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Droperidol

Droperidol ( lat. Droperidolum ) - a drug. Light cream crystalline powder, practically insoluble in water, slightly soluble in alcohol. When stored in air and light yellow.

Droperidol
Droperidolum
Droperidol.png
Chemical compound
IUPAC1- {1- [3-para-Fluorobenzoyl) propyl] -1, 2, 3, 6-tetrahydro-4-pyridyl} 2-benzimidazolinone
Gross formulaC 22 H 22 FN 3 O 2
Molar mass379.428 g / mol
Cas
PubChem
Drugbank
Classification
ATX
Dosage Forms
injection 2.5 mg / ml, injection 4.0 ml.

Content

The use of the drug

Antipsychotic from the group of butyrophenones . It has a quick, strong, but short-lived effect. The effect with intravenous administration appears after 2-5 minutes, reaches a maximum after 20-30 minutes. The action, depending on the dose, lasts up to 2-3 hours.

The drug potentiates the effect of analgesic and hypnotics. It has anti-shock and antiemetic properties. It has an alpha-adrenolytic effect; blocks central dopamine receptors; does not have anticholinergic activity. Lowers blood pressure, has an antiarrhythmic effect. It has a strong cataleptogenic activity.

In psychiatric practice, droperidol is used for psychomotor agitation, hallucinations. It is mainly used in anesthetic practice for neuroleptanalgesia, usually in combination with fentanyl or other analgesics.

Anesthetic Use

The combined use of droperidol and fentanyl causes a quick antipsychotic and analgesic effect, drowsiness, muscle relaxation, prevents shock, and has an antiemetic effect. Patients easily come out of a state of antipsychotic analgesia.

Droperidol is used for sedation, during the operation and in the postoperative period. Used for endotracheal anesthesia, as well as for operations using local anesthesia.

Droperidol is administered under the skin, intramuscularly and intravenously.

With premedication and antipsychotics, droperidol is usually administered intramuscularly 30–45 minutes before surgery at a dose of 2.5–5 mg (1-2 ml of a 0.25% solution) along with 0.05–0.1 mg (1-2 ml of 0.005 % solution) fentanyl or 20 mg (1 ml 2% solution) of promedol. At the same time, 0.5 mg (0.5 ml of a 0.1% solution) of atropine or metacin is administered.

In endotracheal anesthesia, droperidol is first administered at the rate of 2.5 mg per 5 kg of body weight together with fentanyl at the rate of 0.05 mg per 5 kg of body weight (which corresponds to 1 ml of the combined preparation of thalamonal per 5 kg of body weight). Then, non-inhalation anesthetics, sodium oxybutyrate or tranquilizers (diazepam, sibazon) are used for anesthesia. Anesthesia is supported by nitrous oxide with oxygen in a ratio of 1: 1 or 3: 1. During the operation, fentanyl of 0.05-0.1 mg (1-2 ml) is additionally administered every 15-30 minutes or when signs of weakening appear. In case of cardiac arrhythmias, droperidol (2.5-5 mg) is additionally administered.

Muscle relaxants are used to relax muscles.

During the injection of droperidol and fentanyl, the patient breathes a mixture of oxygen with nitrous oxide (1: 1).

With general anesthesia, droperidol is administered intravenously (slowly) or intramuscularly at the rate of 0.1 mg / kg. 8-10 minutes after the end of droperidol administration, a test dose of fentanyl is slowly administered intravenously (0.005 mg = 0.1 ml of a 0.005% solution). A test dose is necessary to identify possible hypersensitivity, expressed by severe bradycardia, difficulty breathing, chest tightness. If well tolerated, surgery is performed under local anesthesia and is administered intravenously (within 2 minutes) every 6-8 minutes to 0.005-0.01-0.015 mg of fentanyl (depending on the patient’s body weight) and 0.09 every 30-40 minutes mg / kg droperidol.

To relieve pain, reduce nausea and vomiting in the postoperative period, if necessary, 2.5-5 mg of droperidol and 0.05-0.1 mg of fentanyl are administered intramuscularly.

Neuroleptanalgesia with droperidol with fentanyl has been used to combat pain and shock in myocardial infarction and in patients with severe angina attacks. 2.5-5 mg (1-2 ml) of droperidol and 0.05-0.1 mg (1-2 ml) of fentanyl diluted in 20 ml of a 5-40% glucose solution are injected slowly into a vein. A positive result was also noted with pulmonary edema.

To stop hypertensive crises, droperidol is administered intravenously in a dose of 0.1 mg / kg (usually 2 ml of a 0.25% solution). The drug is most effective in crises in patients with stage IIA hypertension and sclerotic hypertension.

To prepare for painful instrumental diagnostic procedures, 2.5-5 mg of droperidol is administered intravenously for half an hour.

Droperidol and fentanyl are used not only in a hospital, neuroleptanalgesia is used at the prehospital stage for myocardial infarction.

Thalamonal (Thalamonal) * - a combined foreign drug, contains 1 ml of 2.5 mg of droperidol and 0.05 mg of fentanyl. Used for antipsychotics and in other cases, instead of separate use of both drugs.

Side Effects

Side effects of the drug include extrapyramidal disorders , depression with a predominance of fear, hypotension (with an overdose) [1] . In Western countries, in 1998, droperidol received caution in the form of a black insert for a potentially deadly lengthening of the QT interval . A few years after this, droperidol was withdrawn from the market by its manufacturers [2] .

Precautions

When using droperidol, it is necessary to carefully monitor the state of blood circulation and respiration. Large doses can cause a decrease in blood pressure and respiratory depression. The action of muscle relaxants , analgesics , drugs is significantly enhanced.

In patients treated with insulin and corticosteroids , with severe atherosclerosis , impaired conduction of the heart muscle, diseases of the cardiovascular system in the decompensation stage, caution is necessary.

Interactions

Droperidol increases the activity of opioid analgesics , drugs for general anesthesia . It enhances the effect of other drugs that depress the central nervous system , and therefore, after their use, droperidol should be prescribed in a lower dose, and after the use of droperidol, such drugs should also be prescribed in a lower dose. Dopaminergic drugs for the treatment of parkinsonism reduce the effect of droperidol [3] .

Contraindications

Droperidol is contraindicated in extrapyramidal disorders , hypotension [1] , as well as for individuals who have been taking antihypertensive drugs for a long time (a sharp decrease in blood pressure is possible). In combination with fentanyl, it is contraindicated in cesarean section due to inhibition of the respiratory center of the fetus.

Storage

Storage: List B. In a dry, dark place at a temperature of 0 to +5 ° C.

Notes

  1. ↑ 1 2 Davydov A.T., Krupitsky E.M., Remizov L.M. Features of the clinical use of typical antipsychotic drugs in psychiatric and narcological practice // Reviews of clinical pharmacology and drug therapy. - 2007. - T. 5, No. 1.
  2. ↑ Limankina I.N. Syndrome of an extended QT interval and safety problems of psychopharmacotherapy // Bulletin of Arrhythmology. - 09/18/2008. - No. 52 . - S. 66-71 .
  3. ↑ Drug Interaction and Pharmacotherapy Effectiveness / L.V. Derimedved, I.M. Pertsev, E.V. Shuvanova, I.A. Zupanets, V.N. Khomenko; under the editorship of prof. I. M. Pertseva. - Kharkov: Publishing house "Megapolis", 2001. - 784 p. - 5,000 copies. - ISBN 996-96421-0-X.
Source - https://ru.wikipedia.org/w/index.php?title=Droperidol&oldid=96724496


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