Atenolol
Active material: Atenolol
When ATH: C07AB03
CCF: Beta1-adrenoblokator
ICD-10 codes (testimony): I10, i20, I21, I47.1, I49.4
When CSF: 01.01.01.02
Manufacturer: M.J.BIOPHARM Pvt.Ltd. (India)
PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING
| Pills | 1 tab. |
| atenolol | 100 mg |
Excipients: corn starch (dry), methylparaben, propyl, magnesium stearate, sodium starch glycolate, colloidal silicon dioxide, water.
10 PC. – packings Valium planimetric (3) – packs cardboard.
14 PC. – packings Valium planimetric (2) – packs cardboard.
Pharmacological action
Cardioselective beta1-blocker without intrinsic sympathomimetic activity. Provides antihypertensive, antianginalnoe, and antiaritmicescoe action.
Reduces the stimulating effect on the heart of the sympathetic innervation and circulating Catecholamines in the blood. Has negative Chrono, dromo-, ʙatmo- and inotropic action: reduces heart rate, oppressing conductivity and anxiety, reduces myocardial contractility. ROUND at the beginning of the use of beta blockers (first 24 hours after oral administration) increases (as a result of reciprocal increase in the activity of α-adrenergic stimulation and removal of β2-adrenoreceptorov), through 1-3 day returns to the original, but with long-term use reduces.
The hypotensive effect is associated with a decrease in cardiac output, decreased activity of the renin-angiotensin system (It is more important for patients with initial hypersecretion of renin), baroreceptor sensitivity of the aortic arch (not going to enhance their activity in response to the decline of HELL) and the influence of the central nervous system; shown a decrease in both systolic, and diastolic blood pressure, a decrease in stroke volume and cardiac output. The average therapeutic doses has no effect on the tone of the peripheral arteries.
Antianginalny effect is determined by the reduction in myocardial oxygen demand as a result of a decrease in HEART RATE (the lengthening of the diastolic pressure and myocardial perfusion improvement) and contractility, as well as the decrease in myocardial sensitivity to the effects of the sympathetic innervation. Decrease in heart rate occurs at rest and during exercise. At the expense of increasing end-diastolic pressure in the left ventricle and increased tensile ventricular muscle fibers can increase oxygen demand, especially in patients with chronic heart failure.
The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP, hypertension), decrease speed of spontaneous excitation of the sine and jektopicheskogo pacemakers and slowing AV conduction. Inhibition of pulses observed mainly in the antegrade and to a lesser extent in the retrograde direction through the AV node and an additional paths.
In contrast, nonselective beta-adrenoblokatorov, when used in therapeutic doses medium has a less pronounced effect on organs, содержащие b2-adrenoreceptory (pancreas, skeletal muscle, smooth muscle peripheral arteries, bronchial and uterine), and carbohydrate metabolism; the severity of atherogenic actions no different from the actions of propranolol. To a lesser degree the negative BATM expressed, hrono-, ino- and dromotropic action. When used in high doses (more 100 mg / day) It causes blockade of both subtypes of β-adrenoceptor.
The hypotensive effect lasts 24 no, when taken regularly will stabilize by the end of 2 week of treatment. The negative chronotropic effect is manifested through 1 h after administration, It reaches a maximum 2-4 hours and continues until 24 no.
Pharmacokinetics
After ingestion of absorption from the gastrointestinal tract 50-60%, bioavailability – 40-50%.. Practically not metabolized in the body. Poor penetrate the BBB. Plasma protein binding – 6-16%.
T1/2 is 6-9 no. Write mainly kidneys unchanged. Renal dysfunction accompanied by mainly increase in T1/2 and cumulation: at least QC 35 ml/min T1/2 is 16-27 no, at least QC 15 ml / min – more 27 no, if extended to anuria 144 no. Displayed during hemodialysis.
Elderly patients T1/2 increases.
Testimony
Arterial hypertension, hypertensive crisis, mitral valve prolapse, hyperkinetic cardiac syndrome functional genesis, cardiopsychoneurosis of hypertensive type.
Treatment: CHD, angina (voltage, peace and unstable).
Treatment and prevention: myocardial infarction (acute phase under stable hemodynamic, secondary prevention).
Arrhythmias (incl. general anesthesia, congenital long QT syndrome, myocardial infarction without signs of congestive heart failure, thyrotoxicosis), sinus tachycardia, paroksizmalynaya predserdnaya tachycardia, supraventricular and ventricular premature beats, supraventricular and ventricular tachycardia, atrial tachyarrhythmia, auricular flutter.
The essential and senile tremor, agitation and tremors with withdrawal syndrome.
In the combined therapy: gipertroficheskaya obturatsionnaya cardiomyopathy, pheochromocytoma (only with alpha-blockers), thyrotoxicosis; migraine (prevention).
Dosage regimen
Establish individually. The usual dose for adults – inside, at the beginning of treatment is 25-50 mg 1 time / day. gradually increase the dose if necessary. If the kidney function in patients with CC 15-35 ml / min – by 50 mg / day; at least QC 15 ml / min – by 50 mg a day.
The maximum dose: adult ingestion – 200 mg / day 1 or 2 admission.
Side effect
Cardio-vascular system: in some cases – bradycardia, hypotension, violations AV conduction, symptoms of heart failure.
From the digestive system: at the beginning of therapy, nausea, constipation, diarrhea, dry mouth.
From the central and peripheral nervous system: at the beginning of therapy may be tired, dizziness, depression, mild headache, sleep disorders, feeling cold and paresthesias in the extremities, reduction in the reaction capacity of the patient, reduced secretion of tear fluid, conjunctivitis.
On the part of the endocrine system: reduced potency, gipoglikemicakie State in patients with diabetes mellitus.
The respiratory system: in predisposed patients – the appearance of symptoms of bronchial obstruction.
Allergic reactions: itching.
Other: increased sweating, erythema.
Contraindications
AV-blockade II and III degrees, sinoatrialynaya blockade, SSS, bradycardia, (HR less 40 u. / min), hypotension (in the case of myocardial infarction, systolic blood pressure less than 100 mmHg.), cardiogenic shock, chronic heart failure stage IIB-III, acute heart failure, Prinzmetal angina, lactation, simultaneous MAO inhibitors, Hypersensitivity to atenolol.
Pregnancy and lactation
Atenolol crosses the placental barrier, therefore use during pregnancy is possible only in the case, if the expected benefit to the mother outweighs the potential risk to the fetus.
Atenolol is excreted in breast milk, so it is recommended to stop breast-feeding if necessary, use during lactation.
Cautions
C Caution should be used for patients with diabetes, chronic obstructive pulmonary disease (incl. bronchial asthma, emphysema), metabolic acidosis, gipoglikemii; allergic reactions in the anamnesis, chronic heart failure (compensated), occlusive peripheral arterial disease (intermittent claudication, Raynaud's syndrome), pheochromocytoma, hepatic insufficiency, chronic renal failure, myasthenia, thyrotoxicosis, depression (incl. history), psoriaze, Pregnancy, in elderly patients, in pediatrics (efficacy and safety have not been determined).
In the application of atenolol possible to reduce the production of tear fluid, that has implications for patients, using contact lenses.
Atenolol cancellation after a prolonged course of treatment should be carried out gradually under medical supervision.
Upon termination of the combined use of atenolol and clonidine clonidine treatment was continued for a few days after discontinuation of atenolol, otherwise it may cause severe arterial hypertension.
When the need for inhalational anesthesia in patients, receiving atenolol, a few days before the anesthesia should stop taking atenolol or pick up an agent for anesthesia with minimal negative inotropic effects.
Effects on ability to drive vehicles and management mechanisms
Patients, activities which require high concentration of attention, the question of the application of outpatient atenolol should be addressed only after the evaluation of the individual response.
Drug Interactions
With the simultaneous use of diuretics enhanced antihypertensive activity.
With simultaneous use of funds for inhalation anesthesia increases the risk of increasing cardiodepressive action and the development of arterial hypotension.
There are about development messages bradycardia and hypotension during concomitant use alcuronium chloride.
With simultaneous use of verapamil amplified negative inotropic effect, develops bradycardia, ʙradiaritmija, expressed conduction disorders; describes cases postural hypotension, dizziness, left ventricular failure, letargia. Under the influence of verapamil pharmacokinetic parameters of atenolol did not change significantly, although the case has been described atenolol increase AUC.
When applied simultaneously increases disopyramide Css, decreased clearance of disopyramide, possible violation of conductivity.
With simultaneous use of dipyridamole, a case of bradycardia and asystole then (during ECG test with dipyridamole patient, receiving atenolol).
With simultaneous application of indomethacin, Naproxen and other NSAIDs may reduce the antihypertensive effect of atenolol, which to some extent it is due to violation of (under the influence of NSAIDs) synthesis in the kidney and released into the bloodstream of prostaglandin PGA and PGE, which have a strong vasodilator effect on peripheral arterioles.
With simultaneous application of insulin may increase blood pressure.
With simultaneous application of clonidine is possible additive antihypertensive effect, sedation, dry mouth.
With simultaneous application of caffeine may decrease the effectiveness of atenolol.
With simultaneous application of nizatidine, a case cardiodepressive amplification steps.
With simultaneous application of nifedipine described cases of severe arterial hypotension and heart failure, that may be due to increased inhibitory effect of nifedipine on the myocardium.
With simultaneous use of orlistat reduced antihypertensive action of atenolol, that can lead to a significant improvement in HELL, development gipertoniceski kriza.
With simultaneous application prenylamine may increase QT interval.
With simultaneous use of chlorthalidone enhanced antihypertensive activity.
