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Blocker of slow calcium channels. The active ingredient is verapamil. The drug inhibits the transport of calcium ions into smooth muscle fibers. The main component is derived difenilalkilamina. The drug has antihypertensive, antianginal,
antiarrhythmic effects
. Antianginal effect is due to a direct effect on the myocardium,
peripheral hemodynamics
. When the blockade of flow of calcium ions into the cell of ATP is reduced, decreased myocardial contractility. Chronotropism, vasodilatory, negative inotropic effects are manifested with a decrease in myocardial oxygen demand. Lekoptin suppresses automaticity, prolongs the refractory period
sinus node
It reduces atrioventricular conduction, reduces the tone of the walls of the myocardium increases during the diastolic relaxation of the left ventricle. In some cases, Lekoptin prescribed for the relief of headaches caused by vascular disease. Due to the blockade of calcium is prevented, attenuated vasodilatation. The drug inhibits the metabolism, which involved enzyme cytochrome P450.
Tolerance
It does not develop, and antianginal effects is dose-dependent. When intravenous bolus Lekopten starts its action immediately. Available as a solution, capsules, pills, tablets.
Indications:
Lekoptin prescribed for angina voltage, stable vasospastic angina , Stable angina without vasoconstriction, with supraventricular tachycardia , With the syndrome WPW, atrial tachyarrhythmia, sinus tachycardia , Hypertension, atrial flutter, primary hypertension in the pulmonary circulation, with atrial arrhythmia . At hypertensive crisis drug is administered intravenously.
Contraindications:
Lekoptin not indicated in severe hypotension , Pregnancy, intolerance of verapamil, atrioventricular block grade 2-3, breastfeeding. In severe aortic stenosis, bradycardia, atrioventricular block of 1 degree, myocardial infarction, hypotension, heart failure, pediatric, with renal disease, hepatic failure system, the elderly Lekoptin prescribed with caution after prior consultation of doctors.
Side effect:
Nervous system: fainting, headache, dizziness, fatigue, difficulty swallowing, ataxia, tremors, depression, drowsiness, extrapyramidal disorder , Lethargy, fatigue, stiffness in the joints of the arms and legs, anxiety. Cardiovascular system: tachycardia , Worsening of heart failure flow, pronounced decrease in blood pressure, bradycardia, arrhythmia, rarely evolving myocardial infarction, collapse, asystole, with rapid intravenous possible degree atrioventricular block 3. Digestive system: increased appetite, increased liver enzymes concentrations, constipation , Nausea, gingival hyperplasia, swelling of the gums. Rarely develop allergic reactions, agranulocytosis, pulmonary edema, transient loss of vision, arthritis, galactorrhoea, flushing of the skin, peripheral edema, thrombocytopenia .
Overdose:
Manifests a pronounced fall in blood pressure, bradycardia, atrioventricular block, shock, asystole . Requires early gastric lavage, enterosorbents, in violation of the conduction rate intravenous atropine, norepinephrine, isoprenaline, calcium gluconate, plazmozameschayuschie solutions . For high blood pressure prescribed phenylephrine, alpha adrenostimulyatorov . It is unacceptable and isoprenaline administration norepinevrina simultaneously. Hemodialysis is recognized as ineffective.
Mode of application:
Lekoptin taking thrice per day at 40-80 mg supraventricular tachycardia , Angina. In patients with hypertension -2 reception. Babies verapamil amount calculated by the circuit 10 mg / kg / day. Dosing of prolonged forms of the drug is made individually, taking into account all the features of the underlying disease, comorbidities, age of the patient. Prolonged use of verapamil daily amount should not exceed 480 mg. The increase in dosage is permissible only in exceptional cases, for a short time. When maintenance therapy drug is administered intravenously. In severe liver disease Lekoptin system is administered in a dose of less than 120mg.
Special instructions:
Before therapy is carried out compensation Heart Failure . During treatment, control the operation of the respiratory system, the cardiovascular system, blood sugar, the amount of urine, the level of electrolytes in blood. In infants, newborns are registered heavy hemodynamic effects . It is unacceptable abrupt discontinuation of supply of the drug in the human body Lekoptin.
Drug Interactions:
Lekoptin able to raise the level muscle relaxants . carbamazepine , Prazosin, theophylline, digoxin, cyclosporin, valproic acid, quinidine blood, due to the suppression of metabolism, wherein the enzyme is actively involved Cytochrome P450 . Under the action of cimetidine increases the bioavailability of the verapamil 40-50 percent due to the reduction in hepatic metabolism of the system. Influenced calcium supplements efficacy Lekoptin znaichtelno falls. Nicotine rifampicin Barbiturates accelerate the metabolic processes in the liver, leading to a decrease in drug levels in the blood, respectively, decreases the severity of antiarrhythmic, antianginal, antihypertensive effects. The simultaneous use Anesthetic It can be the cause of heart failure, atrioventricular block, bradycardia . Minus inotropic effect enhanced in combination with beta-blockers That may cause bradycardia, atrioventricular conduction break. The hypotensive effect is reduced by the action of alpha-blockers, prazosin. Lekoptin increases cardiac glycosides in blood. The antihypertensive effect is reduced when taking sympathomimetic. Estrogen causes fluid retention in the body, which is the reason for the decline of the hypotensive effect of verapamil. The neurotoxic side effects enhanced by prescribing lithium. Requires change the dosage of muscle relaxants because of increasing their activity.