Anapriline

Anapriline is the trade name of a medicinal product, the main active ingredient of which is propranolol. Propranolol belongs to the class of beta-blockers, which are used to treat various conditions related to the cardiovascular system.

Propranolol has several pharmacologic properties including:

1. Antiarrhythmic action: Prevents the occurrence or reduces the frequency of cardiac arrhythmias.
2. Antihypertensive action: Reduces blood pressure.
3. Antianginal action: Reduces the frequency and intensity of angina attacks (chest pain caused by insufficient blood supply to the heart).
4. Anti-stress action: Reduces the body's responses to stress, such as palpitations and shaking.
5. Migraine prophylaxis: Some migraine patients may benefit from propranolol.

Anaprilin is used for the treatment of hypertension, angina pectoris, arrhythmias, hypertrophic cardiomyopathy, thyrotoxicosis (in combination with other drugs), as well as for the prevention of migraine. However, the use of Anaprilin should take place under the supervision of a doctor, since it has side effects and contraindications, and the dosage should be individualized for each patient.

Indications Anaprilina

1. Hypertension: Anapriline is used to lower blood pressure in patients with hypertension.
2. Angina: The drug may be used to reduce the frequency and intensity of angina attacks (chest pain caused by insufficient blood supply to the heart).
3. Arrhythmias: Anapriline can be used to treat various types of arrhythmias, including atrial ventricular tachycardia, atrial fibrillation, and extrasystole.
4. Hypertrophic cardiomyopathy: Propranolol may be used to reduce symptoms and slow the progression of this condition.
5. Thyrotoxicosis: In combination with other medications, propranolol may help control some symptoms of thyrotoxicosis, such as rapid heartbeat and shaking.
6. Migraine prophylaxis: Anapriline may be used for migraine prophylaxis in some patients.

Release form

1. Pills

Tablets are the most common form of release of Anaprylin. They are intended for oral administration and come in different dosages:

• Regular tablets: Usually contain 10 mg, 40 mg, or 80 mg of propranolol. These tablets are taken several times a day, depending on the dosage and your doctor's prescription.

2. Prolonged-release capsules

Prolonged-release capsules are designed to maintain stable levels of a drug in the blood for a long time:

• Prolonged-release capsules: Often contain 80 mg or 160 mg of propranolol. These forms of release allow you to reduce the number of times you take the drug during the day, usually to once a day.

3. Solution for injection

Although not as common, Anapriline is also available in the form of an injectable solution that is used in clinical settings:

• Injectable solution: Used for rapid relief of cardiac symptoms when oral administration is not possible or is ineffective.

4. Solution for oral administration

In some cases, an oral solution may be available, which is convenient for use in patients who have difficulty swallowing tablets.

Pharmacodynamics

1. Beta-adrenoreceptor blockade: Propranolol is a direct blocker of beta-adrenoreceptors, mainly beta-1 and beta-2 adrenoreceptors. Blocking these receptors results in a decreased response to adrenaline and norepinephrine, which are neurotransmitters of the sympathetic nervous system.
2. Reduction of cardiac output: Blocking beta-1 adrenoreceptors in the heart leads to a decrease in cardiac output and a decrease in heart rate. This may lead to a decrease in blood pressure and a decrease in the workload of the heart.
3. Reduction of blood pressure: Propranolol also has a direct vasoconstrictor effect by blocking beta-2 adrenoreceptors on blood vessels. This results in peripheral vasoconstriction and a decrease in blood pressure.
4. Antiarrhythmic action: Propranolol has antiarrhythmic action due to reduction of cardiac automatism, inhibition of conduction and reduction of myocardial excitability.
5. Migraine prophylaxis: Propranolol can be used for prophylaxis of migraine attacks due to its effect on vascular tone and reduction of excitability of neuronal structures associated with the genesis of migraine.
6. Anti-anxiety effects: Propranolol is sometimes used to reduce symptoms of anxiety, as it may reduce the body's physiological response to stress.

Pharmacokinetics

1. Absorption: Anapriline is usually well absorbed from the gastrointestinal tract after oral administration. Absorption may be reduced by concomitant administration with food.
2. Distribution: Propranolol penetrates well through the blood-brain barrier and enters the brain. It is also distributed in body tissues, including the liver, kidneys, lungs, and heart.
3. Metabolism: Propranolol undergoes extensive metabolism in the liver, mainly involving cytochrome P450 2D6 isoenzyme. The main metabolites of propranolol are alpha-naphthoxyacetic acid and 4-hydroxypropranolol.
4. Excretion: Propranolol and its metabolites are excreted mainly through the kidneys. Approximately 90% of the dose is excreted within 4 days, mainly as metabolites.
5. Half-life: The blood half-life of propranolol is about 3-6 hours, but may be prolonged in elderly patients and patients with impaired hepatic function.

Dosing and administration

Method of application

• Oral administration: Anapriline is taken orally, preferably at the same time each day to ensure a uniform concentration of the drug in the blood.
• Injections: The injectable form of propranolol is used in inpatient settings to quickly stabilize the patient's condition.

Dosage

The dosage of Anaprylin depends on the specific disease, its severity, and the patient's response to treatment. Here are general recommendations:

For Adults

1. Hypertension:

   • Initial dose: 40 mg twice daily.
   • Maintenance dose: 120-240 mg per day, divided into several doses.

2. Angina:

   • Initial dose: 40 mg three times a day.
   • Maintenance dose: 120-240 mg per day.

3. Arrhythmias:

   • Starting dose: 10-40 mg three or four times daily.

4. Migraine (prevention):

   • Starting dose: 40 mg two or three times daily.
   • Maintenance dose: 80-240 mg per day.

5. Tremor:

   • Initial dose: 40 mg two to three times a day.
   • Maintenance dose: up to 120 mg per day.

6. Help with withdrawal from alcohol addiction:

   • Dose: 10-40 mg three or four times daily.

For Children

• Arrhythmias, hypertension and other cardiovascular conditions:
  • Initial dose: 0.5-1 mg/kg per day, divided into several doses.
  • Maintenance dose: The dose is gradually increased according to clinical response and tolerability.

Special Instructions

• Propranolol should be taken before or with meals to improve absorption.
• When discontinuing Anapriline, the dose should be gradually reduced to avoid the risk of withdrawal.
• Propranolol may mask symptoms of hypoglycemia in diabetic patients.
• Caution should be taken in patients with bronchial asthma, as propranolol may increase bronchospasm.

Use Anaprilina during pregnancy

The use of anapriline (propranolol) during pregnancy should only be done under the strict supervision of a doctor, as it can have serious consequences for both the mother and the fetus.

Propranolol, as a beta-blocker, can penetrate the placental barrier and affect fetal development. Here are some of the possible risks of using anaprylin during pregnancy:

1. Fetal heart rate slowing: Propranolol may cause fetal heart rate slowing.
2. Low blood pressure: This drug can lower the blood pressure of both the mother and fetus, which can lead to hypoxia and other complications.
3. Risk of preterm labor: Use of propranolol in pregnant women may increase the risk of preterm labor.
4. Birth defects: Some studies indicate a possible risk of birth defects with the use of beta-blockers, such as propranolol, in the first trimester of pregnancy.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to anapriline or to any of the ingredients of the drug should avoid its use.
2. Heart failure: Anapriline is contraindicated in patients with severe heart failure or those with significant symptoms of cardiac decompensation.
3. Heart block: Anapriline is contraindicated in the presence of AV conduction blockade (second and third degree).
4. Sinus bradycardia syndrome: The drug should be used with caution in patients with sinus bradycardia syndrome, as it may aggravate bradycardia.
5. Asthma and obstructive airway disease: Patients with bronchial asthma or chronic obstructive pulmonary disease should use anapriline with caution because of the possibility of increased bronchospasm.
6. Reiter's syndrome: The use of anaprylin may be contraindicated in patients with Reiter's syndrome due to the risk of worsening the condition.
7. Pregnancy and lactation: The use of anapriline during pregnancy and lactation may be contraindicated due to insufficient data on its safety for fetus and child.
8. Pediatric: The safety and effectiveness of anaprylin in children has not been established, so it is not generally recommended for children.

Side effects Anaprilina

1. Fatigue and weakness: Some patients may experience fatigue, weakness, or a general feeling of tiredness.
2. Decrease in blood pressure: Propranolol, as a beta-blocker, may cause a decrease in blood pressure, which may lead to dizziness or even loss of consciousness, especially with sudden changes in body position.
3. Bradycardia: This is a decrease in heart rate to below normal. It may cause patients to feel palpitations, weakness, or dizziness.
4. Sleep problems: Propranolol may cause insomnia or changes in sleep quality in some patients.
5. Digestive problems: Dyspeptic symptoms such as nausea, vomiting, abdominal pain, or diarrhea may occur.
6. Masking symptoms of hypoglycemia: Propranolol has the ability to mask some symptoms of low blood sugar in patients with diabetes.
7. Breathing problems: Some patients may experience worsening symptoms of asthma or obstructive lung disease.
8. Sexual dysfunction: Propranolol may cause decreased libido or erection problems in some patients.
9. Decrease in blood platelet count: In rare cases, especially with prolonged use, changes in hemostasis, including a decrease in platelet count, may be observed.

Overdose

1. Decreased blood pressure: An overdose of anaprylin can cause a sudden drop in blood pressure, which can cause dizziness, fainting, or even shock.
2. Bradycardia: Propranolol can slow the heart rate and excessive use may cause the heart to beat too slowly (bradycardia).
3. Breathing problems: Some people may have breathing problems such as prolonged apnea, especially if there is asthma or other respiratory conditions.
4. Hypoglycemia: Propranolol may mask symptoms of hypoglycemia (low blood sugar), which can be dangerous for patients with diabetes.
5. Increased drowsiness: Excessive use of anapriline may cause drowsiness or even coma.
6. Loss of consciousness: In severe cases of anapriline overdose, loss of consciousness or coma may occur.

Interactions with other drugs

1. Antihypertensive agents: Propranolol may increase the hypotensive effect of other antihypertensive drugs, such as diuretics, ACE inhibitors and calcium channel blockers, which may lead to a decrease in blood pressure to dangerous levels.
2. Antiarrhythmic drugs: Combined administration of propranolol with other antiarrhythmic agents, such as amidarone or class III antiarrhythmics, may result in increased antiarrhythmic action and increased risk of cardiac arrhythmias.
3. Cardiac glycosides: Propranolol may increase the effects of cardiac glycosides such as digoxin, which may lead to an increase in their toxic effects on the heart.
4. Monoamine oxidase inhibitors (MAOIs): Propranolol may increase the hypotensive effect of MAOIs, which may lead to a dangerous drop in blood pressure.
5. Anesthetics: Propranolol may increase the depressant effect of anesthetics and increase the hypotensive effect of some anesthetics.
6. Bronchodilators: Propranolol may block the bronchodilator effect of beta-agonists and increase the risk of bronchospasm in patients with asthma or chronic obstructive pulmonary disease.