Urapidil permeates the intact blood-brain barrier

Intensive Care Medicine
G Castor, U Schmidt

Abstract

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. Open, single-dose study. Post-surgery following neurosurgical removal of the hypophysis (n = 5) or aneurysm clipping (n = 1). 6 patients, aged 32-71 years, with intact blood-brain barrier (BBB); 1 patient was studied twice. Single dose of 25 mg urapidil i.v. as prophylaxis of BP increase during extubation or as treatment of hypertensive episodes. 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. After administration of a therapeutic dose, urapidil permeates the BBB and may interact with central 5-HT1A-receptors.

References

Apr 1, 1987·Biological Psychiatry·B G AlmayL Oreland
Dec 1, 1988·Journal of Hypertension. Supplement : Official Journal of the International Society of Hypertension·C AngerP Lawin
Jan 1, 1984·Comparative Biochemistry and Physiology. C, Comparative Pharmacology and Toxicology·L Laxmyr

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