2010/12/12

Atenolol Belupo

Release form, composition and packing

Tablets, film-coated white, round, biconvex.

1 tab. atenolol 25 mg.

Excipients: microcrystalline cellulose, lactose monohydrate, povidone, corn starch, talc, colloidal silicon dioxide, croscarmellose sodium, magnesium stearate.

The composition of the shell: hypromellose 5 cP, hypromellose 15 cps, talc, titanium dioxide, disodium edetate dihydrate.

Tablets, film-coated white, round, biconvex, with Valium on one side.

1 tab. atenolol 50 mg.

Excipients: microcrystalline cellulose, lactose monohydrate, povidone, corn starch, talc, colloidal silicon dioxide, croscarmellose sodium, magnesium stearate.

The composition of the shell: hypromellose 5 cP, hypromellose 15 cps, talc, titanium dioxide, disodium edetate dihydrate.

Tablets, film-coated white, round, biconvex, with Valium on one side.

1 tab. atenolol 100 mg.

Excipients: microcrystalline cellulose, lactose monohydrate, povidone, corn starch, talc, colloidal silicon dioxide, croscarmellose sodium, magnesium stearate.

The composition of the shell: hypromellose 5 cP, hypromellose 15 cps, talc, titanium dioxide, disodium edetate dihydrate, carnauba wax.

Clinico-pharmacological group

Beta1-blocker.

Pharmacological action

Exerts antianginal, antihypertensive and antiarrhythmic action. Has no membrane stabilizing and intrinsic sympathomimetic activity. Reduces catecholamines stimulated cAMP formation from ATP.

In the first 24 hours after oral administration against decrease in cardiac output observed reactive increase in the total peripheral vascular resistance, the severity of which is within 1-3 days, gradually decreases.

Hypotensive effect is associated with a decrease in cardiac output, decreased activity of the renin-angiotensin system, baroreceptor sensitivity and the influence on the CNS. Hypotensive effect is manifested as a reduction in systolic and diastolic blood pressure, stroke and minute volumes. In the medium therapeutic doses has no effect on the tone of peripheral arteries. Hypotensive effect lasts 24 hours, with regular use will stabilize by the end of the second week of treatment.

Antianginal effect of the decrease in myocardial oxygen demand by decreasing heart rate (lengthening of diastole, and improved myocardial perfusion) and contractility, as well as reduced sensitivity of myocardium to the effects of sympathetic stimulation. Slowed heart rate at rest and during exercise. By increasing end-diastolic pressure in the left ventricle and increase the tension of ventricular muscle fibers can increase oxygen demand, especially in patients with chronic heart failure.

Antiarrhythmic effect is manifested in the suppression of sinus tachycardia and associated with the elimination of arrhythmogenic sympathetic effects on the conducting system of the heart, decreasing the velocity of propagation of excitation through the sinoatrial node, and lengthening the refractory period. Inhibits impulse conduction in the antegrade and to a lesser extent - in a retrograde direction through the AV-node and for additional ways of carrying out.

Negative chronotropic effect manifested by 1 h after administration, reaches a maximum after 2-4 hours, lasts up to 24 hours

Reduces the automaticity of sinus node, slowed heart rate, slows AV-conduction, reduces myocardial contractility, reduces myocardial oxygen demand. Reduces the excitability of the myocardium.

When used in the medium therapeutic doses has a less pronounced effect on smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers.

Pharmacokinetics

Absorption from the gastrointestinal tract is fast, part time (50-60%). Bioavailability - 40-50%. Time to achieve Cmax in blood plasma - 2-4 pm poorly crosses the blood-brain barrier, takes place in small amounts through the placenta and into breast milk. Relationship to plasma proteins - 6-16%.

Practically not metabolized in pecheni.T1 / 2 - 6-9 hours (increases in the elderly). Excreted by the kidneys by glomerular filtration rate (85-100% - unchanged).

Renal failure is accompanied by a lengthening of T1 / 2 and cumulation: with CC below 35 ml/min/1.73 m2 T1 / 2 of 16-27 h, with CC below 15 ml/min/1.73 m2 - more than 27 hours (you need to decrease dose). Displayed during hemodialysis.

Indications for use of the drug
hypertension;
prevention of angina (excluding Prinzmetal angina);
cardiac rhythm: sinus tachycardia, supraventricular tachyarrhythmia prevention, ventricular premature beats;
Acute myocardial infarction with stable hemodynamic parameters.

Dosing regimen

Inside.

Assign inside before eating, not chewing, drinking a small amount of liquid.

Hypertension: Treatment is initiated with 50 mg of atenolol Belupo 1 time / To achieve a stable hypotensive effect requires 1-2 weeks of reception. In case of insufficient expression of the hypotensive effect of the dose was increased to 100 mg in one sitting. Further increase in dose is not recommended because it is not accompanied by increased clinical effect.

Angina: an initial dose of 50 mg / If within a week is not reached optimal therapeutic effect, increasing the dose to 100 mg /

In the presence of renal insufficiency recommend dose adjustment based on creatinine clearance (CC). In patients with renal insufficiency at values above 35 QC ml/min/1.73m2 (normal values are 100-150 ml/min/1.73 m 2) a significant accumulation of atenolol Belupo happens.

Patients on hemodialysis, Atenolol Belupo appoint 50 mg immediately after each dialysis session, which should be carried out in stationary conditions, as may occur BP reduction.

For elderly patients the initial single dose - 25 mg (can be increased under the control of blood pressure, heart rate).

Acute myocardial infarction with stable hemodynamic parameters - 100 mg 1 time or 50 mg of 2 for 6-9 days or until discharge from hospital (under the control of blood pressure, ECG, blood glucose levels). Increasing daily doses above 100 mg are not recommended as a therapeutic effect is not amplified, and the likelihood of side effects increases.

Side effect
With the cardiovascular system: development (worsening) of symptoms of chronic heart failure (swelling of ankles, feet, shortness of breath), the violation of atrioventricular conduction, arrhythmia, bradycardia, marked reduction in blood pressure, orthostatic hypotension, tachycardia, conduction disturbances infarction, myocardial relaxation, the manifestations angiospasm (poholodenie lower extremities, Raynaud's syndrome), vasculitis, chest pain.
CNS and peripheral nervous system: dizziness, decreased ability to concentrate, decreased the reaction rate, drowsiness or insomnia, depression, hallucinations, fatigue, headache, weakness, nightmares, anxiety, confusion, or short-term memory loss, paresthesia in extremities (patients with "intermittent" claudication and Raynaud's syndrome), muscle weakness, muscle cramps.
From the digestive system: dry mouth, nausea, vomiting, diarrhea, abdominal pain, constipation, change in taste.
With the respiratory system: dyspnea, bronchospasm, apnea, nasal congestion.

Hematologic response: platelet purpura, anemia (aplastic), thrombosis.
From the Endocrine: gynecomastia, reduced potency, decreased libido, hyperglycemia (in patients with insulin-dependent diabetes), hypoglycemia (in patients treated with insulin), hypothyroid state.

Metabolic reactions: hyperlipidemia.

Skin reactions: rash, dermatitis, itching, photosensitivity, increased potootde leniya, skin hyperemia, exacerbation of psoriasis, reversible alopecia.

Senses: visual disturbances, reduced secretion of tear fluid, dryness and soreness of the eyes, conjunctivitis.

Effect on the fetus: fetal growth retardation, hypoglycemia, bradycardia.
From the laboratory parameters: agranulocytosis, leukopenia, elevated liver enzymes, hyperbilirubinemia, thrombocytopenia (unusual bleeding and hemorrhage).

Other: back pain, arthralgia, withdrawal syndrome (increased angina, increased blood pressure).

The frequency of side effects increases with dose

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