Anaprilin-Zdorovye, the tab. on 40 mg No. 50

General characteristics. Structure:

International and chemical names: propranolol; (RS) -1-изопропиламино-3-нафт-1-илоксипропан-2-ола hydrochloride; main physical and chemical properties: tablets white or almost colors, a ploskotsi-lindrichesky form, with a facet; structure: 1 tablet contains propranolol of a hydrochloride 10 mg or 40 mg;
excipients: refined sugar, potato starch, talc, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Blocks b1-and b2-adrenoceptors, has membrane stabilizing effect. Automatism of a sinuatrial node, emergence of the ectopic centers in auricles, an atrioventricular node and, to a lesser extent, in ventricles oppresses. Reduces the speed of carrying out excitement in atrioventricular connection on Kent bunch preferential in the anterograde direction. Reduces frequency and reduces force of cordial reductions, the need of a myocardium for oxygen. Lowers cordial emission, arterial pressure, secretion of a renin, renal clearance and a glomerular filtration rate. Suppresses reaction of baroreceptors of an aortic arch to lowering of arterial pressure.
The lipolysis in fatty tissue oppresses, interfering with increase in level of free fatty acids (the coefficient of an aterogennost can increase). Suppresses a glycogenolysis, secretion of a glucagon and insulin, transformation of thyroxine into triiodothyronine. Raises a tone of muscles of bronchial tubes and contractility of a uterus. Increases secretory and motor activity of digestive tract.
At patients with an ischemic disease of heart reduces the frequency of attacks of stenocardia, increases portability of exercise stresses, reduces the need for nitroglycerine. Has cardioprotective effect, authentically reducing risk of a repeated myocardial infarction and sudden death by 20–50%.
After reception of a single dose of propranolol decrease in systolic and diastolic arterial pressure in situation is observed both lying, and standing; the lasting hypotensive effect develops by the end of the second week of treatment.

Pharmacokinetics. At intake quickly and almost it is completely soaked up from digestive tract (90%). Bioavailability makes 30–40% (effect of "the first passing" through a liver) and depends on character of food and intensity of a hepatic blood-groove, increases at prolonged use. The maximum concentration in a blood plasma is reached in 1–2 h after intake. The volume of distribution of 3-5 l/kg contacts proteins of plasma for 90–95%. Has high lipophilicity, collects in pulmonary fabric, a brain, kidneys and heart. Gets through hematoencephalic and placental barriers, into breast milk. It is metabolized in a liver by a glyukuronirovaniye (99%). The elimination half-life of 3-5 h, at prolonged use increases to 12 h. It is removed preferential by kidneys in the form of metabolites (to 90%), in not changed look – less than 1%. Is not removed at a hemodialysis.

Indications to use:

Arterial hypertension, stenocardia, sinus tachycardia (including at a thyrotoxicosis), supraventricular and ciliary tachycardias, a myocardial infarction, a hypertrophic cardiomyopathy (including a subaortal stenosis), a prolapse of the mitral valve, an essential tremor, neurocirculatory dystonia, migraine (prevention of attacks). As a part of a combination therapy – a pheochromocytoma (in combination with a-adrenoblockers), an abstinence syndrome (excitement and a tremor).

Route of administration and doses:

Appoint inside in 10–30 min. prior to food, washing down with enough liquid. Dosing mode individual. The dose and term of treatment are established by the doctor.
Arterial hypertension. The initial dose makes 40 mg 2–3 times a day. If necessary the dose is gradually increased every week, to the supporting daily dose – 160–320 mg in 2–3 receptions. The maximum daily dose – 320 mg.
Stenocardia. The initial dose makes 40 mg 2–3 times a day. The supporting daily dose – 120–240 mg in 3–4 receptions. The maximum daily dose – 240 mg.
Myocardial infarction (systolic arterial pressure – more than 100 mm of mercury) on 20–40 mg 3–4 times a day under control of ChSS.
Arrhythmias, tachycardia at nervousness, a thyrotoxicosis. Appoint 10-30 mg 3-4 times a day.
Hypertrophic cardiomyopathy. Appoint 20–40 mg 3–4 times a day.
Migraine, excitement, tremor. The initial dose makes 40 mg 2–3 times a day. The supporting daily dose – 80–160 mg in 2–3 receptions. The maximum daily dose – 160 mg.
Pheochromocytoma (only in a combination with a-adrenoblocker). Appoint 30–60 mg a day in 2–3 receptions within 3 days before operation; not operated patient – 30–60 mg a day.
To children 1 years as anti-hypertensive or antiarrhytmic means are more senior appoint in an initial dose 0,5–1 mg/kg/days in 2–4 receptions, a maintenance dose – 2–4 mg/kg/days in two steps. Daily doses are selected individually.

Features of use:

Treatment should be carried out at regular medical control. Restrictions to a medical use of drug are chronic bronchitis, emphysema, a diabetes mellitus, a hypoglycemia, a metabolic acidosis, an abnormal liver function and kidneys, psoriasis, a spastic colitis, a myasthenia, a depression now or in the anamnesis, an atrioventricular block І degrees, pregnancy. At elderly patients the risk of development of side effects from the central nervous system is increased. At an abnormal liver function the dose decline and observation of the doctor in the first is recommended to a chetira of week of therapy. Use at pregnancy is possible only in that case when the expected therapeutic effect exceeds potential risk for a fruit. In case of pregnancy it is necessary to interrupt therapy with propranolol for 48–72 h to the estimated term of childbirth for the purpose of prevention of bradycardia, arterial hypotension, respiratory depression (neonatal asphyxia) at the newborn. The newborn during 48–72 h has to be under observation of the doctor.
For the period of treatment it is necessary to exclude the use of alcoholic beverages. It is necessary to cancel drug gradually, within 2 weeks, because of risk of manifestation of "withdrawal".
Some days before carrying out an anesthesia it is necessary to stop administration of drug or to pick up anesthetic with the smallest negative inotropic effect. Drug can mask hypoglycemia symptoms (tachycardia) at the patients with a diabetes mellitus accepting insulin or other glucose-lowering drugs. Against the background of the burdened allergological anamnesis strengthening of expressiveness of reaction of hypersensitivity and lack of the expected effect of usual doses of Epinephrinum is possible. Patients with a pheochromocytoma should appoint blockers of a-adrenoceptors previously.
During treatment change of results of tests when carrying out laboratory researches is possible (increase in level of urea, transaminases, phosphatases, lactate dehydrogenases).
With care appoint to drivers of vehicles or when performing potentially dangerous types of activity because of a possibility of development of side effects from the central and cardiovascular systems.

Side effects:

From cardiovascular system and a hemopoiesis: arterial hypotension, sinus bradycardia, atrioventricular blockade, development/progressing of heart failure, disturbance of peripheric circulation, Werlhof's disease, leukopenia, agranulocytosis. From a nervous system and sense bodys: adynamy, dizziness, headache, sleeplessness or drowsiness, nightmares, reduction of speed of mental and motor reactions, depression, concern, confusion of consciousness or short-term amnesia, paresthesias, visual acuity disturbance, reduction of secretion of the lacrimal liquid, dryness and morbidity of eyes, keratoconjunctivitis, hallucinations, spasms. From the alimentary system: nausea, vomiting, pains in epigastric area, diarrhea or a lock, thrombosis of a mezenterialny artery, ischemic colitis, abnormal liver functions (including a cholestasia). From respiratory system: pharyngitis, cough, short wind, respiratory distresssindry, bronkho-and laryngospasm. From endocrine system: hypoglycemia. Allergic reactions: skin reactions, itch, fever. From integuments: alopecia, exacerbation of psoriasis. Other: arthralgia, weakening of a libido, decrease in a potentiality, Peyroni's disease.

Interaction with other medicines:

Antihypertensives (especially nifedipine), sympatholytics, гидралазин, raise nitrates (nitroglycerine), monoaminooxidase inhibitors, anesthetics, and non-steroidal anti-inflammatory drugs, glucocorticosteroids, estrogen, cocaine reduce hypotensive effect of propranolol. At simultaneous use with a clonidine, Reserpinum, metildopy – development of excessive hypotension and bradycardia is possible. Inductors of a microsomal oxidation (rifampicin, barbiturates), antacids and heparin reduce, and fenotiazina and Cimetidinum increase concentration of propranolol in a blood plasma. At simultaneous use with iodinated radiopaque substances the risk of development of anaphylactic reactions (intravenously) increases; with not hydrogenated ergot alkaloids – risk of development of disturbances of peripheric circulation; with verapamil, diltiazem – the risk of development or aggravation of bradycardia, an atrioventricular block, heart failure and a cardiac standstill, with hypoglycemic means – amplifies hypoglycemic effect and its symptoms mask (for example, tachycardia). At combined use with Norepinephrinum perhaps sharp increase in arterial pressure. Propranolol extends anticoagulating effect of coumarins, slows down lidocaine removal, prolongs action of not depolarizing muscle relaxants, slows down metabolism of theophylline (Euphyllinum), increasing its concentration in blood. When using allergens for an immunotherapy or extracts of allergens for skin tests against the background of treatment by propranolol the risk of emergence of heavy system allergic reactions increases.

Contraindications:

Hypersensitivity to drug components, cardiogenic shock, an atrioventricular block of II and III degrees, sinuatrial blockade, a sick sinus syndrome, a sinus bradycardia (frequency of cordial reductions less than 50 beats/min), Printsmetal's stenocardia, arterial hypotension, acute and chronic heart failure, the heavy course of bronchial asthma, Reynaud's syndrome and other obliterating diseases of peripheral vessels, the feeding period of a breast, children's age till 1 year.

Overdose:

Symptoms: dizziness, the expressed hypotension, bradycardia, arrhythmia, cordial insufficiency, a collapse, a Crocq's disease, spasms, breath difficulty, a bronchospasm. Treatment: a gastric lavage, purpose of the adsorbing means. In the absence of signs of a fluid lungs appoint infusions of plasma substituting solutions, at inefficiency – Epinephrinum, a dopamine, Dobutaminum; at heart failure – cardiac glycosides, a-adrenomimetiki, diuretics, a glucagon; at spasms – diazepam, intravenously; at a bronchospasm - b-adrenostimulyatory, is inhalation or parenterally. In the presence of disturbance of atrioventricular conductivity – 1–2 mg of atropine, intravenously, at a low performance – installation of a temporary pacemaker. At ventricular premature ventricular contraction apply lidocaine (the antiarrhytmic drugs IA of a class are not used). The hemodialysis is inefficient.

Storage conditions:

To store in dry, protected from light and the place, at a temperature from 8 °C to 25 °C. To store in the place, unavailable to children.
Period of storage – 4 years.

Issue conditions:

According to the recipe

Packaging:

Tablets No. 10х5, No. 50 in a blister strip packaging and in a pack; No. 50 in a container plastic and in a pack.