Side effects of droperidol. The neuroleptic antipsychotic drug Droperidol is a very strong anesthetic drug. Release form and cost of the medicine

Droperidol is an antipsychotic drug used for premedication.

Release form and composition

Droperidol is produced in the form of a colorless or slightly greenish transparent solution for injection, in glass ampoules of 2 and 5 ml. The composition of 1 ml of solution includes 2.5 mg of droperidol and excipients - methylparaben, propyl parahydroxybenzoate, tartaric acid and water for injection.

Indications for use

Droperidol is prescribed for induction of anesthesia, premedication, and also in cases of:

• Pulmonary edema;
• General and regional anesthesia (for their potentiation);
• Hypertensive crisis;
• Neuroleptanalgesia (in combination with fentanyl or other opioids);
• The appearance of pain and vomiting in the postoperative period;
• Surgical and diagnostic procedures to exclude nausea and vomiting;
• The appearance of hallucinations, psychomotor agitation, pain and shock during myocardial infarction, burns, injuries and severe attacks of angina.

Contraindications

The use of Droperidol is contraindicated in children under 2 years of age, with hypersensitivity to the components included in the product, as well as in the following cases:

• Hypokalemia;
• Long Q-T interval syndrome;
• Arterial hypotension;
• Extrapyramidal disorders;
• Carrying out a caesarean section.

Droperidol should be prescribed with caution to patients suffering from alcoholism, renal or liver failure, depression, epilepsy, pregnancy and decompensated chronic heart failure.

Directions for use and dosage

The solution is administered intramuscularly or intravenously. The dosage of Droperidol is determined individually depending on the type of anesthesia to be performed, the nature of the disease, concomitantly used drugs, as well as the age, general physical condition and body weight of the patient,

Typically, adults are administered intramuscularly with 2.5-5 mg of solution for premedication over 15-45 minutes. before surgery, children - 100 mcg per 1 kg of body weight.

To maintain anesthesia in cases of prolonged operations, 2.5-5 mg of Droperidol is administered intravenously.

When injecting adults into anesthesia, 15-20 mg of solution is administered intravenously. For children, the dose is determined based on the calculation - 0.2-0.4 mg of the drug per 1 kg of body weight, or the drug is administered intramuscularly at a dose corresponding to 0.3-0.6 mg/kg.

In the postoperative period, adults are administered 2.5-5 mg of Droperidol intramuscularly every 6 hours.

Side effects

The instructions for Droperidol indicate that the drug can cause side effects such as:

• Tachycardia;
• Bronchospasm;
• Drowsiness;
• Depression;
• Dysphonia;
• Dizziness;
• Laryngospasm;
• Hallucinations;
• Tremor;
• Reduced blood pressure.

In cases of high doses of Droperidol, psychomotor agitation, extrapyramidal disorders, anxiety, anaphylactoid reactions and fear may occur. When used simultaneously with fentanyl, blood pressure may increase.

A symptom of a drug overdose is a sharp decrease in blood pressure. In such cases, the prescription of sympathomimetic drugs or analeptics is required.

special instructions

The use of Droperidol is permissible only in a hospital setting.

Patients with pheochromocytoma may experience a sharp increase in blood pressure and tachycardia after administration of the drug. In this regard, during the use of the solution, it is necessary to have medications whose action is aimed at correcting blood pressure.

Patients with cardiac arrhythmias should not be prescribed a dose of Droperidol exceeding 25 mg, as this can lead to sudden death.

If antihypertensive drugs were used to treat the patient, it is necessary to gradually reduce their dose in the preoperative period until complete withdrawal, and then use Droperidol.

In cases of using the drug in surgical practice, it is recommended to monitor the parameters of the physiological state of the body.

When using the drug against the background of spinal or epidural anesthesia, suppression of the sympathetic nervous system and development of blockade of intercostal nerves is possible. This, in turn, helps reduce blood pressure and dilate peripheral blood vessels.

Due to the fact that orthostatic hypotension may develop during the administration of the solution, it is necessary to be careful during transportation and avoid a sudden change in the patient’s body position.

It should be taken into account that Droperidol reduces the pressor effect of epinephrine, enhances the effect of narcotic analgesics, barbiturates, muscle relaxants, benzodiazepines, antihypertensive drugs and hypnotics. The drug may also weaken the effect of dopamine receptor agonists.

Analogs

There are no synonyms for the drug. Analogs of Droperidol include Medxenon, XeMed, Sodium hydroxybutyrate, Propofol Fresenius, Rekofol, Nitrous oxide, Proviv and Diprivan.

Terms and conditions of storage

In accordance with the instructions, Droperidol should be stored in a place protected from light, dry and out of reach of children, at a temperature not exceeding 30 ºС.

The drug is dispensed from pharmacies according to a doctor's prescription. The shelf life of the solution, subject to the manufacturer's recommendations, is five years.

The neuroleptic Droperidol is used in the treatment of shock conditions, and also as an antipsychotic drug. Today we will talk about the pharmacological group, features and indications for the use of Droperidol, find out whether it is available without a prescription, and also consider other important nuances associated with the drug.

Features of the drug

Areas of use of Droperidol are anesthesiology and psychotherapy. It is used in the treatment of shock conditions and as an antipsychotic drug.

The neuroleptic is a powder of light pastel colored crystals that changes color to yellow in the presence of light and contact with open air.

Water is not a solvent for this powder, nor is alcohol, the degree of dissolution in which is very low.

Compound

The main active component of Droperidol is a crystalline powder of the same name with a drug, the degree of dissociation of which in water is 0%. The powder is not an ether derivative, so it has no odor.

The substance under the medical name Droperidol is a chemical derivative of a number of butyrophenones with the substitution of four hydroxo groups and fluorine in the molecule with benzimidazolinone.

Dosage forms

Release form: Droperidol in the form of an injection solution is available in 10 ml ampoules. 50 ampoules are packed in a cardboard box. The content of pure substance in a 25% solution of the drug is 25 mg.

pharmachologic effect

In addition to its effect on the nervous system, Droperidol prevents vomiting and has a sedative effect on the regulation of somatic and autonomic functions. The medicinal effect of Droperidol is associated with inhibition of dopamine receptors localized in various structures of the brain: reticular pharmacy, medulla oblongata and diencephalon, neuroendocrine cells of the hypothalamus. Hence the variety of effects on the vegetative and somatic functions of the body.

Let's also look at the mechanism of action of Droperidol.

Pharmacodynamics

Droperidol does not inhibit the functioning of receptors sensitive to the mediator acetylcholine. The use of the drug helps reduce pulmonary pressure due to a wave reduction in the pressor effect in the pulmonary artery. When it occurs with an epinephrine etiology, the use of Droperidol has the opposite effect, normalizing the heart rhythm. Pathology with a different etiology is not eliminated by Droperidol.

The inhibitory activity of the drug on individual receptors is detected within 4 hours, and the effects of the drug on the nervous system are observed 12 hours after administration of the drug.

Droperidol, when administered intravenously or intramuscularly, begins to have a therapeutic effect after 3 minutes. The maximum concentration of Droperidol in histological analysis of nervous tissue is observed half an hour after administration of the drug.

Pharmacokinetics

The blood plasma is maximally saturated with the drug 15 minutes after its administration. Transport of Droperidol into the tissues of the central nervous system occurs by binding to blood proteins. The half-life of the substance is approximately 2.5 hours.

Intermediate and final metabolic products are formed in the epithelial tissue of the liver. The substance is excreted primarily through urine (3/4 of the volume). Almost 25% of Droperidol is excreted through the digestive tract. Less than 1% of the substance remains in the blood plasma for a long time.

Indications

Droperidol has found application in surgical and therapeutic practice. In surgery the drug is used:

• in the initial stage of anesthesia;
• as a medication in preparing a patient for surgery;
• as an antipsychotic agent under local anesthesia;
• during surgical and diagnostic procedures as a sedative;
• to reduce muscle tone and put the patient to sleep to achieve neuroleptanalgesia.

In therapy, Droperidol is used in the following cases:

• acute crises during ;
• prevention of anaphylactic shock in case of injury;
• acute crisis period;
• pulmonary failure due to edema;

The drug is used in psychiatric practice in cases of hyperexcitability of receptor activity and the occurrence of hallucinations.

Instructions for using Droperidol in ampoules will be discussed below.

Instructions for use

The dosage of the administered drug is calculated based on the weight, age and general condition of the patient. The calculation also includes individual tolerance to the drug, the nature of the disease, other anesthetics administered and the type of anesthesia.

• Approximately half an hour before surgery, the patient receives up to 5 mg of the drug intramuscularly; for children, Droperidol is calculated per 1 kg - 100 mcg of injection solution.
• When using Droperidol as anesthesia, intravenous administration of 15 mg of the drug is practiced; children are given 0.3 mcg per 1 kg of body weight.

According to the instructions for use, the dosage of Droperidol is reduced or the drug is limited for use in cases of liver and kidney failure, prolonged depressive states, and severe epilepsy.

Patients whose general condition is noted to be weak or who have significant problems with body weight should receive a lower dose of Droperidol. As it develops, the body experiences an increase in heart rate and a condition.

Droperidol also has some contraindications, and we’ll talk about them.

Contraindications

• It is not recommended to use the drug in gynecological practice during cesarean section operations, since inhibition of the work of the medulla oblongata centers in the fetus may occur, one of which may be respiratory depression.
• Extrapyramidal disorders (impaired muscle tone activity) are also an obstacle to drug administration.
• Long-term use of an antihypertensive drug and Droperidol is not recommended for the risk of a severe decrease in systolic pressure.
• The drug is contraindicated in patients with long-term depression aggravated by phobias.

Side effects from Droperidol

In small cases of using Droperidol in clinical practice, side effects may occur:

• allergic reactions in the form of spasms of the respiratory tract;
• after operations, patients complain of drowsiness, and with an overdose of Droperidol, on the contrary, of excessive anxiety and, sometimes, a depressive state;
• Nausea, icteric symptoms, loss of appetite are often observed;
• natural decrease in systolic pressure.

special instructions

The injection drug Droperidol is approved when prescribed only in a clinical setting. The inhibitory effect on some brain structures allows us to conclude that it is undesirable to go to work within 24 hours after using the drug, especially for those types of work that require concentration and mobility of nervous processes.

Exceeding the dose (25 mg or higher) can cause death of the patient. It is also undesirable to move the patient after using the drug or change his position. The extinction of inhibition occurs at a much slower rate than when it is excited, so the administration of the drug requires regular monitoring of the parameters of the state of the physiological systems of the body.

Let's find out what reviews there are about taking Droperidol.

Gross formula

Pharmacological group of the substance Droperidol

Nosological classification (ICD-10)

CAS Code

Characteristics of the substance Droperidol

Neuroleptic, butyrophenone derivative.

Crystalline powder, white or light yellowish-brown, odorless. Practically insoluble in water, slightly soluble in ethanol. When stored in air or light it turns yellow. Molecular weight 379.43.

Pharmacology

Blocks dopamine receptors (mainly D2) in the subcortical areas of the brain (substantia nigra, striatum, tubercular, interlimbic and mesocortical areas), inhibits central alpha-adrenergic structures, disrupts reverse neuronal uptake and deposition of norepinephrine. Dilates peripheral vessels, reduces peripheral vascular resistance and blood pressure. Reduces pressure in the pulmonary artery (especially if it is significantly increased). Reduces the pressor and arrhythmogenic effects of epinephrine (does not prevent cardiac arrhythmias of other etiologies). Has strong cataleptogenic activity.

With intravenous and intramuscular administration, Cmax in plasma is achieved within 15 minutes. 85-90% binds to plasma proteins. T 1/2 averages 134 minutes. Metabolized in the liver. It is excreted in the form of metabolites (75%) and unchanged (1%) by the kidneys and through the intestines (11%).

After parenteral administration, the effect occurs within 3-10 minutes, the maximum effect is achieved within 30 minutes. The duration of neuroleptic and sedative effects is usually 2-4 hours (possibly up to 12 hours). Combined use with fentanyl (neuroleptanalgesia) causes a rapid neuroleptic and analgesic effect, muscle relaxation, and prevents shock.

Carcinogenicity, mutagenicity, effect on fertility

No studies have been conducted to evaluate the potential carcinogenicity of droperidol.

No mutagenicity of droperidol was detected in the micronucleus test in female rats at single oral doses above 160 mg/kg.

There was no effect of droperidol on fertility in either male or female rats at oral doses of 0.63; 2.5 and 10 mg/kg (approximately 2, 9 and 36 times the MRDC IM or IV).

The effectiveness of the use of droperidol has been shown to reduce the incidence of nausea and vomiting during diagnostic and surgical procedures, for the treatment of hiccups, as well as nausea and vomiting induced by chemotherapy, for the relief of hypertensive crises, in psychiatric practice for psychomotor agitation, hallucinations.

Use of the substance Droperidol

Neuroleptanalgesia (usually in combination with fentanyl or other opioids), premedication, to prepare for instrumental studies, incl. endoscopic and surgical interventions; induction of anesthesia, potentiation of general anesthesia, psychomotor agitation in the postoperative period, pain shock (including myocardial infarction, burns), poisoning (as part of complex therapy); in narcology - alcoholic delirium.

Contraindications

Hypersensitivity, extrapyramidal disorders, appointment of cesarean section during surgery, hypokalemia, arterial hypotension, long QT interval syndrome, early childhood (up to 2 years).

Restrictions on use

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

Use during pregnancy and breastfeeding

When administered intravenously to rats, droperidol caused a slight increase in the number of deaths of newborn rat pups at doses exceeding the MRDC by 4.4 times. Droperidol did not have a teratogenic effect in animals.

During pregnancy, it is used in cases where the expected benefit to the mother outweighs the potential risk to the fetus. Contraindicated in late pregnancy (for example, during cesarean section).

Should not be used during breastfeeding (it is unknown whether droperidol is excreted in breast milk).

Side effects of the substance Droperidol

From the cardiovascular system and blood (hematopoiesis, hemostasis): decreased blood pressure, tachycardia.

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 postoperative hallucinations (sometimes associated with transient periods of depression).

Rarely - dizziness, chills and/or trembling, laryngospasm, bronchospasm, anaphylactic reactions. 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).

Interaction

Enhances the effect of benzodiazepines, barbiturates, opioid analgesics, hypnotics and narcotics, muscle relaxants and antihypertensive drugs. Weakens the effect of dopamine receptor agonists (bromocriptine). Reduces the pressor effect of epinephrine.

Overdose

Symptoms: a sharp decrease in blood pressure, increased severity of side effects.

Treatment: symptomatic therapy, if extrapyramidal disorders occur, anticholinergic drugs are used, the decrease in blood pressure is treated with analeptics and sympathomimetic drugs, and in case of hypovolemia, replacement of blood volume is indicated.

Droperidol

Composition and release form of the drug

5 ml - ampoules (10) - cardboard boxes.
5 ml - ampoules (5) - contour plastic packaging (2) - cardboard packs.

pharmachologic effect

Antipsychotic drug (neuroleptic), butyrophenone derivative. It has antipsychotic, cataleptogenic, sedative, antishock, and also effects.

The mechanism of antipsychotic action is associated with blockade of dopamine D 2 receptors of the mesolimbic and mesocortical systems. The sedative effect is due to the blockade of adrenergic receptors in the reticular formation of the brain stem, the antiemetic effect is due to the blockade of dopamine D 2 receptors in the trigger zone of the vomiting center, the hypothermic effect is due to the blockade of dopamine receptors in the hypothalamus.

A decrease in blood pressure is possible due to dilation of peripheral vessels and a decrease in peripheral vascular resistance; reduces pulmonary artery pressure (especially if it is significantly elevated) and reduces the pressor effect of epinephrine. Droperidol reduces the incidence of arrhythmias caused by epinephrine, but does not prevent arrhythmias of other etiologies.

Does not have anticholinergic activity.

With intravenous or intramuscular administration, the effect of droperidol develops after 3-10 minutes, the maximum effect is observed after 30 minutes. The sedative effect lasts 2-4 hours, the total duration of action on the central nervous system can reach 12 hours.

Pharmacokinetics

Dosage

The dose is determined individually, taking into account age, body weight, general physical condition, the nature of the disease, drugs used simultaneously, and the type of anesthesia to be performed.

For premedication, adults are administered 2.5-5 mg intramuscularly 15-45 minutes before surgery; children - 100 mcg/kg.

For induction of anesthesia - IV: adults - 15-20 mg, children - 200-400 mcg/kg (or 300-600 mcg/kg IM).

For long-term operations, repeated intravenous administration is carried out to maintain anesthesia at a dose of 2.5-5 mg.

In the postoperative period, adults are prescribed 2.5-5 mg intramuscularly every 6 hours.

Side effects

From the side of the central nervous system: dysphoria, drowsiness in the postoperative period and, on the contrary, when used in high doses - anxiety, motor excitability, fear; rarely - extrapyramidal symptoms; in isolated cases, hallucinations and depression are observed in the postoperative period.

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

From the digestive system: nausea, loss of appetite, dyspeptic symptoms; rarely - jaundice, transient liver dysfunction.

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

Drug interactions

When used simultaneously with drugs that have a depressant effect on the central nervous system (benzodiazepine derivatives, anesthetics, opioid analgesics, hypnotics), droperidol enhances the depressant effect on the central nervous system.

With simultaneous use, droperidol exhibits antagonism towards epinephrine and other adrenergic and sympathomimetic drugs.

With simultaneous use, droperidol potentiates the effect of antihypertensive drugs.

Because droperidol blocks dopamine receptors; when used simultaneously, it can inhibit the action of agonists, incl. bromocriptine, lisuride and levodopa.

special instructions

Droperidol is used only in hospital settings.

Use with caution in cases of liver and kidney dysfunction, epilepsy and conditions preceding an epileptic seizure, and depression.

In patients with pheochromocytoma, severe arterial hypertension and tachycardia may occur after administration of droperidol.

When using droperidol, the possibility of developing severe arterial hypotension should be anticipated and the availability of means for its timely correction should be provided. Droperidol may cause a decrease in pulmonary artery pressure, which should be kept in mind during surgical and diagnostic procedures. Patients receiving droperidol require close medical supervision.

In elderly patients, physically weakened and depleted patients, as well as at high risk, the initial dose of droperidol should be reduced. When increasing the dose, you must be guided by the effect already obtained.

Against the background of the action of drugs that have a depressant effect on the central nervous system, droperidol should be prescribed in a lower dose, and, accordingly, after using droperidol, such drugs should be administered in lower doses.

It should be borne in mind that the use of droperidol in an increased dose (up to 25 mg or more) can cause sudden death in patients with cardiac arrhythmias due to hypoxia, electrolyte imbalance or alcohol withdrawal.

When using droperidol in surgical practice, parameters of the physiological state of the body should be carefully monitored. It must be emphasized that EEG changes disappear slowly after surgery. The use of droperidol during spinal or epidural anesthesia can cause blockade of the intercostal nerves and the sympathetic nervous system, which, in turn, complicates breathing, contributes to the dilation of peripheral vessels and the development of arterial hypotension.

To avoid orthostatic hypotension, care should be taken when transporting the patient and avoid sudden changes in body position.

Impact on the ability to drive vehicles and operate machinery

Against the background of the action of droperidol and for 24 hours after its use, potentially hazardous activities that require a high concentration of attention and rapid psychomotor reactions should be avoided.

Pregnancy and lactation

Use during pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

Adequate and well-controlled studies of the safety of droperidol during lactation have not been conducted. Butyrophenones are excreted in milk and are not recommended for use during lactation. If it is necessary to use droperidol in the mother, breastfeeding should be discontinued.