Anaprilin (propranolol hydrochloride) tablets 0.04 №50

active ingredient: propranolol;

1 tablet contains propranolol hydrochloride 40 mg;

excipients: talc, corn starch, hypromellose, colloidal silicon dioxide, calcium stearate, microcrystalline cellulose.

Tablets.

Basic physical and chemical properties : tablets of white or almost white color, flat-cylindrical shape, with a chamfer.

Drugs affecting the cardiovascular system. Non-selective blockers of β-adrenergic receptors. Propranolol. ATX code C07A A05.

Propranolol is a hypotensive, antianginal, antiarrhythmic drug.

Propranolol blocks b1- and b2-adrenergic receptors, exhibits a membrane-stabilizing effect, suppresses the automatism of the sinoatrial node, the occurrence of ectopic foci in the atria, atrioventricular node and, to a lesser extent, in the ventricles. Reduces the speed of excitation in the atrioventricular junction along the Kent bundle, mainly in the anterograde direction. Reduces the frequency and reduces the strength of heart contractions, myocardial oxygen demand. Reduces cardiac output, blood pressure, renin secretion, renal clearance and glomerular filtration rate. Suppresses the response of baroreceptors of the aortic arch to a decrease in blood pressure.

It inhibits lipolysis in adipose tissue, preventing an increase in the level of free fatty acids (the atherogenic coefficient may increase). Suppresses glycogenolysis, the secretion of glucagon and insulin, the conversion of thyroxine to triiodothyronine. Increases the tone of the muscles of the bronchi and uterine contractility. Enhances the secretory and motor activity of the digestive tract.

In patients with coronary heart disease, it reduces the frequency of angina attacks, increases exercise tolerance, and reduces the need for nitroglycerin. Shows a cardioprotective effect, probably reducing the risk of recurrent myocardial infarction and sudden cardiac death by 20-50%.

After a single dose of propranolol, there is a decrease in systolic and diastolic blood pressure in the supine position and standing; persistent hypotensive effect develops by the end of the second week of treatment.

When ingested, it is rapidly and almost completely (90%) absorbed from the digestive tract. Bioavailability is 30-40% (the effect of the first pass through the liver) and depends on the nature of the food and the intensity of hepatic blood flow, increases with prolonged use. Cmax in plasma is achieved 1-2 hours after ingestion. It binds to plasma proteins by 90-95%, the volume of distribution is 3-5 l / kg. Shows high lipophilicity, accumulates in lung tissue, brain, kidneys and heart. Penetrates through the blood-brain and placental barriers, as well as into breast milk. Metabolized in the liver by glucuronidation (99%). T½ – 3-5 hours, with prolonged use increases to 12 hours. It is excreted mainly by the kidneys in the form of metabolites (up to 90%), unchanged – less than 1%.

Control of essential and renal hypertension, angina pectoris, long-term prophylactic therapy after myocardial infarction, control of most forms of cardiac arrhythmias, prevention of migraine, essential tremor, control of excitation and tachycardia of excitation, additional therapy for thyrotoxicosis and thyrotoxic crisis; as part of combination therapy – pheochromocytoma (only in combination with α-adrenergic receptors).

Hypersensitivity to the components of the drug cardiogenic shock, AV blockade II and III degree, sinoatrial blockade, sick sinus syndrome, sinus bradycardia (heart rate less than 50 beats / min), Prinzmetal’s angina, arterial hypotension, uncontrolled heart failure, bronchial asthma or history of bronchospasm, severe peripheral circulatory disorders, metabolic acidosis (including diabetic acidosis), after prolonged fasting, untreated pheochromocytoma, diabetes mellitus, chronic liver disease.