:

Active ingredient: capreomycin; 1 bottle contains a kapreomitsin sulfate sterile, in terms of капреомицин - 1,0 g.

Pharmacological properties:

Pharmacodynamics. Inhibits synthesis of protein in a bacterial cell, shows bacteriostatic action. It is selectively active concerning the mycobacteria of tuberculosis which are localized out of - and in a cell. At monotherapy quickly causes emergence of resistant strains, it is characterized by existence of cross resistance to Kanamycinum.

Pharmacokinetics. Badly (less than 1%) it is soaked up from digestive tract. At introduction in oil in a dose of 1 g of Cmax in plasma (20-47 mg/l) it is reached in 1-2 hours. Later in hourly infusion in a dose of 1 g of Cmax makes 30 mg/l. Does not pass through a blood-brain barrier, passes through a placental barrier. It is not metabolized, excreted by kidneys (for 12 hours – 52% of a dose) by glomerular filtering in not changed active look and in high concentration (in small amounts – with bile). Concentration in urine for 6 hours after introduction in a dose of 1 g makes, on average, 1,68 mg/ml. The elimination half-life (T1/2) makes 3-6 hours. Does not kumulirut at daily introduction in a dose 1 g for 30 days at patients with normal function of kidneys. At a renal failure of T1/2 the tendency to cumulation increases and comes to light.
Main physical and chemical properties. amorphous powder of white or almost white color. Incompatibility. Not to mix with other medicines, except those which are specified in the section. "Route of administration and doses".

Indications to use:

The combined treatment of the pulmonary tuberculosis caused by mycobacteria, sensitive to a kapreomitsin, at inefficiency or intolerance of drugs І a row.

Route of administration and doses:

Apply only parenterally – intramusculary (in oil) (preferential) or intravenously (in/in). 1 g of drug dissolve previously in 2 ml 0,9% of solution of sodium of chloride or sterile water for injections (in oil enter deeply into a muscle), for in/in infusion in addition dissolve 0,9% of solution of sodium of chloride in 100 ml (enter for 60 min.). Adult - 1 g of 1 times a day, daily for 60-120 days, then 2-3 times a day for 12-24 months, in a combination with others
antitubercular drugs. The maximum daily dose - is no more than 20 mg/kg. At renal failures: at clearance of creatinine less than 110, 100, 80 і 60 ml/min. - on 13,9; 12,7; 10,4 і 8,16 mg/kg respectively each 24 hours; at clearance of creatinine it is less than 50 and 40 ml/min. - on 7,01 and 5,87 mg/kg each 24 hours or on 14,0 and 11,7 mg/kg each 48 hours respectively; at clearance of creatinine it is less than 30, 20 and 10 ml/min. - on 4,72; 3,58 and 2,43 mg/kg each 24 hours or on 9,45; 7,16 і 4,87 mg/kg each 48 hours, or on 14,2; 10,7 and 7,3 mg/kg each 72 hours respectively; at the clearance of creatinine equal 0 - on 1,29 mg/kg each 24 hours or to 2,58 mg/kg are each 48 hours, or to 3,87 mg/kg there are each 72 hours.

Features of use:

To and during treatment it is necessary to carry out periodically an audiometriya (1-2 times a week) for diagnosis of a hearing disorder at high frequencies, definitions of indicators of function of a vestibular mechanism; kidneys (weekly) and a liver, potassium level in blood serum (monthly). At a renal failure correction of the mode of dosing depending on clearance of creatinine is necessary.
In time and after surgical intervention with care apply against the background of means which cause neuromuscular blockade (especially at high probability of the incomplete termination of neuromuscular blockade 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 injections the drug is administered as soon as possible, only if there did not come time of introduction of the following dose; do not double a dose. Kapreomitsin's appointment perhaps after definition of sensitivity of a strain.
Use for patients with defeat of the VII couple of cranial nerves, a myasthenia, parkinsonism, dehydration, a renal failure, including in advanced age is limited. Ability to influence speed of response at control of motor transport or work with other mechanisms. It was not investigated, but it is necessary to consider a possibility of emergence of side effects therefore it is recommended to keep from control of motor transport or work with other mechanisms.

Side effects:

From urinogenital system: nephrotoxicity - toxic nephrite, injury of kidneys with a necrosis of tubules, a dysuria (increase/reduction of frequency of an urination or amount of urine), a renal failure, increase in level of an urea nitrogen in blood is more than 20-30 mg / 100 of ml (46%) and creatinine in blood serum, emergence in urine of an abnormal deposit or uniform elements of blood.
From a nervous system and sense bodys: unusual fatigue or weakness, drowsiness; 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, unsteadiness of gait, dizziness; neuromuscular blockade.
From the alimentary system: nausea, vomiting, anorexia, thirst, a hepatotoxic with disturbance of functional indicators of a liver (especially at liver diseases in the anamnesis). Allergic reactions: skin rashes, itch, erubescence, hypostases, fever.
From cardiovascular system and blood (a hemopoiesis, a hemostasis): disturbance of a cordial rhythm, leukocytosis, leukopenia, eosinophilia (5%), thrombocytopenia.
Others: disturbances of electrolytic balance, including hypopotassemia; a mialgiya, breath difficulty (owing to decrease in a tone of respiratory muscles); fervescence (it was noted at complex therapy); infiltration, development of sterile abscesses or the strengthened bleeding in an injection site.

Interaction with other medicines:

Kapreomitsin's appointment along with polymyxin sulfate A, colistin, amikacin, gentamycin, Tobramycinum, Vancomycinum, Kanamycinum and Neomycinum needs to be begun carefully because of possible summation nefro-and ototoksichesky effects. Simultaneous use with the solutions containing a complex of vitamins of group B is not recommended. Co-administration with antidiarreyny drugs increases risk of development of pseudomembranous colitis. It is incompatible with erythromycin, ampicillin, diphenylhydantoin, barbiturates, aminophylline, calcium a gluconate and magnesium sulfate. It is not necessary to apply Kapreomitsin along with other injection antitubercular drugs (streptomycin, biomycin) because of possible strengthening of toxic effect, especially on the VIII couple of cranial nerves and function of kidneys. It is incompatible with drugs which show ototoksichesky (aminoglycosides, polymyxins, furosemide, Acidum etacrynicum) and nephrotoxic (aminoglycosides, polymyxins, метоксифлуран) action and drugs which cause neuro muscular blockade (aminoglycosides, polymyxins, diethyl ether and galogenuglevodoroda for an inhalation anesthesia, citrate preservatives of blood). Neuro muscular blockade is weakened neostigminy.

Contraindications:

Hypersensitivity to a kapreomitsin. Pregnancy, feeding period breast. Children's age.

Use during pregnancy or feeding by a breast. Contraindicated. Children. Do not apply.

Overdose:

Symptoms: a renal failure, up to an acute necrosis of tubules (the risk increases at patients of advanced age, at secretory dysfunction of kidneys, dehydration), damage of acoustical and vestibular departments of V ІІІ couples of cranial nerves, neuromuscular blockade, up to an apnoea (especially at bystry in introduction), an electrolytic imbalance (a hypopotassemia,
hypocalcemia, hypomagnesiemia).
Treatment. Symptomatic therapy: support of breath and blood circulation, hydration which will provide outflow of urine at the level of 3-5 ml/kg/h (at normal function of kidneys); for stopping of neuromuscular blockade, including respiratory depression and an apnoea - introduction of antikholinesterazny means, calcium drugs, carrying out a hemodialysis (especially at patients with heavy renal failures); monitoring of water electrolytic balance and clearance of creatinine is necessary.

Storage conditions:

Period of validity 2 years. To store in original packaging at a temperature not above 25 °C, the place, unavailable to children. After cultivation to apply at once.

Issue conditions:

According to the recipe

Packaging:

On 1,0 g in a bottle.