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    Sedative-hypnotic drugs like benzodiazepines, barbiturates, and others produce dose-dependent central nervous system depression, causing sedation which reduces anxiety and hypnosis which induces sleep. They are well absorbed from the gastrointestinal tract and distributed to the brain. Most are metabolized in the liver, and some benzodiazepines form active metabolites. Their effects range from sedation and relief of anxiety to hypnosis, anesthesia, and coma depending on dose. They are used to treat anxiety, sleep disorders, and seizures, and for anesthesia induction. Toxicity includes cognitive impairment, decreased psychomotor skills, and overdose can cause severe respiratory and cardiovascular depression.

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    Sedative-hypnotic drugs like benzodiazepines, barbiturates, and others produce dose-dependent central nervous system depression, causing sedation which reduces anxiety and hypnosis which induces sleep. They are well absorbed from the gastrointestinal tract and distributed to the brain. Most are metabolized in the liver, and some benzodiazepines form active metabolites. Their effects range from sedation and relief of anxiety to hypnosis, anesthesia, and coma depending on dose. They are used to treat anxiety, sleep disorders, and seizures, and for anesthesia induction. Toxicity includes cognitive impairment, decreased psychomotor skills, and overdose can cause severe respiratory and cardiovascular depression.

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    109 views21 pages

    Sedative Hypnotic Drugs

    Uploaded by

    tama
    Sedative-hypnotic drugs like benzodiazepines, barbiturates, and others produce dose-dependent central nervous system depression, causing sedation which reduces anxiety and hypnosis which induces sleep. They are well absorbed from the gastrointestinal tract and distributed to the brain. Most are metabolized in the liver, and some benzodiazepines form active metabolites. Their effects range from sedation and relief of anxiety to hypnosis, anesthesia, and coma depending on dose. They are used to treat anxiety, sleep disorders, and seizures, and for anesthesia induction. Toxicity includes cognitive impairment, decreased psychomotor skills, and overdose can cause severe respiratory and cardiovascular depression.

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    © All Rights Reserved
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    SEDATIVE-HYPNOTIC DRUGS

    Department of Pharmacology
    Medical School of Malahayati
    University

    Sedative Hypnotic Drugs


    The sedative-hypnotic produce dose
    dependent CNS depressant effect
    Sedation
    : Reduction of anxiety
    Hypnosis
    : Induction of sleep
    Subgroup
    :
    - Benzodiazepine (Chlordiazepoxide,
    diazepam,
    temazepam)
    - Barbiturat (Phenobarbital, pentobarbital,
    thiopental)
    - Others (buspirone, zolpidem,
    chloralhydrate,
    zaleplon)

    Sedative Hypnotic Drugs


    Benzodiazepine :
    - short acting (triazolam)
    - intermediate acting (estazolam,
    temazepam)
    - long acting (flurazepam,
    quazepam)

    Sedative Hypnotic Drugs


    Barbiturates :
    - Ultra short acting
    - Short acting
    - Long acting

    Sedative Hypnotic Drugs


    (Pharmacokkinetics)
    All sedative hypnotic are lipid
    soluble and absorbed well from GI
    tract
    Good distribution to the brain in
    oral administration

    Sedative Hypnotic Drugs


    (Metabolism and Excretion)
    Metabolized mainly by hepatic
    enzymes
    Many benzodiazepine are converted
    to active metabolites
    Accumulation of active metabolites
    can lead to excessive sedation
    The barbiturates are extensively
    metabolized,except phenobarbital

    Sedative Hypnotic Drugs


    (Mechanisms of Action)
    BENZODIAZEPINES
    Receptors for benzodiazepines (BZ
    receptors) are present in the
    thalamus,limbic structures,and the
    cerbralcortex.
    Binding of Benzodiazepines facilitates the
    inhibitory actions of GABA,which are exerted
    through increased chloride ion conductance.
    GABA is the major inhibitoric
    neurotransmitter in the CNS

    Sedative Hypnotic Drugs


    (Mechanisms of Action)
    Barbiturates
    Barbiturates depress neuronalactivity in the
    midbrain reticular formation, facilitating and
    prolonging the inhibitory effects of GABA
    Other drugs
    Mechanism of anxiolytic effect of buspirone
    is unknown, but buspirone interact with the
    5-HT as partial agonist
    Zolpidem & zaleplon interact with BZ1 bind
    selectively with GABAA receptor

    Sedative Hypnotic Drugs


    (Pharmacodynamics)
    The CNS effect depend on dose
    Effects : sedation & relief of anxiety,
    through hypnosis (facilitation of sleep) to
    anesthesia and coma
    When 2 or more drugs are given
    togetherdepressant effect +++
    Sedation : sedative action with relief of
    anxiety
    Hypnosis : promote sleep onset and
    duration of the sleep state

    Sedative Hypnotic Drugs


    (Pharmacodynamics)
    Anesthesia : conscious with amnesia &
    supressions of reflexes (at highdose). Can
    produce by most barbiturates
    (eg,thiopental) & certain benzodiazepines
    (eg,midazolam)
    Anticonvulsant actions : supression of
    seizure activity (high dose),usually
    accompany by sedation effect.
    Selective anticonvulsant (supression of
    convulsion at dose that do not cause severe
    sedation is Phenobarbital, clonazepam

    Sedative Hypnotic Drugs


    (Pharmacodynamics)
    Muscle relaxation : relaxation of skeletal
    muscle (at high dose)
    Diazepam at sedative dose effective for
    spasticity states
    Selective muscle relaxant : Meprobomate
    Medullary depression :
    High dose can cause depression of
    medullarry neurons,leading to respiratory
    arrest, hypotension & CV collapse death

    Sedative Hypnotic Drugs


    (Pharmacodynamics)
    Tolerance& dependence :
    tolerance a decrease in responsiveness,
    occurs when used chronically or in high dose
    physiologic dependence an altered state
    that leads to an abstinence syndrome
    (withdrawal state) when the drug is
    discontinued
    Sign : anxiety, tremors,hyperreflexia, seizure

    Sedative Hypnotic Drugs


    (Clinical Uses)
    Anxiety states (alprazolam, clonazepam,
    buspirone)
    The anxiolityc effect of buspirone occur
    without sedation or cognitive impairment
    Sleep disorder (estazolam,flurazepam,
    triazolam)
    Induction of anesthesia (thiopental,
    diazepam, midazolam)
    Management of seizure disorders
    (clonazepam,phenobarbital)

    Sedative Hypnotic Drugs


    (Clinical Uses)
    Management of withdrawal states
    in persons physiologically
    dependent on ethanol & sedative
    hypnotics (chlordiazepoxide,
    diazepam)

    Sedative Hypnotic Drugs


    (Toxicity)
    Cognitive impairment

    Decreased psychomotor skills


    Unwanted daytime sedation
    Anterograde amnesia
    Additive CNS depression
    when used with other drugs in the class
    (antihistamines,antipsychotic drugs, opioid
    analgesics, tricyclic antidepressants)
    Overdosage severe respiratory & CV depression
    Flumazenil may reverse CNS depressant effect of
    benzodiazepines, zolpidem & zaleplon

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