$39.00
Manufacturer: Germany
Ischemic heart disease, including stable stress angina; unstable angina (progressive angina, resting angina); vasospastic angina (variant angina, Prinzmetal angina); postinfarction angina in patients without heart failure, unless b-blockers are indicated. Arrhythmias: paroxysmal supraventricular tachycardia; atrial flutter / flicker with rapid atrioventricular conduction (except for wolf-Parkinson-white syndrome (WPW). Arterial hypertension.
Description
Izoptin SR Composition
active substance: verapamil hydrochloride;
1 tablet contains 240 mg of verapamil hydrochloride;
excipients: microcrystalline cellulose, sodium alginate, povidone, magnesium stearate, purified water, hypromellose, macrogol 400, macrogol 6000, talc, titanium dioxide (E 171), quinoline yellow (E 104) + indigotin (E 132) (aluminum varnish E104 + E 132), mountain wax glycol.
Izoptin SR Dosage form
Extended-release tablets.
Basic physical and chemical properties: film-coated tablets, light green, oblong in shape, have transverse marks on both sides; on the one hand – embossed with two company logos.
Izoptin SR Pharmacotherapeutic group
Selective calcium channel blockers with direct effects on the heart, phenylalkylamine derivatives. ATX code С08D A01.
Pharmacodynamics
Verapamil blocks the transmembrane flow of calcium ions into cardiomyocytes and vascular smooth muscle cells. It directly reduces myocardial oxygen demand by affecting the energy-consuming metabolic processes in myocardial cells and indirectly affects the reduction of afterload. By blocking the calcium channels of the smooth muscle cells of the coronary arteries, blood flow to the myocardium increases, even in the post-stenotic areas, and the spasm of the coronary arteries is eliminated. The antihypertensive efficacy of verapamil is due to a decrease in peripheral vascular resistance without an increase in heart rate as a reflex response. No undesirable changes in the physiological values of blood pressure are observed. Verapamil has a pronounced antiarrhythmic effect, especially in supraventricular arrhythmias. It delays the conduction of the impulse in the atrioventricular node, as a result of which, depending on the type of arrhythmia, the sinus rhythm is restored and / or the ventricular rate is normalized. The normal heart rate level does not change or decreases slightly.
Pharmacokinetics
Verapamil hydrochloride is a racemic mixture consisting of equal parts of the R-enantiomer and the S-enantiomer. Verapamil is actively metabolized. Norrapamil is one of 12 metabolites that are detected in urine, has 10-20% of the pharmacological activity of verapamil and accounts for 6% of the excreted drug. Equilibrium plasma concentrations of norverapamil and verapamil are the same. Equilibrium concentration is achieved 3-4 days after repeated administration of the drug once a day.
Absorption
More than 90% of verapamil after administration is rapidly and almost completely absorbed in the small intestine. The average bioavailability after a single dose of long-acting verapamil is approximately 33%, which is explained by extensive metabolism during the first passage through the liver. Bioavailability doubles after repeated administration.
After taking verapamil of prolonged action, the maximum concentration of verapamil in the blood plasma is reached after 4-5 hours, norverapamil – after 5 hours. Food intake does not affect the bioavailability of verapamil.
Distribution
Verapamil is widely distributed in body tissues, in healthy volunteers the volume of distribution is from 1.8 to 6.8 l / kg. Plasma protein binding of verapamil is about 90%.
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