Benserazide
Structural formula | ||||||||||||||||
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Structural formula without stereochemistry | ||||||||||||||||
General | ||||||||||||||||
Non-proprietary name | Benserazide | |||||||||||||||
other names |
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Molecular formula | C 10 H 15 N 3 O 5 | |||||||||||||||
Brief description |
white to yellowish white or orange-white, crystalline and polymorphic powder (HCl) |
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External identifiers / databases | ||||||||||||||||
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Drug information | ||||||||||||||||
ATC code | ||||||||||||||||
Drug class |
L -DOPA- decarboxylase inhibitors |
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properties | ||||||||||||||||
Molar mass | ||||||||||||||||
Physical state |
firmly |
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Melting point |
146-148 ° C (HCl) |
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solubility |
slightly soluble in water, very sparingly soluble in absolute ethanol , practically insoluble in acetone (HCl) |
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safety instructions | ||||||||||||||||
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Toxicological data | ||||||||||||||||
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . |
Benserazide is a drug from the group of L -DOPA decarboxylase inhibitors .
Indications
Benserazide inhibits the metabolism of levodopa ( L- DOPA) and is used exclusively in combination with levodopa for the treatment of Parkinson's disease that is not triggered by drugs . Today, Restless Legs Syndrome (RLS) is often treated with the combination of levodopa and benserazide.
effect
Dopamine itself is unsuitable for treating Parkinson's disease patients because it barely crosses the blood-brain barrier . Its precursor ( prodrug ) levodopa, on the other hand, is transported as an amino acid through the blood-brain barrier and is now the most effective and important Parkinson’s drug . Levodopa is administered almost exclusively orally and almost always together with benserazide or carbidopa . These substances are inhibitors of the enzyme aromatic L-amino acid decarboxylase (dopadecarboxylase), which catalyzes the conversion of levodopa into dopamine. Benserazide does not cross the blood-brain barrier, so it only blocks the enzyme peripherally (outside the central nervous system ). There, levodopa would be 95% decarboxylated to dopamine without a dopa decarboxylase inhibitor.
The combination of levodopa with benserazide causes
- First, the oral dose of levodopa can be reduced,
- secondly , reduce the side effects caused by the peripheral formation of dopamine (as well as noradrenaline and adrenaline ); these include nausea and vomiting , cardiac arrhythmias and orthostatic dysregulations .
Other Information
The mass ratio of the combination of benserazide with levodopa is one to four.
Trade names
Levobens (A), Levodopa comp (D), Levopar (D), Madopar (D, A, CH), PK-Levo (D), Restex (D, A)
literature
- Ernst Mutschler et al .: Mutschler - drug effects textbook of pharmacology and toxicology . 9th edition. Wissenschaftliche Verlagsgesellschaft, Stuttgart 2008, ISBN 978-3-8047-1952-1 .
Web links
Individual evidence
- ↑ a b European Pharmacopoeia Commission (ed.): EUROPEAN PHARMACOPOE 5TH EDITION . tape 5.0-5.8 , 2006.
- ↑ a b Entry on benserazide. In: Römpp Online . Georg Thieme Verlag, accessed on May 30, 2014.
- ↑ a b Benserazid data sheet from Sigma-Aldrich , accessed on March 9, 2011 ( PDF ).
- ↑ Mutschler: drug effects. 9th edition, Wissenschaftliche Verlagsgesellschaft Stuttgart, 2008 ISBN 978-3-8047-1952-1 .