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

Excipients: sucrose (sugar) 50.0 mg, potato starch 52.6 mg, lactose monohydrate (milk sugar) 50,0 mg, calcium stearate 2,0 mg, talcum powder 5,0 mg.

Description:

Tablets of white or almost white color are round plane-cylindrical with a facet and a risk.

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.It has antianginal, antihypertensive and antiarrhythmic effect. Not selectively blocking beta-adrenoceptors (75% beta₁- and 25% beta₂-adrenoceptors), reduces catecholamine-stimulated formation of cyclic adenosine monophosphate from adenosine triphosphate, resulting in decreased intracellular intake of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect (reduces the number of cardiac contractions, inhibits conduction and excitability, reduces myocardial contractility) .

At the beginning of beta-blockers application, the total peripheral vascular resistance in the first 24 h - increased (as a result of the reciprocal increase in the activity of alpha-adrenergic receptors and elimination of beta stimulation₂adrenoreceptors of vessels of skeletal musculature), but after 1-3 days it returns to the initial one, and for a long-term purpose it decreases.

Antihypertensive effect is associated with a decrease in cardiac output, a decrease in the sympathetic innervation of peripheral vessels, a decrease in the activity of the reninangiotensin-aldosterone system (important in patients with initial hypersecretion of renin),a decrease in 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 antihypertensive effect is stabilized by the end of week 2 of the drug.

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

Antiarrhythmic effect is caused by the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of cyclic adenosine monophosphate, 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 mainly in antegrade and, to a lesser extent, in retrograde directions through the atrioventricular node and along additional paths. According to the classification of antiarrhythmic drugs belongs to the 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 migraine in vascular genesis is due to a decrease in the expansion of cerebral arteries due to beta adrenoblockade of vascular receptors.

Reduction of tremor in the background of the use of propranolol is due, mainly, to the blockade of peripheral beta₂adrenoreceptors.

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 administration 30-40% (effect of "primary" passage throughliver, 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. The maximum concentration in the blood plasma is reached after 1-1.5 hours. It has high lipophilicity, accumulates in the lung tissue, brain, kidneys, heart. Penetrates through the blood-brain barrier, the placental barrier, into breast milk. The volume of distribution is 3-5 l / kg. The connection with plasma proteins is 90-95%.

It is metabolized in 3 ways - aromatic hydroxylation, n- Dealkylation, glucuronation in the liver (including with the participation of cytochrome isoenzymes CYP2D6, CYP1A2, CYP2C19) - getting bile into the intestines, deglukuroniruetsya and reabsorbiruetsya, as a result, the half-life period against the background of the course of administration may extend to 12 hours, also in elderly patients and patients with impaired renal and hepatic function, the concentration of the drug in the blood plasma increases and the half-life extends. Half-life is 3-5 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 with thyrotoxicosis), supraventricular tachycardia, ciliary tachyarrhythmia, supraventricular and ventricular extrasystole;

- myocardial infarction (to reduce cardiovascular mortality after myocardial infarction in patients with stable hemodynamic parameters, systolic blood pressure more than 100 mm Hg);

- essential tremor;

- migraine (prevention of seizures);

- pheochromocytoma (with simultaneous use of alpha-blockers);

- diffuse-toxic goiter and thyrotoxic crisis (as an auxiliary drug, including intolerance of thyreostatic drugs), sympathoadrenal crises against the background of the diencephalic syndrome.

Contraindications:

Hypersensitivity to the drug components, acute and chronic heart failure in the stage of decompensation, cardiogenic shock, atrioventricular block II- III degree, severe sinus bradycardia (the number of heartbeats is less than 50 (beats) per minute), sinoatrial blockade,sick sinus syndrome, Prinzmetal angina, cardiomegaly, severe peripheral circulatory disorders, metabolic acidosis, asthma, susceptibility to bronchial obstruction, chronic obstructive pulmonary disease, simultaneous monoamine oxidase inhibitors, simultaneous antipsychotic and anxiolytic agents, lactation, chronic heart failure, indicating functional class, pulmonary edema, diabetes mellitus, lactose intolerance, lactase deficiency, glucose-galactate malabsorption, sugar / isomaltase deficiency, fructose intolerance, because preparation contains sucrose, age 18 years, severe hypotension (systolic blood pressure less than 90 mm Hg. v.), acute myocardial infarction (systolic blood pressure above 100 mmHg), simultaneous intravenous verapamil and diltiazem, pheochromocytoma ( without simultaneous use of alpha-blockers).

Carefully:

When I degree atrioventricular block, liver and / or kidney failure, hyperthyroidism, myasthenia gravis, chronic heart failure I-II functional class for NYHA, psoriasis, with pregnancy, a burdened allergological anamnesis, violation of peripheral circulation, depression, elderly patients, pheochromocytoma (with simultaneous use of alpha-blockers).

Pregnancy and lactation:

Use in pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus. If it is necessary to use during this period, careful monitoring of the fetus should be done, since the use of the drug Anaprilin in pregnancy can cause intrauterine growth retardation, hypoglycemia and bradycardia in the fetus. For 48-72 hours before delivery, the drug should be withdrawn.

In the period of lactation, the use is contraindicated. If it is necessary to use propranolol during this period, breastfeeding should be discontinued.

Dosing and Administration:

Anaprilin is taken internally.

With arterial hypertension - Inward, 40 mg twice a day. If the antihypertensive 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 daily dose is gradually increased to 80-120 mg (taken 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 per day.

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 4 times a day for 2-3 days. Then in a dose of 80 mg 2 times a day.

With pheochromocytoma - apply only with alpha-adrenoblockers in the preoperative period of 60 mg per day for 3 days.

If there is a violation of the kidney function, dose adjustment does not require.

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

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.

Side effects:

From the central nervous system: increased fatigue, weakness, dizziness, headache, drowsiness or insomnia, bright dreams, asthenic syndrome,decreased ability to rapid mental and motor reactions, agitation, depression, anxiety, confusion or short memory loss, hallucinations, tremor, nervousness, paresthesia, catatonia, emotional lability.

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

From the side of the cardiovascular system: sinus bradycardia, atrioventricular blockade (up to the development of complete transverse blockade and cardiac arrest), palpitations, conduction disturbances of the myocardium, arrhythmia, development of chronic heart failure, marked decrease in arterial pressure, orthostatic hypotension, manifestation of angiospasm (increased peripheral circulatory disturbance, cooling of limbs, Raynaud's syndrome), chest pain, mesenteric thrombosis.

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

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

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

From the endocrine system: decreased thyroid function.

Allergic reactions: skin itching, skin rash, hives, Stevens-Johnson syndrome.

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

Laboratory indicators: agranulocytosis, thrombocytopenia (unusual hemorrhages and hemorrhages), leukopenia, eosinophilia, increased activity of "hepatic" transaminases and bilirubin level, lactate dehydrogenase, an increase in the titer of antinuclear antibodies.

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

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

If any of the side effects indicated in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor!

Overdose:

Symptoms: severe bradycardia, dizziness or fainting, atrioventricular blockade, marked decrease in arterial pressure, arrhythmias, ventricular extrasystole, heart failure, cyanosis of the fingernails or palms, convulsions, difficulty breathing, bronchospasm.

Treatment: gastric lavage, the use of activated charcoal, with violation of atrioventricular conduction - intravenously inject 1-2 mg of atropine, epinephrine, at a low efficiency, a temporary pacemaker is performed; with ventricular extrasystole - lidocaine (preparations IA class do not apply); with a decrease in blood pressure - the patient should be in the Trendelenburg position; with bradycardia - 1-2 mg of atropine intravenously, if necessary staging the pacemaker. If there are no signs of pulmonary edema, intravenously injected plasma-substituting solutions, with inefficiency - epinephrine, dopamine, dobutamine; with heart failure - cardiac glycosides, diuretics; with convulsions - intravenously diazepam; with bronhospazme - inhalation or parenteral - beta-adrenomimetiki.

Interaction:

With simultaneous use with monoamine oxidase inhibitors, there is a significant increase in antihypertensive action, so this combination is contraindicated; a break in the treatment between taking monoamine oxidase inhibitors and propranolol should be at least 14 days.

With simultaneous use with diuretics, reserpine, hydralazine and other antihypertensive agents, as well as ethanol, the antihypertensive effect of propranolol is enhanced (which can lead to an excessive decrease in blood pressure).

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

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

With the simultaneous use of propranolol and amiodarone, verapamil and diltiazem, the severity of negative chrono-, ino- and dromotropic action is enhanced.

With intravenous iodine-containing radiocontrast preparations against the background of taking Anaprilin, the risk of anaphylactic reactions increases.

Phenytoin with intravenous administration, means for inhalation anesthesia (derivatives of hydrocarbons) with simultaneous application with propranolol increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

Propranolol with simultaneous application changes the effectiveness of insulin and hypoglycemic agents for oral administration, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

Cardiac glycosides, methyldopa, reserpine and guanfacine, antiarrhythmic drugs with simultaneous reception with propranolol they increase the risk of developing or worsening bradycardia, atrioventricular blockade, cardiac arrest and heart failure.

The simultaneous use of propranolol and nifedipine can lead to a significant reduction in blood pressure.

Propranolol prolongs the action of nondepolarizing muscle relaxants and the anticoagulant effect of warfarin.

Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics increase the inhibitory effect on the central nervous system.

Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.

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

Cimetidine, hydralazine and ethanol increase the bioavailability of propranolol.

Propranolol increases the concentration of lidocaine in the blood plasma.

With the simultaneous administration of propranolol with phenothiazine derivatives, the concentrations of both drugs in the blood plasma increase.

Propranolol reduces the clearance of xanthines (except diphylline) and increases their concentration in the plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.

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

Simultaneous intravenous administration of verapamil and diltiazem can provoke cardiac arrest.

Sympathomimetics reduce the activity of propranolol.

Contraindicated the joint use of propranolol with antipsychotic and anxiolytic drugs.

Special instructions:

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

You should teach the patient how to count the number of heartbeats and instruct you about the need for medical advice with a heart rate less than 50 beats per minute.

Before using propranolol, patients with chronic heart failure (early stages) should use cardiac glycosides and / or diuretics.

Treatment of coronary heart disease and persistent arterial hypertension should be long - taking propranolol is possible for several years.

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

Patients who use contact lenses should take into account that a reduction in tear fluid production is possible against the background of treatment.

Patients with pheochromocytoma are prescribed only in combination with the use of alpha-blockers.

With thyrotoxicosis propranolol can mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, as it can strengthen symptoms.

When prescribing beta-blockers, patients receiving hypoglycemic drugs should be careful, because during prolonged interruptions in eating can develop hypoglycemia. And such her symptoms, like 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 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.

A few days before the general anesthesia should stop taking the drug. If the patient has taken the drug before surgery, he should choose a medicine for general anesthesia with a minimum negative inotropic effect.

Reciprocal activation of the vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg).

Drugs that reduce catecholamine stores (for example, reserpine), can enhance the action of beta-blockers, so patients who take such combinations of drugs should be under constant medical supervision for the diagnosis of arterial hypotension or bradycardia.

Against the background of treatment with the drug Anaprilin, intravenous administration of verapamil, diltiazem should be avoided.

In the case of the appearance in elderly patients of an increasing bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mm Hg.st.), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe violations of the liver and kidneys, 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.

It should be canceled before testing in the blood plasma and urine catecholamines, normetanefrin and vanillylmandelic acid; titers of antinuclear antibodies. The cessation of treatment is carried out gradually, under the supervision of a doctor, as a sharp cancellation can increase myocardial ischemia, pain syndrome in angina pectoris, worsen tolerance to physical exertion. Cancellation of the drug is carried out for 2 weeks or more, gradually reducing the dose (by 25% every 3-4 days).

Contraindicated simultaneous use of the drug with antipsychotic drugs (neuroleptics), anxiolytic drugs (tranquilizers) and monoamine oxidase inhibitors. The interval between taking monoamine oxidase inhibitors and propranolol should be at least 14 days.

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

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 period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, 40 mg.

Packaging:

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

3, 5 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry, 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.

Terms of leave from pharmacies:On prescription

Registration number:P N003239 / 01

Date of registration:03.12.2008 / 09.02.2012

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp28.08.2017

Illustrated instructions

Instructions

Anaprilin (Anaprilin)