Reg. No: 18/05/551 from 30.05.2018 - Validity period of reg. beats is not limited
Solution for intravenous administration colorless or slightly yellowish, transparent.
Excipients: tartaric acid, water d / i.
5 ml - ampoules (5) - contoured cell packaging (1) - packs.
5 ml - ampoules (5) - contoured cell packs (2) - packs.
Description of the medicinal product DROPERIDOL was created in 2010 on the basis of instructions posted on the official website of the Ministry of Health of the Republic of Belarus. Updated date: 03/14/2019
It also has neuroleptic, sedative, anti-shock, antiemetic, antihypertensive and antiarrhythmic effects. The antipsychotic effect is due to the blockade of dopamine B 2 receptors of the mesolimbic and mesocortical systems. The sedative effect is due to the blockade of adrenergic receptors of the reticular formation of the brain stem; antiemetic action - blockade of dopamine B 2 -receptors of the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus. Expands peripheral vessels and reduces total peripheral vascular resistance; reduces pressure in the pulmonary artery (especially if it is significantly increased) and reduces the pressor effect of epinephrine. Reduces the incidence of epinephrine-induced arrhythmias, but does not prevent arrhythmias of other etiology. Possesses strong cataleptogenic activity. When administered intravenously or intramuscularly, the action occurs in 5-15 minutes, the maximum effect is achieved in 30 minutes; sedation lasts 2-4 hours, the total duration of action on the central nervous system is 12 hours.
With intravenous or intramuscular administration, C max in plasma is achieved after 15 minutes. Communication with plasma proteins - 85-90%. T 1/2 averages 120-130 minutes. Metabolized in the liver. Excreted by the kidneys as metabolites (75%), unchanged (1%); through the intestines (11%).
During use against the background of conduction anesthesia (spinal, epidural), blockade of intercostal nerves and the sympathetic nervous system may develop, which makes breathing difficult, promotes expansion of peripheral vessels and hypotension. Patients taking antihypertensive drugs, a few days before using droperidol, need a gradual decrease in the dose of these drugs, and then their complete withdrawal. Patients with pheochromocytoma after administration of droperidol may experience severe hypertension and tachycardia.
The drug is administered intramuscularly and intravenously.
The dosage regimen is individual, taking into account age, body weight, general physical condition, the nature of the disease, the drugs used, the type of upcoming anesthesia.
For premedication, adults, 15-45 minutes before the start of the surgical intervention, are injected intramuscularly with 2.5-5 mg (1-2 ml of a 0.25% solution); children - 0.1 mg / kg.
For introduction into anesthesia - IV:
- adults - 15-20 mg;
- children - 0.2-0.4 mg / kg (or 0.3-0.6 mg / kg i / m).
For prolonged operations, to maintain anesthesia, repeated intravenous administration is performed at a dose of 2.5-5 mg.
In the postoperative period, adults are prescribed IM, 2.5-5 mg every 6 hours.
To relieve hypertensive crises, 0.1 mg / kg is administered intravenously, in a stream (usually 2 ml of a 0.25% solution).
Decrease in blood pressure, tachycardia, dysphoria, drowsiness in the postoperative period.
When used in high doses - anxiety, psychomotor agitation, fear, extrapyramidal disorders, anaphylactoid reactions.
Seldom:
- dizziness, tremor, laryngospasm, bronchospasm, increased blood pressure (with the combined use of droperidol with fentanyl), hallucinations, depression (in the postoperative period).
Hypersensitivity, extrapyramidal disorders, surgical interventions in late pregnancy (including during caesarean section), hypokalemia, arterial hypotension, Q-T interval lengthening syndrome, period breastfeeding, early childhood (up to 2 years old).
Carefully: hepatic and / or renal failure, alcoholism, decompensated chronic heart failure, epilepsy, depression, pregnancy.
Applied only in a hospital setting. In view of the existing possibility of a pronounced decrease in blood pressure, funds for timely correction should be available. If arterial hypotension cannot be prevented by parenteral administration of fluids, vaso-pressor drugs must be administered.
Patients with pheochromocytoma may experience severe hypertension and tachycardia after administration. Prescription in an increased dose (25 mg or more) can cause sudden death in patients with cardiac arrhythmias (against the background of hypoxia, electrolyte imbalance or alcohol withdrawal).
If antihypertensive drugs were used in therapy, in the preoperative period (before the use of droperidol), it is necessary to gradually reduce their dose (up to complete cancellation).
When used in surgical practice, it is necessary to control the parameters of the physiological state of the body; changes in electroencephalogram after surgery disappear slowly.
When used against the background of conductive anesthesia (spinal, epidural), it is possible to develop blockade of intercostal nerves and suppression of the sympathetic nervous system, which makes breathing difficult, promotes expansion of peripheral vessels and the development of hypotension.
In order to avoid orthostatic hypotension, care should be taken when transporting the patient; body position cannot be changed quickly. The initial doses of droperidol should be reduced in elderly patients, physically weakened, with hepatic and renal insufficiency, with decompensated heart failure, alcoholism, epilepsy, depression. Elderly patients are at higher risk of orthostatic hypotension.
Influence on the ability to drive and potentially dangerous mechanisms:
- during the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
Symptoms: a sharp decrease in blood pressure, tachycardia, a change in the QRS waves, areflexia or hyperreflexia, blurred vision, confusion, convulsions, vomiting, pulmonary edema or respiratory depression.
Treatment:
- the decrease in blood pressure is eliminated by analeptics and sympatomimetic drugs;
- for estrapyramidal disorders - antiparkinsonian drugs;
- with hypovolemia - replenishment of the circulating blood volume;
- for convulsions - diazepam (avoid the appointment of barbiturates due to the possible subsequent depression of the central nervous system and respiratory depression);
- if necessary, other symptomatic therapy.
Strengthens the action of barbiturates, benzodiazepines, narcotic analgesics, hypnotics and drugs for general anesthesia, muscle relaxants and antihypertensive drugs. Combined use with fentanyl causes a rapid neuroleptic and analgesic effect, muscle relaxation, prevents shock, and has an antiemetic effect.
Weakens the effect of dopamine receptor agonists. Reduces the pressor effect of epinephrine.
The neuroleptic drug 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 if 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 antipsychotic is a powder of light pastel crystals that changes color to yellow in the presence of light and contact with open air.
Water is not a solvent for this powder, like alcohol, in which the degree of dissolution is very low.
Composition
The main active ingredient 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 ester derivative, therefore it has no smell.
The substance under the medical name Droperidol is a chemical derivative of a series 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 the pure substance in a 25% drug solution is 25 mg.
pharmachologic effect
In addition to the effect on the nervous system, Droperidol prevents vomiting, 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 activity of receptors that are sensitive to the mediator acetylcholine. The use of the drug helps to reduce pulmonary pressure due to the wave reduction of the pressor effect in the pulmonary artery. When it occurs with epinephrine etiology, the use of Droperidol has the opposite effect, which normalizes the heart rate. Pathology with a different etiology with Droperidol is not eliminated.
The inhibitory activity of the drug on individual receptors is detected within 4 hours, and the effects of the drug from the nervous system are noted 12 hours after drug administration.
Droperidol, when administered intravenously or intramuscularly, begins to have a therapeutic effect after 3 minutes. The maximum concentration of Droperidol in the histological analysis of nervous tissue is noted half an hour after the administration of the drug.
Pharmacokinetics
Blood plasma is maximally saturated drug 15 minutes after its introduction. Droperidol is transported to the tissues of the central nervous system 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 excretion of the substance is carried out mainly with urine (3/4 of the volume). Almost 25% of Droperidol is excreted through the digestive tract. Less than 1% of the substance remains in 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 medication in preparing the patient for surgical intervention;
- as an antipsychotic agent for local anesthesia;
- in 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 when injured;
- the crisis period of the acute;
- pulmonary insufficiency due to edema;
The drug is used in psychiatric practice in the course of super-excitability of receptor activity and the occurrence of hallucinations.
Instructions for the use of 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 the individual tolerance of the drug, the nature of the disease, other anesthetics administered and the type of anesthesia.
- Approximately half an hour before the surgical intervention, the patient receives up to 5 mg of the drug intramuscularly, for children Droperidol is calculated for 1 kg - 100 μg of the injection solution.
- When using Droperidol as anesthesia, intravenous administration of 15 mg of the drug is practiced, 0.3 μg per 1 kg of body weight is administered to children.
According to the instructions for use, the dosage of Droperidol is reduced or the drug is limited to use in hepatic and renal failure, protracted depression, severe epilepsy.
Patients whose general condition is mild, who have major problems with body weight, should receive a lower dose of droperidol. With development in the body, an increase in heart rate and condition is observed.
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 the medulla oblongata centers in the fetus may be inhibited, one of which may be respiratory depression.
- Extrapyramidal disturbances (disturbances in the activity of muscle tone) are also an obstacle to drug administration.
- Long-term use of an antihypertensive drug and Droperidol is not recommended for the risk of a strong decrease in systolic pressure.
- The drug is contraindicated in patients with prolonged depression, aggravated by phobias.
Side effects from Droperidol
In small cases of the use of Droperidol in clinical practice, side effects may occur:
- allergic reactions in the form of respiratory tract spasms;
- after operations, patients complain of drowsiness, and in case of an overdose with Droperidol, on the contrary, of excessive anxiety and, at times, a depressive state;
- nausea, jaundice, loss of appetite is often noted;
- natural decrease in systolic pressure.
special instructions
The drug for injection Droperidol is approved when administered only in a clinical setting. The inhibitory effect on some structures of the brain allows us to conclude that there is an unwanted exit to work within 24 hours after using the drug, especially for those types of work that require concentration of attention and mobility of nervous processes.
Exceeding the dose (25 mg or more) can lead to death of the patient. It is also undesirable to move the patient after taking the drug, change his position. The extinction of inhibition occurs at a much slower rate than when it is excited, therefore 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.
Dosage Form: & nbspinjection Composition:1 ml of solution contains:
active substance:
droperidol 2.5 mg; excipients: tartaric acid up 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 (neuroleptic) ATX: & nbspN.05.A.D.08 Droperidol
Pharmacodynamics:DROPERIDOL refers to antipsychotics, a derivative of butyrophenone. It has a high neuroleptic activity, it also has a pronounced tranquilizing, sedative, anti-shock, hypothermic, antiarrhythmic and antiemetic effect. It causes extrapyramidal disorders, has a pronounced cataleptogenic activity. Does not possess anticholinergic activity.
The main effects are due to the effect of the drug on the dopaminergic structures of the brain, mainly on the dopamine D 2 receptors of the mesolimbic and mesocortical systems.
The sedative effect is due to the blockade of adrenergic receptors of the reticular formation of the brain stem.
Droperidol increases the duration and intensity of the action of hypnotics, drugs, analgesics, local anesthetic, anticonvulsants and alcohol.
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.
The effect on peripheral alpha-adrenergic receptors is associated with the expansion of blood vessels caused by the drug and a decrease in total peripheral resistance, as well as a decrease in pressure in the pulmonary artery (especially if it is high) and a decrease in the pressor effect of adrenaline and norepinephrine.
DROPERIDOL attenuates adrenaline-induced arrhythmias, but does not prevent cardiac arrhythmias of other etiologies.
Pharmacokinetics:When administered intravenously or intramuscularly, the effect of the drug occurs after 5-15 minutes, the maximum effect is achieved after 30 minutes. Plasma protein binding is 85-90%, half-life is 120-130 minutes. The neuroleptic, tranquilizing and sedative effects of the drug last 2-4 hours, but to varying degrees, the expressed general depressive effect on the central nervous system can reach 12 hours in duration.
Excreted by the kidneys in the form of metabolites (75%), 1% unchanged; 11% is excreted through the intestines.
Indications:Premedication before anesthesia, induction anesthesia, potentiation of the action of drugs in general and regional anesthesia.
Neuroleptanalgesia (in combination with opioid analgesics, often with fentanyl).
Providing a sedative effect, preventing nausea and vomiting during diagnostic and surgical procedures.
Pain and vomiting in the postoperative period, psychomotor agitation, hallucinations.
Pain syndrome and shock (with injuries, myocardial infarction, severe attacks of angina pectoris, burns).
Pulmonary edema.
For relief of hypertensive crises.
Contraindications:Increased individual sensitivity to the drug;
Extrapyramidal disorders;
Cesarean section;
Hypokalemia;
Arterial hypotension;
QT lengthening syndrome;
Children's age (up to 3 years old).
Carefully:Hepatic and / or renal failure, alcoholism, decompensated chronic heart failure, epilepsy, depression, pregnancy.
Pregnancy and lactation:During pregnancy, it is used in case of emergency, when the therapeutic effect justifies the possible risk of use.
When using droperidol during lactation, breastfeeding should be discontinued.
Method of administration and dosage:The administered dose of droperidol should be determined individually, taking into account the patient's age, body weight, general physical condition, the nature of the disease, the medications he uses, and the type of anesthesia to be taken.
Droperidol is administered subcutaneously, intramuscularly and intravenously.
When the drug is administered, the vital physiological functions of the body should be monitored.
Premedication .
injected intramuscularly 30-60 minutes before surgery at a dose of 2.5 -10 mg (1-4 ml). The dose is determined individually.General anesthesia .
For introduction into anesthesia used intravenously at a dose of 2.5 mg (1 ml) per 10 kg of body weight in combination with analgesics and / or general anesthetics. In some cases, smaller doses can be used. The total dose of droperidol is set individually.During the operation, the maintenance dose of droperidol is 1.25-2.5 mg (0.5-1.0 ml) intravenously.
Use of droperidol in diagnostic procedures without the use of general anesthesia .
injected intramuscularly at a dose of 2.5-10 mg (1-4 ml) 30-60 minutes before the procedure. Additionally, it can be administered intravenously at a dose of 1.25-2.5 mg (0.5-1 ml). (Some procedures, like bronchoscopy, require local anesthesia.)Local anesthesia . To provide additional sedative effect, it is administered intramuscularly or intravenously slowly at a dose of 2.5-5 mg (1-2 ml).
For relief of hypertensive crises . administered in a dose of 2.5-5 mg (1-2 ml) intravenously or intramuscularly, if necessary, simultaneously with other drugs. The injections can be repeated after 45 to 90 minutes.
Use of droperidol in pediatric practice . Children aged 3 to 12 years are used 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 induction of anesthesia.
The safety of using droperidol for children under 3 years of age has not been confirmed!
Before use, a visual inspection of the droperidol injection solution should be carried out. Do not use a solution that has lost its transparency, acquired a colored color, as well as a solution from an unsealed package.
Side effects:Arterial hypotension of moderate severity and tachycardia, which can be stopped without special therapy.
Dysphoria, drowsiness in the postoperative period are possible and, on the contrary, when using higher doses - anxiety, motor excitability, fear. Sometimes there is extrapyramidal symptoms, which should be stopped by anticholinergic drugs.
Less common are anaphylaxis, dizziness, tremor, laryngospasm, bronchospasm.
In very rare cases, arterial hypertension and tachycardia are observed - 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.
Nausea, loss of appetite, dyspeptic symptoms are possible; rarely - jaundice, transient liver dysfunction, allergic reactions.
Overdose:Overdose symptoms are due to pharmacological action drug.
Symptoms: a sharp decrease in blood pressure.
Treatment: lowering blood pressure is eliminated by analeptics and sympathomimetic agents. To eliminate extrapyramidal symptoms, it is necessary to use antiparkinsonian drugs.
In case of respiratory failure, artificial ventilation of the lungs should be applied and provided. Careful monitoring of the state of the body for 24 hours is required. The patient should be warmed up, 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 effect of other drugs that depress the central nervous system (eg, barbiturates, tranquilizers, opioids, general anesthetics). This should be considered when choosing the dose of drugs: the dose of droperidol must be reduced if other depressants of the central nervous system were used and, conversely, the doses of other drugs that depress the central nervous system should be reduced after using droperidol.
Droperidol is antagonistic to adrenaline and other sympathomimetic agents.
Droperidol potentiates the action of antihypertensive drugs.
Since it blocks dopamine receptors, it can inhibit the action of dopamine agonists.
With the simultaneous use of anticonvulsants with droperidol, an increase in the dose of the latter may be required.
Special instructions:Droperidol is used only in a hospital setting.
When using droperidol, one should foresee the possibility of arterial hypotension and have funds for its timely correction.
Patients receiving should be under close medical supervision.
Initial doses of droperidol should be reduced in elderly patients, physically weakened patients and others with a high degree of risk. Increasing the dose of the drug, it is necessary to be guided by the effect already obtained.
It should be borne in mind that the doses of opioids used in conjunction with droperidol should be reduced.
Droperidol rarely causes neuroleptic malignant syndrome.
In the preoperative period, the diagnosis of neuroleptic hyperthermia is difficult. Appropriate therapy should be started immediately if there is an increase in temperature, increased heart rate and hypercapnia.
It should be borne in mind that high doses of droperidol (25 mg or more) in patients at risk of cardiac arrhythmias associated with hypoxia, electrolyte imbalance or alcohol withdrawal can cause sudden death.
With some types of conduction anesthesia (for example, spinal, epidural), blockade of intercostal nerves and sympathetic innervation may develop, which, in turn, makes breathing difficult, promotes expansion of peripheral vessels and the development of hypotension. in turn also affects blood circulation. Therefore, in cases where they are used in addition to these types of anesthesia, the anesthesiologist should anticipate possible changes and carefully monitor the vital functions of the body.
Hypotension can be accompanied by hypovolemia, therefore fluid therapy is necessary to prevent it. The patient should be positioned to improve venous flow to the heart. During spinal or epidural anesthesia, it is necessary to ensure that the patient's head does not hang down - this position enhances the effect of anesthesia and impairs venous circulation.
To avoid orthostatic hypotension, care should be taken when transporting the patient; it is impossible to quickly change his body position. However, if this complication cannot be prevented by parenteral administration of fluids, it is necessary to introduce pressor agents, with the exception of epinephrine, which, after using droperidol, can significantly reduce pressure.
Droperidol can lower the pressure in the pulmonary artery. This should be borne in mind during surgical and diagnostic procedures in order to determine the further treatment of the patient.
The parameters of the physiological state of the body should be carefully monitored. It should be emphasized that EEG changes disappear slowly after surgery.
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 may occur.
Impact on the ability to drive vehicles. Wed and fur .:After using droperidol, patients are not recommended for 24 hours to perform work that requires a quick reaction and is associated with risk, for example, driving a vehicle.
Release form / dosage:Solution for injection, 2.5 mg / ml.
Packaging:2 ml or 5 ml in ampoules of neutral glass of the NS-1 or NS-3 brand or imported from glass of the first hydrolytic class.
5 ampoules in a blister strip made of polyvinyl chloride film and aluminum foil printed varnished or flexible packaging based on aluminum foil.
1 or 2 blister packs with instructions for use of the drug, a knife or an ampoule scarifier in a carton box.
20, 50 or 100 blisters with 20, 50 or 100 instructions for the use of the drug, respectively, with knives or ampoule scarifiers in cardboard boxes or in corrugated cardboard boxes.
When packing ampoules with notches, rings or break points, ampoule knives or scarifiers are not inserted.
5 ml in vials made of glass tube HC-3 or imported from glass of the first hydrolytic class.
5 vials in a blister strip made of polyvinyl chloride film and printed aluminum foil varnished or flexible packaging based on aluminum foil.
1 blister strip with instructions for use of the drug in a cardboard box.
30 or 50 blisters with 30 or 50 instructions for use of the drug, respectively, in cardboard boxes or corrugated cardboard boxes.
Storage conditions:In a dark place at a temperature not exceeding 25 ° C.
Shelf life: Do not use after expiration date, indicated on the package. Pharmacy dispensing conditions:For hospitals Registration number:R N000369 / 01 Registration date:17.04.2007 / 23.10.2013 Marketing Authorization Holder:MOSCOW ENDOCRINE PLANT, FSUE Russia Manufacturer: & nbsp Representative office: & nbspMOSCOW ENDOCRINE PLANT FSUE Russia Date of information update: & nbsp20.01.2016 Illustrated instructionsDroperidol is an antipsychotic drug used for premedication.
Release form and composition
Droperidol is released 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 the solution contains 2.5 mg of droperidol and auxiliary substances - methylparaben, propyl parahydroxybenzoate, tartaric acid and water for injection.
Indications for use
Droperidol is prescribed for induction anesthesia, premedication, as well as in the following cases:
- Pulmonary edema;
- General and regional anesthesia (for their potentiation);
- Hypertensive crisis;
- Neuroleptanalgesia (in combination with fentanyl or other opioids);
- Pain and vomiting in the postoperative period;
- Surgical and diagnostic procedures to exclude nausea and vomiting;
- Appearance with myocardial infarction, burns, trauma and severe attacks of angina pectoris, hallucinations, psychomotor agitation, pain and shock.
Contraindications
The use of Droperidol is contraindicated in children under 2 years of age, with hypersensitivity to the components that make up the drug, as well as in cases:
- Hypokalemia;
- Q-T interval lengthening syndrome;
- Arterial hypotension;
- Extrapyramidal disorders;
- Carrying out a caesarean section.
With caution, Droperidol is prescribed to patients suffering from alcoholism, with renal or hepatic insufficiency, depression, epilepsy, pregnancy and decompensated chronic heart failure.
Method of administration and dosage
The solution is administered intramuscularly or intravenously. The dosage of Droperidol is determined on an individual basis depending on the type of anesthesia to be taken, the nature of the disease, the drugs used simultaneously, as well as the age, general physical condition and body weight of the patient,
Usually, for sedation, adults are injected intramuscularly with 2.5-5 mg of the solution for 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 re-administered intravenously.
When injected into anesthesia, adults are injected intravenously with 15-20 mg of the solution. 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, 2.5-5 mg of Droperidol is administered intramuscularly to adults every 6 hours.
Side effects
The instructions for Droperidol indicate that the drug can cause such side effects, as:
- Tachycardia;
- Bronchospasm;
- Drowsiness;
- Depression;
- Dysphonia;
- Dizziness;
- Laryngospasm;
- Hallucinations;
- Tremor;
- Decrease in blood pressure.
In cases of using high doses of Droperidol, psychomotor agitation, extrapyramidal disorders, anxiety, anaphylactoid reactions and fear may occur. With the simultaneous use of the drug with fentanyl, blood pressure may increase.
A symptom of a drug overdose is a sharp drop in blood pressure. In such cases, the appointment of sympathomimetic drugs or analeptics is required.
special instructions
The use of Droperidol is permissible only in a hospital setting.
Patients with pheochromocytoma after drug administration may experience sharp rise blood pressure and tachycardia. In this regard, during the application of the solution, it is necessary to have medicines, the action of which is aimed at correcting blood pressure.
Patients with cardiac arrhythmias should not be given 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 they are completely canceled, and then use Droperidol.
In cases of using the drug in surgical practice, it is recommended to control the parameters of the physiological state of the body.
When using the drug against the background of spinal or epidural anesthesia, it is possible to suppress the sympathetic nervous system and develop intercostal nerve blockade. This, in turn, helps to reduce blood pressure and vasodilatation.
Due to the fact that orthostatic hypotension may develop against the background of the injection of the solution, it is necessary to be careful during transportation and not to allow a sharp change in the patient's body position.
It should be borne in mind that Droperidol lowers the pressor effect of epinephrine, enhances the effect of narcotic analgesics, barbiturates, muscle relaxants, benzodiazepines, antihypertensive drugs and hypnotics. Also, the drug can weaken the effect of dopamine receptor agonists.
Analogs
Synonyms for the drug are not released. Droperidol analogues include Medksenon, KseMed, Sodium oxybutyrate, Propofol Fresenius, Recofol, Nitrogen nitrous, Provive and Diprivan.
Terms and conditions of storage
In accordance with the instructions, Droperidol should be stored in a dark, dry place out of the reach of children, at a temperature not exceeding 30 ° C.
From pharmacies medicine dispensed by prescription. The shelf life of the solution, subject to the manufacturer's recommendations, is five years.
Gross formula
C 22 H 22 FN 3 O 2Pharmacological group of the substance Droperidol
Nosological classification (ICD-10)
CAS code
548-73-2Characteristics of the substance Droperidol
A neuroleptic, a derivative of butyrophenone.
Crystalline powder of white or light yellowish-brown color, odorless. Practically insoluble in water, slightly soluble in ethanol. When stored in air and light it turns yellow. Molecular weight 379.43.
Pharmacology
pharmachologic effect - antipsychotic, anti-shock, antiemetic, sedative.Blocks dopamine receptors (mainly D 2) in the subcortical regions of the brain (substantia nigra, striatum, tuberous, interlimbic and mesocortical regions), inhibits central alpha-adrenergic structures, disrupts neuronal reuptake and norepinephrine deposition. Expands peripheral vessels, reduces OPSS 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 etiology). Possesses strong cataleptogenic activity.
With intravenous and intramuscular administration, C max in plasma is achieved after 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, effects on fertility
Studies assessing the potential carcinogenicity of droperidol have not been conducted.
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 higher than the MRSA IM or IV).
The effectiveness of the use of droperidol 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 with psychomotor agitation, hallucinations has been shown.
Application 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 anesthesia, potentiation of general anesthesia, psychomotor agitation in the postoperative period, pain shock (including with myocardial infarction, burns), poisoning (as part of complex therapy); in narcology - alcoholic delirium.
Contraindications
Hypersensitivity, extrapyramidal disturbances, prescription during cesarean section, hypokalemia, arterial hypotension, QT prolongation syndrome, early childhood (up to 2 years).
Restrictions on use
Hepatic and / or renal failure, alcoholism, decompensated chronic heart failure, epilepsy, depression.
Application during pregnancy and lactation
When administered intravenously to rats, droperidol caused an insignificant increase in the number of deaths of newborn rat pups at doses that were 4.4 times higher than the MRDC. Droperidol was not teratogenic in animals.
During pregnancy, it is used in cases where the intended benefit to the mother outweighs the potential risk to the fetus. Contraindicated in later dates pregnancy (for example, during a caesarean section).
Do not use during breastfeeding (it is not known whether droperidol is excreted in breast milk).
Side effects of the substance Droperidol
From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): lowering 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 tremors, 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
Strengthens the effect of benzodiazepines, barbiturates, opioid analgesics, hypnotics and anesthetic drugs, 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, in the event of extrapyramidal disorders, anticholinergic agents are used, a decrease in blood pressure is stopped with analeptics and sympathomimetic agents, with hypovolemia, BCC compensation is indicated.