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At present, there are two types of hypnotic drugs commonly used in clinical practice, namely benzodiazepines (BZDs) and non-BZDs. Non-benzodiazepine-like hypnotics are preferred in the elderly and those with cardiovascular disease. Sappiclone (including eszopiclone), zaleplon, and zolpidem, although all belong to non-benzodiazepine class hypnotics, but the three drugs are quite different.

I. Differences from benzodiazepines

Benzodiazepines: Non-selectively agonistic inhibitory gamma-aminobutyric acid receptors (GABAa) with anti-anxiety, sedation, hypnosis, muscle relaxation, and anticonvulsant effects;

Non-benzodiazepines: Selectively agonize GABAa receptors, with sedative and hypnotic effects, but weak muscle relaxation and anticonvulsant effects.

The Beers Standard of the American Gerontological Society believes that benzodiazepines have cognitive impairment and fall risk, and elderly insomnia patients should avoid using benzodiazepines.

II. Differences between Zolpidem, Zopiclon, and Zaleplon

1. Half-life

Non-benzodiazepines have a short half-life, and the residual effect on the next day is reduced, generally not causing daytime drowsiness. However, it should be noted that non-benzodiazepines may produce transient insomnia rebound after sudden withdrawal.

Zolpidem: The half-life is 0.7 to 3.5 hours (average 2.4 hours) with large individual differences. About 2.8 to 14 hours after taking the medicine, about 94% of the drug is eliminated from the body and can be used for patients with sleep disorders.

Zaleplon: With a half-life of 1 hour and about 4 hours after taking the drug, about 94% of the drug is eliminated from the body and can be used for patients with sleep disorders. It is not used for patients with sleep maintenance disorders (without prolonging the total sleep time and not reducing the number of wakefulness).

2. Adverse reactions

Zolpidem: The incidence of sleepwalking (sleepwalking, cooking, calling, etc.) is high. Not only appears at the time of the initial medication, but also suddenly appears after a period of medication. Only for the treatment of patients with severe sleep disorders, medication time does not exceed 4 weeks.

Zopiclone: ​​It can be excreted in saliva. The most common adverse reaction is bitterness or metallic taste in the oral cavity (the incidence is about 4%). S-zopiclone is S-zopiclone. Compared to zopiclone, eszopiclone is less tolerated and withdrawal symptoms (such as convulsions and insomnia rebound).

special reminder:

With benzodiazepines, long-term use of non-benzodiazepines can also result in tolerance and physical dependence, especially in high-dose applications.

Benzodiazepines and non-benzodiazepines can also be treated with benzodiazepine antagonist flumazenil.

3. Medication time

If you are having difficulty falling asleep, take zopiclone, eszopiclone, and zaleplon 5 to 10 minutes before bedtime. It is recommended that you take zolpidem immediately before you go to bed (which theoretically reduces the risk of sleepwalking).

Zaleplon has a short half-life, elimination is fast, and the residual effect is small the next day. If you can’t wake up at night and wake up more than 4 hours before you expect to get up, you can take Zaleplon.

special reminder:

Non-benzodiazepines hypnotics should start with a small dose, and when the effective dose is reached, the dose is not easily reduced or increased.

Non-benzodiazepine-like hypnotics have a short half-life, but the study results show that taking the drug 3 to 5 days a week can meet the sleep requirement and do not need medication every night.

In conclusion, the use of hypnotics is not the preferred and ideal method for treating insomnia, but it is very important to use hypnotics rationally when taking hypnotics, including the time of administration.

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