Venlafaxine occupation at the noradrenaline reuptake site: in-vivo determination in healthy volunteers
| Autor: | A. Haida, Jan K. Melichar, David J. Nutt, Alan H. Reynolds, Andrea Malizia, Christopher G. Rhodes |
|---|---|
| Rok vydání: | 2001 |
| Předmět: |
Adult
Male medicine.medical_specialty Sympathetic Nervous System Contrast Media Venlafaxine Pharmacology Norepinephrine 03 medical and health sciences 0302 clinical medicine Oral administration Internal medicine medicine Humans Pharmacology (medical) Ephedrine Neurons Adrenergic Uptake Inhibitors business.industry Venlafaxine Hydrochloride Cyclohexanols Receptors Adrenergic 030227 psychiatry Psychiatry and Mental health Endocrinology Area Under Curve Catecholamine Antidepressive Agents Second-Generation Antidepressant Female Serotonin Reuptake inhibitor business 030217 neurology & neurosurgery Tomography Emission-Computed medicine.drug |
| Zdroj: | Journal of Psychopharmacology. 15:9-12 |
| ISSN: | 1461-7285 0269-8811 |
| DOI: | 10.1177/026988110101500102 |
| Popis: | Venlafaxine, a serotonin and noradrenaline reuptake inhibitor, is an effective antidepressant at doses of 75 mg p.o. daily and above. Preclinical and healthy volunteer studies have demonstrated that venlafaxine is more potent at the serotonin than at the noradrenaline reuptake site, with noradrenergic blocking effects being observed at doses >75 mg p.o. in man. We used the Multiple Organs Coincidences Counter and [11C] meta hydroxy ephedrine (MHED) to test whether significant occupation of cardiac sympathetic neurones was achieved in man in vivo after the acute administration of venlafaxine 75 mg p.o. in nine healthy volunteers. MHED is a tracer which binds at the noradrenaline reuptake site. This study demonstrates that the [11C]MHED signal is significantly reduced after the administration of venlafaxine 75 mg p.o. thus showing that noradrenaline reuptake blockade is observable at this dose. This effect is predominantly seen in volunteers who received > 1 mg/kg venlafaxine. |
| Databáze: | OpenAIRE |
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