Buspirone
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| Non-proprietary name | Buspirone | |||||||||||||||||||||
| other names |
8- {4- [4- (pyrimidin-2-yl) piperazin-1-yl] butyl} -8-azaspiro [4.5] decane-7,9-dione ( IUPAC ) |
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| Mechanism of action |
selective serotonin agonist |
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| Molar mass | 385.50 g · mol -1 | |||||||||||||||||||||
| Melting point |
109-110 ° C; 201.5–202.5 ° C (hydrochloride) |
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | ||||||||||||||||||||||
Buspirone is an anti-anxiety drug . Its main advantage over benzodiazepines is that, according to the current state of research, it is not addictive. It is also not sedating . In contrast to benzodiazepines, the effect does not occur immediately after ingestion, but only after a few weeks (two or more) of regular use. Buspirone has no affinity for GABA receptors . Presumably it acts as a partial agonist at 5-HT 1A receptors and as an antagonist at D 2 receptors . The active ingredient was patented by Bristol Myers in 1971 and by Mead Johnson in 1973 . There are also generic drugs on the market. It is used as a hydrochloride . Buspirone was first approved in 1986 for the indication of generalized anxiety disorder .
Side effects
The most common side effects (<1:10) are dizziness, tiredness, nausea and headache. Frequently (<1: 100) tachycardia , nervousness , insomnia , paresthesia , diarrhea , accommodation disorders , depressive discomfort, nightmares , confusion and blurred vision occur.
Interactions
Buspirone is metabolized via the cytochrome P450 3A4 . This has the consequence that the plasma level of buspirone is lowered by inducers of this enzyme (e.g. carbamazepine ) or increased by inhibitors (e.g. grapefruit juice , cimetidine ).
Serotonin syndrome can occasionally occur in connection with drugs with a strong serotonergic effect ( SSRI , clomipramine , St. John's wort ) .
Individual evidence
- ↑ a b c Entry on buspirone. In: Römpp Online . Georg Thieme Verlag, accessed on June 27, 2019.
- ↑ a b Data sheet for Buspirone hydrochloride from Sigma-Aldrich , accessed on March 14, 2011 ( PDF ).
- ↑ https://www.netdoktor.de/medikamente/buspiron/
Trade names
Anxut (D), Busp (D), Bespar (D)
Web links
- Independent pharmaceutical information about Buspirone ( Buspar ) from 1989 ( memento from September 20, 2013 in the Internet Archive ) at the Medical University of Innsbruck
