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Droperidol - Uses, Side Effects, and Precautions

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Droperidol is used to prevent nausea and vomiting post-surgery or other procedures. Read the article to learn more.

Written by

Dr. Saima Yunus

Medically reviewed by

Dr. Kaushal Bhavsar

Published At May 28, 2024
Reviewed AtJune 11, 2024

Overview:

Droperidol primarily received US Food and Drug Administration (FDA) approval back in 1970 as an antiemetic and tranquilizing agent. It has been used for over 30 years. Droperidol prevents nausea and vomiting post-surgery or other procedures. It blocks substances in the body that may cause nausea and vomiting. It belongs to a class of medications called antiemetics. This comprehensive article explores its pharmacology, clinical uses, side effects, and the ongoing debates surrounding its administration.

Dosage:

  • Droperidol is used in the form of an injection to prevent vomiting and nausea, which can be seen after surgery or diagnostic procedures.

  • It is administered only by or under the supervision of a doctor.

  • This product is available as a solution.

Warnings:

Despite its efficacy and extensive use, Droperidol has been mired in controversy, primarily stemming from concerns regarding its cardiac safety profile. In 2001, the U.S. Food and Drug Administration (FDA) issued a black box warning involving the risk of QT prolongation and torsades de pointes associated with Droperidol use, leading to restrictions on its administration in certain clinical settings.

This regulatory action led to a debate within the medical community, with proponents arguing that the risk of cardiac adverse events is low when Droperidol is used prudently and with appropriate monitoring. They emphasize its unparalleled efficiency in managing post-operative nausea, vomiting, and acute agitation, contending that the benefits outweigh the potential risks, particularly when alternative drugs might be less effective or associated with their adverse effects.

For Patients:

Why Is Droperidol Prescribed?

Droperidol injections are prescribed to prevent nausea and vomiting seen after surgery or specific diagnostic procedures. This medicine will be administered only by or under the doctor's supervision. Droperidol has also been used as an antipsychotic in dosages ranging from five to ten milligrams given as an intramuscular injection. Generally, it is used in cases of severe agitation in a psychotic patient who is refusing oral medication. Intramuscular preparations of Haloperidol and Olanzapine have replaced their use in intramuscular sedation.

How to Use This Medication?

Droperidol is used in the form of an injection that is administered into a muscle or as a slow infusion into a vein. It is always administered in a hospital or clinic setup. Discuss using this medication with the healthcare team in pediatric patients. Special care might be required. While this medication might be used for children as young as two years for certain conditions, precautions must be taken.

What Should the Patient Inform the Doctor Before Taking Droperidol?

Inform the doctor about the following before taking the medication:

  • Alcohol drinking habit.

  • Heart disease, such as heart failure.

  • Irregular heartbeats.

  • Slow heart rate.

  • Liver disease.

  • Kidney disease.

  • An allergic reaction to Droperidol, other medications, foods, dyes, or preservatives.

Missed Dose:

This is not applicable.

Side Effects:

Any of the following side effects must be reported to the healthcare provider as soon as possible:

  • Allergic Reactions - Itching, skin rash, swelling of the face, hives, lips, tongue, or throat

  • Heart Rhythm Changes - Fast or irregular heartbeat, dizziness, lightheadedness, chest pain, difficulty breathing.

  • CNS Depression - Slow or shallow breathing, dizziness, shortness of breath, confusion, trouble staying awake.

  • Low Blood Pressure - Feeling faint or lightheaded, dizziness, blurry vision.

  • Stiff muscles, high fever, fast or irregular heartbeat, increased sweating, and confusion might indicate neuroleptic malignant syndrome (a life-threatening reaction to antipsychotic drugs).

  • Muscle stiffness or spasms, uncontrolled and repetitive body movements, tremors, loss of balance or coordination, and restlessness are signs of extrapyramidal symptoms (EPS).

Side effects that usually do not require medical attention. However, these must be reported if they continue.

  • Anxiety, nervousness.

  • Drowsiness.

  • Dizziness.

  • Restlessness.

  • Hallucinations.

How to Store This Medication?

This medication is administered in a hospital or clinic and should not be stored at home.

For Doctors:

Indications:

  • Antipsychotic Therapy: Droperidol is utilized in the management of acute psychotic episodes, particularly in emergency settings where rapid tranquilization is necessary. Its potent sedative and antipsychotic effects make it valuable for calming agitated or aggressive individuals experiencing acute psychosis.

  • Antiemetic Therapy: In the perioperative setting, Droperidol is commonly employed to prevent and treat postoperative nausea and vomiting, which can significantly impact patient comfort and satisfaction after the surgery. Its efficacy in this regard has been well-documented, contributing to its widespread use in anesthesia practice.

  • Adjunctive Therapy in Migraine: Certain studies have explored the potential of Droperidol as an adjunctive therapy in the management of migraines, especially in cases refractory to conventional treatment. Its antiemetic properties, coupled with its ability to provide sedation and alleviate anxiety, render it a promising option in this context.

Pharmacology:

Droperidol is rapidly absorbed when administered intramuscularly or intravenously. It has a large volume of distribution, extensively distributes to the body tissues, and easily crosses the blood-brain barrier to show its effects on the central nervous system. Droperidol undergoes hepatic metabolism primarily via the cytochrome P450 enzyme system, with the primary metabolite being 4-hydroxy droperidol. It is mainly eliminated via the kidneys, with approximately fifty percent of the administered dose excreted unchanged in the urine.

Like other medications, Droperidol follows certain pharmacokinetic principles, including absorption, distribution, metabolism, and elimination.

  • Absorption: Droperidol can be administered via various routes, including intramuscular (IM), intravenous (IV), and oral (though oral formulations are less common). When administered intramuscularly or intravenously, Droperidol is rapidly absorbed into the bloodstream due to its high lipid solubility.

  • Distribution: Droperidol has a large volume of distribution, indicating that it distributes extensively throughout the body tissues. It readily crosses the blood-brain barrier, which allows it to exert its effects on the central nervous system. Protein binding of Droperidol is moderate, with around 90 percent of the drug binding to plasma proteins.

  • Metabolism: Droperidol undergoes extensive hepatic metabolism primarily via the cytochrome P450 enzyme system, particularly CYP3A4. The primary metabolite of Droperidol is 4-hydroxy droperidol, which also exhibits pharmacological activity. This metabolite is further conjugated with glucuronic acid before being excreted from the body.

  • Elimination: In healthy individuals, Droperidol's elimination half-life is approximately two to four hours. The parent drug and its metabolites are mainly eliminated through the kidneys, with roughly fifty percent of the administered dose excreted unchanged in the urine. The remainder is excreted as metabolites.

It is essential to note that individual variations in pharmacokinetics can occur based on factors such as age, liver function, and co-administration of other drugs that may affect metabolism. Additionally, Droperidol can accumulate in patients with impaired hepatic or renal function, so dosage adjustments may be necessary in these populations.

Mechanism of Action:

Droperidol is a medication mainly used as an antiemetic (to prevent nausea and vomiting) and also as a tranquilizer. Its mechanism of action involves antagonism of dopamine receptors in the brain, particularly D2 receptors. By blocking these receptors, Droperidol inhibits dopamine-mediated neurotransmission, leading to its sedative and antiemetic effects. Additionally, Droperidol also has some activity at serotonin receptors (5-HT2A), contributing to its antiemetic properties. However, its exact mechanism of action in producing tranquilization is not entirely understood. Droperidol's blockade of dopamine receptors plays a key role in its therapeutic effects.

Adverse Reactions:

While Droperidol offers therapeutic benefits across various clinical scenarios, its use is not without risks. Like other antipsychotic medications, Droperidol is associated with a range of potential side effects, including:

  • Extrapyramidal Symptoms (EPS): The blockade of dopamine receptors by Droperidol can lead to EPS, encompassing symptoms such as dystonia, akathisia, and parkinsonism. These movement disorders can be distressing for patients and may necessitate dose adjustment or discontinuation of therapy.

  • QT Prolongation: Droperidol has been associated with QT interval prolongation, which can predispose patients to potentially life-threatening ventricular arrhythmias, including torsades de pointes (a specific type of ventricular tachycardia or increased heart rhythm that starts in the ventricles of the heart). Consequently, caution is warranted when administering Droperidol, especially in patients with an underlying cardiac disorder or those taking other medications that prolong the QT interval.

  • Sedation and Hypotension: Droperidol possesses soothing properties that can result in excessive sedation, particularly when administered in high doses or in combination with other sedating agents. Additionally, Droperidol may cause hypotension, necessitating vigilant monitoring of blood pressure during administration.

Interactions:

Do not take this medication with any of the following:

  • Alfuzosin.

  • Abarelix.

  • Amoxapine.

  • Arsenic trioxide.

  • Apomorphine.

Certain antibiotics, such as:

  • Ciprofloxacin.

  • Clarithromycin.

  • Erythromycin.

  • Gatifloxacin.

  • Gemifloxacin.

  • Levofloxacin.

  • Moxifloxacin.

  • Ofloxacin.

  • Norfloxacin.

  • Pentamidine.

  • Sparfloxacin.

  • Troleandomycin.

  • Telithromycin.

Certain medications for cancer:

  • Daunorubicin.

  • Doxorubicin.

Certain medications for fungal infections:

  • Fluconazole.

  • Itraconazole.

  • Ketoconazole.

  • Posaconazole.

  • Voriconazole.

Certain medications for irregular heartbeat:

  • Dronedarone.

  • Chloroquine.

  • Clozapine.

  • Cisapride.

General and local anesthetics:

  • Halofantrine.

  • Haloperidol.

  • Methadone.

  • Maprotiline.

  • Octreotide.

Other medications for nausea and vomiting:

  • Dolasetron.

  • Palonosetron.

Phenothiazines:

  • Chlorpromazine.

  • Fluphenazine.

  • Mesoridazine.

  • Perphenazine.

  • Prochlorperazine.

  • Thioridazine.

  • Trifluoperazine.

Tricyclic antidepressants:

  • Amitriptyline.

  • Desipramine.

  • Nortriptyline.

This medication may also interact with the following:

  • Barbiturates.

  • Certain medications for depression.

  • Opioid medications for pain.

  • Dofetilide.

  • Diuretics.

  • Laxatives.

  • Ziprasidone.

Inform the healthcare provider of all the medicines, herbs, non-prescription drugs, or dietary supplements being taken. Also, inform them about smoking, drinking alcohol, or using illegal drugs. Some items may interact with this medicine.

Other Interactions

Certain medicines must not be administered at or around eating time or certain food types, as interactions may occur. Consuming alcohol or tobacco with certain medicines might also lead to interactions. Discuss with the healthcare professional the use of the medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems might affect the use of this medicine. Ensure to inform the doctor in case of other medical problems, especially:

  • Bradycardia (slow heartbeat).

  • Cardiac hypertrophy (the heart is larger than normal).

  • Congestive heart failure.

  • Heart disease.

  • Hypokalemia (low potassium in the blood).

  • Hypomagnesemia (low magnesium in the blood).

  • Pheochromocytoma (adrenal gland tumor). It might cause side effects to become worse.

  • Cardiac arrhythmias (abnormal heartbeats).

  • Hypotension (low blood pressure).

  • Congenital long QT syndrome (heart rhythm problem).

  • QT prolongation (heart rhythm problem). It must not be used in patients with these conditions.

  • Kidney disease.

  • In cases of liver disease, it must be administered with caution. The effects can be increased due to the slower removal of the medicine from the body.

Precautions:

Before administering this medicine, its risks must be compared with its benefits. This is a decision taken by the doctor. For this medicine, the following must be considered:

  • Allergies: Inform the doctor of any unusual or allergic reaction to this medicine or other medicines. Also, inform the health care provider about other types of allergies, like dyes, foods, preservatives, or animals. For non-prescription products, go through the label or ingredients thoroughly.

  • Pediatric: Adequate studies have yet to be performed on the relationship of age to the effects of Droperidol injection in children under two years of age. Safety and efficacy have yet to be established.

  • Geriatric: No data is available on the effects of Droperidol injection in geriatric patients. However, elderly patients show age-related heart or kidney problems that might require caution and an adjustment in the dose for patients receiving Droperidol injections.

  • Breastfeeding: No adequate studies in women have found the infant risk while using this medication while breastfeeding; before administering this medication, the potential benefits must be calculated against the risks.

Droperidol stands as a versatile medication with a spectrum of clinical applications, ranging from antiemesis to sedation and tranquilization. Its mechanism of action, primarily mediated through dopamine receptor antagonism, underscores its efficacy in alleviating symptoms such as nausea, anxiety, and agitation. However, clinicians must be cautious and vigilant when prescribing Droperidol, ensuring judicious dosing and close monitoring to mitigate the risk of adverse effects. With careful consideration of its benefits and risks, Droperidol continues to play a vital role in modern medicine, enhancing patient comfort and facilitating optimal clinical outcomes. Despite the controversies associated with its cardiac safety, Droperidol plays a significant role in clinical practice, particularly in anesthesia and emergency medicine. Ongoing research aims to elucidate the optimal dosing strategies and patient selection criteria to reduce the risk of cardiac adverse events while maximizing therapeutic efficacy.

Dr. Kaushal Bhavsar
Dr. Kaushal Bhavsar

Pulmonology (Asthma Doctors)

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