Capreomycin

Capreomycin is an anti-TB substance.

[1], [2], [3],

Indications Capreomycin

It is used in pulmonary tuberculosis that develops due to drug-sensitive Mycobacterium strains (Koch's wand is a microorganism that provokes the occurrence of tuberculosis), in situations where the first type of TB drugs do not have the desired effect or cannot be used due to toxic effects or the presence of resistant tuberculosis bacilli.

[4], [5]

Release form

The release of the medication is performed in the form of a powder for injections produced intramuscularly.

[6], [7],

Pharmacodynamics

An antibiotic that is extracted from the Streptomyces capreolus element. The drug demonstrates the activity of relatively diverse strains of Koch sticks.

Not observed cross-resistance between capreomycin, and cycloserine, isoniazid, PAS, streptomycin, ethionamide, and also ethambutol. At the same time, cross-resistance is found when the substance is combined with kanamycin, florimycin or neomycin.

[8], [9], [10]

Pharmacokinetics

The drug is almost not absorbed inside the digestive tract (less than 1%). After intramuscular administration, a 1000 mg plasma dose of Cmax (equal to 20–47 mg / l) is noted after a lapse of 1–2 hours. When using a 60-minute intravenous infusion of 1000 mg of the drug, the Cmax values are 30-50 mg / l. The level of AUC after intramuscular and intravenous administration is the same. The drug passes through the placenta, but not through the BBB.

It does not undergo metabolic processes, the excretion is performed in an unchanged condition, mainly through the kidneys (for 12 hours - approximately 50-60% of the portion), using filtration of the glomeruli. A small part of the element is excreted along with the bile. Inside the urine, the indicators of the substance for 6 hours after the use of the drug in a portion of 1 g are on average 1.68 mg / ml. Half-life is in the range of 3-6 hours.

In individuals with healthy renal activity, the substance does not accumulate when used every day in a dose of 1000 mg (for a 30-day period). If a kidney disorder is present, the half-life increases and a tendency to the accumulation of drugs develops.

[11], [12], [13]

Dosing and administration

Before use, it is recommended to determine the sensitivity of the patient regarding the microflora drug that provoked the disease. The drug should be administered in a deep, intramuscular way. It is used cautiously in persons with any forms of allergies (especially with medication).

Often, 1000 mg of drug is injected daily (maximum 20 mg / kg of substance per day) during the 60-120-day period, and later, 2-3 times per week in the same dose. Therapy should last 1-2 years.

Persons with kidney problems need to adjust the dosage and the duration of the interval between injections (taking into account the values of QC). The more pronounced the disorder of renal function, the longer the intervals between injections should be made.

Medicinal powder is pre-dissolved in a physiological injection fluid or sterile injectable water (2 ml). It takes 2-3 minutes to completely dissolve the substance.

Renal activity must be constantly monitored throughout the entire period of treatment (1 time per week), and in addition, audiometry should be performed (assess hearing acuity) and the functioning of the vestibular apparatus should be checked.

Because the use of Capreomycin can provoke the occurrence of hypokalemia, it is required to constantly monitor plasma parameters of potassium.

[16]

Use Capreomycin during pregnancy

There is no information regarding the safety of capreomycin during breastfeeding or pregnancy, which is why it can be prescribed only after evaluating all possible risks and benefits.

Contraindications

Main contraindications:

• severe intolerance associated with the use of drugs;
• combined administration with other parenteral anti-tuberculosis substances that have an oto- and nephrotoxic effect (for example, florimitsin or streptomycin);
• the use of the drug together with amikacin, tobramycin, and in addition with polymyxin sulfate or vancomycin, neomycin or colimycin, kanamycin or gentamycin should be done very carefully, because this can sum up ot-and nephrotoxic activity.

Side effects Capreomycin

The use of medication can cause some side effects:

• an increase in plasma values of creatinine and urea, as well as the appearance inside the urine of erythrocytes with leukocytes;
• there are single data on the development of electrolyte disorders and toxic nephritis;
• appearance of ototoxicity (damage to the functionality of the auditory organs);
• there were changes in indications during tests of hepatic function in many people who used the drug for complex anti-tuberculosis treatment;
• eosinophilia, leukopenia or leukocytosis. Thrombocytopenia is rarely observed;
• Allergy symptoms in the form of maculopapular eruptions, urticaria and an increase in temperature (observed with combined treatment);
• compaction and pain in the injection area;
• there is information about the appearance of severe bleeding and abscesses of the "cold" type (abscesses or abscesses of a tuberculous nature, with a weak inflammatory manifestation) at the site of drug administration.

[14], [15]

Overdose

In case of poisoning, the work of the kidneys is impaired, which can develop into an acute type of tubular necrosis (increased risks in this case in the elderly and people with dehydration or an existing problem in the work of the kidneys). Damage to the vestibular and auditory zones of the 8th pair of cranial neurons is also noted. It is possible to block the activity of the neuromuscular system, sometimes reaching the cessation of the respiratory processes (often due to the rapid introduction of drugs) and an imbalance of electrolytes (hypokalemia, magneemia or calcium).

Symptomatic measures are carried out: support of blood flow and respiratory function, and in addition, hydration, which allows urine outflow to reach 3-5 ml / kg / hour (normal kidney function), which will help prevent neuromuscular blocking. To prevent apnea and suppression of respiration, anticholinesterase substances or calcium medications are used, and hemodialysis is also performed (especially in people with severe forms of renal dysfunction). It is also required to track the values of VEB and KK.

[17], [18]

Interactions with other drugs

Cisplatin with vancomycin increases the risk of nephro- or ototoxic manifestations.

There is no compatibility with drugs that have ototoxic (furosemide with aminoglycosides, and ethacrynic acid with polymyxins) and nephrotoxic (aminoglycosides with methoxyflurane and polymyxins) effects, and besides with substances that cause the blocking of neuromuscular activity (myimomas), and in addition to the substances that provoke the blocking of the neuromuscular activity (Iems). For inhalation anesthesia, diethyl ether, as well as citrated blood preservatives).

The muscle relaxant effect is reduced when using neostigmine methyl sulfate.

[19], [20], [21]

Storage conditions

Capreomycin is required to be kept in a place closed to small children. Temperatures are a maximum of 25 ° C.

[22]

Shelf life

Capreomycin can be used for a 2-year period from the time the pharmaceutical substance is manufactured.

[23], [24]

Application for children

There are no data regarding the safety of the use of the drug in pediatrics.

[25], [26]

Analogs

Analogues of the drug are means Benemycin, Rifampicin, Cycloserin with Kapocin, Msserin with Rifabutin, and in addition Coxerine, Rifapentin, Makoks with P-zinex and P-butin with Rifacin. The list also includes Micobutin, R-ching and Rifapex.

[27], [28], [29]