Atenolol
When ATH:
C07AB03
Characteristic.
Crystalline powder. Soluble in water (26,5 mg / mL - temperature 37 °C), good - 1M hydrochloric acid (300 mg / mL - temperature 25 °C) and bad - chloroform (3 mg / mL - temperature 25 °C).
Pharmacological action.
Gipotenzivnoe, antianginalnoe, antiarrhythmic.
Application.
Arterial hypertension, angina, acute myocardial infarction (with stable hemodynamic), tachycardia: sinus, predserdnaya, Ventricular, paroxysmal and others., arrythmia, atrial flutter and atrial fibrillation, hyperkinetic cardiac syndrome, mitral valve prolapse, cardiopsychoneurosis of hypertensive type; complex therapy of hypertrophic cardiomyopathy, pheochromocytoma, thyrotoxicosis, essential tremor; migraine (prevention).
Contraindications.
Hypersensitivity, sinusovaya bradycardia (HR less 50 u. / min), sinoatrialynaya blockade, sick sinus syndrome, AV block II-III degrees, hypotension (Sad less than 90 mm Hg. Art.), acute or chronic heart failure decompensation, cardiogenic shock, the peripheral blood circulation, pregnancy, lactation.
Restrictions apply.
Diabetes, gipoglikemiâ, chronic obstructive pulmonary disease (эmfizema, bronchial asthma), liver dysfunction and / or kidney, myasthenia, depression, psoriasis, pheochromocytoma, metabolic acidosis, children's (efficacy and safety have not been determined) and old age.
Pregnancy and breast-feeding.
Category actions result in FDA - D. (There is evidence of the risk of adverse effects of drugs on the human fetus, obtained in research or practice, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk, if the drug is needed in life-threatening situations or severe disease, when safer agents should not be used or are ineffective.)
At the time of treatment should stop breastfeeding.
Side effects.
From the nervous system and sensory organs: fatigue, weakness, dizziness, headache, drowsiness or insomnia, nightmares, depression, anxiety, confusion or short-term memory loss, hallucinations, weakening of reactivity, paraesthesia, convulsions; blurred vision, reduced secretion of saliva and tear, conjunctivitis.
Cardio-vascular system and blood (hematopoiesis, hemostasis): bradycardia, heartbeat, conduction disturbances infarction, OF блокада, Arrhythmia, weakening of myocardial contractility, heart failure, gipotenziya, syncope, Raynaud's phenomenon, vasculitis, chest pain, thrombocytopenia, agranulocytosis.
From the digestive tract: dry mouth, nausea, vomiting, abdominal pain, diarrhea, constipation, abnormal liver function.
From the respiratory system: breathlessness, laringo- and bronchospasm.
Allergic reactions: itch, rash, эritema, hives, psoriasiform and dystrophic skin changes.
Other: obratimaya alopecia, hyperhidrosis, cold extremities, myasthenia, the weakening of the libido, impotence, Peyronie's disease, changes in the activity of enzymes, bilirubin, withdrawal, hypothyroid state, gipoglikemiâ.
Cooperation.
Antiarrhythmic and anesthetic agents enhance cardiodepressive action (increased risk of bradycardia, Arrhythmia, gipotenzii, Heart Failure). Reserpine, methyldopa, klonidin, guanfaцin, cardiac glycosides potentiate negative chrono, dromo- and the effect bathmotropic, insulin and other antidiabetic agents - hypoglycemia. NSAIDs, Estrogens, sympathomimetic, xanthines weaken hypotensive effect, absorption, increase - sympatholytics, nitroglycerin, hydralazine and other antihypertensive drugs, antacids - slow down the absorption. Cimetidine inhibits the metabolism. Prolongs the effect of muscle relaxants antidepolyarizuyuschih, anticoagulant effect of coumarins. Three / tetracyclic antidepressants, neuroleptics, sedativnыe, hypnotics and alcohol potentiate the CNS depression. Incompatible with MAO inhibitors.
Overdose.
Symptoms: bradycardia, AV block II-III degrees, heart failure, respiratory failure, gipotenziya, bronchospasm, gipoglikemiâ.
Treatment: gastric lavage and appointment of absorbent; simptomaticheskaya therapy: atropyn, Isoprenaline, orciprenaline, cardiac glycosides or glucagon, Diuretic, vasopressor agents (Dopamine, dobutamine or norepinephrine), selective beta-agonists, glucose (I /), installing artificial pacemaker. Perhaps dialysis.
Dosing and Administration.
Inside, before eating, liquid squeezed small amounts of liquid. The mode set individually. When hypertension - 25-50 mg once, optionally at 100-200 mg 1-2 times a day. In CHD, tachysystolic cardiac arrhythmias - 50 mg 1 once a day; if necessary, and good tolerance dose can be increased within weeks to 100-200 mg / day. In acute myocardial infarction with stable hemodynamic parameters - across 12 h - again 50 mg; then - 50 mg 2 once a day for 6-9 days (under the control of blood pressure, ECG, Glucose). When functional disorders of the cardiovascular system - 25 mg 1 once a day. If the kidney function depending on Cl creatinine: Cl at 15-35 ml / min - 50 mg / day (or 100 mg a day), less 15 ml / min - 50 mg every other day (or 100 mg 1 once every 4 day); patients, hemodialysis - 25-50 mg / day immediately after dialysis. In elderly patients, the initial single dose is 25 mg (It can be increased under the control of blood pressure, Heart Rate).
Precautions.
Treatment is carried out under regular medical supervision. Before starting therapy should be compensated heart failure. During treatment requires monitoring of heart rate, FROM, Blood Glucose (possible dose adjustment of antidiabetic drugs) and control over the appearance of the symptoms of heart failure.
Be wary of during the drivers of vehicles and people, skills relate to the high concentration of attention. At the time of treatment is recommended to eliminate the use of alcohol.
In patients with diabetes mellitus and hyperthyroidism may mask tachycardia, cause hypoglycemia or hyperthyroidism. When pheochromocytoma should be used simultaneously alpha adrenolytics. Perhaps the increased severity of hypersensitivity reactions and the lack of effect of conventional doses of epinephrine with aggravated allergic history.
In the case of elderly patients increasing bradycardia (less 50 u. / min), gipotenzii (Sad below 100 mmHg.), AV blockade, bronchospasm, ventricular arrhythmias, Serious liver and kidney, necessary to reduce the dose or stop treatment. Discontinue therapy should be gradual, reducing the dose, within 10-14 days. Patients with coronary artery disease should be in the period of withdrawal of the drug be monitored carefully. Atenolol should be abolished for 48 hours prior to surgery with general anesthesia (chloroform or ether) or select an anesthetic with the least negative inotropic effects.
Cooperation
Active substance | Description of interaction |
Acetylsalicylic acid | If concomitant use caution (possible adverse effects). |
Verapamil | FMR: synergism. Increases (mutually) the likelihood of violations of automaticity, conduction and myocardial contractility, It increases the risk of excessive hypotension and bradycardia, AV blockade (up to complete). When concomitant administration of caution. |
Glipizide | FMR: synergism. Against the background of enhanced effect of atenolol. |
Guanfaцin | FMR: synergism. Enhances negative chrono, dromo- and the effect bathmotropic, It increases the risk of excessive bradycardia. |
Diltiazem | FMR: synergism. Strengthens (mutually) cardiodepressivny effect; the combined appointment of caution. |
Insulin dvuhfaznыy [human genetic engineering] | FMR. Against the background of atenolol (Unlike non-selective beta-blockers) effect increases slightly; the patient should be warned, that the development of hypoglycemia tachycardia and tremor may be missing, Although hunger, irritability, nausea Reserved, and even increased sweating. |
Klonidin | FMR: synergism. Enhances negative chrono, dromo- and the effect bathmotropic. Against the background of atenolol may increase hyperthermia, occurs when a sudden cancellation of clonidine. |
Methyldopa | FMR: synergism. Enhances negative chrono, dromo- and the effect bathmotropic. |
Nitroglycerin | FMR: synergism. Increases hypotensive effect. |
Octreotide | FMR: synergism. It does effect and increases the likelihood of excessive bradycardia, aritmii, conduction disturbances. |
Procarbazine | FMR. Inhibits MAO unpredictable and can change effects; concomitant use is not recommended. |
Rifampicin | FKV. It induces biotransformation enzymes and accelerates the destruction of atenolol, normally excreted almost entirely unchanged. |
Selegiline | Inhibits MAO unpredictable and can change effects; concomitant use is not recommended. |