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    Home > Active Ingredient News > Study of Nervous System > Zaleplon, zolpidem, dexzopiclone...How to choose the elderly insomnia medicine?

    Zaleplon, zolpidem, dexzopiclone...How to choose the elderly insomnia medicine?

    • Last Update: 2022-01-09
    • Source: Internet
    • Author: User
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    *It is only for medical professionals to read for reference.
    This article counts the medicines that fit the physiological conditions of elderly patients with insomnia

    .

     Insomnia is common in geriatric clinics.
    The main complaint is difficulty falling asleep or sleep maintenance disorder, which produces obvious daytime symptoms, including difficulty concentrating and mood disorders

    .

    Today, as the aging is getting worse, there are more than 205 million people over 60 years old, and it is expected to reach 2 billion by 2050 [1]
    .

    As many as 50% of the elderly suffer from insomnia, and the prevalence rate is higher than that of the young [2]
    .

    The treatment of insomnia is divided into non-drug treatment and drug treatment
    .

    As age increases, body fat content increases, body fluids and plasma proteins decrease, resulting in prolonged elimination half-life of drugs and increased adverse drug reactions
    .

    Therefore, it is generally believed that non-drug treatment is better than drug treatment for elderly patients with insomnia
    .

    Non-drug treatment mainly refers to the treatment of cognitive behavior.
    When the treatment of cognitive behavior is ineffective, it can be combined with drug treatment.
    The following is an inventory of insomnia drugs suitable for the elderly based on the physiological characteristics of the elderly

    .

    ▌ Benzodiazepinedrugs (BZDs) BZDs act on non-selective γ-aminobutyric acid receptors, and common ones include estazolam, clonazepam, and alprazolam
    .

    BZDs help reduce anxiety, relax muscles and induce sleep
    .

    They are addictive and dangerous to use with other drugs and alcohol, so they can only be used for a short period of time
    .

    The half-life of BZDs is relatively long.
    For example, the half-life of estazolam is 10-24h.
    The main adverse reactions are drowsiness, dizziness, ataxia, and addiction

    .

    And BZDs are contraindicated in patients with severe chronic obstructive pulmonary disease
    .

    In elderly patients, the increase in fat and the decrease in plasma protein lead to an increase in free drugs and a slowdown in drug clearance, which increases the strength and duration of the drug in a disguised manner
    .

    Therefore, elderly patients are more sensitive to the adverse reactions of BZDs, and are more likely to have adverse reactions such as hangover reactions, dizziness, confusion, cognitive impairment, and delirium.
    Even short-acting BZDs may affect the motor function and memory of the next day.
    Function

    .

    Moreover, even though BZDs are effective in inducing and prolonging sleep at first, they are easily tolerated after repeated administration
    .

    Studies have also shown that higher serum concentrations of BZDs are associated with falls [3]
    .

    The 2019 American Geriatrics Association Standards for Potentially Unreasonable Drug Use (AGS Beers) strongly recommends avoiding the use of BZDs in the treatment of senile insomnia
    .

    Unless it can be used for a short time when it is necessary to use it
    .

    ▌ Non-benzodiazepinedrugs (non-BZDs) non-BZDs act on the α1 subunit of the γ-aminobutyric acid receptor, such as zopiclone, dexzopiclone, zolpidem, etc.
    , can also be used Induce sleep

    .

    Compared with BZDs, their action time is shorter, and they are less likely to cause residual drowsiness and have fewer side effects
    .

    The US Food and Drug Administration (FDA) recommends low-dose non-BZDs for the treatment of elderly insomnia
    .

    However, there is also a meta-analysis that shows a significant correlation between non-BZDs and the risk of falls and fractures [4]
    .

    Early research supports the use of non-BZDs for the treatment of insomnia in the elderly, but the AGS Beers standard strongly does not recommend non-BZDs for the treatment of insomnia in the elderly, because the adverse effects of adverse reactions exceed the improvement effect of insomnia
    .

     ■ 1.
    Zaleplon has a half-life of 1h, which is used for difficulty falling asleep

    .

    During the treatment, there was no drug resistance, no rebound insomnia or no withdrawal symptoms after stopping the drug
    .

    ■ 2.
    Zolpidem Zolpidem (half-life 2.
    5-2.
    9h) can be used for short-term treatment of insomnia with difficulty falling asleep

    .

    Compared with BZDs, Zolpidem has less side effects such as disturbed sleep structure, cognitive impairment, mental disorder and withdrawal reaction
    .

    However, since Zolpidem and BZDs are both regulated by the γ-aminobutyric acid receptor complex, they theoretically have similar risks.
    Therefore, it is not recommended to use Zolpidem for more than 4 weeks

    .

    Zolpidem usually has no significant hangover effect or tolerability, but rebound insomnia has been reported
    .

    For Zolpidem used in elderly patients with insomnia, the FDA recommends the lowest dose (5mg/d)
    .

    ■ 3.
    Ezopiclone has the longest half-life of all non-BZDs, about 6h, and the half-life can reach 9h after taking it for older people

    .

    Most studies have shown that dexzopiclone 2mg/d can improve difficulty falling asleep, maintain sleep, and feel good the next day
    .

    Therefore, for dexzopiclone, intermittent administration is recommended.
    For a small number of elderly people who need to take sleeping pills for a long time, ezzopiclone is also an option

    .

    ▌ Doxepin is a selective histamine receptor 1 antagonist when used in small doses
    .

    Among all antidepressants, only doxepin is approved by the FDA for the treatment of insomnia, with a dose of 3-6 mg/d
    .

    A 12-week study showed that taking 1 mg/d or 3 mg/d doxepin in elderly people over 65 can significantly improve difficulty falling asleep, sleep duration, sleep quality and overall treatment effect [5]
    .

    All in all, Doxet is usually used to treat elderly insomnia, but it is recommended to take it in small doses
    .

    ▌ Mirtazapine Mirtazapine is a serotonin receptor antagonist, which can be used for the treatment of elderly insomnia patients suffering from depression
    .

    ▌ Trazodone Trazodone is often used to treat insomnia with a dose of 25-100mg/d
    .

    A study comparing the effects of trazodone and zolpidem in people aged 21-65 years showed that trazodone has similar effects to zolpidem in sleep latency and sleep efficiency, but these effects are in the first week After disappearing [6]
    .

    Adverse reactions such as dizziness, arrhythmia, orthostatic hypotension, and underlying penile erection may be significant in the elderly
    .

    The clinical practice guidelines of the American Academy of Sleep Medicine recommend that because trazodone treatment does more harm than good, clinicians are advised not to use trazodone to treat difficulty falling asleep or sleep maintenance disorders [7]
    .

    ▌ Other therapeutic drugs include melatonin and orexin receptor antagonists, which have been approved by relevant European agencies or the US FDA for the treatment of insomnia, but there is still a lack of long-term study results
    .

    Key points 1.
    Cognitive behavior is the first-line treatment plan for the treatment of insomnia in the elderly

    .

    2.
    If medication must be used, low-dose non-BZDs or the antidepressant drugs doxepin and mirtazapine can be used

    .

    3.
    BZDs are not recommended for the treatment of elderly insomnia due to their high dependence and serious adverse reactions

    .

    References: [1]United Nations, New York, Ny.
    Department of Economic and Social Affairs.
    World population ageing, 1950-2050[M].
    United Nations Publications, 2002.
    [2]Crowley K.
    Sleep and sleep disorders in older adults[J].
    Neuropsychology review, 2011, 21(1): 41-53.
    [3]Ensrud KE, Blackwell TL, Mangione CM, et al.
    Central nervous system–active medications and risk for falls in older women[J] .
    Journal of the American Geriatrics Society, 2002, 50(10): 1629-1637.
    [4]Andrade C.
    Sedative Hypnotics and the Risk of Falls and Fractures in the Elderly[J].
    The Journal of clinical psychiatry, 2018, 79 (3): 0-0.
    [5]Krystal AD, Durrence HH, Scharf M, et al.
    Efficacy and safety of doxepin 1 mg and 3 mg in a 12-week sleep laboratory and outpatient trial of elderly subjects with chronic primary insomnia [J].
    Sleep, 2010, 33(11): 1553-1561.
    [6]Walsh JK, Erman M, Erwin CW,et al.
    Subjective hypnotic efficacy of trazodone and zolpidem in DSMIII–R primary insomnia[J].
    Human Psychopharmacology: Clinical and Experimental, 1998, 13(3): 191-198.
    [7]Sateia MJ, Buysse DJ, Krystal AD, et al.
    Clinical practice guideline for the pharmacologic treatment of chronic insomnia in adults: an American Academy of Sleep Medicine clinical practice guideline[J].
    Journal of Clinical Sleep Medicine, 2017, 13(2): 307-349.
    Source of this article: Medicine World Neuropathy Channel Author of this article: Liu Yujuan Review of this article: Li Tuming, Deputy Chief Physician Responsible Editor: Mr.
    Lu Li In order to learn more about readers’ thoughts on our channel, a small voting event is set up, and I hope that we can make better ideas in the future.
    The content of the refill ~ The medical community strives to be accurate and reliable when the content is reviewed, but does not make any promises and guarantees on the timeliness of the published content, and the accuracy and completeness of the cited information (if any).
    , And does not assume any responsibility due to the outdated content, the possible inaccuracy or incompleteness of the referenced materials, etc.
    Clinical practice guideline for the pharmacologic treatment of chronic insomnia in adults: an American Academy of Sleep Medicine clinical practice guideline[J].
    Journal of Clinical Sleep Medicine, 2017, 13(2): 307-349.
    Source of this article: Medical Neuropathy Channel Author of this article: Liu Yujuan Review of this article: Deputy Chief Physician Li Tuming Editor: Mr.
    Lu Li In order to further understand the readers’ thoughts on our channel, a small voting event is set up.
    I hope that we can make better content based on your ideas in the future.
    Refill ~ The medical community strives for the accuracy and reliability of its published content when it is approved, but it does not make any promises or guarantees on the timeliness of the published content, and the accuracy and completeness of the cited information (if any).
    Take any responsibility for the outdated content, the possible inaccuracy or incompleteness of the cited information, etc.
    Clinical practice guideline for the pharmacologic treatment of chronic insomnia in adults: an American Academy of Sleep Medicine clinical practice guideline[J].
    Journal of Clinical Sleep Medicine, 2017, 13(2): 307-349.
    Source of this article: Medical Neuropathy Channel Author of this article: Liu Yujuan Review of this article: Deputy Chief Physician Li Tuming Editor: Mr.
    Lu Li In order to further understand the readers’ thoughts on our channel, a small voting event is set up.
    I hope that we can make better content based on your ideas in the future.
    Refill ~ The medical community strives for the accuracy and reliability of its published content when it is approved, but it does not make any promises or guarantees on the timeliness of the published content, and the accuracy and completeness of the cited information (if any).
    Take any responsibility for the outdated content, the possible inaccuracy or incompleteness of the cited information, etc.

    .

    Relevant parties are requested to check separately when adopting or using this as a basis for decision-making
    .

    Contribution/Reprint/Business Cooperation: yxjsjbx@yxj.
    org.
    cn
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