Kapocin

Capocin is an antibiotic from the category of anti-TB drugs.

Indications Kapocina

It is used in the treatment of pulmonary tuberculosis, triggered by exposure to mycobacteria, which are sensitive to capreomycin (if the first-line drugs do not have the desired 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 vials of 1 g. In a box - 1 such bottle.

Pharmacodynamics

The drug inhibits protein binding inside the bacterial cells and demonstrates bacteriostatic activity. Selective effect on tuberculous mycobacteria, which are located in the intracellular and extracellular space.

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

Pharmacokinetics

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

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

With daily injections (for the first month), 1000 mg of drug does not accumulate in individuals with healthy renal activity.

If a person has problems with the work of the kidneys, the half-life of the drug increases, and besides this, there is a tendency for the substance to accumulate.

Dosing and administration

It is necessary to use the drug only by parenteral administration - intramuscular administration. You need to pre-dilute 1000 mg of powder in 0.9% NaCl or sterile injectable fluid (2 ml). For an adult, the size of a serving of a deep intramuscular injection is 1000 mg 1 time per day, every day, within the 60-120 day period. Next, the drug is administered 2-3 times per week over a 1-2-year term, combining with other anti-TB substances.

A day is allowed to use a maximum of 20 mg / kg of the drug.

Dosages for disorders of renal activity:

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

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Use Kapocina during pregnancy

Do not appoint pregnant or lactating women.

Contraindications

It is contraindicated to appoint people with intolerance to capreomycin.

Side effects Kapocina

The introduction of a drug substance can trigger the appearance of separate side symptoms:

• disorders affecting the urogenital system: nephrotoxicity, renal damage, accompanied by tubular necrosis, kidney failure, dysuria, an increase in blood nitrogen levels to over 20-30 mg / 100 ml (46%), as well as serum creatinine. The occurrence of an abnormal sediment or shaped blood particles inside the urine;
• disorders in the area of the senses and NA: strange weakness or fatigue, drowsiness and ototoxicity. A weakening of hearing (subclinical in nature - in 11% of cases, and having clinical severity - in 3%), sometimes incurable, and besides this humming, ringing, noise, or a feeling of ear congestion may be noted. Perhaps the development of vestibulotoxicity - movement coordination disorder, dizziness, unstable gait and blockade of neuromuscular activity;
• lesions of the digestive organs: feeling of thirst, nausea, anorexia or vomiting, and in addition hepatotoxicity, accompanied by a disorder of hepatic activity (especially in individuals with a history of liver disease);
• signs of allergy: itching, swelling, epidermal rash, fever and redness of the skin;
• problems with the work of the blood system (hemostasis and hematopoietic processes) and cardiovascular disease: leukocytosis, thrombocyte or leukopenia, upset heart rate and eosinophilia;
• other: problems with electrolyte balance (hypokalemia possible), difficulty in respiratory processes (due to weakening of the tone of the respiratory muscles), myalgia. Possible increase in temperature (with combined treatment). There may be infiltration, increased bleeding or sterile abscesses in the injection area.

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Overdose

During intoxication, a disorder of renal work occurs, which can reach the tubular necrosis in the acute stage (the likelihood increases in the elderly, during dehydration, or in already existing renal dysfunction), and in addition, the vestibular and auditory portion of the 8th pair of cranial neurons is affected. Neuromuscular blockade may also occur, which can lead to the cessation of the respiratory process (often due to the rapid rate of drug administration). Possible development of electrolyte imbalance (hypomagnesaemia, -caliemia or -calcemia).

Symptomatic procedures are carried out: support of blood flow and respiration processes, and in addition, hydration, ensuring the flow of urine within the limits of 3-5 ml / kg / hour (healthy renal activity). This is necessary to relieve the neuromuscular blockade (for example, preventing the development of apnea or suppressing breathing). Anticholinesterase substances and calcium drugs are also used, hemodialysis is performed (especially for people with severe kidney problems); At the same time, it is necessary to monitor the indicators of QA and VEB.

Interactions with other drugs

Kapocin should be used together with colistin, as well as polymyxin A sulfate, either gentamicin, and in addition with amikacin or kanamycin, vancomycin or neomycin, and in addition, tobramycin should be extremely cautious, because in these cases summation of otso- and nephrotoxic effects can occur.

It is forbidden to combine the drug with solutions that contain the B-vitamin complex.

Combination with antidiarrheals increases the likelihood of colitis of a pseudomembranous nature.

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

It is forbidden to use the drug together with other injecting drug type TB (biomitsin or streptomycin), because it can potentiate toxic effects (especially regarding renal work and the 8th pair of cranial neurons).

There is no compatibility with drugs that have oto- (polymyxin, ethacrynic acid and aminoglycosides with furosemide) and nephrotoxic (methoxyflurane with aminoglycosides and polymyxin) activity, and at the same time with drugs that trigger the blockade of the neuromuscular function (polymyxin, citrate, citrate, citrate, citrate, and citrate, and citrate, and citroxin). With diethyl ether, as well as halohydrocarbons used in inhalation anesthesia). The weakening of the blockade of neuromuscular activity occurs when using neostigmine.

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Storage conditions

Capocin must be kept out of the reach of small children. Temperature marks - within 25 ° С.

Shelf life

Capocin is allowed to be used within a 2-year period from the time the therapeutic drug is manufactured.

Application for children

Capocin is forbidden to use in pediatrics.

Analogs

Analogues of the drug are the substances Kapastat, Kapreostat, Kapreom with Capremabol, and in addition, Leikocin, Capreomycin and Capreomycin Sulfate.