Impaired Clearance From the Brain Increases the Brain Exposure to Metoclopramide in Elderly Subjects.

ABSTRACT: The antiemetic and gastroprokinetic drug metoclopramide is a weak substrate of the blood-brain barrier (BBB) efflux transporter P-gp and displays central nervous system (CNS) side effects (i.e., extrapyramidal symptoms and tardive dyskinesia) caused by dopamine D₂ receptor blockade in the basal ganglia. These side effects occur with a higher incidence in elderly people. We used positron emission tomography to assess the brain distribution of [¹¹ C]metoclopramide in young (n = 11, 26 ± 3 years) and elderly (n = 7, 68 ± 9 years) healthy men both after administration of a microdose (9 ± 7 µg) and a microdose co-injected with a therapeutic dose of unlabeled metoclopramide (10 mg). For both doses, elderly subjects had a significantly higher total volume of distribution (V<

SUBMITTER: Bauer M 

PROVIDER: S-EPMC7983943 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature