Ilepcimide is a piperidine derivative with the chemical name 3-(3',4'-hypomethyldioxyphenyl)-acryloylpiperidine that mainly found in black pepper. It is an antiepileptic drug, also known as antiepilepserine, which is mainly used in the treatment of various types of epilepsy. The structure of ilepcimide is shown in fig. 1.
Epilepsy is a group of non-communicable neurological disorders, which is the clinical manifestation of an abnormal, excessive, purposeless and synchronized electrical discharge in the brain cells called neurons. The symptoms of epilepsy vary from person to person. Some people with epilepsy simply stare for a few seconds blankly during a seizure, while others repeatedly twitch their arms or legs. In most cases, the cause of seizures is unknown.
As of 2020, about 50 million people had epilepsy. Nearly 80% of cases occur in developing countriesEpilepsy caused 125 000 deaths in 2015, up from 112 000 in 1990. Fortunately, about 69% of epilepsy cases can be controlled with medications. As a new type of traditional Chinese medicine, ilepcimide has been used in China for decades. A study showed that ilepcimide has good efficacy in children with epilepsy, which has a large safety range, few side effects, and is well tolerated by patients, especially patients with other systemic diseases.
Ilepcimide contains a lipophilic aromatic ring and a hydrophilic amine group, which is structurally similar to the traditional antiepileptic drug lamotrigine (LTG). LTG exerts its antiepileptic effect by inhibiting voltage-gated Na+ channel (NaV) activity. Therefore, it is speculated that ilepcimide has a similar mechanism of action in the treatment of epilepsy.
Zeng et al studied the inhibition of NaV activity by ilepcimide in acutely isolated mouse hippocampal pyramidal neurons. The results showed that NaV activity in hippocampal pyramidal neurons was inhibited by ilepcimide in a concentration-dependent and voltage-dependent manner. Therefore, the main reason for the antiepileptic effect of ilepcimide may be the small influx of Na+.
Ilepcimide is derived from natural plants and has little toxicity. After long-term clinical observation, patients did not have obvious mental and neurological side effects after taking the drug containing ilepcimide. A small number of patients may have mild or transient side effects, such as tiredness.
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