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  • Benzodiazepines: Mechanism of Action

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    Ariane Benina
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    Barbiturates and benzodiazepines both act in the brainstem to depress the reticular activating system. They bind to GABA-A receptors, increasing the duration that chloride ion channels remain open. Benzodiazepines can be reversed by flumazenil, which is an antagonist that counters their central nervous system effects. Diazepam and lorazepam are insoluble in water, so parental preparations contain propylene glycol which can cause venous irritation. Barbiturates and benzodiazepines are absorbed orally, intramuscularly, or intravenously, reaching peak plasma levels within 1-2 hours. They are also used intranasally or via

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    obat2an anestesi

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    OBAT2AN

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    Barbiturates and benzodiazepines both act in the brainstem to depress the reticular activating system. They bind to GABA-A receptors, increasing the duration that chloride ion channels remain open. Benzodiazepines can be reversed by flumazenil, which is an antagonist that counters their central nervous system effects. Diazepam and lorazepam are insoluble in water, so parental preparations contain propylene glycol which can cause venous irritation. Barbiturates and benzodiazepines are absorbed orally, intramuscularly, or intravenously, reaching peak plasma levels within 1-2 hours. They are also used intranasally or via

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    © All Rights Reserved
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    5 views2 pages

    Benzodiazepines: Mechanism of Action

    Uploaded by

    Ariane Benina
    Barbiturates and benzodiazepines both act in the brainstem to depress the reticular activating system. They bind to GABA-A receptors, increasing the duration that chloride ion channels remain open. Benzodiazepines can be reversed by flumazenil, which is an antagonist that counters their central nervous system effects. Diazepam and lorazepam are insoluble in water, so parental preparations contain propylene glycol which can cause venous irritation. Barbiturates and benzodiazepines are absorbed orally, intramuscularly, or intravenously, reaching peak plasma levels within 1-2 hours. They are also used intranasally or via

    Copyright:

    © All Rights Reserved
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    of 2

    BARBITURATES

    MECHANISM OF ACTION
     Depress RAS in brainstem
     Bind to GABAA receptor, increasing duration opening of CL-
    specific ion channel

    BENZODIAZEPINES

    MECHANISM OF ACTION
     Depress RAS in brainstem
     OBat yang antagonist & reverses CNS effects dari benzo 
    Flumazenil
     Diazepam and lorazepam insoluble in water  parental prep
    ada propylene glycol, bisa bikin venous irritation

    PHARMACOKINETICS
     ABSORPTION
    o Orally, IM, IV
    o Peak plasma levels  1 and 2h
    o Intranasal 0.2-0.3 mg/kg, Bucca (0.07 mg/kg),
    sublingual (0.1 mg/kg) buat PREOPERATIVE sedation
    o Intramuscular Diazepam  painful + gak teralu diabsorb
    tapi Midazolam & Lorazepam well absorb peak 30-90
    min
     DISTRIBUTION
    o Diazepam lipid soluble and penetrates BBB
    o Initial half life distribution  3-10 menit
     BIOTRANSFORMATION
    o Liver for biotransformation

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