Benzodiazepines are mostly derivatives of 1, 4- benzodiazepines. There are more than 20 kinds commonly used in clinic. Although their structures are similar, their anti-anxiety, sedative-hypnotic, anticonvulsant, muscle relaxation and sedative effects are different in different derivatives. Derivatives used for sedation and hypnosis include diazepam, fludiazepam, azone, oxazepam and triazolam. These drugs are benzodiazepine receptor agonists, which can cause inhibition in different parts of the central nervous system. One of the ways to find lead compounds is lucky to find that 1, 4- benzodiazepines are new sedative and hypnotic drugs discovered by accident.
Benzodiazepines (including diazepam and valium) sedatives and hypnotics. It has anti-anxiety effect, sedative and hypnotic effect, and does not produce anesthetic effect when the dose is increased, but it is dependent after long-term application. It has anticonvulsant and antiepileptic effects and is the first choice for the treatment of status epilepticus. Relax the central muscles. Increase the effect of other central depressants. Pharmacokinetics: fast and complete oral absorption, intestinal and hepatic circulation. Because of its high fat solubility, its action is rapid and short-lived. It is mainly transformed by liver drug enzymes. Mechanism: Central inhibitory neuron γ -aminobutyric acid (GABA) has high affinity benzodiazepine receptors on the postsynaptic membrane of nerve endings.
Levopiptan, which appeared in 1993, is the latest sleeping pill. This is the first non-benzodiazepine sleeping pill developed in the United States. Users' addiction to levopitan seems to be slower than that of benzodiazepines. Moreover, if levopirtan is used according to the recommended dosage, it will not cause rebound insomnia. The recommended dose is 5 ~ 10 mg. But if used in large doses, there will be rebound and addiction. The effect of levopirtan is mainly aimed at sleep and will not affect other functions of the body. Its half-life is very short, even if it is taken in the middle of the night, it will not have after-effects in the morning.