Pharmacokinetics of the active metabolite of the prodrug repirinast in healthy Caucasian volunteers after a single oral dose. The pharmacokinetics of BAY w 8199, the active metabolite of the prodrug repirinast (BAY u 2372), has been investigated after oral administration of 150, 300 and 450 mg repirinast to twelve healthy male Caucasians. Plasma BAY w 8199 concentrations were very variable
The effect of repirinast on airway responsiveness to methacholine and allergen. Repirinast, a novel ingested antiallergic asthma medication from Japan, was compared versus placebo on airway responsiveness to methacholine and was compared versus placebo and cromolyn on airway responses to allergen. In 14 patients with mild, stable, atopic asthma, we performed a double-blind, double-dummy, random -order trial with ingested repirinast 300 mg twice daily for 7 days, inhaled cromolyn 40 mg spincaps single dose, and double placebo on allergen-induced early (EAR) and late (LAR) asthmatic responses and increased airway responsiveness. In the 14 subjects, no difference occurred in methacholine PC20 after 6 days of repirinast or 6 days of placebo. In the 13 subjects who completed the allergen study
Mechanism of action of MY-1250, an active metabolite of Repirinast, in inhibiting histamine release from rat mast cells. 1. When MY-1250 (3.6 x 10(-5) M) was added to mast cells, it caused a rapid increase in adenosine 3':5'-cyclic monophosphate (cyclic AMP) and decrease in adenosine 5'-triphosphate (ATP), both of which recovered to their original levels within 2 min. The accumulation of cyclic
Lack of effect of repirinast on the pharmacokinetics of theophylline in asthmatic patients. A possible pharmacokinetic interaction between theophylline and repirinast has been investigated in asthmatic patients. The kinetics of theophylline was studied in seven adult in-patients given theophylline 400-800 mg b.d. alone and after three weeks of co-administration of repirinast. There was no effect
Effect of food on the pharmacokinetics of the active metabolite of the prodrug repirinast. The effect of food on the pharmacokinetics of the active metabolite of the new antiasthmatic drug repirinast was investigated in two different studies after oral administration of 300 mg of repirinast. In each study, 12 healthy volunteers received the repirinast dose under fasting or fed conditions in a crossover manner. In one study, a high-fat meal (American breakfast) was used and in another study, a low-fat, high-carbohydrate meal (continental breakfast) was used. Concentrations of the active metabolite in plasma and urine were determined by reversed-phase high-performance liquid chromatography with UV detection. After administration of repirinast with a low-fat and a high-fat meal, the relative