Droperidol (Droperidol)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
Read on
Active substanceDroperidolDroperidol
Similar drugsTo uncover
  • Droperidol
    solution w / m in / in 
    DALHIMFARM, OJSC     Russia
  • Droperidol
    solution for injections 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
    • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    In 1 ml of solution contains:

    active substance: droperidol 2.5 mg;

    Excipients: tartaric acid to pH 3.3 (about 1.5 mg), water for injection up to 1 ml.

    Description:Transparent, colorless or slightly colored liquid.
    Pharmacotherapeutic group:antipsychotic agent (antipsychotic)
    ATX: & nbsp

    N.05.A.D.08   Droperidol

    Pharmacodynamics:

    Antipsychotic agent (neuroleptic), a derivative of butyrophenone. It also has sedative, anti-shocks, antiemetic, hypothermic, antihypertensive and antiarrhythmic effects.

    The antipsychotic effect is due to the blockade of dopamine D2receptors of the mesolimbic and mesocortical system.

    Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brain stem.

    Droperidol enhances the duration and intensity of the action of hypnotics, narcotic and non-narcotic analgesics, local anesthetics, anticonvulsants and alcohol.

    Antiemetic effect due to blockade of dopamine D2receptors of the trigger zone of the vomiting center.

    Hypothermic effect is due to blockade of dopamine receptors of the hypothalamus.

    Droperidol dilates peripheral vessels and reduces overall peripheral vascular resistance; reduces the pressure in the pulmonary artery (especially if it is significantly increased) and reduces the pressor effect of adrenaline.

    Reduces the incidence of arrhythmias caused by adrenaline, but does not prevent cardiac arrhythmias of another etiology.

    Has a strong catalepogenic activity.

    With intravenous or intramuscular injection, the effect occurs after 5-15 minutes, the maximum effect is achieved after 30 minutes; sedation lasts 2-4 hours, the total duration of action on the central nervous system is 12 hours.
    Pharmacokinetics:

    Time to reach the maximum concentration in the plasma - after 15 minutes. Binding to plasma proteins is 85-90%, half-life is 120-130 min. Metabolism is in the liver. It is excreted by the kidneys in the form of metabolites - 75%, unchanged by kidneys - 1%, through the intestine - 11%.

    Indications:

    Premedication before general anesthesia, introductory anesthesia, potentiation of the action of drugs with general and local anesthesia.

    Neuroleptanalgesia (in combination with narcotic analgesics, more often with fentanyl).

    Providing a sedative effect, preventing nausea and vomiting during diagnostic and surgical manipulation.

    Pain and vomiting in the postoperative period, psychomotor agitation, hallucinations.

    Pain syndrome; pain shock in injuries.

    Contraindications:

    Increased individual sensitivity to the drug, coma, extrapyramidal disorders, caesarean section, hypokalemia, arterial hypotension, pregnancy, children's age (up to 3 years).

    Carefully:

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

    Pregnancy and lactation:

    Use in pregnancy is possible only in cases where the intended use for the mother exceeds the potential risk to the fetus.

    For the duration of treatment, stop breastfeeding.

    Dosing and Administration:

    The administered dose of droperidol should be determined individually, taking into account the age of the patient, the weight of his body, the general physical condition, the nature of the disease, concomitantly used drugs, the type of anesthesia.

    Droperidol is used intramuscularly and intravenously. When administering the drug, you should monitor the vital physiological functions of the body.

    Premedication. Droperidol injected intramuscularly for 30-60 minutes before surgery at a dose of 2.5-10 mg (1-4 ml). The dose is determined individually.

    General anesthesia. For the introduction into anesthesia use Droperidol intravenously at a dose of 2.5 mg (1 ml) per 10 kg of body weight in combination with narcotic analgesics and / or means for general anesthesia. In a number of cases, smaller doses may be used. The total dose of droperidol is determined individually.

    During the operation, the maintenance dose of droperidol is 1.25-2.5 mg (0.5-1.0 ml) intravenously.

    The use of droperidol in diagnostic procedures without general anesthesia. Droperidol is administered intramuscularly at a dose of 2.5-10 mg (1-4 ml) for 30-60 minutes before the procedure. Additionally droperidol can be administered intravenously at a dose of 1.25-2.5 mg (0.5-1 ml). (Some procedures, like bronchoscopy, require the use of local anesthesia.)

    Local anesthesia. To provide an additional sedative effect Droperidol injected intramuscularly or intravenously slowly at a dose of 2.5-5 mg (1-2 ml).

    For relief of hypertensive crises. Droperidol administered at a dose of 2.5-5 mg (1-2 ml) intravenously or intramuscularly, if necessary simultaneously with other agents. Injections can be repeated after 45-90 minutes.

    The use of droperidol in pediatric practice. For premedication, children aged 3 years are prescribed Droperidol in a dose of 100-150 μg / kg of body weight. For introductory anesthesia intravenously at a dose of 200-400 μg / kg body weight or intramuscularly at a dose of 300-600 μg / kg body weight.

    Side effects:

    Decrease in arterial pressure of average severity and tachycardia, which can be stopped without special therapy.

    Possible dysphoria, drowsiness in the postoperative period and, on the contrary, with the use of increased doses - anxiety, motor excitability, fear; extrapyramidal symptoms, which should be quenched with anticholinergics.

    Anaphylaxis, dizziness, tremor, laryngospasm, bronchospasm.

    Increased blood pressure and tachycardia - with the combined use of droperidol with fentanyl or other narcotic analgesics administered parenterally.

    In the postoperative period, hallucinations and depression are possible.

    Overdose:

    Overdose Symptoms are caused by the pharmacological action of the drug. Reduction of blood pressure is eliminated by analeptics and sympathomimetic agents.

    Treatment extrapyramidal symptoms are carried out by m-holinoblokatorami. In case of respiratory failure, oxygen and provide artificial ventilation. A careful monitoring of the body's condition is necessary for 24 hours. The patient should be warmed, warm solutions should be introduced into the body. With the development of a severe or prolonged reduction in blood pressure, infusion therapy should be used to avoid hypovolemia.

    Interaction:

    Droperidol strengthens the action of other drugs that depress the central nervous system (barbiturates, tranquilizers, narcotic analgesics, funds for general anesthesia). This should be provided by choosing the dose of medicines: the dose of droperidol should be reduced if other depressants of the central nervous system were applied and, conversely, the doses of other agents that depress the central nervous system should be reduced after the administration of droperidol.

    Droperidol exhibits antagonism against the pressor action of epinephrine and other sympathomimetic agents.

    Droperidol potentiates the action of antihypertensive drugs.

    As droperidol blocks dopamine receptors, it can inhibit the action of dopamine receptor agonists.

    With simultaneous application with droperidol anticonvulsants may require an increase in the dose of the latter.

    Special instructions:

    Droperidol is used only in a hospital.

    When using droperidol should anticipate the possibility of reducing blood pressure and have the means to timely correct it.

    Patients receiving droperidol, should be under medical supervision.

    Initial doses of droperidol should be reduced in elderly patients and physically impaired.

    Increasing the dose of the drug should be guided by the effect already obtained.

    It should be borne in mind that the doses of narcotic analgesics used together with droperidol should be reduced.

    Droperidol rarely causes a malignant neuroleptic syndrome.

    In the pre-operative period, the diagnosis of neuroleptic hyperthermia is difficult.

    Immediately begin appropriate therapy (for example, apply dantrolene), if there is a rise in temperature, increased heart activity and increased formation of carbon dioxide.

    High doses of droperidol (25 mg or more) in patients at risk of arrhythmia against hypoxia, electrolyte imbalance, or alcohol withdrawal can cause sudden death.

    With some types of conductive anesthesia (for example, spinal, peridural), blockade of the intercostal nerves and sympathetic innervation are possible, which in turn makes breathing more difficult, contributes to the expansion of peripheral vessels and lowering blood pressure. Droperidol, in turn, also affects blood circulation; therefore, in those cases when droperidol are used in addition to these types of anesthesia, the anesthetist should foresee possible changes and carry out careful monitoring of vital body functions.

    Reducing blood pressure may be accompanied by hypovolemia, so to prevent it requires infusion therapy. The patient should be put in such a way as to improve the venous influx to the heart.During spinal or epidural anesthesia, care should be taken that the patient's head does not hang down - this position increases the effect of anesthesia and worsens the venous circulation.

    To avoid orthostatic hypotension, care should be taken when transporting the patient, you can not quickly change the position of his body.

    Droperidol can reduce the pressure in the pulmonary artery. This should be borne in mind during surgical and diagnostic procedures to determine the further treatment of the patient.

    In patients with pheochromocytoma after the administration of droperidol, there may be a sharp increase in blood pressure and tachycardia.

    Effect on the ability to drive transp. cf. and fur:

    When treating the drug, patients are advised not to perform a work that requires quick reaction and associated risks, for example, to drive vehicles within 24 hours.

    Form release / dosage:

    Solution for intravenous and intramuscular injection, 2.5 mg / ml.

    Packaging:

    2 ml, 5 ml in neutral glass ampoules.

    For 10 ampoules together with a vial for opening ampoules or a scarifier ampoule and instructions for use in a cardboard box.

    5 ampoules in a contour cell box made of polyvinylchloride film and aluminum foil printed lacquered. 2 contoured cell packs together with an ampoule opener or an ampoule scaler and an instruction for use in a pack of cardboard. When using ampoules with notches, rings and dots, the ampoule scaper or ampoule opener is not inserted.

    Storage conditions:

    In the dark place at a temperature of 8 to 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-000492
    Date of registration:01.03.2011
    The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspDALHIMFARM, OJSCDALHIMFARM, OJSC
    Information update date: & nbsp20.01.2016
    Illustrated instructions
      Instructions
      Up