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Lekoptin
Last reviewed: 23.04.2024
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Indications Lekoptina
It is used in such conditions:
- exertional angina ;
- vasospastic form of angina, having a stable character;
- stable form of angina, not accompanied by angiospasm;
- supraventricular tachycardia;
- WPW syndrome;
- atrial fibrillation;
- sinus tachycardia;
- elevated blood pressure values;
- atrial flutter;
- essential hypertension associated with a small circle of blood flow;
- extrasystole associated with the atria.
In the case of a hypertensive crisis, the medicament should be used in the IV method.
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Release form
The release of the drug substance takes place in tablet form - 25 tablets inside a cellular packaging and 2 packs per box (40 mg volume), or 10 tablets inside a plate and 5 plates inside a pack (80 mg volume).
Pharmacodynamics
The active ingredient of the drug is the substance verapamil. The drug slows down the movement of calcium ions in the area of the fibers of the tissues of smooth muscles. The active substance is a diphenylalkylamine derivative.
The drug has antianginal, antihypertensive and antiarrhythmic activity.
Antianginal effects develop with direct effects on peripheral hemodynamics and myocardium. The blockade of calcium ions moving inside the cells leads to a decrease in ATP transformation and weakens the contractile activity of the myocardium.
Vasodilator, chronotropic and negative inotropic properties develop with decreasing oxygen demand of the myocardium.
Lekoptin inhibits the processes of automatism, prolongs the refractory period of the sinus node, reduces the AV-conduction, reduces the tone of the myocardial membranes and prolongs the period of left ventricular diastolic relaxation.
Sometimes the medication is used to eliminate headaches caused by vascular disease.
Calcium ion blocking prevents and reduces vasodilation.
The drug inhibits metabolic processes in which the hemoprotein P450 enzyme is involved.
With regard to drugs, tolerance is not manifested, and the nature of the antianginal effect depends on the size of the dosage portion.
In the case of a bolus intravenous injection, the therapeutic effect develops immediately.
Pharmacokinetics
Suction.
More than 90% of the medicament is almost completely absorbed at high speed inside the small intestine. The average values of bioavailability in volunteers with 1-time use of Lekoptin are 22%, which can be explained by extensive metabolic processes during the 1st intrahepatic passage. The level of bioavailability doubles with repeated use.
Plasma values of Cmax verapamil when using tablets with quick release are recorded after 1-2 hours, and norverapamil - after 1 hour. Eating has no effect on the bioavailability of verapamil.
Distribution processes.
Verapamil is distributed within a variety of tissues; in volunteers, distribution volume is 1.8-6.8 l / kg. The intraplasma synthesis of the drug with protein is about 90%.
Exchange processes.
Verapamil undergoes active metabolism. In vitro metabolism tests revealed that the substance is involved in metabolism with the help of hemoprotein P450 CYP3A4, as well as CYP1A2 with CYP2C8 and CYP2C9 together with CYP2C18.
It was revealed that with the introduction of drugs to male volunteers, verapamil hydrochloride undergoes intensive intrahepatic metabolic processes with the formation of 12 metabolic products, most of which are observed in trace amounts. The main metabolic products are registered as a variety of N-and O-dealkylated elements of verapamil. Of these metabolites, only norverapamil has drug activity (about 20% of the original ligament), which was found during testing on dogs.
Excretion.
Half-life is 3-7 hours after ingestion. Approximately 50% of the ration is excreted through the kidneys throughout the 24-hour period, and 70% over the 5-day period. About 16% of the dosage is excreted with feces. Approximately 3-4% of drugs are excreted through the kidneys in an unchanged state.
The general values of verapamil clearance are practically as high as those of the hepatic circulation, and are about 1 l / hour / kg (range limits: 0.7-1.3 l / hour / kg).
Dosing and administration
The drug is used 3 times a day, in the amount of 40-80 mg in the case of treatment of angina or supraventricular tachycardia.
With elevated rates of blood pressure requires 2-time reception of drugs.
For children, the size of the dosage is calculated in a proportion of 10 mg / kg per day.
The sizes of the portions of the prolonged tablets of the drug are calculated personally, taking into account all the properties of the course of the underlying disease, related disorders and the age of the patient.
In the case of prolonged therapy, a maximum of 0.48 g of verapamil should be taken per day. It is allowed to increase the dosage portion only in emergency situations and for a short period of time.
In the case of maintenance treatment, the medication is injected through an IV drip.
People with liver disease in the severe stage need to use the medicine in dosages not exceeding 0.12 g.
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Contraindications
The main contraindications:
- reduced blood pressure in severe;
- the presence of hypersensitivity associated with verapamil;
- AV-blockade of the 2-3rd degree.
Caution and prior medical consultation is required in such situations:
- bradycardia;
- aortic stenosis having a severe form of leakage;
- myocardial infarction;
- AV blockade of the 1st degree;
- CHF;
- reduced blood pressure;
- kidney disease;
- liver failure;
- elderly age.
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Side effects Lekoptina
Among the main side effects:
- lesions in the NA: severe fatigue, fainting, dizziness with headaches, trembling in the limbs, problems with swallowing and depression. In addition, ataxia, extrapyramidal symptoms, a sense of inhibition, anxiety or drowsiness, asthenia, and increased mobility of the joints in the legs and arms;
- disorders of the function of the cardiovascular system: a significant decrease in blood pressure, tachycardia, arrhythmia with bradycardia, worsening of the flow of heart failure. Occasionally there is a collapse, myocardial infarction or asystole. In case of intravenous infusion, high-grade AV-blockade may develop at a high rate;
- digestive disorders: increased liver enzymes, increased appetite, swelling or hyperplasia affecting the gums, as well as nausea and constipation;
- others: rarely agranulocytosis, arthritis, signs of allergies, temporary loss of vision, peripheral edema, galactorrhea, thrombocytopenia, pulmonary edema, and epidermis hyperemia.
Overdose
When poisoning develops shock, AV-blockade, bradycardia and asystole, as well as significantly reduced blood pressure levels.
The victim needs to conduct gastric lavage as soon as possible and give enterosorbents. If rhythm and conduction disorder is noted, norepinephrine, calcium gluconate with atropine, isoprenaline, and plasma-substituting fluids are used.
To increase the values of blood pressure, using α-stimulants and phenylephrine.
Isoprenaline should not be co-administered with norepinephrine.
Hemodialysis does not have the desired therapeutic effect.
Interactions with other drugs
The drug can increase the blood indices of prazosin and digoxin, muscle relaxants with cyclosporine, and with it carbamazepine and theophylline with quinidine and valproic acid (due to the inhibition of metabolic processes, which are actively involved in the hemoprotein P450 enzyme).
The effect of cimetidine increases the bioavailability of verapamil by 40-50%, because it weakens the intrahepatic metabolism.
Exposure to calcium drugs significantly weakens the therapeutic efficacy of Lekoptin.
Rifampicin with nicotine and barbiturates increase the rate of intrahepatic metabolism, which reduces the blood parameters of the drug, which causes a weakening of antianginal, antiarrhythmic and antihypertensive properties.
Combination with an anesthesia of an inhalation type can cause AV-blockade, HF or bradycardia.
Negative inotropic effects are potentiated when combined with β-blockers, as a result of which bradycardia may occur or AV conduction may be disturbed.
The antihypertensive activity of the drug is reduced under the influence of prazosin or α-blockers.
The drug increases blood counts SG.
The antihypertensive effect is weakened in the case of the use of drugs with sympathomimetics.
Estrogens lead to fluid retention within the body, due to which the antihypertensive activity of verapamil is weakened.
Neurotoxic negative effect is potentiated when used in combination with lithium agents.
It is necessary to change the dosage regimen of using muscle relaxants, because the potentiation of their drug activity occurs.
Storage conditions
Lekoptin is required to be kept in a place closed from the penetration of children and sunlight.
Shelf life
Lekoptin can be used for a 5-year period from the time the drug is manufactured.
Application for children
Use in pediatrics is allowed only if the child has heart rhythm disorders.
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Analogs
Analogues of the medication are drugs Finoptin, Verogalid with Verathard and Isoptin with Verapamil.
Attention!
To simplify the perception of information, this instruction for use of the drug "Lekoptin" 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.