Active substancePropranololPropranolol
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: propranolol hydrochloride 40 mg;

    Excipientslactose monohydrate 48,10 mg, potato starch 41,90 mg, talc 11,70 mg, sodium carboxymethyl starch (type A) 3.80 mg, gelatin 2.3 mg, magnesium stearate 1.60 mg, silicon dioxide colloid 0, 60 mg.

    Description:

    White, round tablets with bevelled edges. On one side of the tablet - risk, on one side the risks are squeezed out "4", on the other "0". The other side of the tablet is smooth.

    Pharmacotherapeutic group:Beta-blocker
    ATX: & nbsp

    C.07.A.A   Non-selective beta-blockers

    C.07.A.A.05   Propranolol

    Pharmacodynamics:

    Non-selective beta-blocker.Has antianginal, hypotensive and antiarrhythmic effect. Nonselectively blocking beta-adrenergic receptors (75% beta1 and 25% beta2-adrenergic receptors) reduces catecholamine-stimulated cAMP production from ATP, resulting in reduced intracellular calcium intake, negative chrono-, dromo-, batmo-, and inotropic effects (urezhaet frequency cardiac contractions, inhibits conduction and excitability, reduces myocardial contractility).

    At the beginning of beta-blockers application, the total peripheral vascular resistance increases in the first 24 hours (as a result of the reciprocal increase in the activity of alpha-adrenergic receptors and elimination of stimulation of beta2-adrenoreceptors of the vessels of skeletal muscles), but after 1-3 days it returns to the initial one, .

    The hypotensive effect is associated with a decrease in the minute volume of the heart, sympathetic stimulation of the peripheral vessels, a decrease in the activity of the renin-angiotensin system (important in patients with initial hypersecretion of renin), sensitivity of the aortic baroreceptors (there is no increase in their activity in response to a decrease in blood pressure) andinfluence on the central nervous system. The hypotensive effect is stabilized by the end of 2 weeks of the course appointment.

    Antianginal action is due to a decrease in myocardial oxygen demand (due to a negative chronotropic and inotropic effect). Reducing the heart rate leads to diastole lengthening and improvement of myocardial perfusion. By increasing the end diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles can increase the need for oxygen, especially in patients with chronic heart failure.

    Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and slowing of atrioventricular conduction. Oppression of impulses is noted predominantly in the antegrade and to a lesser extent in the retrograde direction through the atrioventricular node and along additional pathways. According to the classification of antiarrhythmic drugs belongs to the drugs group II. Reducing the severity of myocardial ischemia - by reducing myocardial oxygen demand, postinfarction mortality may also decrease due to antiarrhythmic action.

    The ability to prevent the development of headache of vascular genesis is due to a decrease in the expansion of cerebral arteries due to beta-adrenoblockade of vascular receptors, inhibition of catecholamine-induced platelet aggregation and lipolysis, a decrease in platelet adhesiveness, prevention of activation of clotting factors during adrenaline release, stimulation of oxygen supply to tissue and a decrease in secretion renin.

    Reduction of tremor with the use of propranolol may be due to blockade of beta2-adrenergic receptors.

    Increases atherogenic properties of blood.

    Strengthens uterine contractions (spontaneous and caused by drugs, stimulating the myometrium).

    Increases bronchial tone.

    Pharmacokinetics:

    Quickly and fairly fully (90%) is absorbed when taken orally and is relatively quickly eliminated from the body.Bioavailability after oral intake is 30-40% (the effect of "first passage" through the liver, microsomal oxidation), with prolonged intake increases (metabolites that inhibit liver enzymes are formed), its magnitude depends on the nature of food and the intensity of hepatic blood flow. Metabolized by glucuronation in the liver. The maximum concentration in blood plasma is reached after 1-1.5 hours. It has high lipophilicity, accumulates in lung tissue, brain, kidneys, heart.

    Penetrates through the blood-brain and placental barriers, into breast milk. Connection with blood plasma proteins - 90-95%. The volume of distribution is 3-5 l / kg.

    It comes with bile in the intestines, deglukuroniziruetsya and reabsorbed.

    Period half-life - 3-5 hours, against the background of the course of administration may extend to 12 hours. It is excreted by the kidneys - 90%, unchanged - less than 1%. It is not removed during hemodialysis.

    Indications:

    Arterial hypertension, angina pectoris, unstable angina, sinus tachycardia (including hyperthyroidism), supraventricular tachycardia, ciliary tachyarrhythmia, supraventricular and ventricular extrasystole, prevention of myocardial infarction (systolic blood pressure - more than 100 mm Hg) essential tremor, migraine (prevention of attacks), as an adjunct in the treatment of hyperthyroidism and thyrotoxic crisis (intolerance thyreostatics medicaments), sympathetic-adrenal crises against the background of the diencephalic syndrome.

    Contraindications:

    Hypersensitivity to the drug, atrioventricular blockade of II and III degree, sinoauricular block, sinus bradycardia, hypotension (systolic blood pressure below 90 mm Hg. v.), uncontrolled congestive heart failure IIB-III degree, acute heart failure, acute myocardial infarction (systolic blood pressure - 100 mm Hg), cardiogenic shock, pulmonary edema, sick sinus syndrome, Prinzmetal angina, cardiomegaly (without heart failure), vasomotor rhinitis, occlusive disease peripheral vascular (complicated gangrene, "intermittent claudication" alone or pain), diabetes mellitus, metabolic acidosis (in, includingdiabetic ketoacidosis), bronchial asthma, propensity to bronchospastic reactions, chronic obstructive pulmonary disease (including history), pheochromocytoma (without simultaneous use of alpha-blockers), spastic colitis, simultaneous reception with antipsychotic agents and anxiolytics (chlorpromazine, trioxazine, etc.), MAO inhibitors, lactation period.

    Carefully:

    Hepatic and / or renal failure, hyperthyroidism, myasthenia gravis, heart failure, pheochromocytoma, psoriasis, pregnancy, history of allergic reactions, Raynaud's syndrome, elderly, under 18 years of age (efficacy and safety not established).

    Pregnancy and lactation:Admission during pregnancy is possible only if the benefit to the mother exceeds the risk of side effects in the fetus and the baby. If you need to take during pregnancy, careful monitoring of the fetus is required, the drug should be discontinued 48-74 hours before the birth.
    Dosing and Administration:

    Inside, before eating, without chewing and washing down with a small amount of liquid.

    With arterial hypertension - Inward, 40 mg twice a day. If the hypotensive effect is insufficient, the dose is increased to 40 mg three times or 80 mg twice a day. The maximum daily dose is 320 mg.

    With angina pectoris, heart rhythm disturbances - in an initial dose of 20 mg 3 times a day, then increase the dose to 80-120 mg for 2-3 doses. The maximum daily dose is 240 mg.

    For the prevention of migraine, as well as with essential tremor - in an initial dose of 40 mg 3 times a day.

    If the liver and kidney function is impaired, a dose reduction is necessary.

    With impaired renal function, it is necessary to reduce the initial dose or increase the interval between doses of the drug.

    Prevention of recurrent myocardial infarction - The therapy should be started between the 5th and 21st day after a myocardial infarction in a dose of 40 mg 3 times a day for 2-3 days. Then in a dose of 80 mg 2 times a day. If necessary, you can prescribe 180-240 mg per day in divided doses.

    With hyperthyroidism (an adjuvant) - 40 mg 3-4 times a day, if necessary, it is possible to increase the dose to 120-160 mg per day.

    Side effects:

    From the cardiovascular system: sinus bradycardia, atrioventricular blockade, heart failure, palpitation, conduction disturbance of the myocardium,arrhythmias, lowering blood pressure, orthostatic hypotension, chest pain, spasm of the peripheral arteries, cold extremities.

    From the digestive tract: dry mouth, nausea, vomiting, diarrhea, constipation, epigastric pain, liver dysfunction, taste change.

    From the nervous system: rarely - headache, insomnia, nightmarish dreams, asthenic syndrome, decreased ability to rapid mental and motor reactions, agitation, depression, paresthesia, fatigue, weakness, dizziness, drowsiness, confusion or short-term memory loss, hallucinations, tremor.

    From the respiratory system: rhinitis, nasal congestion, dyspnea, bronchospasm, laryngospasm.

    From the side of metabolism: hypoglycemia (in patients with type I diabetes mellitus), hyperglycemia (in patients with type II diabetes mellitus).

    From the sense organs: dryness of the mucous eye (decreased secretion of tear fluid), visual acuity, keratoconjunctivitis.

    On the part of the reproductive system: decreased libido, decreased potency.

    From the skin: alopecia, exacerbation of psoriasis, increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions.

    From the endocrine system: decreased thyroid function.

    Allergic reactions: skin rash, itching.

    Laboratory indicators: agranulocytosis, increased activity of "hepatic" transaminases and bilirubin levels.

    Influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

    Other: muscle weakness, pain in the back or joints, chest pain, leukopenia, thrombocytopenia and withdrawal syndrome.

    Overdose:

    Symptoms: bradycardia, dizziness or fainting, lowering blood pressure, arrhythmias, shortness of breath, cyanosis of the fingernails or palms of the cramps.

    Treatment: gastric lavage, the appointment of activated charcoal, with violation of atrioventricular conduction - intravenously injected with 1-2 mg of atropine, epinephrine, at a low efficiency, a temporary pacemaker is performed; with ventricular extrasystole - lidocaine (preparations of the IA class do not apply); with arterial hypotension the patient should be in the Trendelenburg position.

    If there are no signs of pulmonary edema, intravenously injected plasma-substituting solutions, with inefficiency - epinephrine, dopamine, dobutamine; with convulsions - intravenously diazepam; with bronhospazme inhalation or parenteral - beta-adrenostimulyatory.

    Interaction:

    The hypotensive effect of propranolol is enhanced when combined with diuretics, reserpine, hydralazine and other antihypertensive agents, as well as ethanol.

    The hypotensive effect weakens non-steroidal anti-inflammatory drugs (sodium retention and blockage of prostaglandin synthesis by the kidneys), estrogens (sodium retention) and MAO inhibitors.

    Cimetidine increases bioavailability.

    Increases the concentration of lidocaine in the blood plasma, reduces the clearance of theophylline.

    Simultaneous administration with phenothiazine derivatives increases the concentrations of both drugs in blood plasma.

    Strengthens the action of thyreostatic and uterotonizing drugs; reduces the effect of antihistamines.

    Increases the likelihood of developing severe systemic reactions (anaphylaxis) against the background of the administration of allergens used for immunotherapy or for skin tests.

    Amiodarone, verapamil and diltiazem - increased severity of negative chrono, foreign and dromotropic effects of propranolol.

    Iodine-containing radiopaque drugs for intravenous administration increase the risk of developing anaphylactic reactions.

    Phenytoin with intravenous administration, drugs for inhalation of general anesthesia (derivatives of hydrocarbons) increase the severity of cardio-depressive action and the likelihood of lowering blood pressure.

    Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

    Reduces the clearance of xanthines (except diphylline).

    The hypotensive effect weakens the glucocorticosteroids.

    Cardiac glycosides, methyldopa, reserpine and guanfacine, antiarrhythmic drugs increase the risk of developing or aggravating bradycardia, atrioventricular blockade, cardiac arrest and heart failure.

    Nifedipine can lead to a significant reduction in blood pressure.

    Lengthens the effect of nondepolarizing muscle relaxants and anticoagulant effect of coumarins.

    Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedative and hypnotic drugs increase the inhibition of the central nervous system.

    It is not recommended simultaneous use with MAO inhibitors due to a significant increase in antihypertensive effect, a break in treatment between the intake of MAO inhibitors and propranolol should be at least 14 days.

    Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.

    Strengthens the action of thyreostatic and uterotonizing drugs; reduces the effect of antihistamines.

    Sulfasalazine increases the concentration of propranolol in the blood plasma (inhibits metabolism), rifampicin shortens the half-life.

    Special instructions:

    Control of patients receiving Obsidan should include monitoring the heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months), ECG.

    In elderly patients it is recommended to monitor the kidney function (1 time in 4-5 months).

    In the case of an increasing bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure less than 100 mmHg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe violations of the liver and / or kidney function in elderly patients, it is necessary reduce the dose of the drug or discontinue treatment.

    The patient should be taught how to calculate the heart rate and instructed about the need for medical advice at a heart rate of less than 50 beats per minute.

    It is recommended to stop therapy with the development of depression caused by the use of beta-blockers.

    Patients who use contact lenses should take into account that, on the background of treatment, tear fluid production can be reduced.

    Before appointment, Obsidan, patients with heart failure (early stages) should use digitalis and / or diuretics.

    Treatment of coronary heart disease and persistent arterial hypertension should be long-lasting - Adzidan's intake is possible for several years.

    Termination of treatment is carried out gradually, under the supervision of a doctor: a sharp cancellation can dramatically increase myocardial ischemia, anginal syndrome, worsen tolerance to physical exertion.

    Abolition is carried out gradually, reducing the dose for 2 weeks or more (reduce dose by 25% every 3-4 days).

    In patients with diabetes, the drug is administered under the control of blood glucose (1 time in 4-5 months).

    With thyrotoxicosis, Obsidan can mask certain clinical signs of hyperthyroidism (for example, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms.

    With the appointment of beta-blockers, patients receiving hypoglycemic drugs should be careful, because during prolonged interruptions in eating can develop hypoglycemia. And such her symptoms as tachycardia or tremor will be masked by the action of the drug. Patients should be instructed that the main symptom of hypoglycemia during treatment with beta-blockers is increased sweating.

    With caution, appoint together with hypoglycemic agents (the risk of hypoglycemia in the background of insulin therapy and hyperglycemia - against oral hypoglycemic agents).

    With the simultaneous administration of clonidine, his reception may be terminated only a few days after the withdrawal of Obsidan.

    When pheochromocytoma is prescribed only in combination with alpha-blockers.

    It can not be used simultaneously with antipsychotic drugs (neuroleptics) and tranquilizers.

    Drugs that reduce catecholamine stocks (for example, reserpine) can enhance the action of beta-blockers, so patients taking a combination of drugs should be under constant observation of the doctor for the diagnosis of arterial hypotension and bradycardia.

    Against the background of treatment Obsidan should avoid intravenous injection of verapamil, diltiazem.

    Carefully apply together with psychotropic drugs, for example, MAO inhibitors, with their course use for more than 2 weeks.

    A few days before the general anesthesia with chloroform or ether, it is necessary to stop taking the drug (increased risk of oppression of myocardial function and development of arterial hypotension).

    In "smokers" the effectiveness of beta-blockers is lower.

    During treatment it is not recommended to take ethanol (possibly a sharp drop in blood pressure).

    It is necessary to cancel the drug before examining the content in the blood and urine of catecholamines, normetanephrine and vinylamidic acid; titers of antinuclear antibodies.

    During treatment, avoid using natural licorice; food rich in protein, can increase bioavailability.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets, 40 mg.

    Packaging:

    For 20 tablets in blisters of opaque polyvinyl chloride or polypropylene film and lacquered aluminum foil.

    3 blisters together with instructions for use in a cardboard box.

    Storage conditions:

    In the dark place at a temperature of 15 - 25 ° C.

    Keep out of the reach of children.

    Shelf life:5 years.
    Do not use after the expiration date; indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N011665 / 01
    Date of registration:24.01.2012 / 10.09.2013
    Expiration Date:Unlimited
    The owner of the registration certificate:AKTAVIS GROUP, AO AKTAVIS GROUP, AO Iceland
    Manufacturer: & nbsp
    Representation: & nbspAktavis, Open Company Aktavis, Open Company
    Information update date: & nbsp19.05.2017
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