Benserazide Hydrochloride

(BANM, rINNM)
Synonyms: Benseratsidihydrokloridi; Bensérazide, chlorhydrate de; Benserazid-hydrochlorid; Benserazidhydroklorid; Benserazidi hydrochloridum; Benserazido hidrochloridas; Benszerazid-hidroklorid; Hidrocloruro de benserazida; Serazide Hydrochloride.
Cyrillic synonym: Бенсеразида Гидрохлорид.

💊 Chemical information

Chemical formula: C10H15N3O5,HCl = 293.7.
CAS — 14919-77-8; 14046-64-1.

Pharmacopoeias.

In Chin., Eur., and Jpn.

Ph. Eur. 6.2

(Benserazide Hydrochloride). A white or yellowish-white or orange-white crystalline powder. It shows polymorphism. Freely soluble in water; very slightly soluble in dehydrated alcohol; practically insoluble in acetone. A 1% solution in water has a pH of 4.0 to 5.0. Protect from light.

Solubility.

Benserazide is unstable in a neutral, alkaline, or strongly acidic medium. 1 1. Schwartz DE, Brandt R. Pharmacokinetic and metabolic studies of the decarboxylase inhibitor benserazide in animals and man. Arzneimittelforschung 1978; 28: 302–7.

💊 Adverse Effects and Precautions

Nevertheless licensed product information recommends that benserazide should not be given to patients under 25 years of age, nor to pregnant women or to women of child-bearing potential in the absence of adequate contraception.
1. Theiss E, Schärer K. Toxicity of L-dopa and a decarboxylase inhibitor in animal experiments. In: de Ajuriaguerra J, Gauthier G, eds. Monoamines Noyaux Gris Centraux et Syndrome de Parkinson. Geneva: Georg, 1971: 497–504
2. Ziegler WH, et al. Toxicity of L-dopa and a dopa decarboxylase inhibitor in humans. In: de Ajuriaguerra J, Gauthier G, eds. Monoamines Noyaux Gris Centraux et Syndrome de Parkinson. Geneva: Georg, 1971: 505–16.

💊 Pharmacokinetics

Benserazide was rapidly excreted in the urine in the form of metabolites, mostly within the first 6 hours; 85% of urinary excretion had occurred within 12 hours. It is mainly metabolised in the gut and appears to protect levodopa against decarboxylation primarily in the gut, but also in the rest of the organism, mainly by way of its metabolite trihydroxybenzylhydrazine. Benserazide did not cross the blood-brain barrier in rats.
1. Schwartz DE, et al. Pharmacokinetics of the decarboxylase benserazide in man: its tissue distribution in the rat. Eur J Clin Pharmacol 1974; 7: 39–45
2. Schwartz DE, Brandt R. Pharmacokinetic and metabolic studies of the decarboxylase inhibitor benserazide in animals and man. Arzneimittelforschung 1978; 28: 302–7.

💊 Uses and Administration

Benserazide hydrochloride is a peripheral dopa-decarboxylase inhibitor with actions similar to those of carbidopa and is used similarly as an adjunct to levodopa in the treatment of parkinsonism. For details of dosage, see Levodopa.
1. Dingemanse J, et al. Pharmacodynamics of benserazide assessed by its effects on endogenous and exogenous levodopa pharmacokinetics. Br J Clin Pharmacol 1997; 44: 41–8.

💊 Preparations

BP 2008: Co-beneldopa Capsules; Dispersible Co-beneldopa Tablets.

Proprietary Preparations

Ger.: Restex. Multi-ingredient: Arg.: Madopar; Austral.: Madopar; Austria: Dopamed; Levobens; Madopar; Restex; Belg.: Prolopa; Braz.: Prolopa; Canad.: Prolopa; Chile: Melitase; Prolopa; Cz.: Madopar; Denm.: Madopar; Fin.: Madopar; Fr.: Modopar; Ger.: Levodopa comp B; Levopar; Madopar; PK-Levo; Gr.: Madopar; Hong Kong: Madopar; Hung.: Madopar; Indon.: Leparson; Levazide; Levopar; Madopar; Pardoz; Irl.: Madopar; Israel: Levopar Plus; Ital.: Madopar; Malaysia: Madopar; Mex.: Madopar; Neth.: Madopar; Modopar; Norw.: Madopar; NZ: Madopar; Philipp.: Madopar; Pol.: Madopar; Port.: Madopar; Rus.: Madopar (Мадопар); S.Afr.: Madopar; Singapore: Madopar; Spain: Madopar; Swed.: Madopark; Switz.: Madopar; Thai.: Cenparkin†; Madopar; Vopar; Turk.: Madopar; UK: Madopar; Venez.: Madopar.
Published October 17, 2018.