BINDING OF INDAPAMIDE TO SERUM-PROTEINS AND ERYTHROCYTES

被引：27

作者：

URIEN, S

RIANT, P

RENOUARD, A

COULOMB, B

ROCHER, I

TILLEMENT, JP

机构：

[1] INST RECH INT SERVIER, F-92202 NEUILLY, FRANCE

[2] INSERM, F-92202 NEUILLY, FRANCE

来源：

BIOCHEMICAL PHARMACOLOGY | 1988年 / 37卷 / 15期

关键词：

D O I：

10.1016/0006-2952(88)90282-1

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The binding of indapamide to isolated serum proteins and erythrocytes was studied in order to understand its blood distribution. In serum, indapamide was mainly bound to .alpha.1-acid glycoprotein with a high affinity (K = 73.4/mM), and to albumin and lipoproteins. Indapamide was bound to erythrocytes via a saturable process with a high affinity (K = 385/mM and N = 57 .mu.M for an hematocrit value of 0.48), and erythrocytes were the main binding component in blood (more than 80% of indapamide was associated to erythrocytes in blood). The binding to serum proteins affected indapamide distribution in blood, and .alpha.1-acid glycoprotein was shown to be the more effective protein in decreasing the amount of indapamide associated to erythrocytes.

引用

收藏

页码：2963 / 2966

页数：4

相关论文

共 13 条

[1] MULTIPLE BINDING OF BEPRIDIL IN HUMAN-BLOOD [J].

ALBENGRES, E ;

URIEN, S ;

POGNAT, JF ;

TILLEMENT, JP .

PHARMACOLOGY, 1984, 28 (03) :139-149

[2] EVALUATION OF INDAPAMIDE IN THE TREATMENT OF HYPERTENSION [J].

ANAVEKAR, SN ;

LUDBROOKE, A ;

LOUIS, WJ ;

DOYLE, AE .

JOURNAL OF CARDIOVASCULAR PHARMACOLOGY, 1979, 1 (04) :389-394

[3]

BEISENHE.G, 1966, ARCH INT PHARMACOD T, V161, P76

[4] PHARMACOKINETICS AND METABOLISM OF INDAPAMIDE - REVIEW [J].

CAMPBELL, DB ;

TAYLOR, AR ;

HOPKINS, YW ;

WILLIAMS, JRB .

CURRENT MEDICAL RESEARCH AND OPINION, 1977, 5 :13-24

[5] NONLINEAR RELATIONSHIP BETWEEN PLASMA AND RED BLOOD-CELL PHARMACOKINITICS OF CHLORTHALIDONE IN MAN [J].

FLEUREN, HLJ ;

VANROSSUM, JM .

JOURNAL OF PHARMACOKINETICS AND BIOPHARMACEUTICS, 1977, 5 (04) :359-375

[6] MULTIPLE HUMAN-SERUM BINDING OF 2 THIENOPYRIDINIC DERIVATIVES, TICLOPIDINE AND PCR 2362, AND THEIR DISTRIBUTION BETWEEN HSA, ALPHA-1-ACID GLYCOPROTEIN AND LIPOPROTEINS [J].

GLASSON, S ;

ZINI, R ;

TILLEMENT, JP .

BIOCHEMICAL PHARMACOLOGY, 1982, 31 (05) :831-835

[7] CHARACTERIZATION OF A COMMON BINDING-SITE FOR BASIC DRUGS ON HUMAN ALPHA-1-ACID GLYCOPROTEIN (OROSOMUCOID) [J].

MULLER, WE ;

STILLBAUER, AE .

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1983, 322 (02) :170-173

[8] THE PLASMA-PROTEIN BINDING OF BASIC DRUGS [J].

ROUTLEDGE, PA .

BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1986, 22 (05) :499-506

[9] DISTRIBUTION OF SODIUM VALPROATE IN NORMAL WHOLE-BLOOD AND IN BLOOD FROM PATIENTS WITH RENAL OR HEPATIC-DISEASE [J].

SHIRKEY, RJ ;

JELLETT, LB ;

KAPPATOS, DC ;

MALING, TJB ;

MACDONALD, A .

EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY, 1985, 28 (04) :447-452

[10]

TILLEMENT JP, 1984, ADV DRUG RES, V13, P60