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Hypnotic

Hypnotic

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Hypnotic drugs are a class of psychoactives
Psychoactive drug
A psychoactive drug, psychopharmaceutical, or psychotropic is a chemical substance that crosses the blood–brain barrier and acts primarily upon the central nervous system where it affects brain function, resulting in changes in perception, mood, consciousness, cognition, and behavior...

 whose primary function is to induce sleep
Sleep
Sleep is a naturally recurring state characterized by reduced or absent consciousness, relatively suspended sensory activity, and inactivity of nearly all voluntary muscles. It is distinguished from quiet wakefulness by a decreased ability to react to stimuli, and is more easily reversible than...

 and to be used in the treatment of insomnia
Insomnia
Insomnia is most often defined by an individual's report of sleeping difficulties. While the term is sometimes used in sleep literature to describe a disorder demonstrated by polysomnographic evidence of disturbed sleep, insomnia is often defined as a positive response to either of two questions:...

 and in surgical anesthesia
Anesthesia
Anesthesia, or anaesthesia , traditionally meant the condition of having sensation blocked or temporarily taken away...

. When used in anesthesia to produce and maintain unconsciousness, "sleep" is metaphorical and there are no regular sleep stages or cyclical natural states; patients rarely recover from anesthesia feeling refreshed and with renewed energy. Because drugs in this class generally produce dose-dependent effects, ranging from anxiolysis to production of unconsciousness, they are often referred to collectively as sedative-hypnotic drugs. Hypnotic drugs are regularly prescribed for insomnia and other sleep disorders, with over 95% of insomnia patients being prescribed hypnotics in some countries. Many hypnotic drugs are habit-forming and, due to a large number of factors known to disturb the human sleep pattern, a physician may instead recommend alternative sleeping patterns, sleep hygiene
Sleep hygiene
Sleep hygiene can be defined as the controlling of "all behavioural and environmental factors that precede sleep and may interfere with sleep." It is the practice of following guidelines in an attempt to ensure more restful, effective sleep which can promote daytime alertness and help treat or...

, and exercise, before prescribing medication for sleep. Hypnotic medication when prescribed should be used for the shortest period of time possible.

The benzodiazepine
Benzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...

 and nonbenzodiazepine
Nonbenzodiazepine
The nonbenzodiazepines, also called benzodiazepine-like drugs, are a class of psychoactive drugs pharmacologically resembling the benzodiazepines, with similar benefits, side effects and risks, despite having dissimilar or entirely different chemical structures.-Classes:There are currently three...

 hypnotic medications also have a number of side effects such as daytime fatigue, motor vehicle crashes, cognitive impairments, and falls and fractures. In children, prescribing hypnotics is not yet acceptable unless if used to treat night terrors or somnambulism. Elderly people are more sensitive to these side effects and a meta analysis found that the risks generally outweigh any marginal benefits of hypnotics in the elderly. A review of the literature regarding benzodiazepine hypnotic and Z drugs concluded that these drugs caused an unjustifiable risk to the individual and to public health, and lack evidence of long-term effectiveness due to tolerance. The risks include dependence
Substance dependence
The section about substance dependence in the Diagnostic and Statistical Manual of Mental Disorders does not use the word addiction at all. It explains:...

, accidents, and other adverse effects. Gradual discontinuation of hypnotics leads to improved health without worsening of sleep. Preferably they should be prescribed for only a few days at the lowest effective dose, and avoided altogether wherever possible in the elderly.

Benzodiazepines


Benzodiazepines are the most well-known and most frequently-prescribed hypnotic medications, although their use in recent years is being increasingly replaced by newer nonbenzodiazepine
Nonbenzodiazepine
The nonbenzodiazepines, also called benzodiazepine-like drugs, are a class of psychoactive drugs pharmacologically resembling the benzodiazepines, with similar benefits, side effects and risks, despite having dissimilar or entirely different chemical structures.-Classes:There are currently three...

 hypnotic drugs and the hormone melatonin
Melatonin
Melatonin , also known chemically as N-acetyl-5-methoxytryptamine, is a naturally occurring compound found in animals, plants, and microbes...

. Benzodiazepines are effective in the short term but tolerance to their hypnotic effects develops after 1 or 2 weeks, thus making them ineffective for long-term use. They are also a cause of hospital admissions, especially in the elderly who are more sensitive to their effects. Benzodiazepine withdrawal syndrome
Benzodiazepine withdrawal syndrome
Benzodiazepine withdrawal syndrome—often abbreviated to benzo withdrawal—is the cluster of symptoms which appear when a person who has taken benzodiazepines long term and has developed benzodiazepine dependence stops taking benzodiazepine drug or during dosage reductions...

 can also develop upon their discontinuation. This is characterized by rebound insomnia, anxiety
Anxiety
Anxiety is a psychological and physiological state characterized by somatic, emotional, cognitive, and behavioral components. The root meaning of the word anxiety is 'to vex or trouble'; in either presence or absence of psychological stress, anxiety can create feelings of fear, worry, uneasiness,...

, confusion
ConFusion
ConFusion is an annual science fiction convention organized by the Stilyagi Air Corps and its parent organization, the Ann Arbor Science Fiction Association. Commonly, it is held the third weekend of January. It is the oldest science fiction convention in Michigan, a regional, general SF con...

, disorientation, insomnia
Insomnia
Insomnia is most often defined by an individual's report of sleeping difficulties. While the term is sometimes used in sleep literature to describe a disorder demonstrated by polysomnographic evidence of disturbed sleep, insomnia is often defined as a positive response to either of two questions:...

, and perceptual disturbances. Prescription hypnotics are therefore best limited to short term use to avoid tolerance, drug dependence
Substance dependence
The section about substance dependence in the Diagnostic and Statistical Manual of Mental Disorders does not use the word addiction at all. It explains:...

, and the adverse effects of long term use.

Benzodiazepines tend to exert their hypnotic effects at high dosage compared to the more moderate dosage needed for anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...

 effects to be felt. The downside of the hypnotic properties of benzodiazepines is that they actually worsen the sleep architecture
Sleep architecture
Sleep architecture describes the structure and pattern of sleep and encompasses several variables. Sleep quotas refer to the amount of time spent in REM and NREM sleep. Sleep duration is the total time spent asleep in a 24 hour period. The duration of a NREM-REM cycle is also an important aspect...

 and thus the quality of sleep. They are also associated with an increased risk of road traffic accidents.

Nonbenzodiazepines


Nonbenzodiazepines have demonstrated efficacy in treating some sleep disorders. Limited, inconclusive evidence suggests that tolerance to nonbenzodiazepines is slower to develop than with benzodiazepines. Data is also limited with regard to long-term effects of nonbenzodiazepines; further research into the safety and long-term effectiveness of nonbenzodiazepines has been recommended in a review of the literature.

Examples





These drugs include:
  • GABAA PAM
    Positive allosteric modulator
    A positive allosteric modulator is a drug which increases the activity of a receptor indirectly via activation of an allosteric site on the protein. PAMs are similar to agonists in that they contribute to overall receptor activation, but they are different because they do so in a functionally...

    s
    • Barbiturate
      Barbiturate
      Barbiturates are drugs that act as central nervous system depressants, and can therefore produce a wide spectrum of effects, from mild sedation to total anesthesia. They are also effective as anxiolytics, as hypnotics, and as anticonvulsants...

      s
      • Amobarbital
        Amobarbital
        Amobarbital is a drug that is a barbiturate derivative. It has sedative-hypnotic and analgesic properties. It is a white crystalline powder with no odor and a slightly bitter taste. It was first synthesized in Germany in 1923...

      • Pentobarbital
        Pentobarbital
        Pentobarbital is a short-acting barbiturate that was first synthesized in 1928. Pentobarbital is available as both a free acid and a sodium salt, the former of which is only slightly soluble in water and ethanol....

      • Phenobarbital
        Phenobarbital
        Phenobarbital or phenobarbitone is a barbiturate, first marketed as Luminal by Friedr. Bayer et comp. It is the most widely used anticonvulsant worldwide, and the oldest still commonly used. It also has sedative and hypnotic properties but, as with other barbiturates, has been superseded by the...

      • Secobarbital
        Secobarbital
        Secobarbital sodium is a barbiturate derivative drug that was first synthesized in 1928 in Germany. It possesses anaesthetic, anticonvulsant, sedative and hypnotic properties...

      • Sodium thiopental
        Sodium thiopental
        Sodium thiopental, better known as Sodium Pentothal , thiopental, thiopentone sodium, or Trapanal , is a rapid-onset short-acting barbiturate general anaesthetic...

    • Benzodiazepine
      Benzodiazepine
      A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...

      s
      • Alprazolam
        Alprazolam
        Alprazolam is a short-acting anxiolytic of the benzodiazepine class of psychoactive drugs. Alprazolam, like other benzodiazepines, binds to specific sites on the GABAA gamma-amino-butyric acid receptor...

      • Estazolam
        Estazolam
        Estazolam is a benzodiazepine derivative drug developed by Upjohn in the 1970s. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties...

      • Flunitrazepam
        Flunitrazepam
        Flunitrazepam is marketed as a potent hypnotic, sedative, anticonvulsant, anxiolytic, amnestic, and skeletal muscle relaxant drug most commonly known as Rohypnol...

      • Lormetazepam
        Lormetazepam
        Lormetazepam Lormetazepam Lormetazepam (INN, or methyl-lorazepam, is a drug which is a short to intermediate acting 3-hydroxy benzodiazepine derivative. It possesses hypnotic, anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties....

      • Midazolam
        Midazolam
        Midazolam is a short-acting drug in the benzodiazepine class developed by Hoffmann-La Roche in the 1970s. The drug is used for treatment of acute seizures, moderate to severe insomnia, and for inducing sedation and amnesia before medical procedures. It possesses profoundly potent anxiolytic,...

      • Nitrazepam
        Nitrazepam
        Nitrazepam is a type of benzodiazepine drug and is marketed in English-speaking countries under the following brand names: Alodorm, Arem, Insoma, Mogadon, Nitrados, Nitrazadon, Ormodon, Paxadorm, Remnos, and Somnite...

      • Quazepam
        Quazepam
        Quazepam is a benzodiazepine derivative drug developed by the Schering Corporation in the 1970s. Quazepam is indicated for the treatment of insomnia including sleep induction and sleep maintenance...

      • Temazepam
        Temazepam
        Temazepam is an intermediate-acting 3-hydroxy benzodiazepine. It is mostly prescribed for the short-term treatment of sleeplessness in patients who have difficulty maintaining sleep...

      • Triazolam
        Triazolam
        Triazolam is a benzodiazepine drug. It possesses pharmacological properties similar to that of other benzodiazepines, but it is generally only used as a sedative to treat severe insomnia...

    • Nonbenzodiazepine
      Nonbenzodiazepine
      The nonbenzodiazepines, also called benzodiazepine-like drugs, are a class of psychoactive drugs pharmacologically resembling the benzodiazepines, with similar benefits, side effects and risks, despite having dissimilar or entirely different chemical structures.-Classes:There are currently three...

      s
      • Eszopiclone
        Eszopiclone
        Eszopiclone, marketed by Sepracor under the brand-name Lunesta, is a nonbenzodiazepine hypnotic used as a treatment for insomnia. Eszopiclone is the active dextrorotatory stereoisomer of zopiclone, and belongs to the class of drugs known as cyclopyrrolones.Eszopiclone is a short acting...

      • Zaleplon
        Zaleplon
        Zaleplon is a sedative/hypnotic, mainly used for insomnia. It is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class. In terms of adverse effects zaleplon appears to offer little improvement compared to both benzodiazepines and other non-benzodiazepine Z-drugs.Sonata is manufactured by...

      • Zolpidem
        Zolpidem
        Zolpidem is a prescription medication used for the short-term treatment of insomnia, as well as some brain disorders. It is a short-acting nonbenzodiazepine hypnotic of the imidazopyridine class that potentiates gamma-aminobutyric acid , an inhibitory neurotransmitter, by binding to GABAA...

      • Zopiclone
        Zopiclone
        Zopiclone is a non-benzodiazepine hypnotic agent used in the treatment of insomnia. In the United States, zopiclone is not commercially available, although its active stereoisomer, eszopiclone, is sold under the name Lunesta...

    • Others
      • Chloral hydrate
        Chloral hydrate
        Chloral hydrate is a sedative and hypnotic drug as well as a chemical reagent and precursor. The name chloral hydrate indicates that it is formed from chloral by the addition of one molecule of water. Its chemical formula is C2H3Cl3O2....

      • Clomethiazole
        Clomethiazole
        Clomethiazole is a sedative and hypnotic originally developed by Hoffmann-Le Roche in the 1930s. The drug is used in treating and preventing symptoms of acute alcohol withdrawal....

      • Diethyl ether
        Diethyl ether
        Diethyl ether, also known as ethyl ether, simply ether, or ethoxyethane, is an organic compound in the ether class with the formula . It is a colorless, highly volatile flammable liquid with a characteristic odor...

      • Ethanol
        Ethanol
        Ethanol, also called ethyl alcohol, pure alcohol, grain alcohol, or drinking alcohol, is a volatile, flammable, colorless liquid. It is a psychoactive drug and one of the oldest recreational drugs. Best known as the type of alcohol found in alcoholic beverages, it is also used in thermometers, as a...

         (alcohol
        Alcoholic beverage
        An alcoholic beverage is a drink containing ethanol, commonly known as alcohol. Alcoholic beverages are divided into three general classes: beers, wines, and spirits. They are legally consumed in most countries, and over 100 countries have laws regulating their production, sale, and consumption...

        )—also used as a hypnotic, though not medicinally. To quote the British National Formulary
        British National Formulary
        The British National Formulary is a medical and pharmaceutical reference book that contains a wide spectrum of information and advice on prescribing and pharmacology, along with specific facts and details about all medicines available on the National Health Service , including indication,...

        : "Alcohol is a poor hypnotic because its diuretic action interferes with sleep during the latter part of the night. Alcohol also disturbs sleep patterns, and so can worsen sleep disorders."
      • Ethchlorvynol
        Ethchlorvynol
        Ethchlorvynol is a sedative and hypnotic medication developed by Pfizer in the 1950s. It has been used to treat insomnia, but has been largely superseded and is only offered where an intolerance or allergy to other drugs exists....

      • Glutethimide
        Glutethimide
        Glutethimide is a hypnotic sedative that was introduced in 1954 as a safe alternative to barbiturates to treat insomnia. Before long, however, it had become clear that glutethimide was just as likely to cause addiction and caused similarly severe withdrawal symptoms...

      • Methaqualone
        Methaqualone
        Methaqualone is a sedative-hypnotic drug that is similar in effect to barbiturates, a general central nervous system depressant. The sedative-hypnotic activity was first noted by Indian researchers in the 1950s and in 1962 methaqualone itself was patented in the US by Wallace and Tiernan...

      • Valerian
        Valerian (herb)
        Valerian is a hardy perennial flowering plant, with heads of sweetly scented pink or white flowers which bloom in the summer months. Valerian flower extracts were used as a perfume in the sixteenth century....

  • Antihistamine
    Antihistamine
    An H1 antagonist is a histamine antagonist of the H1 receptor that serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions...

    s
    • Diphenhydramine
      Diphenhydramine
      Diphenhydramine hydrochloride is a first-generation antihistamine possessing anticholinergic, antitussive, antiemetic, and sedative properties which is mainly used to treat allergies. Like most other first-generation antihistamines, the drug also has a powerful hypnotic effect, and for this reason...

    • Doxylamine
      Doxylamine
      Doxylamine is one of the many sedating antihistamines used by itself as a short-term sedative, and in combination with other drugs as a night-time cold and allergy relief drug...

    • Hydroxyzine
      Hydroxyzine
      Hydroxyzine is a first-generation antihistamine of the diphenylmethane and piperazine classes. It was first synthesized by Union Chimique Belge in 1956 and was marketed by Pfizer in the United States later the same year, and is still in widespread use today....

    • Promethazine
      Promethazine
      Promethazine is a first-generation antihistamine of the phenothiazine family. The drug has anti-motion sickness, antiemetic, and anticholinergic effects, as well as a strong sedative effect and in some countries is prescribed for insomnia when benzodiazepines are contraindicated...

  • Melatonin agonists
    • Agomelatine
    • Melatonin
      Melatonin
      Melatonin , also known chemically as N-acetyl-5-methoxytryptamine, is a naturally occurring compound found in animals, plants, and microbes...

    • Ramelteon
      Ramelteon
      Ramelteon, marketed as Rozerem by Takeda Pharmaceuticals North America, is the first in a new class of sleep agents that selectively binds to the MT1 and MT2 receptors in the suprachiasmatic nucleus , instead of binding to GABA A receptors, such as with drugs like zolpidem, eszopiclone, and...

  • Mixed MoA
    Mechanism of action
    In pharmacology, the term mechanism of action refers to the specific biochemical interaction through which a drug substance produces its pharmacological effect...

     (antihistamine
    Antihistamine
    An H1 antagonist is a histamine antagonist of the H1 receptor that serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions...

    s, 5-HT2A
    5-HT2A receptor
    The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor . This is the main excitatory receptor subtype among the GPCRs for serotonin , although 5-HT2A may also have an inhibitory effect on certain areas such...

     antagonist
    Receptor antagonist
    A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...

    s, alpha blocker
    Alpha blocker
    Alpha-1 blockers constitute a variety of drugs which block α1-adrenergic receptors in arteries and smooth muscles.-Pharmacology:...

    s, and/or dopamine
    Dopamine
    Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...

     antagonist
    Receptor antagonist
    A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...

    s)
    • Antidepressant
      Antidepressant
      An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...

      s
      • Amitriptyline
        Amitriptyline
        Amitriptyline is a tricyclic antidepressant . It is the most widely used TCA and has at least equal efficacy against depression as the newer class of SSRIs...

      • Doxepin
        Doxepin
        Doxepin is a psychotropic agent with tricyclic antidepressant and anxiolytic properties, known under many brand-names such as Aponal, the original preparation by Boehringer-Mannheim, now part of the Roche group; Adapine, Doxal , Deptran, Sinquan and Sinequan...

      • Mianserin
        Mianserin
        Mianserin is a psychoactive drug of the tetracyclic antidepressant chemical class which is classified as a noradrenergic and specific serotonergic antidepressant and has antidepressant, anxiolytic, hypnotic, antiemetic, orexigenic, and antihistamine effects...

      • Mirtazapine
        Mirtazapine
        Mirtazapine is a tetracyclic antidepressant used primarily in the treatment of depression. It is also sometimes used as a hypnotic, antiemetic, and appetite stimulant, and for the treatment of anxiety, among other indications...

      • Trazodone
        Trazodone
        Trazodone is an antidepressant of the serotonin antagonist and reuptake inhibitor class. It is a phenylpiperazine compound...

      • Trimipramine
        Trimipramine
        Trimipramine is a tricyclic antidepressant . It has antidepressant, anxiolytic, antipsychotic, sedative, and analgesic effects.- Indications :...

    • Antipsychotic
      Antipsychotic
      An antipsychotic is a tranquilizing psychiatric medication primarily used to manage psychosis , particularly in schizophrenia and bipolar disorder. A first generation of antipsychotics, known as typical antipsychotics, was discovered in the 1950s...

      s
      • Chlorpromazine
        Chlorpromazine
        Chlorpromazine is a typical antipsychotic...

      • Olanzapine
        Olanzapine
        Olanzapine is an atypical antipsychotic, approved by the FDA for the treatment of schizophrenia and bipolar disorder...

      • Quetiapine
        Quetiapine
        Quetiapine , is an atypical antipsychotic approved for the treatment of schizophrenia, and bipolar disorder....

      • Risperidone
        Risperidone
        Risperidone is a second generation or atypical antipsychotic, sold under the trade name . It is used to treat schizophrenia , schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in people with autism...

      • Thioridazine
        Thioridazine
        Thioridazine is a piperidine typical antipsychotic drug belonging to the phenothiazine drug group and was previously widely used in the treatment of schizophrenia and psychosis...

    • Others
      • Niaprazine
        Niaprazine
        Niaprazine is a sedative-hypnotic drug of the phenylpiperazine class. It has been used in the treatment of sleep disturbances since the early 1970s in several European countries, including France, Italy, and Luxembourg...

  • Others
    • Cannabis
      Cannabis (drug)
      Cannabis, also known as marijuana among many other names, refers to any number of preparations of the Cannabis plant intended for use as a psychoactive drug or for medicinal purposes. The English term marijuana comes from the Mexican Spanish word marihuana...

    • Opioid
      Opioid
      An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract...

      s
    • Sodium oxybate