[Acebutolol and diacetolol: their binding to plasma proteins and erythrocytes and secretion with the saliva]. / Atsebutolol i diatsetolol: sviaz' s belkami plazmy i éritrotsitami, sekretsiia so sliunoi.

Thirty-two patients with hypertensive disease were treated with a cardioselective blocker of beta-adrenergic receptors acebutolol ("Sectral-400", Rhone Poulenc, France). The binding of the drug and its metabolites diacetolol to plasma proteins and erythrocytes and their excretion with the saliva were studied. The significant binding of acebutolol and diacetolol to erythrocytes was shown. The ratio of the content of the free form of these substances in erythrocytes to plasma content was on the average 1.54 +/- 0.96 for diacetolol and 1.93 +/- 1.01 for acebutolol. A good correlation of acebutolol and diacetolol contents in the saliva with their contents in plasma was found. The mean values of the protein-bound fraction were for acebutolol 0.133 +/- 0.038 and for diacetolol 0.106 +/- 0.050.

[Propranolol binding with plasma proteins and erythrocytes]. / Sviaz' propranolola s belkami plazmy i eritrotsitami.

The binding of propranolol with plasma proteins and erythrocytes after oral administration of 80 mg of anapriline was studied in 12 patients with hypertensive disease. The content of propranolol fraction bound to plasma proteins was on the average 0.84 +/- 0.4. It was shown that propranolol to a considerable degree is captured by erythrocytes. The ratios of the erythrocyte content of propranolol free form to the plasma content were on the average 3.72 +/- 0.92 and 2.70 +/- 1.20, respectively, 2 and 4 hours after anapriline intake. During the assessment of the pharmacological parameters it is recommended to determine the contents of the total and free forms of propranolol in the whole blood rather than in plasma.