Instructions for use of "Anaprilin": indications, doses, compatibility and analogues

Instructions for use of the drug

"Anaprilin" belongs to a group of blockers of adrenergic receptors located in different parts of the human body: blood vessels, muscles of the heart, bronchi, uterus and prostate gland.
The interaction of the drug with sensitive cells prevents the stimulating effect of the nervous system and endocrine glands, which explains its use for idiopathic tremor and endocrinological diseases. In cardiological practice, the drug is most often prescribed to patients with coronary heart disease. The active substance helps reduce the myocardial oxygen demand and prevents remodeling (restructuring) of the heart muscle. The drug has been proven effective in reducing mortality when taken in the first hours after a heart attack.

Indications: what does the medicine help with and when is it used?

The multidirectional effect of the drug on the structures of the body determines its widespread use in medical practice. The instructions for use of "Anaprilin" highlight the following indications for prescribing the medication:

• Essential (primary, idiopathic) arterial hypertension is a disease accompanied by persistent excess of standard pressure values ​​for no apparent reason;
• coronary heart disease (CHD) – a pathology characterized by impaired blood supply to the myocardium with typical pain in the chest during physical activity;
• angina pectoris – a chronic form of coronary artery disease;
• hypertrophic cardiomyopathy – a pathology characterized by the proliferation of muscle fibers, which reduces the volume of the chambers of the heart;
• rhythm disturbances: atrial flutter or fibrillation (atrial fibrillation), supraventricular tachycardia, extrasystoles;
• pheochromocytoma - a tumor of the adrenal tissue that synthesizes catecholamines (adrenaline, norepinephrine);
• essential tremor - “trembling” of the hands or other parts of the body for no apparent reason, familial cases are more often recorded;
• alcohol withdrawal is a complex of disorders caused by abstinence in people with alcoholism;
• infantile hemangiomas - benign tumors of the vascular wall (more common in children);
• diffuse toxic goiter and thyrotoxicosis of another etiology (against the background of thyroiditis) are diseases of the thyroid gland, accompanied by increased synthesis of hormones. "Anaprilin" is prescribed as a second-line drug.

In addition, the product is used to prevent migraine attacks, panic attacks and deep anxiety.

Directions for use: how to take?

The regimen for using “Anaprilin” is determined by the person’s age, disease and severity of the pathology. The average therapeutic doses and frequency of administration of the drug are presented in the table.

In obstetric practice, Anaprilin is used to stimulate the onset of labor and prevent hypotonic bleeding in the postnatal period. The dose of the drug is 20 mg 3 times a day for 3-5 days.

The drug should be stopped gradually due to the risk of developing rebound syndrome (progression of symptoms of the underlying disease). The dose used is reduced by 25% every 3-4 days until complete withdrawal.

Composition and release form

"Anaprilin" (active ingredient - propranolol) is a drug that is used for long-term use and emergency care, therefore, for convenience, it is available in different forms.

Mechanism of action: how quickly and for how long?

Propranolol is a non-selective (no selective effect on the cardiovascular system) beta-blockers without internal sympathomimetic activity, which causes a wide range of therapeutic effects:

1. Decrease in heart rate (due to the effect on receptors in the myocardium).
2. Reducing the oxygen demand of the heart muscle (this is how the antianginal effect of the drug is realized).
3. Decrease in total peripheral vascular resistance (with long-term use). In the first 2 weeks, there is an increase in the tone of smooth muscle fibers, respectively, in diastolic blood pressure, followed by stabilization and decrease.
4. Increased tone of smooth muscles of the bronchi (bronchospasm) and uterus (stimulation of labor).
5. Depressive effect (the drug penetrates the blood-brain barrier and has a direct effect on centers in the brain).
6. Slows down the processes of iodine metabolism in the body (inhibitory effect on the thyroid gland).
7. Hypoglycemic effect: blockade of receptors reduces the counter-insular effect of adrenaline and contributes to a drop in blood glucose levels (one of the contraindications of the drug is diabetes mellitus).

"Anaprilin" belongs to the group of lipophilic beta-blockers, which are quickly and in high concentrations absorbed from the gastrointestinal tract. In the blood they combine with proteins: 95% of the drug is in bound form. The drug begins to act after 1 hour (when taking tablets), reaching its maximum concentration within 2 hours.

The duration of the effect of tableted “Anaprilin” is 4-6 hours, which determines the frequency of administration of the drug.

Metabolism and excretion processes occur in the liver, therefore, in patients with dysfunction of the hepatobiliary system, smaller doses of the drug are recommended due to the risk of accumulation and overdose. Less than 1% of the drug is excreted by the kidneys.

Side effects and symptoms of overdose

Undesirable consequences of using “Anaprilin” are associated with the accumulation of active metabolic products or intake against the background of contraindicated conditions:

• orthostatic hypotension – a drop in blood pressure when changing position from horizontal to vertical;
• bradycardia (decreased heart rate): frequency reaches 40-50 per minute;
• allergic reactions: itchy rash, swelling;
• blurred vision (due to decreased secretion of the lacrimal glands);
• dry tongue, nausea, vomiting, pain in the upper part and bloating, diarrhea;
• redness of the skin, hair loss, the appearance of psoriasis-like peeling;
• collapse - a decrease in vascular tone in the arteries of the brain with loss of consciousness;
• muscle weakness and numbness of the limbs;
• nasal congestion, broncho- or laryngospasm;
• hypoglycemia (in patients with diabetes mellitus, propranolol prolongs and enhances the effect of insulin);
• headache, weakness, increased fatigue;
• sleep disorders (insomnia or pathological daytime sleepiness);
• conduction disorders: atrioventricular block.

If your health worsens and side effects occur, you should stop taking the drug and consult a cardiologist.

Main symptoms of poisoning:

• dizziness;
• severe bradycardia and drop in blood pressure;
• loss of consciousness;
• difficulty breathing (noisy exhalation);
• cyanosis of fingers and toes (in children - faces);
• convulsions;
• on the electrocardiogram: conduction disturbance in the AV node, frequent ventricular extrasystoles.

The toxic dose is individual for each person, depending on the state of the liver enzyme system and the presence of concomitant diseases. In most cases, symptoms of poisoning develop with the simultaneous use of more than 1 gram of the drug.

Alcohol compatibility

According to the instructions for use of the drug, drinking alcohol while taking Anaprilin is not recommended. Toxic exposure occurs due to:

• damage to liver enzyme systems by ethanol metabolism products, disturbances in the processes of metabolism and excretion of the drug;
• additional inhibitory effect on the central nervous system;
• alcohol causes tachycardia and increased blood pressure, which neutralizes the effect of Anaprilin;
• increased side effects of the medication (headache, weakness, nausea).

Compatibility of the drug with other substances that affect the nervous system – increased depressive effects.

Pharmacokinetics

It is quickly and fairly completely (90%) absorbed when taken orally and is relatively quickly eliminated from the body. Bioavailability after oral administration is 30-40% (the “first pass” effect through the liver, microsomal oxidation), with long-term use it increases (metabolites are formed that inhibit liver enzymes), its value depends on the nature of the food and the intensity of hepatic blood flow. Metabolized in 3 ways - aromatic hydroxylation, N-dealkylation and glucuronidation in the liver, including with the participation of cytochrome isoenzymes CYP2D6, CYP1A2, CYP2C19.

The maximum concentration in blood plasma is achieved after 1-1.5 hours. It is highly lipophilic and accumulates in lung tissue, brain, kidneys, and heart. Penetrates through the blood-brain and placental barriers into breast milk. Communication with blood plasma proteins is 90-95%. Volume of distribution - 3-5 l/kg.

It enters the intestine with bile, is deglucuronidated and reabsorbed. The half-life is 3-5 hours; during a course of administration it can be extended to 12 hours. Excreted by the kidneys - 90%, unchanged - less than 1%. It is not removed by hemodialysis.

Features of pharmacokinetics in elderly patients, patients with impaired renal and liver function: due to hypoalbuminemia (age-related or caused by liver or kidney damage), the concentration of the drug in the blood plasma increases significantly, which may cause an increase in the pharmacological effects of the drug. Changes in the metabolic activity of the drug in elderly and senile age are also due to the state of the liver microsomal system and the reduced activity of cytochrome P450 - dependent monooxygenase oxidation in hepatocytes, which contributes to a longer maintenance of high concentrations of propranolol in tissues. The drug is prescribed to such patients with the selection of smaller individual doses.

Is there a lethal dose of Anaprilin?

A lethal outcome when using “Anaprilin” develops with the simultaneous use of 2 grams of the drug. Death occurs due to impaired blood supply in the arteries of the brain, inhibition of the vasomotor and respiratory centers. Patients die from circulatory and respiratory arrest within 2-3 hours.

Emergency assistance when the first signs of an overdose appear includes:

• rinse the stomach (stimulating vomiting is strictly prohibited);
• take enterosorbents (“White Coal”, “Smecta”);
• upon arrival of the ambulance - connection to intravenous detoxification therapy;
• antidote (antidote): Orciprenaline sulfate (“Ac”);
• glucagon intravenously at a dose of 2-5 mg (bolus), maintenance dose - 1 mg/hour;
• atropine sulfate intravenously 1 mg;
• if you have a dosing syringe: “Isadrin” 1-5 mg/hour or “Dopamine” 5-8 mcg/min.

Patients with signs of acute poisoning with Anaprilin are hospitalized in the intensive care unit.

Pharmacological properties

After taking the drug, B-adrenergic receptors are inhibited, resulting in a decrease in the intracellular concentration of calcium ions, due to which the heart rate slows down, myocardial excitability decreases, and the number of heart contractions decreases.

Due to its antiarrhythmic effect, regular use of the drug helps reduce the number of deaths after a heart attack

What pharmacological effect can be achieved with regular use of the medication:

• Hypotensive. Helps reduce minute blood volume, reduces upper and lower pressure, stimulates peripheral vessels. Reduces the activity of the renin-angiotensin system in patients with impaired renal function. The therapeutic effect is achieved 14 days after administration.
• Antianginal. Reduces the need of heart cells for oxygen, slows down the heart rate, thereby improving the capacity of the heart. However, in patients with chronic heart failure, myocardial oxygen demand may increase, which is due to increased diastolic pressure in the left ventricle.
• Antiarrhythmic. Reduces the increased activity of the sympathetic nervous system, prevents spontaneous excitability of the sinus pacemaker. By reducing the heart's need for oxygen, ischemic manifestations are reduced.

The active components are quickly absorbed into the bloodstream, due to which the pressure stabilizes in a short time. Propranolol is excreted by the kidneys in the form of metabolites.

Treatment regimen with "Anaprilin"

The drug is prescribed according to indications and average therapeutic doses for each pathology.

Features of application:

1. The frequency of administration is at least 2 times a day (due to the short half-life: 4-6 hours).
2. Take tablet forms and capsules 10-30 minutes before meals with a sufficient amount of liquid.
3. Dose adjustment is carried out no less than 2 weeks from the start. Monitoring effectiveness - daily measurement of blood pressure and pulse rate before dose selection. After stabilization of indicators - once a week.
4. Weekly monitoring of blood glucose levels is recommended at the beginning of treatment.
5. The dose selection scheme for the patient begins with the average therapeutic dose (calculated per kilogram of body weight). After 10-14 days, assess the effectiveness; if the desired result is not achieved, reduce or increase by 50% (do not exceed the maximum daily dose of 320 mg).

Most often, “Anaprilin” is prescribed for lifelong use; the duration of therapy for infantile hemangioma is 6-8 months.

Modern analogues of the drug

The modern pharmaceutical industry offers the patient a wide choice of drugs in a convenient release form and an acceptable price category.

The most common Anaprilin analogues are presented in the table.

The presence of contraindications and restrictions for use in patients with concomitant endocrine or ophthalmological pathologies requires the selection of a high-quality substitute. The most common selective blockers prescribed in cardiologist practice are: Bisoprolol, Metoprolol, Labetalol, Nebivolol.

The selection of the drug is carried out depending on the patient’s sensitivity to the active substance, the availability of the required dosage in domestic or imported products.

Contraindications

Hypersensitivity to the drug, atrioventricular block II-III degree, sinoauricular block, sinus bradycardia (less than 50 beats per minute), arterial hypotension, uncontrolled chronic heart failure II-III degree, acute heart failure, acute myocardial infarction (systolic blood pressure - less 100 mm Hg), cardiogenic shock, pulmonary edema, sick sinus syndrome, Prinzmetal's angina, cardiomegaly (without signs of heart failure), vasomotor rhinitis, occlusive peripheral vascular disease, diabetes mellitus, sucrase/isomaltase deficiency, fructose intolerance, glucose -galactose malabsorption, metabolic acidosis (including diabetic ketoacidosis), bronchial asthma, tendency to bronchospastic reactions, chronic obstructive pulmonary disease (including history), pheochromocytoma (without simultaneous use of alpha-blockers), spastic colitis, simultaneous use with antipsychotics and anxiolytics (chlorpromazine, trioxazine, etc.), monoamine oxidase inhibitors, lactation period, age up to 18 years (efficacy and safety have not been established).

Carefully

Liver and/or renal failure, hyperthyroidism, myasthenia gravis, chronic heart failure FC I-II, pheochromocytoma, psoriasis, pregnancy, history of allergic reactions, Raynaud's syndrome, old age.

Use during pregnancy and breastfeeding

Use during pregnancy is only possible if the potential benefit to the mother outweighs the potential risk to the fetus. If it is necessary to take it during pregnancy, careful monitoring of the condition of the fetus 48-72 hours before birth should be discontinued.

Propranolol is secreted into breast milk, so if you need to use the drug Anaprilin, you should stop breastfeeding.

conclusions

"Anaprilin" is a non-selective blocker of beta-aderenergic receptors, which is often used in cardiology to treat arterial hypertension of various origins, improve the well-being of patients with coronary heart disease and neurological disorders. A wide range of effects requires dose adjustment with monitoring of the functional state of the body and drug interactions with other pathogenetic drugs. The presence of high-quality and safer substitutes on the pharmaceutical market allows the doctor to choose the most optimal treatment for each patient.

Interaction with other drugs

The antihypertensive effect of propranolol is enhanced when combined with diuretics, reserpine, hydralazine and other antihypertensive drugs, as well as ethanol.

The antihypertensive effect is weakened by non-steroidal anti-inflammatory drugs (sodium retention and blocking renal prostaglandin synthesis), estrogens (sodium retention) and monoamine oxidase inhibitors.

Cimetidine increases bioavailability.

Increases the concentration of lidocaine in the blood plasma, reduces the clearance of theophylline.

Co-administration with phenothiazine derivatives increases the concentrations of both drugs in the blood plasma.

Enhances the effect of thyreostatic and uterotonic drugs; reduces the effect of antihistamines.

Increases the likelihood of developing severe systemic reactions (anaphylaxis) due to the introduction of allergens used for immunotherapy or for skin testing.

Amiodarone, verapamil and diltiazem - increased severity of the negative chrono-, ino- and dromotropic effects of propranolol.

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

Phenytoin when administered intravenously, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressive effect 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 difillin).

The hypotensive effect is weakened by glucocorticosteroids.

Cardiac glycosides, methyldopa, reserpine and guanfacine, and antiarrhythmic drugs increase the risk of developing or worsening bradycardia, atrioventricular block, cardiac arrest and heart failure.

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

Prolongs the effect of non-depolarizing muscle relaxants and the anticoagulant effect of warfarin.

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

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

Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.

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

Side effects

If recommendations for dosing of the drug are not followed, side effects from various systems may occur:

• Cardiovascular (circulatory disorders, arterial hypotension, increasing symptoms of heart failure).
• Hematopoietic (leukopenia, thrombocytopenia).
• Nervous (sleep disorder, dizziness, depression, malaise).
• Respiratory (coughing attacks, shortness of breath, pharyngitis, bronchospasm).
• Gastrointestinal (nausea, vomiting, diarrhea, pain in the epigastric region).
• Skin manifestations (rashes, itching, partial hair loss).
• Visual tract (dry eye mucosa, pain, decreased visual acuity).

Today, Anaprilin remains one of the most common and effective antihypertensive drugs, which at the same time help normalize heart rhythm. However, the medicine has a number of negative effects that affect the activity of all organs and systems. Therefore, for arterial hypertension, the course of treatment should be accompanied by periodic intervals that prevent a decrease in sensitivity to the active components and reduce the number of side effects.

Mechanism of action in hypertension

Before starting a therapeutic course, patients are interested in the question of the effectiveness of the prescribed medication, and does it reduce blood pressure at high levels?

The hypotensive mechanism of action of this drug is due to its ability to block beta-adrenergic receptors of the myocardium and other tissues, which is an integral part of lowering blood pressure. Inhibition of renin production contributes to decreased secretion of angiotensin 2, which leads to a decrease in blood pressure and determines the effectiveness of the antihypertensive effect of pills.

Mechanism of action of the drug for hypertension

The vasodilating effect of Anaprilin is based on the following mechanisms:

• impact on vascular receptors;
• pronounced adrenergic blocking activity;
• increases the release of nitric oxide from endothelial cells;
• expansion of the vascular lumen;
• increased production of vasodilating factors (prostaglandins, prostacyclins);
• decreased production of norepinephrine by sympathetic nerve fibers;
• decreased permeability of blood vessels to potassium and sodium ions.

Features of drug cancellation

If it is necessary to take a break from treatment with Anaprilin, the dose should be reduced gradually until complete withdrawal, since abrupt cessation of use of the drug can cause withdrawal syndrome.

Abrupt refusal to take medication can cause an attack of angina, tachycardia and increased blood pressure

Experts recommend discontinuing the use of the medication in the following cases:

• Reducing the number of heart contractions to 50 beats/min.
• At low pressure, when systolic blood pressure drops to 100 mm. rt. Art.
• Development of bronchial spasm.
• Disturbance in the functioning of the liver excretory system.
• Depressive state.
• Ventricular arrhythmia.

The optimal withdrawal period is considered to be 14 days from the moment the patient reduces the dosage until the patient completely stops using the tablets. As a rule, the dose is reduced by 10–40 mg every 6–7 days.