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EFFECTS OF A SALT OF CHOLESTYRAMINE AND 2‐[4‐( p ‐CHLOROBENZOYL)PHENOXY]2‐METHYL PROPIONIC ACID (α‐1081) ON BILIARY LIPID SECRETION IN RATS
Author(s) -
ALDINI RITA,
BARBARA LUIGI,
BENELLI AUGUSTA,
BORZATTA VALERIO,
GEMINIANI STEFANIA,
MASCELLANI GIUSEPPE,
MORSELLI ANTONIO,
RODA ALDO,
RODA ENRICO
Publication year - 1981
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1981.tb10471.x
Subject(s) - cholestyramine , medicine , enterohepatic circulation , endocrinology , bile acid , cholesterol , chemistry , secretion , biology
1 Hypolipidaemic agents may increase biliary cholesterol in man, inducing a supersaturated bile. 2 To evaluate this possible side‐effect, we have studied bile lipid secretion over a period of 8 h with intact enterohepatic circulation and 4 h with complete interruption in rats treated for two months with a salt of cholestyramine and 2‐[4‐( p ‐chlorobenzoyl)‐phenoxy]2‐methyl propionic acid (α‐1081, 1.150 g/kg body wt., daily), cholestyramine (1.125 g/kgbody wt. daily), procetofenic acid (25 mg/kg body wt. daily) and saline respectively (six rats for each group). 3 Cholesterol saturation index significantly (P< 0.005) increased (from 0.21 ±0.01 to 0.39±0.09, mean±s.d.), in rats fed with procetofenic acid but it did not in α‐1081‐ and cholestyramine‐treated animals. 4 Procetofenic acid and, to a lesser extent, cholestyramine increased the bile flow. Procetofenic acid increased cholesterol secretion from 0.45±0.17 to 0.94 ± 0.19 μmol kg −1 body wt. h −1 (mean±s.d.). 5 Cholestyramine increased both serum cholesterol and bile acid secretion from 0.45±0.17 to 0.68±0.10 and 25.8±9.48 to 39.96 ± 6.68 μol kg −1 body wt. h −1 respectively; α‐1081, on the contrary, had no effect on bile lipid secretion. 6 These data suggest that α‐1081 may be used as a new hypolipidaemic drug without any risk of increasing cholesterol in bile.