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Benserazide

Generic Name
Benserazide
Brand Names
Prolopa
Drug Type
Small Molecule
Chemical Formula
C10H15N3O5
CAS Number
322-35-0
Unique Ingredient Identifier
762OS3ZEJU

Overview

When levodopa is used by itself as a therapy for treating Parkinson's disease, its ubiquitous metabolism into dopamine is responsible for a resultant increase in the levels of circulating dopamine in the blood and to various extracerebral tissues. This can result in a number of side effects like nausea, vomiting, or even cardiac arrhythmias that may diminish patient adherence . A decarboxylase inhibitor like benserazide is consequently an effective compound to combine with levadopa as it is incapable of crossing the blood-brain barrier itself but acts to prevent the formation of dopamine from levadopa in extracerebral tissues - thereby acting to minimize the occurrence of extracerebral side effects . Levodopa/benserazide combination products are used commonly worldwide for the management of Parkinson's disease. In particular, although the specific levodopa/benserazide combination is formally approved for use in Canada and much of Europe, the FDA has approved another similar levodopa/dopa decarboxylase inhibitor combination in the form of levodopa and carbidopa. Moreover, the European Medcines Agency has conferred an orphan designation upon benseraside since 2015 for its potential to be used as a therapy for beta thalassaemia as well .

Background

When levodopa is used by itself as a therapy for treating Parkinson's disease, its ubiquitous metabolism into dopamine is responsible for a resultant increase in the levels of circulating dopamine in the blood and to various extracerebral tissues. This can result in a number of side effects like nausea, vomiting, or even cardiac arrhythmias that may diminish patient adherence . A decarboxylase inhibitor like benserazide is consequently an effective compound to combine with levadopa as it is incapable of crossing the blood-brain barrier itself but acts to prevent the formation of dopamine from levadopa in extracerebral tissues - thereby acting to minimize the occurrence of extracerebral side effects . Levodopa/benserazide combination products are used commonly worldwide for the management of Parkinson's disease. In particular, although the specific levodopa/benserazide combination is formally approved for use in Canada and much of Europe, the FDA has approved another similar levodopa/dopa decarboxylase inhibitor combination in the form of levodopa and carbidopa. Moreover, the European Medcines Agency has conferred an orphan designation upon benseraside since 2015 for its potential to be used as a therapy for beta thalassaemia as well .

Indication

The primary therapeutic use for which benserazide is currently indicated for is as a combination therapy with levadopa for the treatment of Parkinson's disease in adults > 25 years of age, with the exception of drug-induced parkinsonism . At certain doses, the combination product of levodopa and benserazide may also be used to treat restless legs syndrome, which is sometimes associated with Parkinson's disease . There have also been some studies that have prompted the European Medicines Agency to confer orphan designation upon benserazide hydrochloride as a potential therapy for beta thalassaemia . Although studies are ongoing, no evidence has been formally elucidated as of yet .

Associated Conditions

  • Parkinson's Disease (PD)

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
No FDA approvals found for this drug.

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
MADOPAR HBS 125 CAPSULE
SIN05195P
CAPSULE
25 mg
1/17/1990
MADOPAR 125 CAPSULE 125 mg
SIN06121P
CAPSULE
28.5mg
5/17/1991
MADOPAR DISPERSIBLE TABLETS 125 mg
SIN11075P
TABLET
25 mg
8/17/1999
MADOPAR 250 TABLET 250 mg
SIN06119P
TABLET
50 mg
5/17/1991

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
MADOPAR DISP 125 TAB
N/A
N/A
N/A
7/31/1998
MADOPAR HBS CAP "125" CONTROLLED RELEASE
N/A
N/A
N/A
9/20/1988
MADOPAR '250' TAB
N/A
N/A
N/A
5/25/1981
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