Droperidol - instructions for use, dose, side effects, contraindications

Active substanceDroperidolDroperidol

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Droperidol

solution w / m in / in

DALHIMFARM, OJSC Russia

Droperidol

solution for injections

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Dosage form: & nbspinjection

Composition:

1 ml of the 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:

DROPERIDOL refers to neuroleptic drugs, a derivative of butyrophenone. Has a high neuroleptic activity, it also has a pronounced tranquilizing, sedative, anti-shocks, hypothermic, antiarrhythmic and antiemetic effects. Causes extrapyramidal disorders, has a pronounced cataleptogenic activity. Does not have anticholinergic activity.

The main effects are due to the effect of the drug on the dopaminergic structures of the brain, mainly on 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 increases the duration and intensity of the effects of sleeping pills, narcotics, analgesics, local anesthetic, 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.

With the influence on peripheral alpha-adrenergic receptors, the expansion of blood vessels caused by the drug and the reduction of the overall peripheral resistance, as well as the reduction of pressure in the pulmonary artery (especially if it is high) are associated with a decrease in the pressor effect of epinephrine and norepinephrine.

DROPERIDOL relieves arrhythmia-induced arrhythmia, but does not prevent cardiac arrhythmias of another etiology.

Pharmacokinetics:

With intravenous or intramuscular injection, the drug comes in 5-15 minutes, the maximum effect is achieved after 30 minutes. Binding to plasma proteins is 85-90%, half-life is 120-130 minutes. Neuroleptic, tranquilizing and sedative effects of the drug last 2-4 hours, but in a different degree of pronounced general inhibitory effect on the central nervous system can reach a duration of 12 hours.

It is excreted by the kidneys in the form of metabolites (75%), 1% unchanged; 11% is excreted through the intestine.

Indications:

Premedication before anesthesia, anesthesia, potentiation of the effects of drugs in general and regional anesthesia.

Neuroleptanalgesia (in combination with opioid 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 and shock (with trauma, myocardial infarction, severe attacks of angina pectoris, burns).

Pulmonary edema.

For relief of hypertensive crises.

Contraindications:

- Increased individual sensitivity to the drug;

- coma;

- extrapyramidal disorders;

- cesarean section;

- hypokalemia;

- arterial hypotension;

- lengthening interval syndrome QT;

- Children's age (up to 3 years).

Carefully:

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

Pregnancy and lactation:

During pregnancy droperidol are used in case of emergency, when the therapeutic effect justifies the possible risk of use.

When using droperidol during lactation, breast-feeding should be discontinued.

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, the medicines used, the type of anesthesia.

Droperidol is used subcutaneously, 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 the operation in a dose 2,5-10 mg (1-4 ml). The dose is determined individually.

General anesthesia. For the introduction into anesthesia use Droperidol intravenously in a dose 2,5 mg (1 ml) per 10 kg of body weight in combination with analgesics and / or 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 the use of general anesthesia. Droperidol 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. Children aged 3 to 12 years Droperidol use in reduced dosages - 1-1.5 mg (0.4-0.6 ml) per 10 kg of body weight for the purpose of premedication or to provide an initial anesthesia.

The safety of the use of droperidol for children under 3 years is not confirmed!

Before use, visual inspection of the injection solution of droperidol should be carried out. Do not use a solution that has lost transparency, has acquired a colored color, and also a solution from depressurized packaging.

Side effects:

Arterial hypotension of medium severity and tachycardia, which can be stopped without special therapy.

Possible dysphoria, drowsiness in the postoperative period and, conversely, when using elevated doses - anxiety, motor irritability, fear. Sometimes extrapyramidal symptoms are observed, which should be stopped with anticholinergics.

Less common are anaphylaxis, dizziness, tremor, laryngospasm, bronchospasm.

In very rare cases, there is hypertension and tachycardia - with the combined use of droperidol with fentanyl or other analgesics administered parenterally.

In some cases, during the postoperative period, hallucinations and depression are possible.

Possible nausea, loss of appetite, dyspeptic phenomena; rarely - jaundice, transient liver dysfunction, allergic reactions.

Overdose:

Symptoms of overdose are due to the pharmacological action of the drug.

Symptoms: a sharp drop in blood pressure.

Treatment: decrease in blood pressure is eliminated by analeptics and sympathomimetic means.To eliminate extrapyramidal symptoms, the use of antiparkinsonian agents is necessary.

In the 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 severe or prolonged hypotension, in order to avoid hypovolemia, infusion therapy should be used.

Interaction:

Droperidol enhances the action of other agents that depress the central nervous system (eg, barbiturates, tranquilizers, opioids, general anesthetics). 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 displays antagonism with regard to epinephrine and other sympathomimetic agents.

Droperidol potentiates the action of antihypertensive agents.

As droperidol blocks dopamine receptors, it can inhibit the action of dopamine 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, one should foresee the possibility of developing arterial hypotension and have the means to timely correct it.

Patients receiving Droperidol, should be under close medical supervision.

Initial doses of droperidol should be reduced to elderly patients, physically weakened and others with a high degree of risk. Raising the dose of the drug, it is necessary to be guided by the already obtained effect.

It should be borne in mind that the doses of opioids 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. It should immediately begin appropriate therapy, if there is a rise in temperature, increased heart activity and hypercapnia.

It should be taken into account that high doses of droperidol (25 mg or more) in patients with risk of cardiac arrhythmia against hypoxia, electrolyte imbalance or alcohol withdrawal can cause sudden death.

With some types of conductive anesthesia (eg spinal, peridural), the blockade of the intercostal nerves and sympathetic inertia are possible, which in turn makes breathing more difficult, contributes to the expansion of peripheral vessels and the development of hypotension. Droperidol, in turn, also affects blood circulation. Therefore, in cases where droperidol use in addition to these types of anesthesia, the anesthetist should foresee possible changes and carry out careful monitoring of vital body functions.

Hypotension may be accompanied by hypovolemia, so infusion therapy is necessary to prevent it. 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. However, if this complication can not be prevented by parenteral administration of fluids, pressor means should be administered, with the exception of epinephrine, which, after the administration of droperidol, can significantly reduce pressure.

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.

The parameters of the physiological state of the organism should be closely monitored. It should be emphasized that changes in the EEG after the operation disappear slowly.

The drug should be used with caution in patients with impaired liver and kidney function.

In patients with pheochromocytoma after the administration of droperidol, severe hypertension and tachycardia can be observed.

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

After the application of droperidol, it is not recommended for patients to perform work that requires quick reaction and associated risks, for example, to drive vehicles within 24 hours.

Form release / dosage:

Solution for injection, 2.5 mg / ml.

Packaging:

By 2 ml or 5 ml into neutral glass ampoules of grade НС-1 or НС-3 or imported from glass of the first hydrolytic class.

5 ampoules per circuit cell packaging made of polyvinylchloride film and foil of aluminum printed lacquered or flexible packaging on the basis of aluminum foil.

For 1 or 2 contour packs with instruction on the use of the drug, a knife or scarifier ampullum in a pack of cardboard.

For 20, 50 or 100 contour cell packs with 20, 50 or 100 instructions for use, respectively, with knives or scarifiers ampouled into boxes of cardboard or in boxes of corrugated cardboard.

When packing ampoules with notches, rings or break points, knives or scarifier ampoules do not.

For 5 ml in bottles made of glass-grade НС-3 glass tube or imported from glass of the first hydrolytic class.

5 bottles per circuit pack of polyvinylchloride film and foil of aluminum printed lacquered or flexible packaging on the basis of aluminum foil.

1 circuit cell pack with instructions for the use of the drug in a pack of cardboard.

For 30 or 50 contour squares with 30 or 50 instructions for the use of the drug, respectively, in boxes of cardboard or in boxes of corrugated cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Shelf life:

3 years.

Do not use after expiration date, indicated on the package.

Terms of leave from pharmacies:For hospitals

Registration number:P N000369 / 01

Date of registration:17.04.2007 / 23.10.2013

The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia

Manufacturer: & nbsp

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Representation: & nbspMOSCOW ENDOCRINE FACTORY FGUP MOSCOW ENDOCRINE FACTORY FGUP Russia

Information update date: & nbsp20.01.2016

Illustrated instructions

Instructions

Droperidol (Droperidol)