Benserazide

Structural formula
Structural formula without stereochemistry
General
Non-proprietary name	Benserazide
other names	( RS ) -2-Amino-3-hydroxy- N ′ - (2,3,4-trihydroxybenzyl) propane hydrazide ( IUPAC ) DL -Serine-2- (2,3,4-trihydroxybenzyl) hydrazide
Molecular formula	C 10 H 15 N 3 O 5
Brief description	white to yellowish white or orange-white, crystalline and polymorphic powder (HCl)
External identifiers / databases
CAS number 322-35-0 14919-77-8 (benserazide hydrochloride ) PubChem 2327 ChemSpider 2237 DrugBank DB12783 Wikidata Q818165
Drug information
ATC code	N04 BA02 (in combination with levodopa)
Drug class	L -DOPA- decarboxylase inhibitors
properties
Molar mass	257.24 g · mol -1 293.71 g · mol -1 (hydrochloride)
Physical state	firmly
Melting point	146-148 ° C (HCl)
solubility	slightly soluble in water, very sparingly soluble in absolute ethanol , practically insoluble in acetone (HCl)
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS labeling of hazardous substances Caution H and P phrases H: 315-319-335 P: 261-305 + 351 + 338
Toxicological data	5000 mg kg −1 ( LD 50 ,  mouse ,  oral , hydrochloride)
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

Combination preparations

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

Wikibooks: Decarboxylase Inhibitors  - Learning and Teaching Materials

• MeSH benserazide

Individual evidence

1. ↑ ^{a b} European Pharmacopoeia Commission (ed.): EUROPEAN PHARMACOPOE 5TH EDITION . tape 5.0-5.8 , 2006.
2. ↑ ^{a b} Entry on benserazide. In: Römpp Online . Georg Thieme Verlag, accessed on May 30, 2014.
3. ↑ ^{a b} Benserazid data sheet from Sigma-Aldrich , accessed on March 9, 2011 ( PDF ).
4. ↑ Mutschler: drug effects. 9th edition, Wissenschaftliche Verlagsgesellschaft Stuttgart, 2008 ISBN 978-3-8047-1952-1 .

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !