Capicor® [Gamma-butyrobetaine, Meldonium]

Pharmacological properties

Capicor is a complex drug whose therapeutic effects are due to a combination of two active components: meldonium dihydrate and gamma-butyrobetaine dihydrate.

This combination provides a powerful and fast cardio- and cerebroprotective effect of Capicor, eliminating the dependence of the rate of onset of therapeutic effects on the depletion of the body under conditions of ischemia and stress of various origins (including oxidative).

Gamma-butyrobetaine dihydrate enhances the action of Capicor, affecting the induction of NO biosynthesis, protects cells from the toxic effects of free radicals, normalizes oxidative homeostasis at the cellular level, and positively affects endothelial function.

Meldonium dihydrate inhibits the transport of long-chain fatty acids and their metabolites in mitochondria due to a decrease in carnitine biosynthesis, which preserves the aerobic pathway of metabolism under conditions of tissue hypoxia, prevents depletion of ATP and creatine phosphate stores in cells, the accumulation of lactic acid and the occurrence of cellular acidosis, impaired enzymatic processes and dysfunctions channels, and also with it has a certain effect on increasing the concentration in the body of gamma-butyrobetaine dihydrate.

These combined mechanisms provide the optimal level of gamma-butyrobetaine dihydrate, which leads to more pronounced and faster NO-dependent effects: vasodilating, antiplatelet, anticoagulant, antioxidant and others; affects the regulation of apoptosis and proliferation, the maintenance of vascular homeostasis, etc.

The drug has anti-ischemic, cerebro-, cardioprotective and immunocorrective effects.

With heart failure, Capicor improves myocardial contractility, increases exercise tolerance; with stable angina II and III functional class reduces the frequency of heart attacks; provides a moderate hypotensive effect and normalizes the rhythm of heart contractions.

With vascular lesions of the brain, Capicor improves cerebral hemodynamics, normalizes metabolism in nerve cells, optimizes oxygen consumption by the brain tissue, thereby achieving the effect of improving cognitive functions, mental and physical activity, normalizing the psychoemotional state, and reducing the severity of overwork.

Pharmacokinetics After administration, the drug is rapidly absorbed in the digestive tract. Bioavailability is 78%. C_max in blood plasma is achieved 1–2 hours after administration. It is metabolized in the body with the formation of two main metabolites that are excreted by the kidneys. T_½ 3–6 hours

Indications

Capsules

As part of complex therapy

IHD (angina pectoris, myocardial infarction, ischemic cardiomyopathy, post-infarction cardiosclerosis). Chronic heart failure.

Dyshormonal cardiomyopathy.

Acute and chronic disturbances of cerebral circulation (cerebral stroke, discirculatory encephalopathy, cerebrovascular insufficiency).

Cardiopsychoneurosis; vegetovascular dysfunction.

Injection

As part of complex therapy

IHD, angina pectoris, especially with insufficient effectiveness or intolerance to first-line antianginal drugs;

• chronic heart failure;
• post-infarction cardiosclerosis;
• dishormonal cardiomyopathy;
• acute and chronic cerebrovascular accident (stroke, discirculatory encephalopathy, cerebrovascular insufficiency);
• neurocirculatory dystonia and vegetovascular dysfunction;
• during rehabilitation of patients after a heart attack to increase tolerance to physical activity; to restore endothelial function in hypertension, atherosclerosis, coronary heart disease, myocardial infarction, cerebrovascular disease, renal failure, AD, primary pulmonary hypertension,diabetes, erectile dysfunction, gestosis, metabolic syndrome, etc.

Application

Capsules

Adults are prescribed by mouth, regardless of the meal.

As part of complex therapy - 2 capsules 1-3 times a day. The course of treatment is from 2 to 6 weeks.

The maximum daily dose is 6 capsules.

Repeated courses (usually 2-3 times a year) are possible after consultation with a doctor.

Due to the possible development of a stimulating effect, the last dose of the drug is recommended no later than 3-4 hours before bedtime.

Injection

Adults are prescribed iv.

As part of complex therapy - 10 ml once a day. The course of treatment is 14 days.

For further treatment, it is necessary to switch to taking the drug in the form of capsules. The course of treatment is from 2 to 6 weeks.

Repeated courses (usually 2-3 times a year) are possible after consultation with a doctor.

Contraindications

Capsules

Hypersensitivity to the drug and its components. Increased intracranial pressure (in violation of the venous outflow, intracranial tumors). Organic lesions of the central nervous system.

Injection

Hypersensitivity to the drug and its components.

Increased intracranial pressure (in violation of the venous outflow, intracranial tumors).

Pregnancy and lactation.

Childrens age (up to 18 years).

Severe impairment of liver and / or kidney function, renal and hepatic insufficiency.

Side effects

Capsules

The drug is assigned to class V toxicity.

On the part of the immune system: rarely - allergic reactions (redness of the skin, skin rash, itching, swelling).

From the side of the central nervous system: rarely - excitement.

From the cardiovascular system: rarely - tachycardia, changes in blood pressure, arrhythmia.

From the digestive system: rarely - dyspeptic phenomena.

Injection

Adverse reactions are classified according to organ systems and the incidence of MedRA: often (≥1 / 100, 1/10), rarely (≥1 / 10,000, 1/1000).

From the immune system: often - allergic reactions; rarely - hypersensitivity, including allergic dermatitis, urticaria, angioedema, anaphylactic reactions and shock.

From the psyche: rarely - excitement, a sense of fear, obsessive thoughts, sleep disturbances.

From the nervous system: often - headache; rarely - paresthesia, tremor, hypesthesia, tinnitus, vertigo, dizziness, impaired gait, fainting, fainting.

From the side of the heart: rarely - change in heart rhythm, palpitations, tachycardia / sinus tachycardia, atrial fibrillation, arrhythmia, chest discomfort / chest pain.

From the circulatory system: rarely - increase / decrease in blood pressure, hypertensive crisis, hyperemia, pallor of the skin.

On the part of the respiratory system, chest and mediastinum: often - respiratory tract infections; rarely - sore throat, cough, shortness of breath, apnea.

From the gastrointestinal tract: often - dyspepsia; rarely, dysgeusia (metallic taste in the mouth), loss of appetite, nausea, vomiting, flatulence, diarrhea, abdominal pain, dry mouth or hypersalivation.

On the part of the skin and subcutaneous tissue: rarely - rash, general / macular / papular rash, itching.

From the musculoskeletal and connective system: rarely - back pain, muscle weakness, muscle cramps.

From the kidneys and urinary system: rarely - pollakiuria.

General disorders and reactions at the injection site: rarely - general weakness, chills, asthenia, swelling, swelling of the face and legs, sensation of heat or cold, cold sweat, reactions at the injection site, including pain at the injection site.

Research: often - dyslipidemia, increased levels of CRP; rarely - ECG deviation, accelerated heart rate, eosinophilia.

special instructions

The drug is used with caution in chronic diseases of the liver and kidneys.

Due to the possible development of a stimulating effect, the last dose of the drug is recommended no later than 3-4 hours before bedtime.

Use during pregnancy or lactation.The safety of the drug during pregnancy has not been proven. To prevent a possible negative effect on the fetus during pregnancy, the drug is not prescribed.

Not revealed whether Capicor is excreted in breast milk. If Capicor treatment is necessary for the mother, then breast-feeding is stopped.

Children. The use of the drug in children is contraindicated.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. There is no data on the negative effect of the drug on the reaction rate when driving vehicles or working with other mechanisms.

Interactions

Enhances the therapeutic effects of β-adrenergic blockers, cardiac glycosides, and some antihypertensive drugs. combined use with antianginal agents, anticoagulants, antiplatelet agents, antiarrhythmic drugs, diuretics, bronchodilators is also possible.

Injection solution is not to be used simultaneously with other medicines containing meldonium (risk of side effects).

Overdose

Capsules cases of overdose are unknown. in case of overdose, symptomatic therapy.

Rr for injections. Symptoms: decreased blood pressure (manifested as headache, dizziness), tachycardia, central nervous system excitement.

Treatment. Therapy is symptomatic.

In severe overdose, renal and hepatic function should be monitored.

Storage conditions

At a temperature not exceeding 25 ° c.