Droperidol (Droperidolum)

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

Neuroleptics

Included in the formulation
  • Droperidol
    solution w / m in / in 
    DALHIMFARM, OJSC     Russia
  • Droperidol
    solution for injections 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    N.05.A.D.08   Droperidol

    Pharmacodynamics:

    Antipsychotic agent (neuroleptic), a derivative of butyrophenone. Has antipsychotic, cataleptogenic, sedative, anti-shocks, as well as antiemetic effect.

    The mechanism of antipsychotic action is associated with blockade of dopamine D2receptors of the mesolimbic and mesocortical system. Sedative action is due to adrenoreceptor blockade in the reticular formation of the brainstem, antiemetic effect - blockade of dopamine D2receptors of the trigger zone of the vomiting center, hypothermic action - blockade of dopamine receptors of the hypothalamus.

    It is possible to lower arterial pressure due to the widening of the peripheral vessels and to reduce the overall peripheral vascular resistance; reduces pressure in the pulmonary artery (especially if it is significantly increased) and reduces the pressor effect of epinephrine. Droperidol reduces the incidence of arrhythmia caused by epinephrine, but does not prevent the violation of the heart rhythm of another etiology.

    Does not have anticholinergic activity.

    Pharmacokinetics:

    With intravenous or intramuscular injection, the effect of droperidol develops in 3-10 minutes, the maximum effect is observed after 30 minutes. Sedation lasts 2-4 hours, the total duration of action on the central nervous system can be up to 12 hours.

    Cmax droperidol in plasma is achieved within 15 minutes. Binding to plasma proteins is 85-90%. The half-life period averages 134 minutes. Metabolised in the liver. It is excreted by the kidneys - 75% in the form of metabolites, 1% - unchanged; 11% is excreted through the intestine.

    Indications:

    In surgery: premedication, introductory anesthesia, potentiation of general and regional anesthesia. Neuroleptanalgesia (in combination with fentanyl). Sedation, eliminating nausea and vomiting during diagnostic and surgical procedures, pain and vomiting in the postoperative period.

    In psychiatric practice: psychomotor agitation, hallucinations.

    In therapy: pain and shock in trauma, myocardial infarction, severe attacks of angina pectoris, pulmonary edema; hypertensive crisis.

    ICD-10

    V.F10-F19.F10.4   Mental and behavioral disorders caused by alcohol use - abstinent state with delirium

    XVIII.R40-R46.R45.1   Anxiety and Excitement

    XVIII.R50-R69.R52.0   Acute pain

    XVIII.R50-R69.R52   Pain, not elsewhere classified

    XVIII.R50-R69.R57.0   Cardiogenic shock

    XVIII.R50-R69.R57   Shock, not elsewhere classified

    XIX.T36-T50.T50.9   Poisoning with other and unspecified drugs, medicines and biological substances

    XIX.T51-T65.T65   Toxic effect of other and unspecified substances

    Contraindications:

    Hypersensitivity to droperidol and morphine derivatives. Extrapyramidal disorders, severe depression, coma, caesarean section administration, hypokalemia, arterial hypotension, QT interval prolongation syndrome, early childhood (up to 2 years).

    Carefully:

    Hepatic and / or renal failure, alcoholism, decompensated chronic heart failure, epilepsy, depression, pregnancy.

    In elderly patients, the initial dose of droperidol should be reduced. Raising the dose, it is necessary to be guided by the already obtained effect.

    Pregnancy and lactation:

    Recommendations FDA category C. Possible premature birth, in newborns - weight loss. Use in pregnancy is possible only in cases where the intended use for the mother exceeds the potential risk to the fetus.

    Butyrophenones are excreted with milk and are not recommended for use during lactation. If it is necessary to use droperidol in the mother, breastfeeding should be discontinued.

    Dosing and Administration:

    Individually, taking into account the age, body weight, general physical condition, the nature of the disease, the medicines used, the type of anesthesia to be performed.

    For premedication to adults, the drug is administered intramuscularly 15-45 minutes before the beginning of the surgical intervention in a dose of 2.5-5 mg.

    For pain and vomiting in the postoperative period, adults are prescribed intramuscularly 2.5-5 mg every 6 hours.

    For introduction into anesthesia - intravenously in a dose of 15-20 mg.

    Side effects:

    From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): moderate arterial hypotension and tachycardia, which, as a rule, do not require special therapy. In very rare cases, hypertension is observed (most likely with the combined use of droperidol with fentanyl or other analgesics administered parenterally).

    From the nervous system and sensory organs: dysphoria,drowsiness in the postoperative period; when used in high doses - anxiety, fear, increased excitability, extrapyramidal disorders; there are reports of post-operative hallucinations (sometimes associated with transient periods of depression).

    From the digestive system: nausea, loss of appetite, dyspeptic phenomena; rarely - jaundice, transient disorders of liver function.

    Allergic reactions: rarely - anaphylactic reactions, dizziness, tremor, laryngospasm, bronchospasm.

    Overdose:

    Difficulty in breathing, coma, trembling, twitching, muscle stiffness or uncontrolled movements. Treatment is symptomatic. When respiratory depression - artificial ventilation. To maintain blood pressure - intravenous injection of plasma (albumin solution), norepinephrine. Epinephrine in these cases, use is strictly prohibited!

    Akathisia, dystonia, hypotension, increased QT interval, respiratory depression. Treatment: benzthropine or diphenhydramine (to eliminate extrapyramidal reactions); ensuring airway patency (with respiratory depression - artificial ventilation); the fight against hypotension and collapse (intravenous fluids), phenylephrine (to overcome the α-adrenoblocking effects of droperidol).

    Interaction:

    With the combined administration of droperidol with fentanyl or other parenteral analgesics, an increase in blood pressure is possible (regardless of the presence / absence of previous arterial hypertension).

    Alcohol, CNS depressant drugs - increased CNS depression, respiration and hypotensive effect.

    Anesthetics (parenteral, topical) - peripheral vasodilation, hypotension.

    Bromocriptine, levodopa - blockade of dopamine receptors, reduction of therapeutic effect.

    Propofol - decreased antiemetic activity of propofol.

    Means that cause hypotension - severe hypotension.

    Means that cause extrapyramidal reactions (metoclopramide) - increased severity and frequency of extrapyramidal effects.

    Epinephrine - an increase in the hypotensive effect.

    Special instructions:

    In elderly, feeble-minded and weakened patients, it is possible to develop excessive sedation, prolongation of the QT interval, hypotension, increased prolactin concentration in the blood; recommended the appointment of a lower initial dose.

    Monitoring: extrapyramidal effects and ECG (for diagnosis of QT interval elongation or signs of flutter / fibrillation of the ventricles).

    Do not use as the sole means for inducing anesthesia in surgery.

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