Included in the formulation
АТХ:C.08.D.A.02 Gallopamil
Pharmacodynamics:Phenylalkylamine, methoxylated derivative of verapamil.It is a competitive antagonist of calcium ions. Reversibly blocks calcium channels. Has antianginal and antiarrhythmic effect. Reduces the need for myocardium in oxygen by decreasing myocardial contractility and decreasing heart rate. Causes coronary artery enlargement and an increase in coronary blood flow. Reduces the tone of the smooth muscles of peripheral arteries and the general peripheral vascular resistance.
Pharmacokinetics:Virtually completely absorbed in the digestive tract. Despite this, bioavailability remains low (23%) due to the high level of cleavage in the liver during the first passage. The maximum concentration in the plasma is 30-50 μg / l. When taking 50 mg 3 times a day for 12 days, the maximum concentration increases and averages 68.3 μg / l. Binding to plasma proteins in vitro 93% and does not depend on dosage, but varies with pH. It is actively metabolized in the liver. The primary metabolite, norhallopamil, is presumably pharmacologically inactive. The accumulation time of the maximum concentration is 0.83 hours. The half-life with oral administration is 4-8 hours. AUC 66.8 μg / l×h. It is excreted in urine (48%) and feces (52%).
Indications:Prevention of angina attacks (including angina prinzmetal). Secondary prevention of myocardial infarction. Arterial hypertension. Treatment and prevention of supraventricular arrhythmias (paroxysmal supraventricular tachycardia, atrial fibrillation, atrial flutter, extrasystole). Secondary prevention of myocardial infarction.
IX.I10-I15.I10 Essential [primary] hypertension
IX.I20-I25.I20 Angina pectoris [angina pectoris]
IX.I20-I25.I20.1 Angina with documented spasm
IX.I20-I25.I21 Acute myocardial infarction
IX.I30-I52.I47.1 Nadzheludochkovaya tachycardia
IX.I30-I52.I48 Atrial fibrillation and flutter
IX.I30-I52.I49.4 Other and unspecified depolarization
Contraindications:Hypersensitivity to the drug; pregnancy and the period of breastfeeding; children under 18 years of age (safety and efficacy not studied). Pronounced bradycardia, syndrome of weakness of the sinus node, cardiogenic shock, atrioventricular blockade of II-III degree, Wolff-Parkinson-White syndrome. Acute complicated myocardial infarction. Heart failure. Violations of rhythm and conduction, marked violations of the liver and kidneys.
Carefully:Moderate dysfunction of the liver and kidneys. AV-blockade of the I degree. Uncomplicated acute myocardial infarction.
Pregnancy and lactation:Do not use during pregnancy! The action category for the fetus by the FDA is C. There have not been well-controlled studies on humans. In animal experiments, the drug caused teratogenic and embryotoxic effects. Do not use the drug in lactation or stop breastfeeding for the period of treatment. There is no data on the penetration of the drug into breast milk.
Dosing and Administration:The drug is taken inwards after eating, with plenty of water, 50 mg 2-3 times a day. The minimum interval between meals is 6 hours. The maximum single dose of 50 mg. The maximum permissible daily dose of the drug is 200 mg.
Side effects:Allergic reactions: skin rash, itching, fever. On the part of the circulatory system: hypotension, bradycardia, decreased myocardial conductivity.
From the skin: swelling, redness of the face.
From the side of the central nervous system: dizziness, headache, nausea, nervousness.
From the digestive tract: constipation, as well as isolated cases of transient elevation in the blood of hepatic transaminase activity,alkaline phosphatase; development of intrahepatic cholestasis.
Overdose:There were no cases of overdose. The goals of therapy with a possible overdose are maintenance of vital functions, rapid administration of symptomatic therapy. The drug can be removed from the body by hemodialysis.
Interaction:With beta-adrenoblockers, potentiation of a negative inotropic effect is possible, an increased risk of AV blockade, bradycardia. With the means for inhalation anesthesia, the risk of developing bradycardia, AV blockade, and heart failure is increased.
With the simultaneous administration of digoxin, carbamazepine, theophylline, their concentrations in the blood plasma increase.
Rifampicin increases the concentration of gallopamil in the blood plasma.
Cimetidine increases the bioavailability of gallopamil by 40-50%.
Special instructions:In severe violations of kidney function, the dose of the drug should be reduced.