Introduction
Zaleplon is an organic compound and a sedative-hypnotic drug. Clinically, it is mainly used for the short-term treatment of insomnia. It can enable insomnia patients to fall asleep quickly, shorten the sleep onset time, extend the sleep duration, and reduce the number of awakenings. It is classified as a Class II psychotropic drug subject to control.
Specifications
CP
Chemical Name
N - [3 - (3 - cyanopyrazolo [1,5 - a] pyrimidin - 7 - yl) phenyl] acetamide
Molecular formula
C17H15N5O
CAS NO.
151319-34-5
Packing
1kg/tin
Category
Sedative-hypnotics
Storage
Store in the dark and keep it sealed.
Indication
It is primarily used for the short - term treatment of insomnia, especially for patients who have difficulty falling asleep. It can help patients fall asleep quickly, improve sleep quality by reducing the number of awakenings during the night, and increase the overall sleep duration.
Pharmacology Properties
Mechanism of Action
Zaleplon selectively binds to the α−1 subunit of the GABAA receptor - chloride ion channel complex in the central nervous system, enhancing the inhibitory effect of GABA, which is an inhibitory neurotransmitter. This leads to the opening of chloride ion channels, hyperpolarization of neuronal membranes, and subsequent inhibition of neuronal activity, thereby producing sedative, hypnotic, anxiolytic, and muscle - relaxing effects.
Pharmacokinetic Characteristics
After oral administration, zaleplon is rapidly absorbed, with an average time to reach peak plasma concentration of about 1 hour. It has a relatively short half - life of approximately 1 hour, which allows for a quick onset of action and a relatively short - acting effect, making it suitable for short - term treatment of insomnia. It is metabolized in the liver mainly by aldehyde oxidase and cytochrome P450 enzymes, and the metabolites are excreted mainly through the kidneys.
Dosage and Administration
The usual recommended dose for adults is 5 - 10 mg taken immediately before going to bed. The maximum dose should not exceed 20 mg per day. For elderly patients or those with hepatic impairment, a lower starting dose of 5 mg is recommended due to their potentially reduced ability to metabolize the drug.
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