Dexmedetomidine (Dexmedetomidinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
Read on
Clinical and pharmacological group: & nbsp

Sedatives

Included in the formulation
  • Dexdor®
    concentrate d / infusion 
    Orion Corporation Orion Pharma     Finland
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    N.05.C.M   Other sleeping pills and sedatives

    N.05.C.M.18   Dexmedetomidine

    Pharmacodynamics:

    The drug is a highly selective agonist α2-adrenergic receptors of a wide spectrum of action. Is strong sympatholytic Effect by reducing the release of norepinephrine from the presynaptic endings of the sympathetic nerves. It also has a sedative effect, which is associated with a decrease in the excitation of the blue spot - the main noradrenergic nucleus, which is located in the brainstem, while simultaneously allowing the patient to be in an awakened and active state.

    Dexmedetomidine has moderate anesthetic and anesthetic effect. Low doses have a central effect, which manifests itself in a decrease in heart rate and blood pressure, and high doses have a peripheral vasoconstrictive effect.

    The effect on the cardiovascular system depends on the speed of administration: at lower infusion rates, the central effect on the nucleus of the solitary tract dominates, which leads to activation of the vagus nerve and a decrease in heart rate and blood pressure.At a higher rate of administration, the drug activates extra-synaptic α2-adrenergic receptors of peripheral vessels, as a result, peripheral vasoconstrictive effects predominate, which leads to an increase in systemic vascular resistance and arterial pressure, while bradycardia becomes more pronounced.

    Dexmedetomidine has practically no inhibitory effect on the respiratory system.

    Pharmacokinetics:

    The connection with plasma proteins is 94%, metabolized in the liver, half-life - 1.5 hours.

    Indications:

    The drug is used to achieve a sedative effect during or after intubation in the intensive care unit.

    ICD-10

    VI.G90-G99.G96.9   Disorder of central nervous system, unspecified

    VI.G90-G99.G97.9   Nervous system disorder after medical procedures, unspecified

    VI.G90-G99.G99.8 *   Other specified disorders of the nervous system in diseases classified elsewhere

    XXI.Z40-Z54.Z51.4   Preparatory procedures for subsequent treatment, not elsewhere classified

    Contraindications:

    Hypersensitivity.

    Carefully:

    Violation of the function of the liver, a violation of the activity of the autonomic nervous system.

    Use with caution in combination with other drugs that have a sedative effect or affect the cardiovascular system, because of the risk of developing additive effects.

    In patients with severe bradycardia, progressive blockade of the heart (AV blockade II-III degree, except when the pacemaker is used), arterial hypotension or in patients with severe ventricular dysfunction, with hypovolemia, chronic arterial hypertension, in elderly patients.

    Pregnancy and lactation:

    Category FDA - C. Dexmedetomidine should not be used during pregnancy, except when the expected benefit to the mother exceeds the risk to the fetus. The potential risk to humans is unknown.

    For the period of application, breastfeeding should be discontinued.

    Dosing and Administration:

    Enter intravenously in the form of infusion.

    Adults in the period after intubation intravenously - 0,7 mkg / kg / h to achieve the desired level of sedation.

    To quickly achieve a sedative effect, first 1.5-3 μg / kg / h for 20 minutes, and then 0.4 μg / kg / h.

    Side effects:

    From the cardiovascular system: bradycardia, ischemia / myocardial infarction, tachycardia, hypertension, reduction in cardiac output, AV-blockade I degree.

    From the respiratory system: dyspnea.

    From the gastrointestinal tract: vomiting, nausea, dry mouth, bloating.

    From the side of metabolism: hypoglycaemia, hyperglycemia, hypoalbuminemia, metabolic acidosis.

    From the nervous system: hallucinations, agitation.

    Other: thirst, withdrawal syndrome, hyperthermia.

    Overdose:

    Bradycardia, excessive sedation, arterial hypotension, cardiac arrest, drowsiness. Treatment - dose reduction or drug withdrawal.

    Interaction:Anesthetics, sedatives, opioids and hypnotics, sevoflurane, propofol, isoflurane, midazolam, alcohol ethyl, alfentanil potentiate the sedative effect of dexmedetomidine.
    Special instructions:

    Only for use in intensive care units.

    During the administration of the drug, it is necessary to monitor the function of the heart and respiratory function.

    Do not use during work drivers of vehicles and people whose activities require a quick mental and physical reaction, and is also associated with increased concentration of attention.

    Instructions
    Up