Anaprilin - instructions for use, reviews, analogs and formulations (tablets 10 mg and 40 mg) of the drug for the treatment of hypertension, tachycardia and angina in adults, children and pregnancy

In this article, you can read the instructions for using the drug Anaprilin. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of experts on the use of Anaprilin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Anaprilin in the presence of existing structural analogues. Use for the treatment of hypertension, tachycardia and angina pectoris in adults, children, as well as during pregnancy and lactation.

Anaprilin non-selective beta-blocker.It has antihypertensive, anti-anginal and antiarrhythmic effects. Due to the blockade of beta-adrenoreceptors, catecholamines-induced cAMP formation from ATP decreases, as a result, reduces the intracellular intake of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect (decreases heart rate, inhibits conduction and excitability, reduces myocardial contractility). At the beginning of the use of beta-blockers OPSS in the first 24 hours 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 it returns to the initial, and with prolonged use decreases.

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

The antianginal effect is due to a decrease in myocardial oxygen demand (due to a negative chronotropic and inotropic effect). The decrease in 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 AV-conduction. Oppression of impulses is noted predominantly in the antegrade and to a lesser extent in the retrograde direction through the AV node and along additional paths. It belongs to the 2nd class of antiarrhythmics. 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 against the background of the use of Propranolol (the active substance of the drug Anaprilin) ​​is due primarily to blockade of peripheral beta2-adrenergic receptors.

Increases atherogenic properties of blood. Increases contractions of the uterus (spontaneous and caused by means that stimulate the myometrium). Increases bronchial tone. In high doses, it causes sedation.

Pharmacokinetics

After ingestion, about 90% of the dose taken is absorbed, but the bioavailability is low due to metabolism during the "first pass" through the liver. It is excreted by the kidneys mainly in the form of metabolites, in unchanged form - less than 1%.

Indications

• arterial hypertension;
• angina pectoris tension;
• unstable angina;
• sinus tachycardia (including hyperthyroidism);
• supraventricular tachycardia;
• tahisystolic form of atrial fibrillation;
• supraventricular and ventricular extrasystole;
• essential tremor;
• prevention of migraine;
• alcohol abstinence (agitation and trembling);
• anxiety;
• pheochromocytoma (auxiliary treatment);
• diffuse-toxic goiter and thyrotoxic crisis (as an auxiliary, including with intolerance of thyreostatic drugs);
• sympatoadrenal crises against the background of diencephalic syndrome.

Forms of release

Tablets 10 mg and 40 mg.

Instructions for use and dosage

Individually. When administered, the initial dose is 20 mg, a single dose of 40-80 mg, the frequency of reception - 2-3 times a day.

Side effect

• increased fatigue;
• weakness;
• dizziness;
• headache;
• drowsiness or insomnia;
• depression;
• anxiety;
• confusion of consciousness;
• hallucinations;
• tremor;
• nervousness;
• anxiety;
• decrease in secretion of tear fluid (dryness and soreness of the eyes);
• sinus bradycardia, AV-blockade (until the development of complete transverse blockade and cardiac arrest);
• arrhythmias;
• development (aggravation) of chronic heart failure;
• a decrease in blood pressure;
• orthostatic hypotension;
• manifestation of angiospasm (increased peripheral circulatory disturbance, coldness of the lower limbs, Raynaud's syndrome);
• chest pain;
• nausea, vomiting;
• discomfort in the epigastric region;
• constipation or diarrhea;
• changes in taste;
• nasal congestion;
• bronchospasm;
• changes in blood glucose concentration (hypo- or hyperglycemia);
• thrombocytopenia (unusual bleeding and hemorrhage), leukopenia;
• increased sweating;
• psoriasis-like skin reactions;
• exacerbation of psoriasis symptoms;
• itching;
• skin rash;
• hives;
• backache;
• arthralgia;
• decreased potency;
• withdrawal syndrome (increased angina attacks, myocardial infarction, increased blood pressure).

Contraindications

• AV-blockade of 2 and 3 degrees;
• sinoatrial blockade;
• bradycardia (heart rate less than 55 bpm);
• syndrome of weakness of the sinus node;
• arterial hypotension (systolic blood pressure less than 90 mm Hg, especially with myocardial infarction);
• chronic heart failure 2B-3 stage;
• acute heart failure;
• cardiogenic shock;
• hypersensitivity to propranolol.

Application in pregnancy and lactation

The use of propranolol 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 fetal condition is necessary, for 48-72 h before the birth of propranolol should be discarded.

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

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

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 vascular occlusive diseases, pregnancy, lactation, elderly patients, in children (efficacy and safety not defined).

During the treatment may exacerbate psoriasis.

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

After a prolonged course of treatment, propranolol should be withdrawn gradually, under the supervision of a doctor.

Against the background of treatment with propranolol should be avoided in / in the introduction of verapamil, diltiazem. A few days before the anesthesia should stop taking propranolol or choose an agent for anesthesia with a minimal negative inotropic effect.

Impact on the ability to drive vehicles and manage mechanisms

In patients whose activities require increased attention, the question of the use of propranolol in an outpatient setting should be addressed only after assessing the patient's individual response.

Drug Interactions

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

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

The cases of development of severe bradycardia in the use of Anaprilin for arrhythmias caused by digitalis preparations are described.

With simultaneous use with funds for inhalation anesthesia, the risk of oppression of myocardial function and development of arterial hypotension increases.

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

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

Anaprilin does not affect the pharmacokinetics of verapamil.

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

With simultaneous application with hydralazine, Cmax in the blood plasma and AUC of propranolol increases. 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 the simultaneous use of propranolol can inhibit the effects of glibenclamide, glyburide, chlorpropamide, tolbutamide, t. nonselective beta2-adrenoblockers are able to block beta-2-adrenergic receptors of the pancreas associated with insulin secretion.

Due to 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 hypoglycemic effect.

With simultaneous use with diltiazem, the concentration of propranolol in the blood plasma increases due to the inhibition of its metabolism under the influence of diltiazem. There is an additive inhibitory effect on the activity of the heart due to the slowing down of the impulse through the AV node caused by diltiazem. There is a risk of development of severe bradycardia, the impact and minute volume significantly decreases.

With simultaneous application, cases of increasing the concentration of Warfarin and phenindione in blood plasma are described.

At simultaneous application with doxorubicin in experimental researches the strengthening of cardiotoxicity is shown.

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

With simultaneous application, the cases of increasing the concentration of imipramine in the blood plasma are described.

With simultaneous use with indomethacin, naproxen, piroxicam, acetylsalicylic acid, a decrease in the antihypertensive effect of propranolol is possible.

At simultaneous application with ketanserinom development of an additive hypotensive effect is possible.

With simultaneous application with clonidine, 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 application with caffeine, a decrease in the effectiveness of propranolol is possible.

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

At simultaneous application with lithium carbonate the case of development of a bradycardia is described.

With simultaneous application, the case of strengthening side effects of maprotiline is described, which is due, apparently, to a slowing of its metabolism in the liver and cumulation in the body.

With simultaneous application with mefloquine, the QT interval increases, the case of cardiac arrest is described; with morphine - exacerbating effect on the CNS, caused by morphine; with sodium amidotrizoate - cases of severe arterial hypotension have been described.

With simultaneous use with nizoldipine, Cmax and AUC of propranolol and nizoldipine in the blood plasma can increase, which leads to severe arterial hypotension. There is a report on reinforcing the beta-blocking action.

With simultaneous application with Nifedipine in patients with ischemic heart disease, it is possible to develop severe arterial hypotension, an increased risk of heart failure and myocardial infarction, which may be due to an increase in the negative inotropic effect of nifedipine.

Patients receiving Anaprilin have a risk of developing severe hypotension after taking the first dose of prazosin.

With simultaneous application with prenylamine, the QT interval increases.

With simultaneous application with propafenone, the concentration of propranolol in the blood plasma increases and toxic action develops. Propafenone is thought to inhibit the metabolism of propranolol in the liver, reducing its clearance and increasing serum concentrations.

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

With simultaneous application, Cmax and AUC of rizatriptan are increased; with rifampicin - the concentration of propranolol in the blood plasma decreases; with suxamethonium chloride, tubocurarine chloride - it is possible to modify the action of muscle relaxants.

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

With simultaneous use with phenyldione, there have been cases of some increase in bleeding without changes in the coagulability of blood.

With simultaneous application with flecainide, additive cardiodepressive action is possible.

Fluoxetine inhibits the isoenzyme CYP2D6, which leads to oppression of propranolol metabolism and its cumulation and can enhance cardiodepressive action (including bradycardia). Fluoxetine and, mainly, its metabolites are characterized by prolonged T1 / 2, so the probability of drug interaction persists even a few days after fluoxetine cancellation.

With simultaneous use in blood plasma, concentrations of propranolol, chlorpromazine, thioridazine increase. Perhaps a sharp decrease in blood pressure.

Cimetidine inhibits the activity of microsomal liver enzymes (including isoenzyme CYP2D6), which leads to oppression of propranolol metabolism and its cumulation: an increase in negative inotropic action and the development of cardiodepressive action are observed.

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

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

There are reports of changes in hemodynamic effects of Anaprilin when used simultaneously with ethanol (alcohol).

Analogues of the drug Anaprilin

Structural analogs for the active substance:

• Inderal;
• Obsidan;
• Propranolobene;
• Propranolol;
• Propranolol Nycomed;
• Propranolol hydrochloride.

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