Clonazepam

Clonazepam , with the formula C15H10ClN3O3 , is a benzodiazepine tranquilizer. Clinically, it is mainly used for: (1) treatment of epilepsy and convulsions, which are effective for all types of epilepsy, especially for small seizures and myoclonic seizures. Intravenous treatment of status epilepticus. (2) Treatment of anxiety and insomnia. (3) It is also effective for choreas. It also has a certain effect on drug-induced hyperactivity, chronic multiple convulsions, stiff man syndrome, and various types of neuralgia.

The effect is similar to diazepam and nitrazepam. However, the anticonvulsant effect is 5 times stronger than the first two, and the effect is rapid. Similar to the central inhibitory effect of other BDZ drugs, due to the acceleration of chloride influx of nerve cells, the cells are hyperpolarized and the excitability of nerve cells is reduced. At the same time, it also has a certain effect on glutamate decarboxylase, so it has a broad-spectrum anti-epileptic effect. This product also has anxiolytic, hypnotic and central muscle relaxation effects.

Oral absorption is good, and the blood concentration peaks in 2 to 4 hours. The plasma half-life is 20 to 40 hours. It is highly fat-soluble and easily passes through the blood-brain barrier. It takes effect after 30 to 60 minutes of oral administration, and the effect can last for 6 to 8 hours. Almost all is metabolized in the liver, mainly by the CYP3A enzyme. Metabolites are excreted in the urine in free or conjugated form, and only a very small amount is excreted in the form of the original drug.