2010/09/21

Aritel

Composition, structure and packing

Tablets, film-coated light-orange, round, biconvex, transverse section of the 2 layers are visible.

1 tab. bisoprolol (in the form of fumarate) 5 mg - - 10 mg.

Excipients: potato starch, povidone (kollidon-30), lactose, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate, gipromelloza, macrogol (polyethylene glycol 400, 4000), titanium dioxide, talc, iron oxide yellow, iron oxide red.

Clinico-pharmacological group: beta1-blocker.

Pharmacological action

Selective beta1-blocker. Do not have your own sympathomimetic activity and clinically significant membrane stabilizing properties. Has antihypertensive, antiarrhythmic and antianginal.

Reduces plasma renin activity, reduces myocardial oxygen demand, reduces heart rate at rest and during exercise. Blocking in low doses, β1-adrenergic receptors of the heart, reduces the formation of catecholamines stimulated cAMP from ATP, reduces the intracellular calcium ion current has a negative chrono-, Drome, BATM-and inotropic effect, depresses conduction and excitability, reduces myocardial contractility. TPVR at the beginning of the drug in the first 24 h, increases (as a result of reciprocal increase in the activity of α-adrenoceptor stimulation and removal of β2-adrenoceptor), which after 1-3 days, returning to the original, but with long-term assignment is reduced.

The hypotensive effect is associated with a decrease in minute volume of blood, sympathetic stimulation of peripheral blood vessels, decreased activity of the renin-angiotensin system (important for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure and influence on the central nervous system.

When hypertension effect after 2-5 days, stable operation - after 1-2 months. Antianginal effect is due to a decrease in myocardial oxygen demand as a result of shortening of heart rate and decrease contractility, prolongation of diastole, improving myocardial perfusion.

Due to increasing end-diastolic pressure in the left ventricle and increase the tension of muscle fibers of the ventricles can increase oxygen demand, particularly in patients with chronic heart failure. Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increase of cAMP, hypertension), decrease in the rate of spontaneous excitation of the sinus and ectopic pacemakers and slowing of the AV-(mainly in the antegrade and to a lesser extent in the retrograde direction through the AV-node) and on additional routes.

When used in the medium therapeutic doses, unlike nonselective beta-blockers, has a less pronounced effect on the organs that contain the β2-adrenergic receptors (pancreas, skeletal muscle, smooth muscle of peripheral arteries, bronchi and uterus) and carbohydrate metabolism, does not cause delays sodium ions in the body, marked atherogenic action is not different from that of propranolol. When used in large doses (> 200 mg) has a blocking effect on both subtypes of β-adrenergic receptors, mainly in the bronchi and smooth muscles of blood vessels.

Pharmacokinetics

Absorption

If ingestion is absorbed from the gastrointestinal tract of 80-90% of the drug; meal does not affect absorption. Cmax plasma levels observed after 1-3 hours

Distribution

Linking to plasma proteins of about 30%. Permeability through the BBB and placental barrier, secretion of breast milk - low.

Metabolism

Bisoprolol is metabolized in the liver.

Putting T1 / 2 sostavlyaet10 12 hours with urine - 50% intact, with the bile <2%.

Statement
hypertension;
prevention of angina attacks in coronary heart disease.

Dosage regimen

The drug, taken orally in the morning fasting, not liquid, at a dose of 5 mg once. If necessary, the dose may be increased to 10 mg 1 time / day. The maximum daily dose - 20 mg / day. Patients with impaired renal function (CC <20 ml / min) or with severe hepatic impairment a maximum daily dose is 10 mg.

Side effect
From the side of the central nervous system and peripheral nervous system: fatigue, weakness, dizziness, headache, sleep disturbance, depression, anxiety, confusion, or short-term memory loss, hallucinations, asthenia, myasthenia gravis, paresthesia in the extremities (in patients with intermittent claudication and Raynaud's syndrome ), tremor.
Since the cardiovascular system: sinus bradycardia, palpitation, myocardial conduction disturbances, AV-block (until the full development of cross-blockade and heart failure), arrhythmia, myocardial relaxation, development (worsening) of chronic heart failure (swelling of the ankles and feet, shortness of breath), lowering blood pressure, orthostatic hypotension, a manifestation of Angiospasm (abnormalities of peripheral circulation, cooling of the lower extremities, Raynaud syndrome), pain in the chest.
On the part of the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, liver problems (dark urine, yellow skin and sclera, cholestasis), changes in taste, changes in the activity of liver enzymes (increased ALT, ACT ), bilirubin, triglycerides.
On the part of the respiratory system: nasal congestion, shortness of breath when administered high doses (loss of selectivity) and / or in predisposed patients - laryngism, bronchospasm.
On the part of the endocrine system: hyperglycemia (in patients with insulin-dependent diabetes), hypoglycemia (in patients receiving insulin), hypothyroid state.
From the senses: visual disturbances, reduced secretion of the lacrimal fluid, dryness and eye pain, conjunctivitis.
The part of the hemopoietic system: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia.

Dermatological reactions: sweating, flushing of skin, rash, psoriazopodobnye skin reactions, exacerbation of symptoms of psoriasis.

Allergic reactions: itching, rash, urticaria.

Other: back pain, arthralgia, weakening of libido, reduced potency, withdrawal syndrome (increased angina attacks, increased blood pressure).

Contraindications
shock (including cardiogenic);
collapse;
pulmonary edema;
acute heart failure;
Chronic heart failure in the stage of decompensation;
AV-block II and III degree;
sinoatrial block;
SSS (sick sinus syndrome);
pronounced bradycardia;
Prinzmetal angina;
cardiomegaly (with no signs of heart failure);
hypotension (systolic BP <100 mm Hg, especially in myocardial infarction);
asthma;
COPD in history;
simultaneous use of MAO inhibitors (except for MAO type B);
later stages of violations of the peripheral circulation (Raynaud's disease);
pheochromocytoma (without the simultaneous use of alpha-blockers);
metabolic acidosis;
childhood and adolescence to 18 years (effectiveness and safety have not been established);
Hypersensitivity to the drug's components and other beta-blockers.

With care use in patients with liver failure, chronic renal insufficiency, myasthenia gravis, thyrotoxicosis, diabetes mellitus, AV-blockade of I degree, depression (including history), psoriasis, in elderly patients.

Pregnancy and lactation

Use of the drug during pregnancy and lactation is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. In applying Aritela during pregnancy of fetal intrauterine growth retardation, hypoglycemia, bradycardia.

Application for violations of liver function

With care use in patients with hepatic insufficiency.

Application for violations of renal function

With care use in patients with chronic renal failure.

Cautions

Monitoring of patients receiving Aritel should include measurement of heart rate and blood pressure (at the beginning of treatment - every day, then 1 every 3-4 months), ECG, determination of blood glucose in patients with diabetes (1 every 4-5 months). In elderly patients are encouraged to monitor renal function (1 every 4-5 months). It should teach the patient methods of calculating heart rate and instruct on the need of medical advice in the HR <50 bpm.

Before starting the treatment recommended for the study of respiratory function in patients with a history of bronchopulmonary anamnesis. Approximately 20% of patients with angina beta-blockers are ineffective.

Underlying causes - severe coronary atherosclerosis with low ischemic threshold (heart rate <100 bpm) and increased end-diastolic volume of the left ventricle, which violates subendokardialny bloodstream.

When you smoke the effectiveness of beta-blockers lower.

Patients who use contact lenses, be aware that during the treatment products may decrease tear fluid.

If you are using in patients with pheochromocytoma are at risk of paradoxical arterial hypertension (if not previously achieved efficient alpha-adrenoblockade).

When thyrotoxicosis Aritel may mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, since symptoms can increase.

In diabetes Aritel may mask the tachycardia caused by hypoglycemia. In contrast to the nonselective beta-blockers practically does not increase insulin-induced hypoglycemia and delay recovery of blood glucose concentration to normal levels.

At the same time taking clonidine its reception can be terminated only after a few days after the cancellation Aritela. Perhaps increased severity of hypersensitivity reactions and the lack of effect of conventional doses of epinephrine on the background of aggravated allergic history.

In the case of the need for routine surgical treatment of the abolition of the drug carried out for 48 hours before the start of general anesthesia. If the patient took the drug before surgery, he should pick up the drug for general anesthesia with minimal negative inotropic effects. Reciprocal activation of the vagus nerve can be removed in / atropine (1.2 mg).

Drugs that reduce the reserves of catecholamines (including reserpine), may enhance the action of beta-blockers, so patients taking combinations of drugs should be under constant medical supervision in order to identify expressed lowering blood pressure or bradycardia. Patients with diseases bronhospasticheskimi can assign cardioselective blockers in case intolerance and / or ineffectiveness of other antihypertensive drugs.

Overdosing is dangerous development of bronchospasm. In case of elderly patients increasing bradycardia (HR <50 bpm), expressed by lowering blood pressure (systolic BP <100 mm Hg), AV-blockade is necessary to reduce the dose or stop treatment. It is recommended to discontinue therapy during the development of depression. Do not abruptly interrupt treatment because of the risk of severe arrhythmias and myocardial infarction. The lifting of the hold gradually, reducing the dose for 2 weeks or more (reduce dose by 25% in 3-4 days). It should cancel before the test content in the blood and urine catecholamines, normetanephrine, vanillylmandelic acid and antinuclear antibody titers.

Effects on ability to drive vehicles and management mechanisms

During the period of treatment must be careful when driving and busy with other potentially hazardous activities that require high concentration and speed of psychomotor reactions.

Overdose

Symptoms: arrhythmia, ventricular extrasystoles, marked bradycardia, AV-block, marked reduction of blood pressure, chronic heart failure, cyanosis of nails of fingers or palms, shortness of breath, bronchospasm, dizziness, fainting, seizures.

Treatment: gastric lavage and the appointment of adsorbing drugs.

Symptomatic therapy: when full-fledged AV-blockade in / 1-2 mg of atropine, epinephrine, or staging a temporary pacemaker with ventricular arrhythmia - lidocaine (class 1A drugs do not apply) with a decrease in blood pressure the patient must be in a position Trendelenburg, with no signs of edema light - in / plazmozameschayuschie solutions with inefficiency - the introduction of epinephrine, dopamine, dobutamine (to maintain the chronotropic and inotropic actions and eliminate BP decrease) in heart failure - cardiac glycosides, diuretics, glucagon, with convulsions - in / diazepam; with bronchospasm - inhaled beta2-adrenostimulyatorov.

Drug Interactions

The allergens used for immunotherapy, allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol. Iodine radiopaque drugs for in / in the introduction increase the risk of anaphylactic reactions.

Phenytoin at a / in the introduction, medicines for inhalation general anesthesia (derivatives of hydrocarbons) increase the severity cardiodepressive action and the likelihood of BP reduction. Change the effectiveness of insulin and oral hypoglycemic drugs, masking the symptoms of developing hypoglycemia (tachycardia, increased BP). Reduces clearance of lidocaine and xanthine (except difillina) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking. Antihypertensive effect of weakening the NSAID (sodium retention, the blockade of prostaglandin synthesis by the kidneys), the SCS and estrogens (sodium retention).

Cardiac glycosides, methyldopa, reserpine, guanfatsin, blockers of slow calcium channels (verapamil, diltiazem), amiodoron and other antiarrhythmic drugs increase the risk of developing / worsening of bradycardia, AV-blockade, cardiac arrest and heart failure. Nifedipine can cause a significant reduction in blood pressure. Diuretics, clonidine, sympatholytic, hydralazine and other antihypertensive drugs may lead to excessive blood pressure decrease. Lengthens action nondepolarizing muscle relaxants and anticoagulant effect of coumarins.

Tricyclic and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics drugs increase CNS depression. Avoid concurrent use with MAO inhibitors due to a significant increase in antihypertensive action, a break in treatment between the intake of MAO inhibitors and bisoprolol should be at least 14 days. Negidrirovannye ergot alkaloids increase the risk of disorders of peripheral circulation. Ergotamine increases the risk of breach of peripheral circulation; sulphasalasyne increases the concentration of bisoprolol in plasma; rifampicin shortens T1 / 2.

Terms and Conditions of storage

The drug should be stored out of reach of children, dry, dark place at temperatures not above 25 ° C. Shelf life - 2 years.