PT  - JOURNAL ARTICLE
AU  - F M Belpaire
AU  - B Chindavijak
AU  - M G Bogaert
TI  - SKF 525A displaces drugs from serum alpha 1-acid glycoprotein binding sites.
DP  - 1987 Feb 01
TA  - Journal of Pharmacology and Experimental Therapeutics
PG  - 628--630
VI  - 240
IP  - 2
4099  - http://jpet.aspetjournals.org/content/240/2/628.short
4100  - http://jpet.aspetjournals.org/content/240/2/628.full
SO  - J Pharmacol Exp Ther1987 Feb 01; 240
AB  - In vivo treatment of rats with beta-diethylaminoethyl-diphenylpropylacetate hydrochloride (SKF 525A), an inhibitor of hepatic monooxygenases, decreases the serum binding of oxprenolol and propranolol, which bind mainly to alpha 1-acid glycoprotein, but not that of phenytoin, which is bound to albumin. The effect was maximal 40 min after treatment and had disappeared after 6 hr, when enzyme inhibition was still present. A displacing effect was also observed when SKF 525A was added in vitro to serum of rats, dogs and humans and to human alpha 1-acid glycoprotein, whereas binding to human serum albumin was not affected. SKF 525A was found to be equipotent with tris(2-butoxyethyl)phosphate, a known displacer of binding of drugs from alpha 1-acid glycoprotein. When studying the pharmacokinetics or the effects of drugs after SKF 525A pretreatment, the possibility that altered protein binding may influence the findings should be considered.