Arzneimittel Forsch
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Arzneimittel Forsch · Apr 1994
Absorption, distribution, metabolism and excretion of [14C]ebastine after a single administration in rats.
Absorption, distribution, metabolism and excretion of ebastine (4'-tert-butyl-4-[4-(diphenylmethoxy)piperidino]butyrophenone, LAS-90, CAS 90729-43-4), a novel antihistamine, were investigated with 14C-labeled compound in rats after a single oral or intravenous administration, in comparison with [14C]carebastine, an active metabolite of ebastine. After intravenous administration of [14C]ebastine at 2 mg/kg, the plasma level of radioactivity decreased biphasically with alpha-phase half-life (t1/2 alpha) of 1.6 h and beta-phase half-life (t1/2 beta) of 3.1 h. After administration of [14C]carebastine, a similar plasma level-time profile was observed with t1/2 alpha of 0.7 h and t1/2 beta of 2.1 h. ⋯ Similar results were observed after oral administration at 0.2, 2 and 20 mg/kg. Following administration of [14C]carebastine, the recovery of radioactivity in urine and feces were around 2% and 96% of the dose, respectively, irrespective of administration route. In the plasma 2 h after oral administration of [14C] ebastine, carebastine and the polar metabolite(s) were observed as major components, whereas ebastine was hardly detected.(ABSTRACT TRUNCATED AT 400 WORDS)
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Arzneimittel Forsch · Apr 1994
Randomized Controlled Trial Comparative Study Clinical TrialKetorolac versus diclofenac sodium in cancer pain.
In a randomized single-blind study carried out simultaneously in five Departments for Pain Therapy and Palliative Care, the analgesic efficacy and side effects of oral ketorolac (ketorolac tromethamine, Tora-Dol, CAS 74103-07-4) and diclofenac sodium were compared in a population of 100 advanced cancer patients suffering from somatic and/or visceral pain. The treatment was carried out in agreement with the first step of the WHO pharmacological strategy in cancer pain. ⋯ A greater number of keterolac patients could pass to the second WHO step later than diclofenac patients. As to the tolerability, both drugs turned out to be similar, except for "sleepiness", which was four times more frequent (p < 0.05) in the diclofenac group.