Emepronium

Abstract: A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.

Abstract: After oral administration of14C-labelled emepronium (150 mg) to two subjects, 1.8 and 3.9% of the radioactivity were recovered from the urine within 24 h, of which 50 and 56% respectively, were excreted during the first 6 h. 23 to 35% of the radioactivity in the urine consisted of emepronium metabolites. 25 mg of the cold compound was injected i.m. in 4 subjects; about 31% was excreted in the urine and about 45% in the faeces within 3 days, probably indicating extensive biliary excretion of unaltered drug. The half-life of emepronium in serum ranged from 1.5 to 2.25 h. The near point of accommodation, salivation and heart rate were compared with the serum concentration of emepronium in a randomized cross-over study in 4 subjects. The heart rate was increased significantly at serum concentrations of about 450 ng/ml, and the secretion of saliva was markedly decreased at about 250 ng/ml. The near point was affected only at the highest serum concentrations.

Abstract: In a randomised, double-blind study, 20 women with idiopathic detrusor instability and associated symptoms were treated with terodiline 25 mg bd, placebo, and emepronium bromide 200 mg tds--each drug being given for 3 weeks with placebo as wash-out period before cross-over. The results were evaluated according to drug preference, frequency charts and elimination of detrusor instability on cystometry. Serum levels of both drugs were monitored as control of tablet intake. The preference for terodiline to placebo was statistically significant: 14/3 women (P less than 0.05), and the majority of women (12/4) preferred terodiline to emepronium. Terodiline also gave a small but significant reduction in 24 h micturition frequency and eliminated detrusor instability in almost 50% of the patients (P less than 0.05). Side effects were frequent but mild in all three treatment periods. It was concluded that terodiline offers an alternative in the treatment of female detrusor instability.