Droperidol

Droperidol is a drug that is commonly used in medical practice to treat a number of conditions, including mental disorders and nausea and vomiting. 

Droperidol is usually used under medical supervision and is available as an injection. It is important to remember that droperidol should only be used as prescribed by a physician, who will determine the appropriate dosage and treatment regimen based on the patient's specific needs and condition.

Indications Droperidol

1. Antipsychotic Action: Droperidol belongs to the class of antipsychotic drugs and is often used to treat various mental disorders such as schizophrenia and bipolar disorder. It usually works by blocking dopamine receptors in the brain, which can help reduce psychotic symptoms such as delusions, hallucinations and thought disorders.
2. Prevention of nausea and vomiting: Droperidol may be used to prevent nausea and vomiting, especially in association with surgery or treatment with radiation or chemotherapy.
3. Sedative effects: The drug may have sedative properties, which may help relieve anxiety and provide calmness in some patients.
4. Antiemetic effect: Droperidol may help reduce nausea and vomiting caused by various causes, such as surgery, illness, or treatment with other drugs.
5. Prevention and treatment of movement disorders: In some cases, droperidol may be used to prevent and treat movement disorders such as tremor or dyskinesia associated with certain neurological or psychiatric conditions.

Release form

Injection solution: This is a solution intended for intravenous or intramuscular administration. Injection solutions are usually provided in ampoules or vials and should be used under the supervision of medical personnel.

Pharmacodynamics

1. Action: Droperidol is a typical antipsychotic drug that acts as an antagonist of dopamine receptors in the brain. It has a primary antagonistic effect on dopamine D2 receptors, which helps reduce the overactivity of the dopaminergic system that may be associated with symptoms of schizophrenia and other mental disorders.
2. Antiemetic effect: Droperidol also has an antiemetic effect due to its effect on dopamine receptors in the vomiting center of the brain. This makes it useful for controlling nausea and vomiting, especially in the case of surgical procedures or chemotherapy.
3. Sedation: Droperidol may cause sedation in some patients, which may be useful in managing anxious or agitated conditions.
4. Dopaminergic activity: Droperidol may also act on other dopamine receptors in the brain, including D1 and D3 receptors, but its main effect is on D2 receptors.
5. Effects on other systems: In addition to its effects on dopamine receptors, droperidol may also affect other neurotransmitter systems such as serotonin and norepinephrine, but its main mechanism of action is related to dopamine.

Pharmacokinetics

1. Absorption: Droperidol may be administered intravenously, intramuscularly, or orally. After oral administration of the drug, absorption occurs in the gastrointestinal tract, but due to low bioavailability (about 50%) other methods of administration are often used to relieve the severity of symptoms.
2. Distribution: Droperidol is well distributed throughout the body. It can cross the blood-brain barrier and form high concentrations in the central nervous system.
3. Metabolism: Droperidol is metabolized in the liver to form active metabolites. The main metabolite is 4-butoxy-4-fluoro-1-piperidinecarboxylic acid (BHPM). This metabolite also has antipsychotic effects.
4. Excretion: Droperidol and its metabolites are excreted primarily through the kidneys. Droperidol and its metabolites excreted in urine are usually in conjugated form.
5. Half-time (t½): The half-time of droperidol is approximately 3-4 hours, and for its main metabolite BHPM - about 20 hours.
6. Protein binding: Droperidol binds to plasma proteins to a significant extent, approximately 90%.

Dosing and administration

Droperidol can be given intravenously or intramuscularly, usually in a medical facility under the supervision of medical personnel. The dosage of the solution is usually determined by the doctor depending on the severity of the symptoms and the needs of the patient. The initial dose is usually 2.5-5 mg, but it can be increased or decreased depending on the body's response.

Use Droperidol during pregnancy

The use of droperidol during pregnancy should be done with caution and only with strict prescription from a doctor. It is important to evaluate the benefits of using the drug for the mother and the potential risks for the development of the fetus.

Although data on the safety of droperidol during pregnancy is limited, some studies have shown a slight increase in the risk of adverse effects on the fetus. This may include premature labor or a decrease in the fetal heart rate. However, in some cases, when the benefits to the mother outweigh the potential risks to the fetus, the doctor may decide to prescribe droperidol.

Contraindications

1. Hypersensitivity: People with a known hypersensitivity or allergic reaction to droperidol or other components of the drug should avoid its use.
2. Parkinsonism: The drug should be used with caution in patients with parkinsonism or signs of parkinsonism, as it may increase the symptoms of this condition.
3. Prolonged QT interval: Droperidol may cause prolongation of the QT interval on the ECG, so its use should be avoided in patients with known prolonged QT interval or those taking other drugs that may worsen this condition.
4. Central depressant effects: The drug should be used with caution in patients with central depressant effects or those taking other central depressant drugs, as this may increase respiratory depression and central effects.
5. Paralytic ileus: Droperidol may be contraindicated in patients with paralytic ileus due to its ability to slow intestinal motility.
6. Epilepsy: When using droperidol, caution should be exercised in patients with a history of epilepsy or susceptible to epileptic seizures, as the drug may reduce the excitability threshold.
7. Pregnancy and breast-feeding: The use of droperidol during pregnancy and breast-feeding may be contraindicated due to insufficient data on its safety in these conditions.
8. Children: Droperidol should be used with caution in children as its safety and effectiveness have not been fully established in this age group.

Side effects Droperidol

1. Sedation and drowsiness: Droperidol may cause drowsiness or central nervous system depression, especially at high doses or in sensitive patients.
2. Extrapyramidal symptoms: These symptoms include tremors, ventricular rhythmic movements, dyskinesias, etc. They can appear either earlier or later during droperidol therapy.
3. Anticholinergic effects: Include dry mouth, constipation, difficulty urinating, and changes in vision.
4. Tachycardia: Rapid heartbeat may be one of the side effects of droperidol.
5. Hypotension: A decrease in blood pressure may occur with the use of droperidol, especially in individuals with low baseline blood pressure.
6. Increased prolactin: Droperidol may cause an increase in blood prolactin levels, which can lead to hyperprolactinemia and associated effects such as gynecomastia, galactorrhea and menstrual irregularities in women.
7. Allergic reactions: Rarely, allergic reactions such as skin rash, itching or angioedema may occur.
8. Effect on the cardiovascular system: In rare cases, droperidol can cause QT interval, which can lead to cardiac arrhythmias.

Overdose

Symptoms of overdose may include drowsiness, decreased consciousness, agitation, agitation, muscle stiffness, tremor, bradycardia, hypotension, arrhythmia, hypothermia, respiratory depression, coma, and other neurological and cardiovascular complications.

Interactions with other drugs

1. Central analgesics and sedatives: Concomitant use of droperidol with analgesics and sedatives, such as opioids or benzodiazepines, may enhance their central action and lead to increased sedation.
2. Antihistamines: Using droperidol with antihistamines such as dimenhydrinate or cetirizine may increase anticholinergic side effects such as dry mouth, constipation and difficulty urinating.
3. Antiarrhythmic drugs: Droperidol may increase the QT duration on the electrocardiogram, so concomitant use with other antiarrhythmic drugs such as amidarone or quinidine may increase the risk of developing cardiac arrhythmias.
4. Drugs that prolong the QT interval: Concomitant use of droperidol with other drugs that may prolong the QT interval, such as macrolide antibiotics or antimycotics, may increase the risk of developing cardiac arrhythmias.
5. Drugs metabolized by the liver: Droperidol is metabolized by the liver, so coadministration with other drugs that are also metabolized by the liver via cytochrome P450 may increase the risk of toxic effects.