Anaprilin - instructions for use, doses, side effects, contraindications

He selectively blocking beta-adrenoceptors (75% of beta1 and 25% of beta2-adrenoreceptors), reduces catecholamine-stimulated cAMP production from ATP,as a result of which intracellular calcium intake decreases; has a negative chrono-, dromo-, batmo- and inotropic action (it reduces heart beats, inhibits conduction and excitability, reduces myocardial contractility).

At the beginning of the use of propranolol, the total peripheral resistance (OPSS) increases (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 of treatment it returns to the initial one, and with prolonged treatment it decreases.

Hypotensive effect is associated with a decrease in the minute volume of the circulation, the sympathetic stimulation of the peripheral vessels, a decrease in the activity of the renin-angiotensin system (important in patients with initial renin hypersecretion), the sensitivity of the aortic baroreceptors (there is no increase in their activity in response to a decrease in blood pressure) and influence on the central nervous system (CNS). Arterial pressure is stabilized by the end of the 2-week course of treatment.

Antianginal action is caused by a decrease in myocardial oxygen demand (due to a negative chronotropic and inotropic effect). Reducing the number of cardiac contractions (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, it can increase the need for oxygen, especially in patients with chronic heart failure (CHF).

Antiarrhythmic effect is caused by 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 (AV) of the conduct. The suppression of impulses is noted predominantly in the antegrade and, to a lesser extent, retrograde direction through AV node and by additional paths.

According to the classification of antiarrhythmic drugs propranolol refers to preparations of 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; decreased adhesion of platelets; preventing the activation of clotting factors during the release of epinephrine; stimulation of oxygen in the tissue and a decrease in renin secretion.

Reduction of tremor on the background of the use of propranolol is due primarily to blockade of peripheral beta2-adrenergic receptors.

Increases atherogenic properties of blood.

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

Increases bronchial tone; in large doses causes a sedative effect.

Pharmacokinetics:

Quickly and fairly fully (90%) is absorbed when taken orally and is relatively quickly eliminated from the body. Bioavailability after oral administration - 30-40% (the effect of "first passage" through the liver), with prolonged admission - increases (metabolites that inhibit liver enzymes are formed),its magnitude depends on the nature of food and the intensity of the hepatic blood flow.

The time to reach the maximum concentration is 1-1.5 hours. It has high lipophilicity, accumulates in lung tissue, brain, kidneys, heart. Penetrates through the blood-brain barrier (GEB), the placental barrier, into breast milk. The volume of distribution is 3-5 l / kg. The connection with plasma proteins is 90-95%.

Metabolized by glucuronation in the liver. It comes with bile in the intestines, deglukuroniziruetsya and reabsorbed, resulting in a half-life (T_1/2) against the background of the course of reception may extend to 12 hours. It is excreted by the kidneys - 90%; in unchanged form - less than 1%. It is not removed during hemodialysis.

Indications:Arterial hypertension, angina pectoris, unstable angina, sinus tachycardia (including thyrotoxicosis), supraventricular tachycardia, ciliary tachyarrhythmia, supraventricular and ventricular extrasystole, secondary prevention of myocardial infarction (systolic blood pressure more than 100 mmHg); essential tremor; pheochromocytoma (auxiliary treatment); migraine (prevention of seizures); diffusive toxic goiter and thyrotoxic crisis (as an auxiliary drug, incl.with intolerance of thyreostatic drugs); sympatoadrenal crises against the background of diencephalic syndrome.

Contraindications:

Hypersensitivity, acute heart failure (CH), or decompensated CHF, cardiogenic shock, AV blockade II-III (systolic blood pressure less than 90 mm Hg, especially with myocardial infarction), arterial hypotension (systolic blood pressure less than 90 mm Hg, angina pectoris), sinus arteriosclerosis, sinus node weakness (SSSU), sinus bradycardia (heart rate less than 55 / min), prinzmetal angina, cardiomegaly (no signs of heart failure) ); chronic obstructive pulmonary disease, bronchial asthma (severe course); Occlusal diseases of peripheral vessels (complicated by gangrene, "intermittent" lameness or pain at rest); diabetes mellitus with ketoacidosis, metabolic acidosis; simultaneous administration of MAO inhibitors; lactation period; age to 18 years (effectiveness and safety not defined).

Carefully:

Allergic reactions in history, CHF, pheochromocytoma, hepatic insufficiency, chronic renal failure, Raynaud's syndrome, myasthenia gravis, thyrotoxicosis, depression (including history), psoriasis, pregnancy, elderly age.

Pregnancy and lactation:

Use in pregnancy and lactation is possible if the benefit to the mother exceeds the risk of side effects in the fetus and the baby.

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

If you need to take during pregnancy - careful monitoring of the fetus, for 48-72 h before delivery should be canceled.

Dosing and Administration:

Inside.

With arterial hypertension - 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 the dose is gradually increased to 80-120 mg for 2-3 doses. The maximum daily dose is 240 mg. Prevention of repeated myocardial infarction: therapy is initiated between the 5th and 21st day after a myocardial infarction in a dose of 40 mg 4 times a day for 2-3 days; then 80 mg twice a day.

Prevention of migraine, with an essential tremor - the initial dose of 40 mg 2-3 times a day, if necessary, the dose is gradually increased to 160 mg / day.

If the liver function is impaired, lower doses are necessary.

Dysregulation of renal dosing does not require correction.

Side effects:

From the sense organs: a violation of visual acuity, a decrease in the secretion of tear fluid, dryness and soreness of the eyes, keratoconjunctivitis.

From the side of the cardiovascular system: sinus bradycardia, palpitation, conduction disturbance of the myocardium, AV blockade (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakening of myocardial contractility, development (aggravation) of CHF; reduction of blood pressure, orthostatic hypotension, angiospasm (increased peripheral circulatory disturbance, lower extremities cooling, Raynaud's syndrome), chest pain.

From the digestive system: dryness of the oral mucosa, changes in taste, nausea, vomiting, epigastric pain, flatulence, constipation or diarrhea, impaired liver function (dark urine, icteric sclera or skin, cholestasis).

From the respiratory system: nasal congestion, rhinitis, difficulty breathing, laryngo- and bronchospasm.

From the nervous system (rarely): increased fatigue, weakness, dizziness, headache, drowsiness or insomnia, nightmarish dreams, depression, anxiety,confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis, paresthesia in the extremities (in patients with intermittent claudication and Raynaud's syndrome), tremor.

From the endocrine system: Hyperglycemia (in patients with insulin-independent diabetes mellitus), hypoglycemia (y of patients receiving insulin), a decrease function thyroid gland.

Allergic reactions: itching, skin rash, hives.

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

Laboratory indicators: Thrombocytopenia, agranulocytosis, leukopenia, increased activity of "hepatic" transaminases, hyperbilirubinemia.

Other: pain in the back, arthralgia, weakening of libido, decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure).

Overdose:

Symptoms: severe bradycardia, dizziness, AV blockade, marked decrease in blood pressure, syncope, arrhythmia, ventricular extrasystole, heart failure, convulsions, difficulty breathing, bronchospasm.

Treatment: gastric lavage, the appointment of activated charcoal, if violated AV conductivity - iv injection of 1-2 mg of atropine, at a low efficiency, a temporary pacemaker is performed; with ventricular extrasystole - lidocaine (preparations Ibut the class does not apply); with a decrease in blood pressure, the patient should be in the Tren Delenburg position. If there are no signs of pulmonary edema, IV injection of plasma-substituting solutions, if ineffective - epinephrine, dopamine, dobutamine; with CH - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam; with bronhospazme - inhalation or parenteral beta-adrenostimulyatory.

Interaction:

Allergens used for immunotherapy, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving propranolol.

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

Phenytoin with IV injection, drugs for inhalation of general anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive 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 lidocaine and xanthines (except diphylline) and increases their concentration in the plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.

The hypotensive effect weakens non-hormonal anti-inflammatory drugs (sodium retention and blockade of prostaglandin synthesis by the kidneys); glucocorticosteroids and estrogens (sodium ion retention in the body).

Cardiac glycosides, methyldopa, reserpine and guanfacine, BCCC (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing bradycardia, AV blockade, cardiac arrest and heart failure.

Nifedipine can lead to a significant reduction in blood pressure.

Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensives can lead to excessive blood pressure lowering.

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

Tri- and tetracyclic antidepressants, antipsychotic drugs (antipsychotics), ethanol, sedatives and hypnotics increase the depression 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.

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

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

Special instructions:

Control of patients receiving propranolol, should include monitoring of heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months), ECG, the concentration of glucose in the blood in patients with diabetes mellitus (1 time in 4-5 months). In elderly patients it is recommended to follow the function of the kidneys (once every 4-5 months).

It is necessary to teach the patient how to calculate heart rate and instruct him about the need for medical consultation with a decrease in heart rate of less than 50 beats per minute.

Before prescribing propranolol, patients with CHF (early stages) should use digitalis and / or diuretics.

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

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

Patients with pheochromocytoma should be prescribed only after taking an alpha-blocker. With thyrotoxicosis propranolol can mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms.

When prescribing propranolol, patients receiving hypoglycemic drugs should be careful, because during prolonged interruptions in eating, hypoglycemia may develop.

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

It is possible to increase the severity of the hypersensitivity reaction and the lack of effect from the usual doses of epinephrine against the background of a burdened allergic anamnesis.

It is necessary to stop taking propranolol several days before the general anesthesia with chloroform or ether.

Drugs that reduce catecholamine stores (for example, reserpine), may increase the effect of propranolol, so patients taking such combinations should be under constant medical supervision on subject identify arterial hypotension or bradycardia.

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

Carefully apply in conjunction with psychoactive drugs, such as MAO inhibitors, with their course use for more than 2 weeks.

In the case of an increased bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mm Hg) in elderly patients, AV blockade, bronchospasm, ventricular arrhythmias, severe impairment of liver and kidney function, it is necessary to reduce the dose or stop treatment.

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

Do not abruptly interrupt treatment because of the risk of developing severe arrhythmias and myocardial infarction.Cancellation is carried out gradually, reducing the dose for 2 weeks or more (by 25% in 3-4 days).

It is necessary to abolish the drug before determining the amount of catecholamines, normetanephrine and vanillylmandelic acid; titers of antinuclear antibodies in the blood and urine of the patient.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:Tablets, 40 mg.

Packaging:

For 10, 15 or 20 tablets per contour cell package.

1, 2, 3 or 5 packs with instructions for use are placed in a pack.

Storage conditions:

Store at a temperature not exceeding 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:LS-002339

Date of registration:05.07.2010

Expiration Date:Unlimited

The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-FORESTRY, OJSC Russia

Information update date: & nbsp28.08.2017

Illustrated instructions

Instructions

Anaprilin (Anaprilin)