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 the supervision of a physician and is available as an injectable solution. It is important to remember that droperidol should only be used under the direction of a physician, who will determine the appropriate dosage and treatment regimen based on the specific needs and condition of the patient.

Indications Droperidol

1. Antipsychotic action: Droperidol belongs to a class of drugs called antipsychotics and is often used to treat various mental disorders, such as schizophrenia and bipolar disorder. It typically 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 connection with surgery or treatment with radiation or chemotherapy.
3. Sedative action: The drug may have sedative properties, which may help relieve anxiety and provide calm in some patients.
4. Antiemetic action: Droperidol can help reduce nausea and vomiting caused by various reasons 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 antagonist effect on dopamine D2 receptors, which helps reduce the hyperactivity of the dopaminergic system that may be associated with symptoms of schizophrenia and other mental disorders.
2. Antiemetic action: Droperidol also has an antiemetic action due to its action on dopamine receptors in the vomiting center of the brain. This makes it useful in controlling nausea and vomiting, especially in the case of surgical procedures or chemotherapy.
3. Sedative effects: Droperidol may cause sedation in some patients, which may be useful in managing anxiety or agitation.
4. Dopaminergic activity: Droperidol may also act on other dopamine receptors in the brain, including D1 and D3 receptors, but its primary action 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 can be administered intravenously, intramuscularly, or orally. After oral administration, absorption occurs in the gastrointestinal tract, but due to low bioavailability (approximately 50%), other routes 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 neuroleptic activity.
4. Excretion: Droperidol and its metabolites are excreted primarily via the kidneys. Droperidol and its metabolites excreted in urine are usually in conjugated form.
5. Half-terminal time (t½): The half-terminal time of droperidol is approximately 3-4 hours, and for its major metabolite BHPM it is approximately 20 hours.
6. Protein binding: Droperidol is highly bound to plasma proteins, approximately 90%.

Dosing and administration

Droperidol can be administered 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 patient's needs. 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 under strict medical supervision. It is important to evaluate the benefits of the drug for the mother and the potential risks to fetal development.

Although there is limited data on the safety of droperidol during pregnancy, some studies have shown a slight increase in the risk of adverse effects on the fetus. This may include premature contractions or decreased fetal heart rate. However, in some cases, when the benefits to the mother outweigh the potential risks to the fetus, a 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 parkinsonian features, as it may worsen 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 a known prolonged QT interval or those taking other drugs that may aggravate this condition.
4. Central depressant action: The drug should be used with caution in patients with central depressant action or those taking other central depressant drugs, as it may increase respiratory depression and central action.
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, since the drug may lower the threshold of excitability.
7. Pregnancy and breastfeeding: The use of droperidol during pregnancy and breastfeeding 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 efficacy have not been fully established in this age group.

Side effects Droperidol

1. Sedation and somnolence: Droperidol may cause somnolence 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 may appear both earlier and 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 droperidol, especially in individuals with low baseline blood pressure.
6. Increased Prolactin: Droperidol may cause an increase in blood prolactin levels, which may 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 develop.
8. Effect on the cardiovascular system: In rare cases, droperidol may cause QT interval, which may lead to cardiac arrhythmias.

Overdose

Symptoms of overdose may include drowsiness, decreased consciousness, agitation, agitation, muscle rigidity, tremor, bradycardia, hypotension, arrhythmia, hypothermia, respiratory depression, coma, and other neurologic 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 sedative effects.
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 prolong the QT duration on the electrocardiogram, so co-administration with other antiarrhythmic drugs such as amidaron 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 antifungals, may increase the risk of developing cardiac arrhythmias.
5. Drugs metabolized in the liver: Droperidol is metabolized in the liver, therefore co-administration with other drugs that are also metabolized in the liver via cytochrome P450 may increase the risk of toxic effects.