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The cytochrome P450s responsible for the regio- and stereoselectivity in the 2- and 3-hydroxylation of the chiral non-steroidal antiinflammatory drug ibuprofen were characterized in human liver microsomes. The rates of formation of both the 2- and 3-hydroxy metabolites exhibited monophasic (N = 2; N is the number of microsomal preparations) and biphasic (N(More)
Organic farming is one of the fastest growing segments of U.S. agriculture. As consumer interest continues to gather momentum, many U.S. producers, manufacturers, distributors, and retailers are specializing in growing, processing, and marketing an ever-widening array of organic agricultural and food products. This report summarizes growth patterns in the(More)
The metabolic fate of azimilide in man is unusual as it undergoes a cleavage in vivo resulting in the formation of two classes of structurally distinct metabolites. During a metabolite profiling study conducted in human volunteers to assess the contribution of all pathways to the clearance of (14)C-azimilide, greater than 82% of radioactivity was recovered(More)
Bupivacaine protein binding was studied with the use of human serum, isolated human serum albumin, and isolated alpha 1-acid glycoprotein. The effect of lactic acid on bupivacaine binding was also studied. Bupivacaine protein binding in serum is best characterized by a model described by two classes of binding sites and that in alpha 1-acid glycoprotein or(More)
BACKGROUND AND OBJECTIVES Lenvatinib is an oral, multitargeted tyrosine kinase inhibitor under clinical investigation in solid tumours. This study evaluated the influence of P-glycoprotein (P-gp) inhibition (single-dose rifampicin) and simultaneous cytochrome P450 3A4 (CYP3A4)/P-gp induction (multiple-dose rifampicin) on lenvatinib pharmacokinetics. (More)
Eight pediatric accidental overdoses of diphenoxylate-atropine (Lomotil) are reported, and 28 literature cases are reviewed. This overdose is primarily an opioid intoxication, occasionally associated with atropine toxicity. Only 6 of 36 children showed signs of atropine overdose (central nervous system excitement, hypertension, fever, flushed dry skin).(More)
Most community-referred, ambulatory chronic alcoholics can be detoxified quickly and safety without the use of psychoactive drugs, according to our data. We believe such detoxification can be done most efficiently in a social setting, with the aid of a staff who will provide reassurance and reality orientation and who will monitor the patients' vital signs,(More)
The biopharmaceutic criteria of Duolip and its active principle, 1-(theophyllin-7-yl)-ethyl-2-[2-(p-chlorophenoxy)-2-methylpropionate] (etofylline clofibrate, ML 1024), are described. ML 1024 was found to be practically insoluble in water at pH values ranging from 2 to 7.4 and in human serum. A very low dissolution rate of the drug from the capsule(More)
Lenvatinib is an orally available multi-targeted tyrosine kinase inhibitor with anti-angiogenic and antitumor activity. To get more insight into the disposition of lenvatinib, a mass balance study was performed in patients with advanced solid tumors. A single oral 24 mg (100 μCi) dose of (14)C-lenvatinib was administered to six patients, followed by(More)
Background: Lenvatinib is an oral, multitargeted, tyrosine kinase inhibitor under clinical investigation in solid tumors. In vitro evidence indicates that lenvatinib metabolism may be modulated by ketoconazole, an inhibitor of CYP3A4 and p‐glycoprotein. (18–55 years; N ¼ 18) were randomized to one of two sequences (ketoconazole ! placebo or vice versa).(More)