Anaprilin
Anaprilin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Anaprilin
ATX code: C07AA05
Active ingredient: propranolol (propranolol)
Producer: Tatkhimfarmpreparaty, JSC (Russia), Zdorov'e - pharmaceutical company (Ukraine), Biosintez, JSC (Russia), Obnovlenie, PFK (Russia), Pharmstandard-Leksredstva (Russia), Irbitsky KhFZ (Russia)
Description and photo update: 2019-19-08
Prices in pharmacies: from 21 rubles.
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Anaprilin is a synthetic drug, belongs to the group of β-blockers, is used in the treatment of high blood pressure and heart disorders.
Release form and composition
Anaprilin dosage form - tablets: flat-cylindrical, white, with or without a risk, with a chamfer (in blister strip packs of 10 pcs., In a cardboard box 1, 3 or 5 packs; 15 pcs., In a cardboard box 1 or 2 packs, 20 pcs., In a cardboard box 1 pack; 50 or 100 pcs. In orange glass jars, 1 jar in a cardboard box).
The active substance is propranolol, in 1 tablet - 10 or 40 mg.
Auxiliary components: milk sugar, potato starch, calcium stearate, talc.
Pharmacological properties
Pharmacodynamics
Propranolol is a non-selective β-blocker with antianginal, antiarrhythmic and antihypertensive effects. Due to the non-selective blocking of β-adrenergic receptors (75% - β 1 - and 25% - β 2 -adrenergic receptors), the formation of cyclic adenosine monophosphate (stimulated by catecholamines) from adenosine triphosphate decreases. As a result, the intracellular intake of calcium decreases, there is a negative dromo-, chrono-, ino- and batmotropic effect (manifests itself in the form of a decrease in the number of heart contractions, inhibition of conduction and excitability, and a decrease in myocardial contractility).
At the beginning of therapy, the total peripheral vascular resistance increases for 24 hours (associated with a reciprocal increase in the activity of α-adrenergic receptors and the elimination of stimulation of β 2 -adrenergic receptors in the vessels of the skeletal muscles). After 1-3 days, this indicator returns to the initial one, and with prolonged treatment it decreases.
The mechanism of action of Anaprilin:
- antianginal action: associated with a decrease in myocardial oxygen demand (due to negative chrono- and inotropic effects). Due to a decrease in the number of heart contractions, diastole lengthens and myocardial perfusion improves. An increase in the end-diastolic pressure in the left ventricle and an increase in the stretching of the muscle fibers of the ventricles of the heart cause an increase in oxygen demand, especially in patients with chronic heart failure;
- antihypertensive effect: associated with a decrease in the minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin-aldosterone system (important for patients with initial hypersecretion of renin), sensitivity of the aortic arch baroreceptors (in response to a decrease in blood pressure, an increase in their activity is not observed) and the effect on the central nervous system. Stabilization of the antihypertensive action occurs by the end of a two-week course of use;
- antiarrhythmic action: associated with the elimination of arrhythmogenic factors (arterial hypertension, increased activity of the sympathetic nervous system, tachycardia, increased content of cyclic adenosine monophosphate), a slowdown in atrioventricular conduction and a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers. Suppression of impulse conduction is observed mainly in the antegrade and, to a lesser extent, in the retrograde directions. According to the classification of antiarrhythmic drugs, it belongs to group II drugs.
The main effects of Anaprilin:
- prevention of the development of migraine of vascular origin (associated with a decrease in the severity of dilation of cerebral arteries due to β-adrenergic blockade of vascular receptors, a decrease in platelet adhesion, inhibition of platelet aggregation and lipolysis caused by catecholamines, a decrease in renin secretion and stimulation of oxygen supply to tissues);
- a decrease in the severity of myocardial ischemia, postinfarction mortality (occurs due to antiarrhythmic action due to a decrease in myocardial oxygen demand);
- increased bronchial tone;
- a decrease in tremor (associated mainly with the blockade of peripheral β 2 -adrenoreceptors);
- increased contractions of the uterus (spontaneous or associated with the use of drugs that stimulate the myometrium);
- increased atherogenic properties of blood.
Pharmacokinetics
When taken orally, propranolol is absorbed quickly and in a fairly complete volume (90%), excreted from the body at a relatively high rate. Bioavailability after oral administration is 30-40% (associated with the effect of primary passage through the liver, microsomal oxidation), this indicator increases with prolonged therapy (metabolites are formed that inhibit liver enzymes). The amount of bioavailability is determined by the nature of the food and the intensity of hepatic blood flow.
The time to reach the maximum concentration in blood plasma is from 1 to 1.5 hours. Possesses high lipophilicity, accumulates in the tissues of the lungs, brain, heart, kidneys.
Propranolol crosses the blood-brain and placental barriers, as well as into breast milk. The volume of distribution is in the range from 3 to 5 l / kg. The connection with plasma proteins is 90–95%.
Propranolol is metabolized in three ways - aromatic hydroxylation, N-dealkylation, glucuronidation in the liver (including with the participation of cytochrome isoenzymes CYP2D6, CYP1A2, CUR2C19). It enters the intestines with bile, where it is deglucuronized and reabsorbed, and therefore the half-life during the course of administration can be extended to 12 hours.
In case of impaired renal / hepatic function and in elderly patients, the plasma concentration of the drug in the blood increases, the half-life is lengthened.
The main route of excretion is the kidneys (about 90%), up to 1% is excreted unchanged. The half-life is 3-5 hours. It is not removed during hemodialysis.
Indications for use
- unstable angina;
- exertional angina;
- various heart rhythm disturbances associated with lesions of the heart of a rheumatic nature (arrhythmia, atrial tachyarrhythmia, paroxysmal and sinus tachycardia, extrasystole);
- hypertonic disease;
- pheochromocytoma (Anaprilin is used with alpha-blockers);
- arterial hypertension;
- prevention of migraine;
- alcohol withdrawal (trembling and agitation);
- thyrotoxic crisis and diffuse toxic goiter - as an adjuvant, including in case of intolerance to thyrostatic drugs.
Taking Anaprilin also allows you to enhance the contractions of the uterus, reduce bleeding during childbirth and in the postoperative period.
Contraindications
- acute heart failure;
- myocardial infarction in the acute stage;
- sinoatrial blockade;
- AV block II – III degree;
- sick sinus syndrome;
- metabolic acidosis;
- arterial hypotension;
- bronchial asthma;
- predisposition to bronchospasm;
- spastic colitis;
- sinus bradycardia [heart rate (heart rate) less than 55 beats / minute];
- diabetes;
- lactation;
- the presence of hypersensitivity to the components of Anaprilin;
- age up to 18 years (safety and efficacy of the drug for this age group have not been established).
According to the instructions, Anaprilin is prescribed with caution for the following diseases / conditions:
- hyperthyroidism;
- pregnancy;
- myasthenia gravis;
- elderly age;
- hepatic and renal failure;
- heart failure;
- psoriasis;
- a history of allergic reactions;
- Raynaud's syndrome.
Instructions for the use of Anaprilin: method and dosage
Doses of the drug are prescribed by the attending physician.
Anaprilin tablets are used regardless of meals, washed down with a large (at least 200 ml) amount of water.
- cardiac arrhythmias, angina pectoris: the initial daily dose is 60 mg (20 mg 3 times a day), then the daily dose is increased to 80–120 mg (divided into 2-3 doses). The maximum daily dose is 240 mg;
- arterial hypertension: the initial daily dose is 80 mg (40 mg 2 times a day), if the hypotensive effect is insufficient, the daily dose is increased to 120–160 mg (40 mg 3 times a day or 80 mg 2 times a day). The maximum daily dose is 320 mg;
- essential tremor, prevention of migraine: initial daily dose - 80-120 mg (40 mg 2-3 times a day), if necessary, the daily dose can be increased to 160 mg;
- prevention of recurrent myocardial infarction: treatment begins between the 5th and 21st days after a heart attack in an initial daily dose of 160 mg (40 mg 4 times a day) for 2 or 3 days, then they switch to a double dose (according to 80 mg 2 times a day).
With pheochromocytoma, the drug is used only in conjunction with alpha-adrenergic receptor blockers.
In the case of an impending surgical intervention, Anaprilin tablets are prescribed within 3 days before the operation in a daily dose of 60 mg.
In case of impaired renal function, the initial dose of the drug is reduced or the interval between doses is increased.
In case of impaired liver function, it is also recommended to reduce the dose of Anaprilin.
Side effects
- digestive system: nausea, vomiting, diarrhea / constipation, dry mouth, abnormal liver function, taste changes, pain in the epigastric region;
- respiratory system: nasal congestion, rhinitis, bronchospasm, shortness of breath, laryngospasm;
- sense organs: decreased secretion of lacrimal fluid (dry eyes), keratoconjunctivitis, impaired visual acuity;
- skin: psoriasis-like skin reactions, exacerbation of psoriasis, alopecia, increased sweating, skin hyperemia, exanthema;
- cardiovascular system: atrioventricular block, palpitations, arrhythmias, orthostatic hypotension, peripheral arterial spasm, sinus bradycardia, heart failure, myocardial conduction disturbances, lowering blood pressure (BP), chest pain, cold extremities;
- nervous system: in rare cases - insomnia / drowsiness, asthenic syndrome, agitation, paresthesia, weakness, short-term memory loss or confusion, tremors, headache, depression, increased fatigue, dizziness, hallucinations, decreased ability to rapid motor and mental reactions;
- metabolism: hypoglycemia (in patients with type 2 diabetes mellitus);
- reproductive system: decreased potency, decreased libido;
- endocrine system: decreased thyroid function;
- allergic reactions: itching, skin rash;
- effect on the fetus: intrauterine growth retardation, bradycardia, hypoglycemia;
- laboratory parameters: increased bilirubin, agranulocytosis;
- others: back and joint pain, chest pain, muscle weakness, thrombocytopenia, leukopenia.
Overdose
The main symptoms: ventricular premature beats, a marked decrease in blood pressure, dizziness, severe bradycardia, atrioventricular block, fainting, arrhythmia, heart failure (aggravation of the course of a chronic disease or acute), cyanosis of the palms or fingernails, bronchospasm, difficulty breathing, convulsions.
Therapy: gastric lavage, the appointment of activated carbon.
Necessary measures, determined by the indications:
- violations of atrioventricular conduction: 1–2 mg of atropine intravenously, in case of low efficiency, the setting of a temporary pacemaker is indicated;
- bradycardia: 1–2 mg of atropine intravenously, in case of low efficiency, the setting of a temporary pacemaker is indicated;
- lowering blood pressure: the patient should be in the Trendelenburg position (lying on his back at an angle of 45 ° with the pelvis raised in relation to the head);
- ventricular premature beats: lidocaine (the use of class IA drugs is not recommended);
- heart failure: diuretics, cardiac glycosides, glucagon;
- atrioventricular block: epinephrine, pacemaker setting; in the absence of signs of pulmonary edema, plasma-substituting solutions are administered intravenously, in case of low efficiency, dopamine, epinephrine, dobutamine are prescribed;
- bronchospasm: β-adrenergic agonists parenteral or inhalation;
- convulsions: diazepam intravenously.
special instructions
The use of Anaprilin simultaneously with hypoglycemic agents is prescribed only under the strict supervision of a physician (in order to avoid the development of hypoglycemia).
When taken orally, Anaprilin is rapidly absorbed and excreted from the body. The half-life of the drug passes in 3-5 hours, and with prolonged use - in 12 hours (90% of the drug is excreted by the kidneys as metabolites, about 1% remains unchanged).
Abrupt withdrawal of the drug can worsen exercise tolerance and increase the risk of myocardial ischemia, therefore, Anaprilin should be stopped gradually and under the supervision of a doctor.
Patients with diabetes mellitus are prescribed the drug under the control of blood glucose.
Influence on the ability to drive vehicles and complex mechanisms
Taking Anaprilin can affect the ability to concentrate and the speed of motor reactions, therefore, during treatment, precautions should be taken when working with potentially dangerous mechanisms, as well as when driving.
Application during pregnancy and lactation
- lactation period: therapy is contraindicated;
- pregnancy: Anaprilin can be used with caution after assessing the ratio of the expected benefit to the possible risk; if the drug was prescribed to a pregnant woman, close monitoring of the fetus is required; therapy is discontinued 48–72 hours before delivery.
Pediatric use
Anaprilin therapy is contraindicated in patients under 18 years of age.
With impaired renal function
Anaprilin for renal failure is prescribed with caution.
For violations of liver function
Anaprilin for liver failure is prescribed with caution.
Use in the elderly
Anaprilin therapy in elderly patients should be carried out under medical supervision.
Drug interactions
Anaprilin should not be taken together with tranquilizers and antipsychotics (antipsychotic drugs).
Due to the possible sharp drop in blood pressure, it is not recommended to take ethanol-containing drugs during treatment.
The antihypertensive effect of the drug increases with the simultaneous administration of reserpine, hydrochlorothiazide, hydralazine and other antihypertensive drugs, weakened when taking estrogens, nonsteroidal anti-inflammatory drugs, MAO inhibitors (the interval between taking propranolol and monoamine oxidase inhibitors should not be less than 14 days)
When taken together with antihistamines, Anaprilin reduces their effect, with uterotonizing and thyreostatic drugs, it enhances.
With simultaneous administration with phenothiazine derivatives, the concentration of both drugs in the blood plasma increases, with cimetidine - the bioavailability of cimetidine increases.
Unhydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.
Rifampicin - shortens the half-life, sulfasalazine - increases the concentration of propranolol in the blood plasma.
Analogs
Anaprilin's analogs: Obzidan, Vero-Anaprilin, Propranolol, Inderal, Propranobene, etc.
Terms and conditions of storage
Store at a temperature of 8-25 ° C in a dry and dark place, out of reach of children.
Shelf life is 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Anaprilin
According to reviews, Anaprilin is an inexpensive and effective drug. It is often described as the simplest and most affordable remedy for arterial hypertension. It is also used as an emergency aid with a rapid heart rate associated with psycho-emotional stress, or when the exact diagnosis is not known. Not addictive, if necessary, it can be used once. The main disadvantages of Anaprilin include the possibility of side effects and a large list of contraindications.
The price of Anaprilin in pharmacies
The approximate price for Anaprilin is 14–18 rubles. (in the package 50 pcs. 10 mg each) or 18-22 rubles. (in the package 50 pcs. 40 mg each).
Anaprilin: prices in online pharmacies
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Drug name Price Pharmacy |
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Anaprilin 10 mg tablets 50 pcs. RUB 21 Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
