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Manufacturer: Ukraine
Drugs affecting the cardiovascular system. Non-selective blockers of β-adrenergic receptors. Propranolol. ATX code C07A A05.
Propranolol is a hypotensive, antianginal, antiarrhythmic drug.
Description
Ingredients
active ingredient: propranolol;
1 tablet contains propranolol hydrochloride 10 mg;
excipients: talc, corn starch, hypromellose, colloidal silicon dioxide, calcium stearate, microcrystalline cellulose.
Dosage form
Pills.
Basic physical and chemical properties : tablets of white or almost white color, flat-cylindrical shape, with a chamfer.
Pharmacotherapeutic group
Drugs affecting the cardiovascular system. Non-selective blockers of β-adrenergic receptors. Propranolol. ATX code C07A A05.
Pharmacodynamics
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 hydrochloride, 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.
Pharmacokinetics
When ingested, propranolol hydrochloride 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%.
Indications
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).
Contraindications
Hypersensitivity to the components of Anaprilin (propranolol hydrochloride) 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.
Dosage and administration
Take orally 10-30 minutes before meals with plenty of liquid. Dosing regimen is individual. The dose and duration of treatment is determined by the doctor.
Adults.
Arterial hypertension: the initial dose is 80 mg 2 times a day. If necessary, gradually increase the dose every week, depending on the patient’s response to treatment. Usually daily doses are 160-320 mg.
Angina pectoris, agitation, migraine, essential tremor: the initial dose is 40 mg 2-3 times a day. If necessary, gradually increase the dose by the same amount at intervals of 1 week, depending on the patient’s response to treatment. Usually in angina pectoris, the range of daily doses is 80-320 mg. An adequate response to the treatment of agitation, migraine and essential tremor is observed when treated in the dose range of 80-160 mg per day, angina – 120-240 mg per day.
Arrhythmias, excitatory tachycardia, thyrotoxicosis: usually doses are 10-40 mg 3-4 times a day.
Long-term prophylactic therapy after myocardial infarction: therapy should be started 5-21 days after myocardial infarction. The initial dose is 40 mg 4 times a day for 2-3 days after that the daily dose can be increased to 80 mg 2 times a day.
Pheochromocytoma (only in combination with α-adrenergic receptors): 60 mg per day for 3 days before surgery; in inoperable cases – 30 mg per day.
Summary table of drug dosing (daily doses) | ||
Indications | Minimum dose per day | Maximum dose per day |
Arterial hypertension | 160 mg | 320 mg |
angina pectoris | 80 mg | 320 mg |
Arrhythmias | 30 mg | 160 mg |
Migraine | 80 mg | 160 mg |
Tremor | 40 mg | 160 mg |
excitations | 80 mg | 160 mg |
excitatory tachycardia | 30 mg | 160 mg |
Pheochromocytoma:
before surgery |
60 mg | 60 mg |
control in non-operated patients | 30 mg | 30 mg |
After myocardial infarction | 160 mg | 160 mg |
Elderly patients. Data on the relationship between the level of the drug in the blood and the age of the patient are contradictory. As a result, in elderly patients, the optimal dosage should be determined individually according to the clinical response.
Children. The dosage should be individual in accordance with the state of the cardiovascular system and the circumstances that led to the need for treatment.
When treating, be guided by the following schemes:
Arrhythmia, pheochromocytoma, thyrotoxicosis: the drug is used in children aged 3 years and older at a dosage of 0.25-0.5 mg/kg of body weight 3-4 times a day.
Migraine: children aged 3 to 12 years – 20 mg 2-3 times a day, over 12 years old – dosage as for adult patients.
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