RESUMO
The article reviews the data on the binding of drugs to erythrocytes. Various mechanisms of the uptake of drugs by the erythrocytes and the role of the red blood cells as carriers of the drugs to the target organs are discussed. Significant correlation of the clinical and pharmacological effect of many drugs with their content in the erythrocytes is shown. Determination of the pharmacological parameters from the content of the drugs in the erythrocytes or whole blood rather than in the plasma is recommended.
Assuntos
Eritrócitos/metabolismo , Preparações Farmacêuticas/metabolismo , Animais , Transporte Biológico Ativo , Proteínas Sanguíneas/metabolismo , Membrana Eritrocítica/metabolismo , Humanos , Plasma/metabolismoRESUMO
In 14 patients with myocardial infarction the degree of verapamil binding with blood erythrocytes after a single oral administration (80 mg/kg) and the dependence pharmacological effect, the minute heart output (+ % MOC), on verapamil content in plasma and erythrocytes were studied. Intraindividual variability of verapamil distribution coefficients between erythrocytes and plasma (RBC/Ptot) is 9.7 +/- 2,3%, and it differs reliably from values of inter-individual variability of this index (33.7 +/- 3.3%).
Assuntos
Débito Cardíaco/efeitos dos fármacos , Eritrócitos/metabolismo , Infarto do Miocárdio/tratamento farmacológico , Verapamil/sangue , Adulto , Cromatografia Líquida de Alta Pressão , Eritrócitos/química , Eritrócitos/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade , Infarto do Miocárdio/sangue , Infarto do Miocárdio/fisiopatologia , Plasma/química , Plasma/efeitos dos fármacos , Plasma/metabolismo , Fatores de Tempo , Verapamil/farmacologiaRESUMO
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.
Assuntos
Acebutolol/análogos & derivados , Acebutolol/sangue , Proteínas Sanguíneas/efeitos dos fármacos , Eritrócitos/efeitos dos fármacos , Saliva/efeitos dos fármacos , Acebutolol/análise , Acebutolol/uso terapêutico , Adulto , Proteínas Sanguíneas/química , Proteínas Sanguíneas/metabolismo , Cromatografia Líquida de Alta Pressão , Eritrócitos/química , Eritrócitos/metabolismo , Humanos , Hipertensão/sangue , Hipertensão/tratamento farmacológico , Pessoa de Meia-Idade , Ligação Proteica/efeitos dos fármacos , Saliva/química , Saliva/metabolismo , Fatores de TempoRESUMO
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.