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Modulation of antagonist binding to histamine H1-receptors by sodium ions and by 2-amino-2-hydroxymethyl-propan-1,3-diol HCl.
Br J Pharmacol
April 1994
Department of Pharmacology, University of Cambridge.
1. NaCl (100 mM) reduced the potency of (+)-N-methyl-4-methyldiphenhydramine ((+)-QMDP) as an inhibitor of the binding of [3H]-mepyramine to histamine H1-receptors on guinea-pig cerebellar membranes to a greater extent than that of mepyramine, consistent with the greater inhibitory effect of Na+ on the binding of [3H]-QMDP than on the binding of [3H]-mepyramine. 2.
View Article and Find Full Text PDFPharmacokinetic interactions between theophylline and other medication (Part I).
Clin Pharmacokinet
January 1991
Department of Pharmacy, University of California, San Francisco.
Many drugs have been found to increase or decrease the clearance of theophylline, probably by interaction with one or more of the variants of the cytochrome P450 drug-metabolising system. Theophylline may be particularly susceptible to alteration of its clearance because of the particular form(s) of the P450 system involved, because its metabolism is saturable, and/or because 90% of its elimination is via metabolism. Its clearance has been found to be decreased (typically by around 25%, but often by far more) by erythromycin, troleandomycin (triacetyloleandomycin), roxithromycin, enoxacin, ciprofloxacin, pefloxacin, norfloxacin, ofloxacin, fluoroquinolone T-3262, pipemidic acid, cimetidine, etintidine, propranolol, verapamil, diltiazem, nifedipine, furosemide (frusemide), at least some anovulent agents, viloxazine, allopurinol, ticlopidine, idrocilamide, thiabendazole, disulfiram, influenza- and BCG-vaccination, interferon, and caffeine (half-life increase).
View Article and Find Full Text PDFThe interaction of temelastine with cytochrome P450 mixed-function oxidase enzymes in vivo and in vitro.
Biochem Pharmacol
January 1989
Smith Kline & French Research Limited, The Frythe, Welwyn Garden City, Herts, U.K.
Digitonin-solubilized histamine H1-receptors bind to polyethylenimine-treated glass-fibre filters.
J Pharm Pharmacol
October 1988
Department of Pharmacology, University of Cambridge, UK.
The binding of [3H]mepyramine to histamine H1-receptors solublized from guinea-pig cerebellum by 1% digitonin could be assayed by adsorption of the receptor-bound [3H]ligand to glass-fibre filters pretreated with 0.3% polyethylenimine (PEI). Non-specific binding was higher than in parallel experiments in which the bound and free [3H]ligand was separated by gel-filtration on Sephadex G-25 columns, but the parameters characterizing the inhibition curves were otherwise similar.
View Article and Find Full Text PDFTemelastine does not affect theophylline pharmacokinetics in normal subjects.
Br J Clin Pharmacol
November 1987
Department of Clinical Pharmacology, Princess Alexandria Hospital, Brisbane, Queensland, Australia.
The pharmacokinetics of theophylline (i.v. aminophylline 250 mg) were studied in a balanced, double-blind crossover following the administration of oral temelastine (100 mg) or placebo, twice daily for 7 days, to 10 normal volunteers.
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