White powder. Melting point (146-148 ℃). Soluble in alcohol, slightly soluble in water, chloroform, Hardly soluble in ethyl ether, slightly smelly.
Atenolol ,also known as atenolol, Aten Yue Er, tamoxifen, downhill Ling blood pressure, Tenormin, blood pressure Ling, is a long-acting cardioselective β1-adrenergic blockers, without intrinsic sympathomimetic activity or membrane stability.The atenolol,s retardation for β1 adrenaline receptors is similar with metoprolol, propranolol and nadolol , which is 1/6 times for pindolol and timolol. But, it does not inhibit the effect of the isoproterenol bronchodilator.When administered in small doses, it does not like non-selective β-adrenergic blockers as aggravated hypoglycemia induced hypertensive crisis, peripheral circulatory impairment or patients with obstructive airways disease worsening airway function and so on. However, When administered in large doses, atenolol also can decrease asthma or chronic obstructive pulmonary disease, airway function. Atenolol, as a long-term treatment of hypertension, also were reported for affecting airway function. Thus, despite atenolol heart selection, chronic obstructive pulmonary disease patients can only use small doses, but also should be given a sufficient amount of β1-adrenergic receptor agonists.
Oral F is 46%~60%, Tmax about 2~4 h, Mainly unchanged since the urine excretion, T1/2 of 6~7 h. Hemodialysis can clear the goods. Rapidly absorbed from the gastrointestinal tract, but not exclusively.The rest of the body is excreted in the stool. Food can reduce the F, fasting and after meals AUC decreased by 20%. Distribution of the central nervous system is relatively few. The ratio of brain tissue to blood concentration was 0.1:1. Easy to achieve in the placenta and the maternal plasma concentrations of same. PPB is less than 5%, Vd is 50~75 L. Atenolol is not metabolized by the liver, most of the drug is excreted from the body in urine, renal insufficiency in patients with T1/2 was significantly prolonged. Patients with renal failure range of T1/2 was 10~28 h, or even up to 100 h. Results at 24 h after, the discharge from the urine of the drug can be reduced by 29%. The T1/2 of patients with hyperthyroidism was significantly shortened, 4.2h.
The above information is edited by the chemicalbook of Kui Ming.
β-blockers. Clinical application in the treatment of hypertension, angina and arrhythmia.
Cardioselective β -adrenergic blocker. Antihypertensive, antianginal, antiarrhythmic.
Selective b1 adrenergic receptor agonist, anti-hypertensive, anti-anginal, anti-arrhythmic
ChEBI: An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.