Kapreomitsina sulfate

General characteristics. Structure:

Active agent - a kapreomitsina sulfate (in terms of капреомицин) 1,0g.

Pharmacological properties:

Pharmacokinetics. At intramuscular introduction in a dose of 1 g the maximum concentration of drug in plasma is reached in 1-2 h. After intravenous hourly infusion in a dose of 1 g the maximum concentration of drug makes 30mg/l. Does not pass through a blood-brain barrier, gets through a placental barrier. It is not metabolized. It is excreted by kidneys (during 12 h – 50-60% of a dose) by glomerular filtering in not changed active look, in small amounts – with bile. The elimination half-life of drug makes 3-6 h. Does not kumulirut at daily introduction in a dose 1 g within 30 days. At a renal failure the elimination half-life of drug increases and shown a tendency to cumulation.

Pharmacodynamics. Antituberculous remedy. An antibiotic the polypeptide emitted from Streptomyces capreolus. Inhibits synthesis of protein in a bacterial cell, has bacteriostatic action. It is selectively active concerning a mycobacterium of tuberculosis, localized out of - and in a cell. Cross resistance between kapreomitsiny and Viomycinum, Kanamycinum, Neomycinum is observed.

Indications to use:

- a pulmonary tuberculosis (as a part of a combination therapy), including at inefficiency or intolerance of antitubercular drugs I of a row.

Route of administration and doses:

Before therapy it is necessary to carry out the analysis for confirmation of existence of Mycobacterium tuberculosis strain, sensitive to a kapreomitsin.

Kapreomitsin always appoint in a combination at least to one more antitubercular drug to which that strain of Mycobacterium tuberculosis which is available for this patient is sensitive.

The average dose for adults and teenagers is more senior than 14 years makes 1 g/days.

The maximum daily dose should not exceed 20 mg/kg/days.

Treatment of tuberculosis should be continued on average within 2-3 months. Duration of a course of treatment and further tactics are determined by the attending physician.

The patient with renal failures drug is used:

- at the clearance of creatinine (CC) less than 110-60 ml/min. - on 13,9-8,16 mg/kg respectively each 24 h;

- at KK less than 50-40 ml/min. - on 7,01-5,87 mg/kg each 24 h or on 14,0-11,7 mg/kg each 48 h respectively;

- at KK less than 30-10 ml/min. - on 4,72-2,43 mg/kg each 24 h or on 9,45-4,87 mg/kg each 48 h, or on 14,2-7,3 mg/kg each 72 h respectively;

- at KK equal 0 - on 1,29 mg/kg each 24 h or 2,58 mg/kg each 48 h, or 3,87 mg/kg each 72 h.

Rules of preparation and administration of solutions. For intramuscular introduction of 1 g of drug (contents of 1 bottle) dissolve in 3 ml 0,9% of solution of sodium of chloride or sterile water for injections (it is necessary to wait 2-3 min. before full dissolution of contents).

Intramusculary enter deeply into a muscle as the superficial injection can cause the increased morbidity and development of aseptic abscesses.

After cultivation of a kapreomitsin for intramuscular injections it is possible to store no more than 24 p in the refrigerator.

For intravenous administration of 1 g of drug, previously dissolve in 3 ml 0,9% of solution of sodium of chloride or sterile water for injections, then for intravenous infusion in addition dissolve 0,9% of solution of sodium of chloride in 100 ml (enter within 60 min.). The solution prepared for intravenous infusion is not subject to storage.

For introduction of a dose of 1 g it is necessary to use all contents of a bottle. Solution can get pale straw coloring and over time darken, but it is not followed by loss of activity or emergence of toxicity.

Features of use:

At a renal failure correction of the mode of dosing depending on the clearance of creatinine (CC) is required. Kapreomitsin in high doses can cause partial nervously – muscular blockade, up to an apnoea (especially at bystry intravenous administration).

With care apply at patients with tendency to allergic reactions, especially at a medicinal allergy. During treatment it is regularly necessary to control indicators of function of kidneys, to carry out an audiometriya and assessment of function of a vestibular mechanism, to control potassium level in a blood plasma.

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

Considering side effects of medicine, it is necessary to be careful at control of motor transport or potentially dangerous mechanisms.

Side effects:

Often:

- nausea, vomiting, anorexia, thirst, a hepatotoxic with disturbance of functional indicators of a liver (especially against the background of liver diseases in the anamnesis);

- nephrotoxicity – a dysuria, emergence in urine of a pathological deposit or uniform elements of blood, increase in level of an urea nitrogen in blood more than 20-30 mg / 100 ml and creatinine in blood serum, a renal failure, injury of kidneys with a necrosis of tubules, toxic nephrite;

- skin rash, itch, erubescence, fever, eosinophilia, small tortoiseshell, hyperthermia;

- peripheral hypostases.

Seldom:

- ototoxicity - a hearing impairment, including irreversible, noise, a ring, buzz or feeling of "mortgaging" in ears;

- lack of coordination of movements, instability of gait, dizziness;

- neuromuscular blockade, up to an apnoea (especially at bystry intravenous administration);

- disturbances of a heart rhythm;

- leukocytosis, leukopenia, eosinophilia, thrombocytopenia;

- disturbance of electrolytic balance, including hypopotassemia, hypocalcemia, hypomagnesiemia;

- mialgiya;

- breath difficulty (owing to decrease in a tone of respiratory muscles);

- fatigue, weakness, drowsiness.

Others:

- morbidity, infiltration, development of sterile abscesses or the strengthened bleeding in an injection site.

Interaction with other medicines:

It is not necessary to apply along with the parenteral antitubercular drugs possessing from - and nephrotoxicity. With care apply in a combination with polymyxin, colistin, amikacin, gentamycin, Tobramycinum, Vancomycinum, Kanamycinum, Neomycinum because of risk of the additive nefro-and ototoksichesky action.

Contraindications:

- hypersensitivity to drug;

- heavy abnormal liver functions and kidneys;

- pregnancy, period of a lactation (breastfeeding);

- children's and teenage age up to 14 years;

- decrease in hearing, otitis.

With care:

- defeat of the VIII couple of cranial nerves;

- myasthenia;

 

- parkinsonism.

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 intravenous administration), an electrolytic imbalance (a hypopotassemia, a hypocalcemia, a hypomagnesiemia).

Treatment - symptomatic. Maintenance of breath and blood circulation, the hydration providing 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 vodno – electrolytic balance and clearance of creatinine is necessary.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 25 °C.

 

To store in the place, unavailable to children!

 

Issue conditions:

According to the recipe

Packaging:

1,0 g of active agent in bottles. On 100 bottles pack into a film polyethylene with a tray from a cardboard. Put instructions on a medical use in packaging in the state and Russian languages.