G Castor1, U Schmidt. 1. Department of Anaesthesiology, Caritas Hospital, Dillingen/Saar, Germany.
Abstract
OBJECTIVE: To determine the plasma and cerebrospinal fluid (CSF) levels of urapidil after i.v. administration and the effect on CSF serotonin and 5-hydroxyindoleacetic acid (5-HIAA) concentrations. DESIGN: Open, single-dose study. SETTING: Post-surgery following neurosurgical removal of the hypophysis (n = 5) or aneurysm clipping (n = 1). PATIENTS: 6 patients, aged 32-71 years, with intact blood-brain barrier (BBB); 1 patient was studied twice. INTERVENTIONS: Single dose of 25 mg urapidil i.v. as prophylaxis of BP increase during extubation or as treatment of hypertensive episodes. MEASUREMENTS AND RESULTS: Urapidil, serotonin and 5-HIAA were measured by HPLC in CSF during 8 h after urapidil administration. Urapidil was detected in CSF as soon as 5 min after injection in 3 patients. The concentration ratio of plasma/CSF after the distribution phase was about 5:1. No significant effect on serotonin and 5-HIAA in CSF was seen. CONCLUSION: After administration of a therapeutic dose, urapidil permeates the BBB and may interact with central 5-HT1A-receptors.
OBJECTIVE: To determine the plasma and cerebrospinal fluid (CSF) levels of urapidil after i.v. administration and the effect on CSF serotonin and 5-hydroxyindoleacetic acid (5-HIAA) concentrations. DESIGN: Open, single-dose study. SETTING: Post-surgery following neurosurgical removal of the hypophysis (n = 5) or aneurysm clipping (n = 1). PATIENTS: 6 patients, aged 32-71 years, with intact blood-brain barrier (BBB); 1 patient was studied twice. INTERVENTIONS: Single dose of 25 mg urapidil i.v. as prophylaxis of BP increase during extubation or as treatment of hypertensive episodes. MEASUREMENTS AND RESULTS:Urapidil, serotonin and 5-HIAA were measured by HPLC in CSF during 8 h after urapidil administration. Urapidil was detected in CSF as soon as 5 min after injection in 3 patients. The concentration ratio of plasma/CSF after the distribution phase was about 5:1. No significant effect on serotonin and 5-HIAA in CSF was seen. CONCLUSION: After administration of a therapeutic dose, urapidil permeates the BBB and may interact with central 5-HT1A-receptors.
Authors: R A Gillis; K J Kellar; J A Quest; I J Namath; A Martino-Barrows; K Hill; P J Gatti; K Dretchen Journal: Drugs Date: 1988 Impact factor: 9.546