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

Active substance:
Propranolol hydrochloride (anaprilin)	10 mg	40 mg
Excipients:	- until a tablet weighing:
	100 mg	200 mg
sucrose (sugar)	68 mg	108 mg
potato starch	18.5 mg	45 mg
calcium stearate	1 mg	2 mg
talc	2.5 mg	5 mg

Description:

Tablets of white color, round, flat-cylindrical with a bevel, marked "R" on one side or without it.

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.Unselectively blocking beta-adrenergic receptors (75% of beta1 and 25% of beta2-adrenergic receptors) reduces the catecholamine-stimulated formation of cAMP from ATP, which reduces the intracellular calcium intake, has a negative chrono-, dromo-, batmo-, and inotropic effect (reduces the 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 peripheral vessels, a decrease in the activity of reninangiotensin system, (it is important in patients with initial hypersecretion of renin), the sensitivity of the aortic arch baroreceptors (there is no increase in their activity in response to a decrease in blood pressure) and influence on the central nervous system.The hypotensive effect is stabilized by the end of the 2-week course appointment.

Antianginal action is due to a decrease in the demand for myocardium in oxygen (for account of 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 content, 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. By classification antiarrhythmic drugs refers to drugs 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 the vascular receptors, inhibition of catecholamine-induced platelet aggregation and lipolysis by decreasing platelet adhesiveness by preventing the activation of clotting factors during the release of epinephrine, stimulation of oxygen supply to the tissue and a decrease in renin secretion.

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

Increases atherogenic properties of blood.

Strengthens uterine contractions (spontaneous and drug-induced, stimulating 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 administration - 30-40% (the effect of "first passage" through the liver, microsomal oxidation), with prolonged admission - 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. The half-life is 3-5 hours, against the background of the course administration, it can be extended 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 tension;

- unstable angina;

- sinus tachycardia (including hyperthyroidism);

- supraventricular tachycardia;

- atrial tachyarrhythmia;

- supraventricular and ventricular extrasystole;

- prevention of myocardial infarction (systolic blood pressure more than 100 mm Hg);

- pheochromocytoma (together with alpha-blockers);

- essential tremor;

- migraine (prevention of seizures);

- as an aid in the therapy of thyrotoxicosis and thyrotoxic crisis (with intolerance of thyreostatic drugs);

- sympathetic-adrenal crises against the background of the diencephalic syndrome.

Contraindications:

Hypersensitivity to the drug, atrioventricular blockade II-III degree, sinoauric blockade / sinus bradycardia, arterial hypotension, uncontrolled chronic heart failure IIB-III degree, acute heart failure / acute myocardial infarction (systolic blood pressure less than 100 mmHg), cardiogenic shock, pulmonary edema, sinus node weakness syndrome, prinzmetal angina, cardiomegaly (no signs of heart failure), vasomotor rhinitis, occlusive diseases peripheral vessels, diabetes mellitus, metabolic acidosis (including diabetic ketoacidosis), bronchial asthma, propensity to bronchospastic reactions, chronic obstructive pulmonary disease (including in the anamnesis ze), pheochromocytoma (without simultaneous use of alpha-adrenoblockers), spastic colitis, simultaneous reception with antipsychotic agents and anxiolytics (chlorpromazine, trioxazine, etc.), monoamine oxidase inhibitors, lactation period, age under 18 years (efficacy and safety not established).

Carefully:

Hepatic and / or renal failure, hyperthyroidism, myasthenia gravis; heart failure, pheochromocytoma, psoriasis, pregnancy, allergic reactions in the anamnesis, Raynaud's syndrome, elderly age.

Pregnancy and lactation:

The use of the drug during pregnancy is possible only if the benefit to the mother exceeds the risk of side effects in the fetus and the child, while careful monitoring of the fetus is necessary. For 48-72 hours before birth the drug should be canceled. Possible effects on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

Propranolol excreted in breast milk. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

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 2-3 times a day, if necessary, the dose is gradually increased to 160 mg / day.

If the liver 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 - therapy should be started 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 in a dose of 80 mg 2 times a day.

With pheochromocytoma - use only with alpha-adrenoreceptor blockers.

Before operation prescribe 60 mg per day, for 3 days.

Side effects:

From the cardiovascular system: sinus bradycardia, atrioventricular blockade, heart failure, palpitations, myocardial conduction disturbances, arrhythmias, lowering of arterial pressure, orthostatic hypotension, chest pain, spasm of peripheral arteries, cooling of extremities, mesenteric thrombosis.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, diarrhea, constipation, epigastric pain, liver dysfunction, taste change, ischemic colitis.

From the nervous system: headache, insomnia, nightmarish dreams, asthenic syndrome, agitation, depression, paresthesia, fatigue, weakness, dizziness, drowsiness, confusion or short-term memory loss, hallucinations, tremor, catatonia, emotional lability, decreased psychomotor reactions.

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

From the side of metabolism: hypoglycemia (in patients with type 1 diabetes mellitus), hyperglycemia (in patients with type 2 diabetes mellitus).

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

On the part of the reproductive system: decreased libido, decreased potency, Peyronie's disease.

From the skin: alopecia, exacerbation of psoriasis, increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis, exfoliative dermatitis, erythema multiforme.

From the endocrine system: decreased thyroid function.

Allergic reactions: skin rash, itching.

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

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

Overdose:

Symptoms: bradycardia, dizziness or fainting, lowering blood pressure, arrhythmias; difficulty breathing; cyanosis of finger nails or palms or 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, setting up a temporary pacemaker; 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, IV injection of plasma-substituting solutions, if ineffective - 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,hydralazine, and other antihypertensive drugs, as well as ethanol.

Hypotensive effect weakens non-steroidal anti-inflammatory drugs (forsodium suppression and blockage of prostaglandin synthesis by the kidneys), estrogens (sodium retention) and monoamine oxidase 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 - strengthening the severity of negative chrono-, foreign- and the dromotropic action of propranolol.

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

Phenytoin with intravenous administration, medicines 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 cumrins.

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

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

Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.

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

Special instructions:

Control of patients taking the drug should include monitoring the heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months), recording the electrocardiogram.

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

In the case of elderly patients increasing bradycardia (less than 50 beats / minute), hypotension (systolic blood pressure less than 100 mm Hg. V.) Atriventrikulyarnoy blockade bronchospasm, ventricular arrhythmias,severe violations of the liver and / or kidneys, you need to reduce the dose of the drug or stop 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 a reduction in tear fluid production is possible against the background of treatment.

Before the appointment of the drug, patients with heart failure (early stages) should use cardiac glycosides and / or diuretics.

Treatment of coronary heart disease and persistent hypertension should be long - taking the drug 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. Cancellation is carried out gradually, reducing the dose by 25% every 3-4 days for 2 weeks or more.

In thyrotoxicosis, the drug may mask certain clinical signs of hyperthyroidism (eg, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, because it can strengthen symptoms.

In patients with diabetes, the drug is administered under the control of blood glucose (1 time in 4-5 months). With caution appoint together with hypoglycemic agents, because during prolonged interruptions in food intake, as well as against the background of insulin therapy, hypoglycemia may develop. And such her symptoms, like tachycardia or tremor, will be masked by the action of the drug. The patient should be instructed that the main symptom of hypoglycemia during treatment with the drug is increased sweating. Also there is a risk of hyperglycemia when taking hypoglycemic agents for oral administration.

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

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

Contraindicated simultaneous use with antipsychotic drugs (neuroleptics) and tranquilizers.

Drugs that reduce stocks catecholamines (e.g., reserpine) may increase the effect of propranolol, so patients taking drug combinations should be under constant medical supervision for arterial hypotension and bradycardia.

On the background of treatment, intravenous administration of verapamil, diltiazem should be avoided.

Use with caution together with psychotropic drugs, for example, monoamine oxidase 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 the drug is reduced.

It is necessary to cancel the drug before examining the content in the blood and urine of catecholamines, normetanephrine and vanillin-mandelic acid, antinuclear antibody titers.

During treatment, it is not recommended to take alcohol (ethanol) - possible a sharp drop in blood pressure.

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 management vehicles and occupations potentially dangerous species activities that require increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, 10 mg and 40 mg.

Packaging:

For 10, 14 tablets in a contour mesh box made of a polyvinylchloride film and aluminum foil.

5, 10 contour cell packs of 10 tablets or 4, 8 contour cell packs of 14 tablets with instructions for use are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002037

Date of registration:29.08.2011 / 24.06.2013

Expiration Date:Unlimited

The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia

Manufacturer: & nbsp

UPDATE, PFC CJSC Russia

Representation: & nbspUPDATE OF PFC, CJSCUPDATE OF PFC, CJSC

Information update date: & nbsp27.08.2017

Illustrated instructions

Instructions

Anaprilin (Anaprilin)