Anaprilin 10 mg tablets 50

$15.50
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Hips(cm) 87.5-89.5 91.5 94 99
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Description
Country
Russia
Active ingredient
Propranolol
Dosage
10 mg.
Composition

Active substance: Propranolol hydrochloride 10 mg.

Excipients: lactose monohydrate 78.7 mg, potato starch -24.8 mg, povidone (polyvinylpyrrolidone medium molecular weight) 3.0 mg, talc 2.3 mg, calcium stearate 1.2 mg.

Pharmacological properties

Non-selective beta-blocker. It has an antihypertensive, antianginal and antiarrhythmic effect. Due to the blockade of β-adrenergic receptors, it reduces the formation of cAMP from ATP stimulated by catecholamines, as a result of which it reduces the intracellular intake of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect (reduces heart rate, inhibits conductivity and excitability, reduces myocardial contractility). At the beginning of use Beta-blockers OPSS in the first 24 hours increases (as a result of a reciprocal increase in the activity of α adrenergic receptors and the elimination of stimulation of β 2 - adrenergic receptors of the vessels of skeletal muscles), but after 1-3 days it returns to its original, and with prolonged use it decreases.

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

The antianginal effect is due to a decrease in myocardial oxygen demand (due to the negative chronotropic and inotropic effect). A decrease in heart rate leads to an elongation of diastole and an improvement in myocardial perfusion. On account Increasing the final 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.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in AV-conduction. Inhibition of impulse conduction is noted mainly in the antegrade and to a lesser extent in the retrograde direction through the AV node and along additional paths. It belongs to the II class of antiarrhythmic drugs. Reducing the severity of myocardial ischemia - by reducing the need for myocardium in oxygen, postinfarction mortality may also decrease due to the antiarrhythmic effect.

Ability to prevent the development of headaches vascular genesis is due to a decrease in the severity of the expansion of the cerebral arteries due to beta-adrene blockade of vascular receptors, inhibition of platelet aggregation and lipolysis caused by catecholamines, a decrease in platelet adhesion, prevention of activation of blood coagulation factors during the release of adrenaline, stimulation of oxygen supply to tissues and a decrease in renin secretion.

The decrease in tremor against the background of the use of propranolol is mainly due to the blockade of peripheral β 2 - Adrenergic receptors.

Increases the atherogenic properties of blood. Enhances uterine contractions (spontaneous and caused by agents that stimulate the myometrium). Increases the tone of the bronchi. In high doses, it causes a sedative effect.

Potential mechanisms of action of propranolol in infantile hemangioma include the following interrelated therapeutic effects: local hemodynamic effect (vasoconstriction due to beta-adrenergic blockade and decreased blood flow to the focus of hemangioma); antiangiogenic effect (decrease in proliferation, neovascularization and tubulogenesis of endothelial cells due to a decrease in the activity of a key factor in the migration of endothelial cells - matrix metalloproteinase MMR-9); the effect of induction of apoptosis in endothelial cells due to the blockade of β-adrenergic receptors. Stimulation of β is known 2 Adrenergic receptors can lead to the release of vascular endothelial growth factors VEGF and bFGF and induce endothelial cell proliferation. Propranolol, blocking β 2 Adrenergic receptors, inhibits the expression of VEGF and bFGF and inhibits angiogenesis. The therapeutic efficacy of propranolol has been defined as complete or almost complete involution (resorption) of the hemangioma. The data obtained in the course of clinical trials show that the effectiveness of the use of propranolol did not differ significantly in the subgroups divided by age (35-90 days / 91-150 days), sex and location of the hemangioma (head / body); positive dynamics after 5 weeks of treatment with propranolol was noted in 88% of patients.

Indications for use

Arterial hypertension; angina pectoris, unstable angina; sinus tachycardia (including hyperthyroidism), supraventricular tachycardia, tachysystolic form of atrial fibrillation, supraventricular and ventricular extrasystole, essential tremor, migraine prevention, alcoholic withdrawal (agitation and trembling), anxiety, pheochromocytoma (auxiliary treatment), diffuse-toxic goiter and thyrotoxic crisis (as an adjuvant, including intolerance to thyrostatic drugs), sympathoadrenal crises against the background diencephalic syndrome.

Proliferating infantile hemangioma requiring systemic therapy: life-threatening or negative hemangioma influence on the functioning of body systems; ulcerative hemangioma, characterized by pain and / or lack of response to previous measures for the treatment of ulceration; hemangioma with a potential risk of persistent scarring or deformities.

Contraindications
  • AV blockade of II and III degree,
  • sinoatrial blockade,
  • pronounced bradycardia (less than 50 beats / min),
  • arterial hypotension,
  • acute or chronic heart failure in the stage of decompensation,
  • acute myocardial infarction (systolic blood pressure less than 100 mm Hg),
  • cardiogenic shock, pulmonary edema,
  • CCSU,
  • Angina pectoris Prinzmetala, cardiomegaly (without signs of heart failure),
  • severe peripheral vascular disorders,
  • metabolic acidosis (including diabetic acidosis),
  • pheochromocytoma (without the simultaneous use of alpha-blockers),
  • bronchial asthma,
  • chronic obstructive pulmonary disease,
  • tendency to bronchospastic reactions,
  • single-faith reception with antipsychotics and anxiolytics (chlorpromazine, trioxazine and others),
  • MAO inhibitors.

For newborns and infants. Reduction of heart rate below the following limits: in children aged 0 to 3 months - 100 beats / min, from 3 months to 6 months - 90 beats / min, from 6 months to 12 months - 80 beats / min; decrease in blood pressure below the following limits: in children aged 0 to 3 months - 65/45 mm Hg, from 3 months to 6 months - 70/50 mm Hg, from 6 months to 12 months - 80/55 mm Hg. Children who are breastfed, if the mother takes medications that are not recommended to be used simultaneously with propranolol.

Increased sensitivity to propranolol.

Use in pregnancy and lactation

The use of propranolol during pregnancy is possible only when the intended benefit to the mother exceeds the potential risk to the fetus. If necessary, use during this period, careful monitoring of the condition of the fetus is necessary, 48-72 hours before delivery, propranolol should be canceled.

It should be borne in mind that there may be a negative effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

Propranolol is excreted in breast milk. If necessary, use during lactation should establish medical supervision of the child or stop breastfeeding.

Use in case of impaired liver function
Use with caution in patients with liver failure.
Use in renal dysfunction
Use with caution in patients with renal Failure.
Use in children
Use with caution in children (efficacy and safety are not defined).
Use in elderly patients
Use with caution in elderly patients.
Special instructions

Use with caution in patients with bronchial asthma, COPD, bronchitis, decompensated heart failure, diabetes mellitus, renal and / or hepatic insufficiency, hyperthyroidism, depression, myasthenia gravis, psoriasis, peripheral occlusive diseases, during pregnancy, lactation, in elderly patients, in children (efficacy and safety are not determined).

With caution in newborns and infants: cardiovascular diseases, heart failure; diabetes mellitus; respiratory diseases; psoriasis; RNACE syndrome; hyperkalemia; allergic reactions in the anamnesis.

During the treatment period, an exacerbation is possible Psoriasis.

With pheochromocytoma, propranolol can be used only after taking an alpha-blocker.

After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a doctor.

Against the background of treatment with propranololol, intravenous administration of verapamil, diltiazem should be avoided. A few days before anesthesia, it is necessary to stop taking propranolol or choose a remedy for anesthesia with minimal negative inotropic effect.

Influence on the ability to drive vehicles and control mechanisms

In patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be decided only after assessing the individual reaction of the patient.

Drug Interactions

With simultaneous use with hypoglycemic agents, there is a risk of developing hypoglycemia by enhancing the action of hypoglycemic agents.

With simultaneous use with MAO inhibitors, there is a possibility of developing undesirable manifestations of drug interactions.

Cases of the development of severe bradycardia with the use of propranolol for arrhythmia caused by digitalis preparations are described.

With simultaneous use with means for inhalation anesthesia, the risk of myocardial dysfunction and the development of arterial hypotension increases.

With simultaneous use with amiodarone, arterial hypotension, bradycardia, ventricular fibrillation, asystole are possible.

With simultaneous use with verapamil, arterial hypotension, bradycardia, dyspnea are possible. Rises C max in the blood plasma, AUC increases, the clearance of propranolol decreases due to inhibition of its metabolism in the liver under the influence of verapamil.

Propranolol does not affect the pharmacokinetics of verapamil.

A case is described the development of severe arterial hypotension and cardiac arrest with simultaneous use with haloperidol.

With simultaneous use with hydralazine, C increases max in the blood plasma and AUC of propranolol. It is believed that hydralazine can reduce hepatic blood flow or inhibit the activity of liver enzymes, which leads to a slowdown in the metabolism of propranolol.

With simultaneous use, propranolol can inhibit the effects of glibenclamide, glyburide, chlorpropamide, tolbutamide, because non-selective beta 2 -Blockers are able to block β 2 - Pancreatic adrenergic receptors associated with insulin secretion.

Caused by the action of sulfonylurea derivatives, the release of insulin from the pancreas is inhibited by beta-blockers, which to some extent prevents the development of a hypoglycemic effect.

While when used with diltiazem, the concentration of propranolol in the blood plasma increases due to inhibition of its metabolism under the influence of diltiazem. There is an additive depressant effect on the activity of the heart due to a slowdown in the conduction of the impulse through the AV node caused by diltiazem. There is a risk of developing severe bradycardia, the shock and minute volume is significantly reduced.

With simultaneous use, cases of an increase in the concentration of warfarin and phenindione in the blood plasma are described.

With simultaneous use with doxorubicin in experimental studies, an increase in cardiotoxicity has been shown.

With simultaneous use, propranolol prevents the development of the bronchodilating effect of isoprenaline, salbutamol, terbutaline.

With simultaneous use, cases of an increase in the concentration of imipramine in the blood plasma are described.

With simultaneous use with indomethacin, naproxen, piroxicam, acetylsalicylic acid can reduce the antihypertensive effect of propranolol.

With simultaneous use with ketanserine, the development of an additive hypotensive effect is possible.

With simultaneous use with clonidine, the antihypertensive effect is enhanced.

In patients receiving propranolol, in the case of a sharp withdrawal of clonidine, the development of severe arterial hypertension is possible. It is believed that this is due to an increase in the content of catecholamines in the circulating blood and an increase in their vasoconstrictor action.

With simultaneous use with caffeine, it is possible to reduce the effectiveness of propranolol.

With simultaneous use, it is possible to enhance the effects of lidocaine and bupivacaine (including toxic), apparently due to a slowdown in the metabolism of local anesthetics in the liver.

With simultaneous use with lithium carbonate, a case of the development of bradycardia is described.

At Simultaneous use describes a case of increased side effects of maprotiline, which is due, apparently, to a slowdown in its metabolism in the liver and cumulation in the body.

With simultaneous use with mefloquine, the QT interval increases, a case of cardiac arrest is described; with morphine - enhances the depressant effect on the central nervous system caused by morphine; with sodium amidothrizoate - cases of severe arterial hypotension are described.

With simultaneous use with nisoldipine, an increase in C is possible max and the AUC of propranolol and nisoldipine in the blood plasma, leading to severe arterial hypotension. There is a report of an increase in beta-blocking action.

Cases of increase C are described max and AUC of propranolol, arterial hypotension and decreased heart rate when used concomitantly with nicardipine.

With simultaneous use with nifedipine in patients with coronary artery disease, the development of pronounced arterial hypotension, an increased risk of developing heart failure and myocardial infarction, which may be due to an increase in the negative inotropic effect of nifedipine.

Patients receiving propranolol are at risk of developing severe arterial hypotension after taking the first dose of prazosin.

With simultaneous use with prenylamin, the QT interval increases.

With simultaneous use with propaphenone, the concentration of propranolol in the blood plasma increases and a toxic effect develops. Propafenone is believed to inhibit the metabolism of propranolol in the liver, reducing its clearance and increasing serum concentrations.

With the simultaneous use of reserpine, other antihypertensive drugs, the risk of developing arterial hypotension and bradycardia increases.

With simultaneous use, C increases max and AUC risatriptane; with rifampicin - concentration decreases propranolol in the blood plasma; with suxametonium chloride, tubocurarine chloride - it is possible to change the action of muscle relaxants.

With simultaneous use, the clearance of theophylline decreases due to a slowdown in its metabolism in the liver. There is a risk of developing bronchospasm in patients with bronchial asthma or with COPD. Beta-blockers can block the inotropic effect of theophylline.

With simultaneous use with phenindione, cases of some increase in bleeding without changes in blood clotting indicators are described.

With simultaneous use with flecainide, an additive cardiodepressive effect is possible.

Fluoxetine inhibits the isoenzyme CYP2D6, which leads to inhibition of propranolol metabolism and its cumulation and can enhance the cardiodepressive effect (including bradycardia). Fluoxetine and mainly its metabolites are characterized by long-term T 1/2 , therefore, the probability of drug use the interaction persists even a few days after fluoxetine is discontinued.

Quinidine inhibits the isoenzyme CYP2D6, which leads to inhibition of propranolol metabolism, while reducing its clearance. Possible increased beta-adrenergic blocking effect, orthostatic hypotension.

With simultaneous use in the blood plasma, the concentrations of propranolol, chlorpromazine, thioridazine increase. A sharp decrease in blood pressure is possible.

Cimetidine inhibits the activity of microsomal liver enzymes (including the CYP2D6 isoenzyme), this leads to inhibition of propranolol metabolism and its cumulation: there is an increase in negative inotropic effect and the development of cardiodepressive action.

With simultaneous use, the hypertensive effect of epinephrine is enhanced, there is a risk of developing severe life-threatening hypertensive reactions and bradycardia. The bronchodilating effect of sympathomimetics (epinephrine, ephedrine) decreases.

With simultaneous use, cases of a decrease in the effectiveness of ergotamine are described.

There are reports of a change in the hemodynamic effects of propranolol when used simultaneously with ethanol.

Dosage and Administration

With arterial hypertension, take orally, 40 mg 2 times a day. With insufficient severity of the antihypertensive effect, the dose is increased to 40 mg 3 times or 80 mg 2 times 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 the dose is gradually increased 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 2-3 times a day, if necessary, the dose is gradually increased to 160 mg / day.

In case of violation of liver function, it is necessary to reduce doses. Impaired renal function dose adjustment does not require.

Prevention of repeated myocardial infarction - therapy should begin between the 5th and 21st day after myocardial infarction at a dose of 40 mg 4 times a day, for 2-3 days. Then in a dose of 80 mg 2 times a day.

With pheochromocytoma - use only with alpha-adrenergic receptor blockers.

Before the operation, 60 mg per day is prescribed, for 3 days.

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

Overdose

Symptoms: severe bradycardia, dizziness, atrioventricular blockade, a pronounced decrease in blood pressure, fainting conditions, arrhythmia, ventricular extrasystole, heart failure - acute or aggravation of the course of chronic heart failure, cyanosis of the nails of the fingers or palms, convulsions, difficulty breathing, bronchospasm.

Treatment: gastric lavage, the use of activated charcoal, in case of violation of atrioventricular conduction - 1-2 mg of atropine is administered intravenously, with low efficiency, a temporary pacemaker is placed; with ventricular extrasystole - lidocaine (class IA drugs are not used); with a decrease in blood pressure - the patient should be in the Trendelenburg position; with bradycardia - 1-2 mg of atropine intravenously, if necessary, setting the rhythm driver; with atrioventricular blockade - epinephrine, the setting of the rhythm driver. If there are no signs of pulmonary edema, plasma-substituting solutions are administered intravenously, with ineffectiveness - epinephrine, dopamine, dobutamine; with heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - intravenous diazepam; with bronchospasm - inhaled or parenterally beta-adrenomimetics.

Side effects

From the nervous system: increased fatigue, weakness, dizziness, headache, drowsiness or insomnia, vivid dreams, depression, restlessness, confusion, hallucinations, tremors, nervousness, restlessness.

From the senses: a decrease in the secretion of tear fluid (dryness and soreness of the eyes).

From the cardiovascular system: sinus bradycardia, AV-blockade (up to the development of a complete transverse blockade and cardiac arrest), arrhythmias, the development (aggravation) of chronic heart failure, a decrease in blood pressure, orthostatic hypotension, the manifestation of angiospasm (increased peripheral circulatory disorders, cooling of the lower extremities, Raynaud's syndrome), chest pain.

From the digestive system: nausea, vomiting, discomfort in the epigastric region, constipation or diarrhea, impaired liver function (dark urine, yellowness of the sclera or skin, cholestasis), taste changes, increased activity of hepatic transaminases, LDH.

From the respiratory side systems: nasal congestion, bronchospasm.

From the endocrine system: a change in the concentration of blood glucose (hypo- or hyperglycemia).

From the hematopoietic system: thrombocytopenia (unusual bleeding and hemorrhage), leukopenia.

Dermatological reactions: increased sweating, psoriasis-like skin reactions, exacerbation of psoriasis symptoms.

Allergic reactions: itching, skin rash, urticaria.

Other: back pain, arthralgia, decreased potency, withdrawal syndrome (increased attacks of angina pectoris, myocardial infarction, increased blood pressure).

In newborns and infants

From the nervous system: insomnia, poor quality of sleep, hypersomnia, nightmares, agitation, irritability, drowsiness.

From the cardiovascular system: AV blockade, bradycardia, decreased blood pressure, angiospasm, Raynaud's disease.

From the respiratory system: bronchitis, bronchiolitis, bronchospasm.

From the digestive system: decreased appetite, diarrhea, vomiting, constipation, abdominal pain.

Other: cooling of the limbs, a decrease in the concentration of glucose in the blood plasma, hyperkalemia, agranulocytosis, hypoglycemic convulsions.

Storage conditions

Store in a dry place at a temperature not exceeding 25 ° C. Store in places inaccessible to children.

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Product Details

Data sheet

Brand
TATCHEMPHARMPREPARATY
service_future
otc_00
Dosage form
Tablets
Dosage
10 mg
INN
Propranolol
Number of tablets
50
INN Russian
Пропранолол
Russian title
Анаприлин
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