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| Other names | Serazide, RO 4-4602 |
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| Formula | C10H15N3O5 |
| Molar mass | 257.246 g·mol−1 |
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Benserazide is aperipherally actingaromaticL-amino acid decarboxylase orDOPA decarboxylase inhibitor, which is unable to cross theblood–brain barrier.[1]
Benserazide is a therapeutic alternative on theWorld Health Organization's List of Essential Medicines.[2]
Benserazide is used in the management ofParkinson's disease in combination withlevodopa asco-beneldopa (BAN), under the brand namesMadopar in the UK andProlopa in Canada, both made byRoche. Benserazide is not approved for use in the US;carbidopa is used, instead, for the same purpose. These combinations are also used for the treatment ofrestless legs syndrome.[3]
Levodopa is aprecursor to theneurotransmitterdopamine, which is administered to increase its levels in thecentral nervous system. However, most levodopa isdecarboxylated to dopamine before it reaches the brain, and since dopamine is unable to cross the blood–brain barrier, this translates to little therapeutic gain with strong peripheral side effects.
Benserazide inhibits the aforementioned decarboxylation,[4] and since it cannot cross the blood–brain barrier itself, this allows dopamine to build up solely in the brain, instead. Adverse effects caused by peripheral dopamine, such asvasoconstriction,nausea, andarrhythmia, are minimized. However, benserazide cannot reduce the centrally mediated side effects of levodopa, particularlydyskinesia.
Benserazide has little therapeutic effect on its own, and its effect occurs synergically in combination with levodopa.[5]
Theenzyme inhibited by benzerazide catalyzes many different decarboxylations. The same effect of concentrating the conversion of levodopa into dopamine to the central nervous system can be achieved with the following decarboxylations being confined to the central nervous system:
Centrally mediated side effects of higher levels ofneuro- andtrace amine-transmitters may worsen in combination withmonoamine oxidase inhibitors. Other side effects in combination withL-DOPA include nausea, vomiting etc.[6]
