Benserazide

  • IUPAC: (RS) -2-amino -3-hydroxy -N'-( 2,3,4- trihydroxybenzyl ) propanhydrazid
  • DL -serine -2-( 2,3,4- trihydroxybenzyl ) -hydrazide
  • Latin: Benserazidum
  • 322-35-0
  • 14919-77-8 ( benserazide · hydrochloride)

N04BA02 (in combination with levodopa)

White to yellowish-white or orange- white, crystalline powder and the polymorphic (HCl)

L-DOPA decarboxylase

  • 257.24 g.mol -1
  • 293.71 g mol-1 · (HCl)

146-148 ° C ( HCl)

Slightly soluble in water, very slightly soluble in absolute ethanol, practically insoluble in acetone ( HCl)

Attention

5000 mg · kg -1 ( LD50, Mouse, oral, hydrochloride)

Template: Infobox chemical / molecular formula search available

Benserazide is a drug from the group of L- DOPA - decarboxylase inhibitor.

Indications

Benserazide inhibits the metabolism of L- DOPA ( levodopa) and is used exclusively in combination preparations with levodopa for the treatment of non-triggered by medications Parkinson 's disease. Today, the Restless Legs Syndrome (RLS ) is often treated with the combination of L- DOPA and benserazide.

Effect

Dopamine itself is used to treat Parkinson's patients unsuitable, mainly because it hardly crosses the blood -brain barrier. Its precursor ( prodrug ) Levodopa is, however, transported as amino acid across the blood -brain barrier and is now the most effective and important means Parkinson. They administered it almost exclusively in oral dosage form, and almost always in conjunction with benserazide or carbidopa. These substances are inhibitors of the enzyme aromatic L- amino acid decarboxylase ( dopa ), which catalyzes the conversion of levodopa into dopamine. Benserazide do not cross the blood -brain barrier, blocks the enzyme that is only peripherally (outside the central nervous system ). There would levodopa is decarboxylated without dopa decarboxylase inhibitor to 95% for dopamine.

Benefits

This combination with benserazide has two major advantages:

  • First, the oral dose of levodopa can be reduced
  • Secondly take side effects, which go back to the peripheral formation of dopamine ( and norepinephrine and epinephrine ) above; This information can include nausea and vomiting, cardiac arrhythmias, and orthostatic dysregulation.

Other Information

The ratio of the combination of benserazide with levodopa is one in four.

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System Dangerous Substances Directive (67/548/EEC) Active ingredient Medical Subject Headings
115787
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