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Lecoptin
Last reviewed: 04.07.2025
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Indications Lecoptina
It is used in the following conditions:
- angina pectoris;
- vasospastic form of angina pectoris, which has a stable character;
- stable form of angina pectoris not accompanied by angiospasm;
- supraventricular tachycardia;
- WPW syndrome;
- atrial fibrillation;
- sinus tachycardia;
- elevated blood pressure;
- atrial fibrillation;
- essential hypertension associated with pulmonary circulation;
- extrasystole associated with the atria.
In case of hypertensive crisis, the medication must be administered intravenously.
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Release form
The medicinal substance is released in tablet form - 25 tablets in a cell package and 2 packages in a box (volume 40 mg), or 10 tablets in a plate and 5 plates in a pack (volume 80 mg).
Pharmacodynamics
The active ingredient of the drug is verapamil. The medication slows down the movement of calcium ions into the smooth muscle tissue fibers. The active ingredient is a diphenylalkylamine derivative.
The drug has antianginal, antihypertensive and antiarrhythmic activity.
Antianginal effect develops with direct influence on peripheral hemodynamics and myocardium. Blockade of calcium ion movement into cells leads to decrease in ATP transformation and weakens contractile activity of the myocardium.
Vasodilatory, chronotropic and negative inotropic properties develop as the oxygen demand of the myocardium decreases.
Lekoptin inhibits the processes of automatism, prolongs the refractory period of the sinus node, reduces the indicators of AV conduction, reduces the tone of myocardial membranes and prolongs the period of left ventricular diastolic relaxation.
Sometimes the medication is used to relieve headaches caused by vascular disease.
Blocking calcium ions prevents and attenuates vasodilation.
The drug inhibits metabolic processes in which the enzyme hemoprotein P450 is involved.
There is no tolerance to the drug, and the nature of the antianginal effect depends on the size of the dosage portion.
When administered as a bolus intravenous injection, the therapeutic effect develops immediately.
Pharmacokinetics
Suction.
More than 90% of the drug is almost completely and at high speed absorbed in the small intestine. Average bioavailability values in volunteers with a single use of Lekoptin are 22%, which can be explained by extensive metabolic processes during the first intrahepatic passage. The level of bioavailability doubles with repeated use.
Plasma Cmax values for verapamil when using immediate-release tablets are recorded after 1-2 hours, and for norverapamil - after 1 hour. Food intake has no effect on the bioavailability of verapamil.
Distribution processes.
Verapamil is distributed into many tissues; in volunteers, distribution volumes range from 1.8 to 6.8 l/kg. Intraplasmic synthesis of the drug with protein is approximately 90%.
Exchange processes.
Verapamil undergoes extensive metabolism. In vitro metabolism tests revealed that the substance is involved in metabolism by hemoprotein P450 CYP3A4, as well as CYP1A2 with CYP2C8 and CYP2C9 together with CYP2C18.
It was found that when the drug was administered to male volunteers, verapamil hydrochloride underwent intensive intrahepatic metabolic processes with the formation of 12 metabolic products, most of which were observed in trace amounts. The main metabolic products were registered as various N- and O-dealkylated elements of verapamil. Of these metabolites, only norverapamil has medicinal activity (about 20% of the original ligament), which was found during testing on dogs.
Excretion.
The half-life is 3-7 hours after oral administration. Approximately 50% of the dose is excreted via the kidneys within a 24-hour period, and 70% over a 5-day period. About 16% of the dose is excreted in the feces. Approximately 3-4% of the drug is excreted via the kidneys unchanged.
The overall clearance values of verapamil are almost as high as the hepatic blood flow indices and are approximately 1 l/h/kg (range: 0.7-1.3 l/h/kg).
Dosing and administration
The drug is taken 3 times a day, in the amount of 40-80 mg in case of treatment of angina pectoris or supraventricular tachycardia.
In case of elevated blood pressure, the medication must be taken twice a day.
For children, the dosage is calculated in the proportion of 10 mg/kg per day.
The portion sizes of prolonged-release tablets of the drug are calculated individually, taking into account all the properties of the course of the underlying disease, concomitant disorders and the age of the patient.
In case of long-term therapy, a maximum of 0.48 g of verapamil per day should be taken. Increasing the dosage portion is allowed only in emergency situations and for a short period of time.
In case of maintenance treatment, the medication is administered intravenously through a drip.
People with severe liver disease are required to take the medicine in doses not exceeding 0.12 g.
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Contraindications
Main contraindications:
- decreased blood pressure values in severe cases;
- presence of hypersensitivity associated with verapamil;
- AV block 2-3 degree.
Caution and prior medical consultation are required in the following situations:
- bradycardia;
- aortic stenosis, which has a severe form of progression;
- myocardial infarction;
- 1st degree AV block;
- CHF;
- decreased blood pressure;
- kidney diseases;
- liver failure;
- old age.
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Side effects Lecoptina
Among the main side effects:
- lesions in the nervous system: severe fatigue, fainting, dizziness with headaches, tremors in the limbs, problems with swallowing and depression. In addition, ataxia, extrapyramidal symptoms, a feeling of inhibition, anxiety or drowsiness, asthenia and difficulty in mobility of the joints in the legs and arms;
- CVS dysfunction: significant decrease in blood pressure, tachycardia, arrhythmia with bradycardia, worsening of heart failure. Collapse, myocardial infarction or asystole may occasionally occur. In case of intravenous administration at high speed, third-degree AV block may develop;
- digestive disorders: increased liver enzyme levels, increased appetite, swelling or hyperplasia affecting the gums, as well as nausea and constipation;
- Others: agranulocytosis, arthritis, signs of allergy, temporary loss of vision, peripheral edema, galactorrhea, thrombocytopenia, pulmonary edema and epidermal hyperemia occasionally occur.
Overdose
In case of poisoning, a state of shock, AV block, bradycardia and asystole develop, and blood pressure levels drop significantly.
The victim should undergo gastric lavage and enterosorbents as soon as possible. If rhythm and conduction disorders are observed, norepinephrine, calcium gluconate with atropine, isoprenaline and plasma-substituting fluids are used.
To increase blood pressure values, α-adrenergic stimulants and phenylephrine are used.
Isoprenaline should not be administered concomitantly with norepinephrine.
Hemodialysis does not have the required therapeutic effect.
Interactions with other drugs
The drug can increase blood levels of prazosin and digoxin, muscle relaxants with cyclosporine, and along with this, carbamazepine and theophylline with quinidine and valproic acid (due to the inhibition of metabolic processes, an active participant of which is the enzyme hemoprotein P450).
The influence of cimetidine increases the bioavailability of verapamil by 40-50%, because it weakens intrahepatic metabolism.
The effect of calcium drugs significantly weakens the therapeutic effectiveness of Lekoptin.
Rifampicin with nicotine and barbiturates increase the rate of intrahepatic metabolism, which causes a decrease in the blood levels of the drug, which also causes a weakening of the antianginal, antiarrhythmic and antihypertensive properties.
Combination with inhalation anesthesia may cause AV block, heart failure or bradycardia.
The negative inotropic effect is potentiated when combined with β-blockers, which may result in bradycardia or disruption of AV conduction.
The antihypertensive activity of the drug is reduced under the influence of prazosin or α-blockers.
The drug increases blood levels of SG.
The antihypertensive effect is weakened when the drug is used together with sympathomimetics.
Estrogens cause fluid retention in the body, which weakens the antihypertensive activity of verapamil.
The neurotoxic negative effect is potentiated when used in combination with lithium agents.
It is necessary to change the dosage regimen for the use of muscle relaxants, because their medicinal activity is potentiated.
Storage conditions
Lekoptin should be kept in a place out of reach of children and sunlight.
Shelf life
Lekoptin can be used for a period of 5 years from the date of production of the medicinal substance.
Application for children
Use in pediatrics is permitted only if the child has heart rhythm disorders.
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Analogues
The analogs of the drug are Finoptin, Verogalid with Veratard and Isoptin with Verapamil.
Attention!
To simplify the perception of information, this instruction for use of the drug "Lecoptin" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.