RESUMO
Radioreceptor assay (RRA) was used to evaluate serum antimuscarinic activity in 10 healthy volunteers after a single dose of scopolamine hydrobromide (ScHBr) solution, 0.02 mg/kg, by a new oral administration method. Cardiac, antisialogogue, and subjective effects of the drug were also recorded. Although clinically useful antisialogogue and sedative effects were obtained 40 to 60 minutes after the administration of ScHBr, no reliable antimuscarinic activity was evaluated in serum samples for up to 3 hours. Clinically useful sedative and antisialogogue effects can be reached by gastrointestinal absorption of ScHBr solution.
Assuntos
Receptores Muscarínicos/efeitos dos fármacos , Escopolamina/administração & dosagem , Administração Oral , Adulto , Atropina/sangue , Ensaios Clínicos como Assunto , Método Duplo-Cego , Feminino , Humanos , Masculino , Ensaio Radioligante , Distribuição Aleatória , Salivação/efeitos dos fármacos , Escopolamina/farmacologia , Fatores de TempoRESUMO
Antisialagogue, cardiac, and subjective effects of oral scopolamine hydrobromide solution (ScHBr), 0.02 mg/kg total body weight, were studied in a double-blind, randomized, placebo-controlled manner with ten healthy volunteers. ScHBr was rinsed in the mouth for 5 minutes before swallowing. ScHBr reduced nonstimulated and paraffin-stimulated salivation at 40 minutes by 52% and 62%, and at 60 minutes by 81% to 80%, respectively. The heart rate decreased significantly (p less than 0.01) when compared with placebo. With the same drug dosing method, the effects of ScHBr also were tested in clinical dental examination procedures in two dental student groups. In the ScHBr group, salivation decreased by 70%, and in the placebo group, it increased by 22% as a result of mechanical stimulus. Subjective sedation and relaxation were experienced by most of the volunteers.