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    Home > Active Ingredient News > Study of Nervous System > How to choose insomnia medication correctly? These 5 points to know!

    How to choose insomnia medication correctly? These 5 points to know!

    • Last Update: 2022-09-22
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    Clinically often encounter many patients have difficulty falling asleep, early awakening, dreams and other symptoms, how to correctly choose insomnia drugs to become the basic ability of clinicians, the author consulted the insomnia drugs related literature, summarized as follows, hope to bring certain help
    to peers.

    is the classification of "insomnia drugs"? Drugs that help with sleep include several categories:
    the first is sedative sleeping pills, including benzodiazepines such as diazepam, esozolam, clonazepam, alprazolam, etc.
    ; Non-benzodiazepine new sleeping pills such as zolpidem, zopiclone, dexzopiclone
    The second type is a chinese proprietary medicine that calms the spirit and promotes sleep, and is commonly used for jujube anshen capsules, sweet dream capsules or oral liquid, sleep relief capsules and so on
    The third category is more special, because most sleep disorders are associated with emotional abnormalities, so patients with chronic insomnia and mood disorders often use drugs to regulate mood and promote sleep, such as mirtazapine, haloperidolamine melirlitracine tablets, citalopram, paroxetine, sertraline, agomelatine and the like
    Due to the large individual differences and different sensitivities to drugs, the effect of combination drugs will be more significant
    in many cases.

    Next, some common insomnia drugs are analyzed from their indications and pharmacokinetics

    Commonly used drug inventory ■ eszolam tablets
    indications: mainly used for anxiolysis, insomnia

    Also used for nervousness, fear, and anti-epileptic and anticonvulsant
    The hypnotic effect is relatively strong, and it can fall asleep 0.
    5-1 hours after oral administration, and the maintenance time is about
    6 hours.

    Toxic side effects are mainly dependent, and long-term use has a certain degree of drug resistance

    If taken in large quantities at a time, poisoning will occur, and respiratory depression or blood pressure reduction is life-threatening

    Clinically, it belongs to the second class of psychotropic drugs and requires a doctor's prescription
    ■ Indications for oxazepam tablets
    : mainly used for short-term relief of anxiety, tension, agitation, can also be used for hypnosis, anxiety accompanied by mental depression of auxiliary drugs, and can alleviate acute alcohol withdrawal symptoms

    Muscle relaxation is stronger
    than other benzodiazepines.
    Oral absorption is slow, 45 to 90 minutes of oral effectiveness, 2 to 4 hours, blood drug concentration peak, blood drug concentration in several days to steady state, plasma protein binding rate of 86% to 89%, T1/2 is generally 5 to 12 hours

    Inactivated in combination with glucuronic acid in the body, all excreted by the kidneys, and the amount accumulated in the body is extremely small

    ▎ Small class

    T1/2 refers to the half-life of the drug and refers to the time
    required for the drug to metabolize half.

    Clinically, it is necessary to decide the frequency of taking drugs according to the half-life of the drug, if the half-life is relatively long, it can be taken once a day or once every other day, if the half-life is relatively short, it needs to be taken three to four times a day, so the half-life is a very important indicator to determine the speed of
    drug metabolism.

    ■ Alprazolam tablets
    indications: mainly used for anxiety, nervousness, agitation, can also be used for hypnosis or anxiety adjuvant medication, can also be used as an anti-panic drug, and can alleviate acute alcohol withdrawal symptoms

    It should be used
    with caution in patients with mental disorders such as depression.
    Oral absorption is fast and complete, and the plasma protein binding rate is about 80%.

    Blood concentrations peak
    within 1 to 2 hours after oral administration.

    The blood concentration reaches a steady state
    within 2 to 3 days.

    T1/2 is generally 12 to 15 hours, and the elderly are 19 hours

    Metabolized by the liver, the metabolite α-hydroxylprazolam, which also has certain pharmacological activity

    Excreted by the kidneys

    The amount of accumulation in the body is very small, and it is quickly
    cleared after stopping the drug.
    ■ Zalepron dispersible tablets
    indications: This product is suitable for short-term treatment
    of insomnia with difficulty falling asleep.

    Clinical studies have shown that Zalepron can shorten the time to sleep, but it has not been shown to increase sleep time and reduce the number of awakenings
    Zalepron is absorbed quickly and completely
    after oral administration.

    Peak plasma concentration
    is reached in about 1 hour.

    Its absolute bioavailability is about 30%, with a clear first-pass effect

    Zalepron is a fat-soluble compound that, when administered intravenously, is evenly distributed throughout the bloodstream without being widely distributed in
    red blood cells.

    After oral administration, zalepron is widely metabolized, in the urine, only no more than 1% of the dose is the original drug
    ■ Indications for dexzopiclone tablets
    : for the treatment of insomnia
    Pharmacokinetic studies
    were conducted on healthy volunteers (adults and the elderly) and patients with liver and kidney disease.

    In healthy subjects, the maximum dose of a single dose reached 7.
    5 mg, and a 7-day continuous dosing trial was performed at doses of 1 mg, 3 mg and 6 mg
    , respectively.

    This product can be absorbed quickly, reaching a peak (tmax) in about 1 hour, and the elimination half-life is about 6 hours

    Healthy adults take this product continuously without accumulation, at 1-6mg, and the distribution is linear with
    the dose.
    ■ Indications for clonazepam tablets
    • Mainly used for the treatment of epilepsy and convulsions, it is effective for all types of epilepsy, especially for small seizures and myoclonus seizures

    Intravenous injection for status epilepticus
    • Can be used to treat anxiety states and insomnia
    • Also effective
    for chorea.

    It also has a certain effect
    on drug-induced ADHD, chronic multiple convulsions, zombie syndrome, and various types of neuralgia.
    Oral absorption is good, and the blood concentration reaches a peak
    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 free or bound form through the urine, and only a very small amount is excreted
    in the form of the original drug.
    ■ Indications for lorazepam tablets
    : suitable for the treatment of anxiety disorders or for short-term treatment to relieve anxiety symptoms and anxiety associated with depressive

    Anxiety or nervousness associated with stress in everyday life usually does not require treatment
    with anxiolytics.

    The effect of long-term application of lorazepam, that is, the effect of more than 4 months of application has not been evaluated by systematic clinical studies

    Physicians should periodically re-evaluate the effectiveness
    of the drug in individual patients.
    Oral larazepam is rapidly absorbed with an absolute bioavailability of 90%.

    Peak blood concentrations occur about 2 hours
    after taking the drug.

    The peak concentration of the plasma drug after oral administration of 2 mg of lorazepam is about 20 ng / ml
    The average elimination half-life of free lorazepam in human plasma is about 12 hours, and the main metabolite, lorazepam glucuronate, is about 18 hours

    At clinically relevant blood concentration levels, the plasma protein binding rate of lorazepam is about 85%.

    ■ Indications for zolpidem tartrate tablets
    : treatment of severe sleep disorders, such as occasional insomnia and temporary insomnia
    The bioavailability of oral zolpidem is about 70%, and the peak time for plasma drug concentrations is between
    5 and 3 hours.

    At therapeutic dose, the pharmacokinetics is linear

    Plasma protein binding rate is about 92%.

    The volume of distribution in adults is 0.
    02 L/kg

    Zolpidem is metabolized by the liver and excreted
    mainly in the form of inactive metabolites by urine (about 60%) and feces (about 40%).

    It has no inducing effect on liver enzymes

    The plasma elimination half-life is approximately 2.
    4 hours (0.
    5 hours).

    In the risk group: a decrease
    in the clearance of the liver can be observed in elderly patients.

    The peak concentration increased by about 50%, while the half-life (averaged 3 hours) did not increase

    The volume of distribution is reduced to 0.
    34± 0.
    05 L/kg

    In patients with renal insufficiency, a moderate reduction
    in clearance can be observed, regardless of whether dialysis is performed or not.

    Other kinetic parameters remain unchanged

    Zolpidem cannot be removed
    by dialysis.

    In patients with hepatic insufficiency, the bioavailability of zolpidem increases

    Its clearance is reduced and the elimination half-life is prolonged (about 10 hours).

    do I need to take insomnia pills?
    Occasional, short-term insomnia does not necessarily require medication

    They are often able to find relevant precipitating factors, such as environmental changes, physiological changes, jet lag, stimulant food, or drug effects

    After removing the trigger or relieving it by self-regulation, some patients can sleep back to normal and do not need drug treatment
    However, if insomnia persists and has an impact on the body, mind, life, work and study, and neither removing triggers nor establishing good sleep habits can improve sleep, medication is needed
    to choose insomnia medication? Drugs should be selected based on the different causes of insomnia, symptom characteristics and age, whether there are other diseases, and whether other drugs are taken

    For different patients, choose drugs for their characteristics, such as: people who are not easy to fall asleep, suitable for drugs that have a fast onset of action and a short duration of action, and can fall asleep quickly after taking, and there is no hangover the next day; People with persistent sleep difficulties and more nightmares are suitable for short- or moderate-acting drugs, which can deepen slow-wave sleep and shorten the time
    to fall asleep.
    The 2017 China Insomnia Diagnosis and Treatment Guidelines recommend that the treatment of insomnia include psychotherapy and medication

    In terms of drug therapy, it is recommended to give hypnotic drugs as appropriate on the basis of psychotherapy, so as to achieve the goals
    of relieving symptoms, improving sleep quality, prolonging effective sleep time, and improving the quality of life of patients.
    Pharmacotherapy should follow the principles of individualization, on-demand, intermittent, and adequate amounts

    The guidelines recommend the order of choice of drug types: short and moderate-acting benzodiazepine receptor agonists (including non-benzodiazepines and benzodiazepines) or melatonin receptor agonists (e.
    , ramemetamide), antidepressants with a sedative effect (trazodone, mirtazapine, fluvoxamine, and doxepine), the latter are particularly indicated in patients
    with insomnia with depression and/or anxiety.

    Guidelines do not recommend antiepileptic drugs and antipsychotics as the drug of choice and are only suitable for certain special cases and populations
    Precautions for insomnia pills • During the medication, do not drink coffee, tea and other exciting and refreshing drinks
    • Do not drink alcohol

    Small amounts of alcohol will quickly excite the brain, anti-drug sedative hypnotic effects

    Excessive alcohol has an inhibitory effect, and together with "insomnia drugs", it has a double inhibition of the cardiovascular system and respiratory system, resulting in slower breathing, decreased blood pressure, and even respiratory arrest and death
    • Elderly people should be cautious when
    taking medication.

    Many elderly people have problems with poor sleep and even take their own medication

    However, the elderly are weak, the function of organs is declining, most people also suffer from other diseases, and if the dose of the drug is large, it will cause many risks

    At the same time, the elderly often take other drugs or health care products, without the guidance of doctors or pharmacists, take "insomnia drugs" on their own, if there is an interaction between drugs, it may affect the efficacy or damage health

    In addition, the elderly should pay special attention to the dizziness that may cause dizziness after taking the drug and then cause falls and fractures
    •Patients with depression or anxiety disorders should be used as directed by a physician in combination with antidepressant or anti-anxiety medications

    Because depression and anxiety can also cause sleep disturbances, sleep will also improve
    after depression and anxiety are relieved.

    • Increase or decrease the dosage or change the dose under the guidance of the doctor, do not arbitrarily change the dose, use it for a long time or stop the drug suddenly, and avoid tolerance and dependence
    •Long-term users are advised to check liver and kidney function and blood routine every 3 months
    Finally, regarding what medicine is best to take for sleep disorders, it is necessary to combine the patient's different causes of insomnia, symptom characteristics and age, whether there are other diseases, whether to take other drugs to choose insomnia drugs, and sleep well, which is the best medicine
    to cure life.


    Liu Aobo,Tang Yonghong.
    Research progress in the treatment of chronic insomnia in the elderly[J].
    World Journal of Sleep Medicine.

    [2] Gao He, Mei Jianqiang, founded.
    Professor Mei Jianqiang's experience in the treatment of drug-dependent insomnia[J].
    Modern Journal of Integrative Medicine.

    Chinese Sleep Research Society.
    Chinese Insomnia Diagnosis and Treatment Guidelines[J].
    Chinese Medical Journal,2017,97(24):1844-1856.

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    The source of this article Medical Neurology Channel Author | Wang Lulu reviewed this article | Li Tuming Deputy Chief Physician
    Responsible Editor Mr.
    Lu Li

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