Many noteworthy events occurred in 1882, such as:
- Robert Koch announced the discovery of the bacterium that causes tuberculosis
- Thomas Edison flipped the switch to the first commercial electrical power plant in the United States, lighting one square mile of lower Manhattan. This is considered by many as the day that began the electrical age
- Franklin D. Roosevelt, our 32nd President, was born
- The first Labor Day Parade was held in New York City
- Serbian inventor Nikola Tesla identifies the Magnetic Induction Field Principle: The idea behind the generation of electricity using rotating magnets
However, in 1882 another event occurred that seemed obscure at the time but eventually had a major impact on modern medicine. An American chemist, B.S. Burton, needed a liquid to dissolve substances that would not dissolve readily in water. The liquid he synthesized was valproic acid, a substance similar to valeric acid found naturally in valerian. (Valerian root is used in herbal medicine for insomnia, anxiety, and stress management.) Valproic acid would remain a common solvent used in chemical laboratories for many decades, but it was not known to have any other use than to dissolve substances that would not dissolve easily in water.
In 1962, Pierre Eymard, a French pharmacology student, needed a substance to dissolve chemicals he was testing for anticonvulsant activity for his graduate thesis. Fortunately, he chose valproic acid as the solvent vehicle in his experiments, and during the testing of these compounds he found they all had anticonvulsant activity. Being a good scientist, he decided to test the solvent without any substances added as a “control.” A control is used in science to make sure the results of the experiments can be attributed to the chemicals added to the solvent. He found the valproic acid solvent alone had anticonvulsant properties.
The drug, valproic acid (also called valproate) was approved for use for seizures in France in 1967, but it was not until 1978 that valproate was approved for use in the US and is now available in over 100 countries. In addition, it is used for other conditions and has been the subject of over 5,000 research publications.
Currently the medical uses of valproate include: epilepsy, mental illness (bi-polar disorder and schizophrenia), and prevention of migraine headaches. Common brand names used in the US are: Depakene, Depakote, and Depacon.
The formulations include immediate release capsules, delayed-release tablets, extended-release tablets, oral liquid, and injectable.
Valproate is not without its side effects and adverse reactions. It can cause nausea, drowsiness, and weakness. The severe adverse reactions include bleeding (low blood platelets), encephalopathy (brain disease), and suicidal behavior and thoughts. The drug is known to be associated with birth defects and should not be used in pregnancy.
The story of valproate is not about an intentional search for a drug, but an excellent illustration of the serendipitous occurrences that happen in science. It all started when a laboratory chemist made a solvent for experiments, then many decades later a French student scientist used that solvent as a “control” during his experiments and discovered the compound valproic acid (valproate) had anticonvulsant activity, which has become an important drug in modern medicine.
Stay informed and stay healthy.
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