Drug therapy in cardiology is often based on pathogenetic action, without affecting the primary cause of the disease. One of the most commonly used groups of drugs are beta-blockers, which have a pronounced hypotensive (lowering pressure), antianginal (elimination of chest pain) and antiarrhythmic effect. One of the first drugs in this group is Anaprilin (the active ingredient is propranolol), which is widely used in clinical practice.
Instructions for use of the drug
"Anaprilin" belongs to the group of adrenergic receptor blockers 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 in idiopathic tremors and endocrinological diseases.
In cardiological practice, the drug is most often prescribed to patients with coronary heart disease. The active ingredient helps to reduce myocardial oxygen demand and prevents remodeling (restructuring) of the heart muscle. The drug has been proven to be effective in reducing mortality when consumed in the first hours after a heart attack.
Indications: what does the medicine help from and when is it used?
The multidirectional effect of the drug on the structure of the body determines its widespread use in medical practice. Instructions for the use of "Anaprilin" highlights the following indications for the appointment of a medication:
- essential (primary, idiopathic) arterial hypertension - a disease accompanied by persistent excess of standard pressure indicators for no apparent reason;
- ischemic heart disease (CHD) - a pathology characterized by a violation of the blood supply to the myocardium with typical chest pain during physical exertion;
- exertional angina - a chronic form of ischemic heart disease;
- hypertrophic cardiomyopathy - a pathology characterized by the proliferation of muscle fibers, which reduces the volume of the heart chambers;
- 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 hands or other parts of the body for no apparent reason, family cases are more often recorded;
- alcohol withdrawal - 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 a different 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, it is used to prevent migraine attacks, panic attacks and deep anxiety.
Directions for use: how to take?
The scheme of using "Anaprilin" is determined by the person's age, disease and the severity of the pathology. Average therapeutic doses and frequency of administration of the drug are presented in the table.
| Disease | Form | Dose (in milligrams) | Multiplicity |
|---|---|---|---|
| Arterial hypertension | Tablets, capsules | 40 | 2 times a day (if ineffective, raise to 4) |
| Angina pectoris, rhythm disturbances | Tablets, capsules | 20 - 2 weeks, with a subsequent increase to 40 | 3 times a day |
| Postinfarction condition | Tablets, capsules | 80 | 3 times |
| Paroxysmal arrhythmias, thyrotoxic crises | Intravenous solution | 1, after 2 minutes - again | In the absence of effect - enter, up to 10 times under the control of the rhythm and pressure level |
| Migraine | Tablets | 40 | 3 times a day |
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.
You should stop taking the drug gradually because of the risk of developing the "rebound" syndrome (progression of symptoms of the underlying disease). The applied dose is reduced by 25% every 3-4 days until complete withdrawal.
Composition and form of release
"Anaprilin" (active ingredient - propranolol) is a drug that is used for long-term use and emergency care, therefore, for convenience, it is produced in different forms.
| Release form | Propranolol dose |
|---|---|
| Tablets | 10 and 40 mg |
| 0.25% solution for intravenous administration 1 mg | 2.5 mg in ampoule |
| 1% solution - 5 ml | 5 mg in ampoule |
| Depot capsules of prolonged (long-acting) action, which are used once a day | 80 mg |
Mechanism of Action: How Fast and How Long?
Propranolol belongs to non-selective (no selective effect on the cardiovascular system) beta-blockers without internal sympathomimetic activity, which causes a wide range of therapeutic effects:
- Decrease in heart rate (due to the effect on receptors in the myocardium).
- Reducing the oxygen demand of the heart muscle (this is how the antianginal effect of the drug is realized).
- Decrease in total peripheral vascular resistance (with prolonged use). In the first 2 weeks, there is an increase in the tone of smooth muscle fibers, respectively - indicators of diastolic blood pressure, followed by stabilization and decrease.
- Increased tone of smooth muscles of the bronchi (bronchospasm) and uterus (stimulation of labor).
- Depressive effect (the drug penetrates the blood-brain barrier and has a direct effect on the centers in the brain).
- Slows down the processes of iodine metabolism in the body (inhibitory effect on the thyroid gland).
- Hypoglycemic effect: blockade of receptors reduces the contrainsular effect of adrenaline and contributes to a drop in blood glucose levels (one of the drug's contraindications is diabetes mellitus).
"Anaprilin" belongs to the group of lipophilic beta-blockers, which are rapidly and in high concentrations absorbed from the gastrointestinal tract. In the blood they combine with proteins: 95% of the drug is bound. The drug begins to act in 1 hour (when taking tablets), the maximum concentration reaches within 2 hours.
The duration of the effect of the tableted "Anaprilin" is 4-6 hours, which determines the frequency of administration of the drug.
The processes of metabolism and excretion occur in the liver, therefore, in patients with impaired function of the hepatobiliary system, lower doses of the drug are recommended due to the risk of accumulation and overdose. Less than 1% of the drug is excreted in the kidneys.
Side effects and symptoms of overdose
The undesirable consequences of the use of "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 (decrease in heart rate): the frequency reaches 40-50 per minute;
- allergic reactions: itchy rash, swelling;
- visual impairment (due to a decrease in the secretion of the lacrimal glands);
- dry tongue, nausea, vomiting, upper pain 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 in 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 abnormal daytime sleepiness);
- conduction disorders: atrioventricular blockade.
In case of deterioration of health and the appearance of side effects, it is necessary to stop taking the drug and consult a cardiologist.
The main symptoms of poisoning:
- dizziness;
- severe bradycardia and a drop in blood pressure;
- loss of consciousness;
- shortness of breath (noisy exhalation);
- cyanosis of the fingers and toes (in children - the face);
- 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, it is not recommended to drink alcohol while taking Anaprilin. Toxic effects arise from:
- damage to the enzyme systems of the liver by the products of ethanol metabolism, disturbances in the processes of metabolism and excretion of the drug;
- additional inhibitory effect on the central nervous system;
- alcohol causes tachycardia, increased blood pressure, which negates the effect of "Anaprilin";
- increased side effects of the medication (headache, weakness, nausea).
The compatibility of the drug with other substances affecting the nervous system is an increase in the depressive effect.
Is there a lethal dose of Anaprilin?
The lethal outcome with the use of "Anaprilin" develops with a single dose of 2 grams of the drug. Death occurs due to impaired blood supply in the arteries of the brain, oppression of the vasomotor and respiratory centers. Patients die from circulatory and respiratory arrest within 2-3 hours.
Emergency care at the first signs of an overdose means:
- flush the stomach (it is strictly forbidden to stimulate vomiting);
- take enterosorbents (White Coal, Smecta);
- upon the arrival of an ambulance - the connection of intravenous detoxification therapy;
- antidote (antidote): Orciprenaline sulfate (Astmopent, Alupent);
- intravenous glucagon at a dose of 2-5 mg (bolus), maintenance dose - 1 mg / hour;
- atropine sulfate intravenously 1 mg;
- in the presence of a syringe-dispenser: "Izadrin" 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.
Anaprilin treatment regimen
The administration of the drug is carried out according to the indications and average therapeutic doses for each pathology.
Application features:
- Multiplicity of admission at least 2 times a day (due to the short half-life: 4-6 hours).
- Tablets and capsules should be taken 10-30 minutes before meals with plenty of liquid.
- Dose adjustment is carried out at least 2 weeks from the beginning. Efficiency control - daily measurement of blood pressure and heart rate before dose selection. After stabilization of indicators - once a week.
- It is recommended at the beginning of treatment weekly monitoring of blood glucose levels.
- The dose selection scheme for the patient begins with the average therapeutic dose (calculated per kilogram of body weight). After 10-14 days, an assessment of the effectiveness, in the absence of the desired result - a decrease or increase by 50% (do not exceed the maximum daily intake 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 selection of drugs in a convenient form of release and an acceptable price category.
The most common analogs of "Anaprilin" are presented in the table.
| Tradename | Release form |
|---|---|
| "Obzidan" |
|
| "Propranolol" |
|
| Inderal |
|
| Anaprilin |
|
| "Gemangiol" |
|
| "Propranobene" |
|
| "Vero-Anaprilin" |
|
The presence of contraindications and restrictions for use in patients with concomitant endocrine or ophthalmic pathology requires the selection of a quality substitute. Most often in the practice of a cardiologist, selective blockers are prescribed: Bisoprolol, Metoprolol, Labetalol, Nebivolol.
The selection of the drug is carried out depending on the patient's sensitivity to the active substance, the presence of the required dosage in domestic or imported products.
Conclusions
Anaprilin is a non-selective beta-adrenergic receptor blocker that 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 control of the functional state of the body and drug interactions with other pathogenetic agents. The availability of high-quality and safer substitutes on the pharmaceutical market allows the doctor to choose the most optimal treatment for each patient.
