Capocin

Kapocin is an antibiotic from the category of anti-tuberculosis substances.

Indications Capocina

It is used in the complex therapy of pulmonary tuberculosis caused by the action of mycobacteria that are sensitive to capreomycin (if first-line drugs do not have the required effect or are not suitable for the patient).

Release form

The release of the therapeutic substance is realized in the form of a lyophilisate for injection liquid, in 1 g vials. There is 1 such vial in a box.

Pharmacodynamics

The drug inhibits protein binding inside bacterial cells and demonstrates bacteriostatic activity. It selectively affects tuberculosis mycobacteria, which are located in the intra- and extracellular space.

Monotherapy leads to the rapid emergence of resistant strains; cross-resistance to kanamycin is also observed.

Pharmacokinetics

After the use of 1000 mg of the substance, the plasma Cmax value is 20-47 mg/l and is observed after 1-2 hours. With an intravenous infusion of 1000 mg of the drug lasting 1 hour, the Cmax values are 30 mg/l. The drug does not penetrate the BBB, but is able to cross the placenta.

The substance does not participate in metabolic processes, is excreted through the kidneys (52% of the portion - over 12 hours) by glomerular filtration, in an active unchanged state and in large quantities. A small part is excreted with bile. The indicators in the urine after using a portion of 1000 mg (after 6 hours) on average equal 1.68 mg / ml. Half-life is within 3-6 hours.

With daily injections (over the course of 1 month) of 1000 mg of the drug, the substance does not accumulate in individuals with healthy renal function.

If a person has problems with kidney function, the half-life of the drug increases, and in addition, there is a tendency for the substance to accumulate.

Dosing and administration

The medication must be used exclusively parenterally - intramuscular injection. It is necessary to pre-dissolve 1000 mg of powder in 0.9% NaCl or sterile injection liquid (2 ml). For an adult, the portion size of a deep intramuscular injection is 1000 mg once a day, every day, within a 60-120-day period. Then the drug is administered 2-3 times a week for a 1-2-year period, combining with other anti-tuberculosis substances.

A maximum of 20 mg/kg of the drug is allowed per day.

Dosages for renal disorders:

• CC values below 110 ml/minute – 13.9 mg/kg of substance per day;
• CC level less than 100 ml/minute – 12.7 mg/kg of the drug per day;
• CC rate less than 80 ml/minute – 10.4 mg/kg;
• CC values less than 60 ml/minute – 8.16 mg/kg;
• CC level below 50 ml/minute – 7.01 per day or 14 mg/kg per 48 hours;
• the CC indicator is less than 40 ml/minute – 5.87 (per day) or 11.7 mg/kg (per 48 hours);
• CC values below 30 ml/minute – 4.72 (per day), 9.45 (per 48 hours) or 14.2 mg/kg (per 72 hours);
• CC values less than 20 ml/minute – 3.58, 7.16 or 10.7 mg/kg of substance;
• the level of CC is less than 10 ml/minute – 2.43, 4.87 or 7.3 mg/kg of the drug;
• CC values equal to zero are 1.29 (per day), 2.58 (per 48 hours) or 3.87 mg/kg (per 72 hours).

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Use Capocina during pregnancy

Not prescribed to pregnant or breastfeeding women.

Contraindications

Contraindicated for use in people with intolerance to capreomycin.

Side effects Capocina

The introduction of a medicinal substance may provoke the appearance of certain side effects:

• disorders affecting the urogenital system: nephrotoxicity, renal damage accompanied by tubular necrosis, renal failure, dysuria, an increase in blood nitrogen levels to a level above 20-30 mg/100 ml (by 46%), as well as serum creatinine. The appearance of abnormal sediment or formed blood particles in the urine;
• disorders in the sensory organs and nervous system: strange weakness or fatigue, drowsiness and ototoxicity. Hearing loss may be observed (subclinical in 11% of cases, and clinically significant in 3%), sometimes incurable, as well as buzzing, ringing, noise or a feeling of congestion in the ears. Development of vestibulotoxicity is possible - motor coordination disorder, dizziness, unsteady gait and blockade of neuromuscular activity;
• damage to the digestive organs: a feeling of thirst, nausea, anorexia or vomiting, and also hepatotoxicity, accompanied by liver dysfunction (especially in people with a history of liver disease);
• signs of allergy: itching, swelling, epidermal rash, fever and redness of the skin;
• problems with the functioning of the blood system (hemostasis and hematopoietic processes) and the cardiovascular system: leukocytosis, thrombocytopenia or leukopenia, heart rhythm disorders and eosinophilia;
• Other: problems with electrolyte balance (hypokalemia is possible), difficulty breathing (due to weakened respiratory muscle tone), myalgia. Temperature may increase (with combined treatment). Infiltration, increased bleeding or sterile abscesses at the injection site may occur.

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Overdose

Intoxication causes renal dysfunction, which may reach tubular necrosis in the acute stage (the probability increases in the elderly, with dehydration or existing renal dysfunction), and in addition, damage to the vestibular and auditory area of the 8th pair of cranial neurons. Neuromuscular blockade may also occur, which can lead to respiratory arrest (often due to the rapid rate of drug administration). Electrolyte imbalance may develop (hypomagnesemia, -kalemia or -calcemia).

Symptomatic procedures are performed: support of blood flow and respiration processes, and in addition, hydration, ensuring urine outflow within the limits of 3-5 ml/kg/hour (healthy renal function). This is necessary to remove the blockade of neuromuscular work (for example, preventing the development of apnea or respiratory depression). Anticholinesterase agents and calcium drugs are also used, hemodialysis is performed (especially in people with severe kidney problems); along with this, it is necessary to monitor the indicators of CC and VEB.

Interactions with other drugs

Kapocin should be used with extreme caution together with colistin, as well as polymyxin A sulfate or gentamicin, as well as amikacin or kanamycin, vancomycin or neomycin, and in addition to tobramycin, because in these cases a summation of oto- and nephrotoxic effects may occur.

It is prohibited to combine the medicine with solutions containing a complex of B-vitamins.

Combination with antidiarrheal agents increases the likelihood of pseudomembranous colitis.

It is not compatible with ampicillin, aminophylline, magnesium sulfate, and also with barbiturates, erythromycin, calcium gluconate and diphenylhydantoin.

It is prohibited to use the medication together with other injectable anti-tuberculosis drugs (biomycin or streptomycin), because this can potentiate the toxic effect (especially with respect to renal function and the 8th pair of cranial neurons).

There is no compatibility with medications that have oto- (polymyxin, ethacrynic acid and aminoglycosides with furosemide) and nephrotoxic (methoxyflurane with aminoglycosides and polymyxin) activity, as well as with drugs that provoke a blockade of neuromuscular function (polymyxin, citrate blood preservatives, aminoglycosides with diethyl ether, as well as halogenated hydrocarbons used in inhalation anesthesia). Weakening of the blockade of neuromuscular activity occurs when using neostigmine.

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Storage conditions

Kapocin should be stored in a place inaccessible to small children. Temperature marks - within 25 ° C.

Shelf life

Kapocin is allowed to be used within a 2-year period from the date of manufacture of the therapeutic drug.

Application for children

Kapocin is prohibited for use in pediatrics.

Analogues

The analogs of the drug are the substances Capastat, Capreostat, Capreom with Capremabol, and in addition to this, Lycocin, Capreomycin and Capreomycin sulfate.