Pharmacological properties Cardioselective beta1-blocker, has no membrane stabilizing and intrinsic sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic action. Blocking in low doses of beta1-adrenergic receptors of the heart, reduces the formation of catecholamines stimulated cAMP from ATP, reduces intracellular current ion calcium, adversely chrono, Dromo,, Butman-and inotropic effect (slows the heart rate (HR), depresses conduction and excitability, reducing myocardial contractility). Total peripheral vascular resistance at the beginning of the use of beta-blockers (in the first 24 hours after ingestion) increases (as a result of reciprocal increase in the activity of alpha-adrenoceptor stimulation and removal of beta2-adrenergic receptors), which after 1-3 days back to original, and with long-term appointment is reduced. The hypotensive effect associated with a decrease in minute volume of blood flow, decreased activity of the renin-angiotensin-aldosterone system (is more important for patients with initial hypersecretion of renin), the sensitivity of the baroreceptors of the aortic arch (not going to increase their activity in response to lowering blood pressure) and the influence of the central nervous system.The antihypertensive effect is a decrease in both systolic and diastolic blood pressure, decrease stroke and minute volume of blood. The average therapeutic doses has no effect on the tone of the peripheral arteries. Antihypertensive effect lasts for 24 hours, when taken regularly is stabilized by the end of 2 weeks of treatment. Antianginal effect is determined by a decrease in myocardial oxygen demand by reducing heart rate (diastole lengthening and improving myocardial perfusion) and contractility, as well as a decrease in the sensitivity of the myocardium to the effects of the sympathetic innervation. It slows heart rate at rest and during exercise. By increasing end-diastolic pressure in the left ventricle and increase the tension of the muscle fibers of the ventricles can increase oxygen demand, especially in patients with chronic heart failure. The antiarrhythmic effect due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP levels, hypertension ), a decrease in the rate of spontaneous excitation of the sinus and ectopic pacemakers and slowing of atrioventricular conduction. Inhibition of pulses observed mainly in the antegrade and to a lesser extent in the retrograde direction through the atrioventricular node, and on additional routes. Increases the survival of patients with myocardial infarction (reduces the incidence of ventricular arrhythmias and angina attacks). In practice, does not weaken the bronchodilatory effect of isoprenaline. In contrast, nonselective beta-blockers when given in therapeutic doses, the average has a less pronounced effect on the organs containing beta2-adrenergic receptors (pancreas, skeletal muscle, smooth muscle of the peripheral arteries, bronchi and uterus), and carbohydrate metabolism; atherogenic action expression is not different from that of propranolol. To a lesser extent has negative BATM, chrono, foreign-and Dromotropic. When used in large doses (over 100 mg / day) has a blocking effect on both beta-adrenoceptor subtype. The negative chronotropic effect appears after 1 hour after administration, reaching its maximum after 2-4 hours and lasts up to 24 hours.
The absorption from the gastrointestinal tract – fast, incomplete (50-60%), the bioavailability – 40-50%, the solubility in fats is very low. Maximum concentration time – 2-4 hours. Poorly penetrates the blood-brain barrier, it passes through the placenta and breast milk. Contact with blood plasma proteins – 6-16%. Practically not metabolized in the liver. The half-life – 6-9 hours (increases in elderly patients).Excreted by the kidneys by glomerular filtration (85-100% unchanged). Impaired renal function accompanied by longer half-life and cumulation (necessary to decrease the dose) with creatinine clearance (CC) below 35 mL / min / 1.73 m². half-life of 16-27 hours, QC below 15 ml / min. – More than 27 hours, anuria extended to 144 hours. Displayed during hemodialysis.
Hypersensitivity to the drug, cardiogenic shock, atrioventricular block P-PG degree, bradycardia (heart rate less than 40 bpm. / Min.), Sick sinus syndrome, sinoatrial block, congestive heart failure, or decompensated chronic heart failure, cardiomegaly without signs of chronic heart failure, Prinzmetal angina, hypotension (in the case of myocardial infarction, systolic blood pressure (BP) of less than 100 mm Hg), lactation, concomitant use of monoamine oxidase inhibitors (MAOIs), age 18 years (effectiveness and safety not installed).
1 diabetes and type 2 diabetes, metabolic acidosis, hypoglycemia, allergic reactions in the history of chronic obstructive pulmonary disease (including asthma, emphysema), chronic heart failure (compensated), obliterating peripheral vascular disease ( “intermittent” claudication Reynaud’s syndrome); pheochromocytoma, liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including history), psoriasis, pregnancy, old age.
Pregnancy and lactation
If pregnancy should appoint Betakard ® only in cases where the benefit to the mother outweighs the potential risk to the fetus. Betakard ® is excreted in breast milk, so breastfeeding is contraindicated drug.
Dosing and Administration
Assign inside before a meal, do not chew, washed down with a small amount of liquid. Hypertension Treatment starts with 50 mg Betakard ® 1 time per day. To achieve a stable hypotensive effect requires 1-2 weeks of reception. With insufficient expression hypotensive effect dose was increased to 100 mg at one time. Further increase of the dose is not recommended, since it is not accompanied by increased clinical benefit. Angina The initial dose is 50 mg per day. If during the week is not an optimal therapeutic effect, increasing the dose to 100 mg per day. Elderly patients and patients with impaired renal excretory function requires correction dosing regime. In the presence of renal failure recommended dose correction according to the creatinine clearance. In patients with renal insufficiency with creatinine clearance values above 35 ml / min / 1.73 m 2 (normal range is 100-150 ml / min / 1,73m 2 ) a significant accumulation of the drug Betakard ® does not occur. The following maximum dose recommended for patients with renal insufficiency:
|Creatinine clearance (ml / min / 1.73 m 2 )||The half-life
|The maximum dose|
|15-35 for at least 15||16-27 more than 27||50 mg per day
of 100 mg a day
to 50 mg a day,
100 mg once in one day four
Patients who are on hemodialysis, Betakard® appoint 25 or 50 mg / day immediately after each dialysis session, which should be carried out under steady-state conditions, as there may be a drop in blood pressure.
In elderly patients, an initial single dose – 25 mg (may be increased under the control of blood pressure, heart rate).
Increasing the daily dose above 100 mg are not recommended because the therapeutic effect is not enhanced, and the likelihood of side effects increases.
On the part of the central nervous system : fatigue, weakness, dizziness, headache, drowsiness or insomnia, “nightmarish” dream, depression, anxiety, confusion, or momentary loss of memory, hallucinations, decreased ability to concentrate, decreased reaction rate, paresthesia in the extremities (in patients with “intermittent” claudication and Raynaud’s syndrome), myasthenia gravis, seizures.from the senses : visual disturbances, reduced secretion of tear fluid, dryness and soreness of eyes, conjunctivitis. On the part of the cardiovascular system : bradycardia, palpitations, conduction disturbances infarction, atrioventricular block (up to cardiac arrest), arrhythmia, weakening of the myocardial contractility and development (worsening) of chronic heart failure, orthostatic hypotension, symptoms vasoconstriction (cooling of the lower extremities, Raynaud’s syndrome), vasculitis, chest pain. digestive system : dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, taste changes. The respiratory system : nasal congestion, difficulty breathing when administered at high doses (selectivity loss) and / or in predisposed patients – laryngo . – and bronchospasm part of the endocrine system .: hyperglycemia (in patients with type 2 diabetes), hypoglycemia (in patients receiving insulin), hypothyroid state Allergic reactions : itching, rash, urticaria. For the skin : increased sweating, flushing of the skin, exacerbation of psoriasis symptoms, psoriasis-like skin rash, reversible alopecia. Laboratory findings: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of “liver” enzymes, hyperbilirubinemia. Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia. Other :. Back pain, arthralgia, weakening of libido, reduced potency, the syndrome of “lifting” (increasing angina attacks, increased blood pressure) The frequency of side effects increases with the dose.
Overdose Symptoms : bradycardia, dizziness, excessive reduction of blood pressure, fainting, arrhythmia, ventricular premature beats, atrioventricular block degree II-III, chronic heart failure, cyanosis of nails or palms, cramps, difficulty breathing, bronchospasm. Treatment : gastric lavage and the appointment of adsorbing drugs; in violation of atrioventricular conduction and / or bradycardia – in / in a 1-2 mg of atropine, epinephrine (adrenaline) or staging a temporary pacemaker; with ventricular arrhythmia – lidocaine (IA class of drugs does not apply); in lowering blood pressure – Patient should be in the Trendelenburg position. If there are no signs of pulmonary edema – in / plasma substituting solutions, with inefficiency – the introduction of epinephrine, dopamine, dobutamine; in chronic heart failure – cardiac glycosides, diuretics, glucagon; in convulsions – in / diazepam; with bronchospasm -ingalyatsionno or parenterally – beta adrenostimulyatorov. Perhaps dialysis.
Interaction with other drugs
allergens used for immunotherapy, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients treated with dianabol results.
Iodine-containing X-ray contrast agent for the on / in the increase the risk of anaphylactic reactions.
Phenytoin at / in the introduction, drugs for inhalation anesthesia (derivatives of hydrocarbons) increase the intensity of cardiodepressive action and the likelihood of lowering blood pressure.
When concomitant administration of insulin and hypoglycemic agents for oral masking the symptoms of developing hypoglycemia.
Reduces clearance of lidocaine and xanthine and increases their concentration in blood plasma , especially in patients with initially increased clearance of theophylline under the influence of smoking.
Antihypertensive effect of weakening non-steroidal anti-inflammatory drugs (delay of sodium ions and blockage of prostaglandin synthesis by the kidneys), corticosteroids, and estrogens (sodium retention).
Cardiac glycosides, methyldopa, reserpine and guanfacine blockers “slow “calcium channels (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening heart failure, bradycardia, atrioventricular block and cardiac arrest. Diuretics, clonidine, sympatholytic, hydralazine, blockers “slow” calcium channel blockers and other antihypertensives may lead to an excessive reduction in blood pressure.
Extends the action of non-depolarizing muscle relaxants and anticoagulant effect of coumarin.
Tri- and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotics increase central nervous system depression.
not recommended simultaneous application with MAO inhibitors due to the significant increase in the hypotensive action, a break in treatment between receiving MAO inhibitors and dianabol results should not be less than 14 days.
Negidrirovannye ergot alkaloids increase the risk of peripheral circulatory disorders.
control for patients taking dianabol results should include monitoring of the heart rate (HR) and blood pressure (BP) (at the beginning of treatment – daily, then 1 every 3-4 months), the content of blood glucose in patients with diabetes 1 and type 2 (one every 4-5 months). In elderly patients, it is recommended to monitor renal function (1 every 4-5 months).
It is necessary to train the patient’s heart rate calculation method and instruct on the need of medical advice in heart rate less than 50 bpm. / Min. Approximately 20% of patients with angina Beta-blockers are ineffective.
The main reason – severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats / min.) And increased end-diastolic. the volume of the left ventricle that violate subendocardial blood flow. At the “smokers” the effectiveness of beta-blockers lower.
Patients who use contact lenses should bear in mind that during treatment may decrease the production of tear fluid.
When thyrotoxicosis dianabol results may mask certain clinical signs of hyperthyroidism (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because the symptoms can increase.
In diabetes may mask tachycardia caused by hypoglycemia. In contrast, nonselective beta-blockers practically no increase insulin-induced hypoglycemia and delay recovery of blood glucose levels to the normal concentration.
At the same time taking clonidine its reception can be terminated only after a few days after discontinuation of dianabol results.
Perhaps the increased severity of the allergic reaction and no effect from the usual doses of epinephrine (adrenaline) with aggravated allergic history.
In just a few days before the general anesthesia with chloroform or diethyl ether is necessary to stop taking the drug. If the patient has taken the drug before surgery, he should pick up the drugs for general anesthesia with minimal negative inotropic effect.
Reciprocal activation n.vagus can eliminate I / atropine (1-2 mg). Drugs that reduce the reserves of catecholamines (eg, reserpine), may enhance the effect of beta-blockers, so patients taking such drug combinations should be under constant medical supervision in order to identify pronounced reduction in blood pressure and bradycardia.
The drug can be administered to patients with bronhospasticheskimi diseases in case of intolerance and / or ineffectiveness of other antihypertensive drugs, but should strictly follow the dosage. Overdosing is dangerous development of bronchospasm. In the case of elderly patients increasing bradycardia (less than 50 u. / Min.), Hypotension (systolic blood pressure below 100 mm Hg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver and kidney function should be reduced dose or to discontinue treatment. It is recommended to discontinue therapy in the development of depression caused by the intake of beta-blockers.
Do not abruptly discontinue the treatment because of the risk of severe arrhythmias and myocardial infarction. Abolition are gradually reducing the dose for 2 weeks or more (reduce dose by 25% in 3-4 days).
It is necessary to cancel prior to the study in blood and urine catecholamines and Normetanephrine vanillylmandelic acid; titers of antinuclear antibodies (1-2 days).
During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions.
Tablets, film-coated, 50 mg, 100 mg.
10 tablets in a blister made of aluminum foil and PVC film; . 3 blisters or 10 blisters with instruction for use in a cardboard box Sample not for sale : 10 tablets in a blister of aluminum foil and PVC film; 1 blister with instruction on use is packed in a cardboard box. cutbol
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