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| ====== Valproate ====== | ====== Valproate ====== |
| Valproic acid (2-propyl pentanoic acid, 2-propyl valeric acid) is a short-chain branched fatty acid. Prior to the serendipitous discovery of its anti-epileptic activity in 1963, valproic acid was used as an organic solvent. | Valproic acid (2-propyl pentanoic acid, 2-propyl valeric acid) is a short-chain branched fatty acid. Prior to the serendipitous discovery of its anti-epileptic activity in 1963, valproic acid was used as an organic solvent[(:cite:panayiotopoulos2005)]. |
| ===== Authorised indications ===== | ===== Authorised indications ===== |
| UK-SmPC: In the treatment of generalized, partial or other epilepsy. | UK-SmPC: In the treatment of generalized, partial or other epilepsy. |
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| ==== History ==== | ==== History ==== |
| Valproic acid (VPA; valproate; di-n-propylacetic acid, DPA; 2-propylpentanoic acid, or 2-propylvaleric acid) was first synthesized in 1882, by Burton[(:cite:burton1882>Burton BS (1882) On the propyl derivatives and decomposition products of ethylacetoacetate. Am Chem J3: 385–395)].Its anticonvulsant activity was fortuitously discovered by Pierre Eymard in France in 1962 while working at the Firma Berthier laboratories in Grenoble. Because valproic acid is a liquid, it was used as a lipophilic vehicle to dissolve water-insoluble compounds during preclinical drug testing. As part of his thesis in 1962, Eymard had synthesized a number of khelline derivatives in the laboratory of G. Carraz at the School of Medicine and Pharmacy in Grenoble, France[(:cite:13935231>{{pubmed>short:13935231}})]. | Valproic acid (VPA; valproate; di-n-propylacetic acid, DPA; 2-propylpentanoic acid, or 2-propylvaleric acid) was first synthesized in 1882, by Burton[(:cite:burton1882>Burton BS (1882) On the propyl derivatives and decomposition products of ethylacetoacetate. Am Chem J3: 385–395)].Its anticonvulsant activity was fortuitously discovered by Pierre Eymard in France in 1962 while working at the Firma Berthier laboratories in Grenoble. Because valproic acid is a liquid, it was used as a lipophilic vehicle to dissolve water-insoluble compounds during preclinical drug testing. As part of his thesis in 1962, Eymard had synthesized a number of khelline derivatives in the laboratory of G. Carraz at the School of Medicine and Pharmacy in Grenoble, France[(:cite:13935231>{{pmid>long:13935231}})]. |
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| Two colleagues, H. Meunier and Y. Meunier, working for a small company, Berthier Laboratories, in Grenoble, had used valproate for a long time as a vehicle for dissolving of a bismuth salt. So the three scientists Eymard, Meunier and Meunier had the idea to use this vehicle also for dissolving some of the khelline derivatives synthesized by Eymard. In order to evaluate the pharmacological activities of the khelline derivatives, Carraz proposed to test the most active derivative in the pentylenetetrazole (PTZ) seizure test. By doing this, the researchers found that the vehicle, valproate, alone exerted an anticonvulsant effect[(:cite:loscher1999>Löscher W. (1999) The discovery of valproate. In: Löscher W. (eds) Valproate. Milestones in Drug Therapy. Birkhäuser, Basel)]. | Two colleagues, H. Meunier and Y. Meunier, working for a small company, Berthier Laboratories, in Grenoble, had used valproate for a long time as a vehicle for dissolving of a bismuth salt. So the three scientists Eymard, Meunier and Meunier had the idea to use this vehicle also for dissolving some of the khelline derivatives synthesized by Eymard. In order to evaluate the pharmacological activities of the khelline derivatives, Carraz proposed to test the most active derivative in the pentylenetetrazole (PTZ) seizure test. By doing this, the researchers found that the vehicle, valproate, alone exerted an anticonvulsant effect[(:cite:loscher1999>Löscher W. (1999) The discovery of valproate. In: Löscher W. (eds) Valproate. Milestones in Drug Therapy. Birkhäuser, Basel)]. |
| ==== References ==== | ==== References ==== |
| ~~REFNOTES~~ | ~~REFNOTES~~ |
| Source: Panayiotopoulos CP. (2005). The Epilepsies: Seizures, Syndromes and Management. Oxfordshire (UK): Bladon Medical Publishing. | |
