Domperidone

Domperidone is a drug used to treat various gastrointestinal disorders. It belongs to a group of drugs called dopamine antagonists. Domperidone is commonly used to reduce nausea and vomiting and to improve digestion.

Domperidone is available in a variety of forms, including tablets and oral suspensions.

It is important to consult with your doctor before starting domperidone to obtain individualized dosing and administration recommendations, as well as to assess the risk of possible side effects.

Indications Domperidone

1. Nausea and vomiting: Domperidone is used to treat nausea and vomiting, which can be caused by a variety of causes, including infections, food poisoning, medications, radiation therapy, and chemotherapy.
2. Gastroparesis: This is a condition in which the stomach muscles do not work properly, which slows the passage of food through the gastrointestinal tract and can cause nausea, vomiting and other symptoms. Domperidone may be used to treat gastroparesis.
3. Reflux esophagitis: Domperidone may be used to treat reflux esophagitis, a condition in which acid from the stomach rises up into the esophagus, causing irritation and inflammation.
4. Other gastrointestinal disorders: Domperidone may be used to treat other gastrointestinal disorders such as functional digestive disorders, constipation and diarrhea.

Release form

1. Oral tablets: This is the most common form of domperidone and is available in both regular and disintegrating tablets. Tablets may contain different amounts of active ingredient, usually from 10 mg to 20 mg.
2. Oral suspension: A liquid form of domperidone that is convenient for children and adults who have difficulty swallowing tablets. The suspension allows you to easily adjust the dosage.

Pharmacodynamics

Its pharmacodynamics are related to its ability to block dopamine receptors in the body.

Domperidone is a D2 dopamine receptor antagonist. It acts primarily in the small intestine and results in increased peristalsis and faster gastric emptying. This explains its effectiveness in treating nausea and vomiting.

Blocking dopamine receptors also results in a decrease in the inhibition of dopamine by the antagonist on prolactin, which may increase its blood levels. In this regard, domperidone can also be used to stimulate lactation in women.

In general, the pharmacodynamics of domperidone are related to its ability to increase gastrointestinal motility and reduce nausea and vomiting by blocking dopamine receptors.

Pharmacokinetics

1. Absorption: Domperidone is usually well absorbed from the gastrointestinal tract when taken orally. It has high bioavailability.
2. Distribution: Domperidone has a relatively low volume of distribution, meaning that it is distributed primarily in body fluids rather than tissues.
3. Plasma protein binding: Approximately 90% of domperidone is bound to plasma proteins.
4. Metabolism: Domperidone is metabolized in the liver, mainly with the participation of the enzyme CYP3A4. Its metabolites do not have pharmacological activity.
5. Elimination: About 30-40% of domperidone is excreted unchanged through the kidneys, and the rest through the intestines. The half-life is about 7-9 hours.
6. Effects on other drugs: Domperidone may interact with drugs that are also metabolized by the enzyme CYP3A4, which may lead to an increase or decrease in their blood levels.
7. Food and antacids: Food and antacids containing aluminum or magnesium may slow the absorption of domperidone from the gastrointestinal tract.
8. Pharmacokinetics in different populations: In elderly patients and in patients with impaired renal function, the pharmacokinetic parameters of domperidone may be altered.

Dosing and administration

For adults and children over 12 years old (or weighing more than 35 kg):

• Oral administration: The usual dose is 10 mg 15-30 minutes before meals and, if necessary, at bedtime. Domperidone can be taken up to 3-4 times a day, the maximum daily dose should not exceed 80 mg.

For children under 12 years old:

• The use of domperidone in children under 12 years of age (or weighing less than 35 kg) should be limited and strictly monitored by a physician due to possible risks and side effects.
• Rectal suppositories can be used for children, but the dosage and frequency of use must be carefully determined by the doctor.

For patients with renal failure:

• Patients with impaired renal function may require dose adjustments and increased intervals between doses. It is important to consult your doctor to determine a safe dosage.

Special instructions:

• Domperidone should be taken 15-30 minutes before meals for maximum effectiveness, as eating may slow its absorption and reduce effectiveness.
• If you miss a dose, take the missed dose as soon as possible, but if it is close to your next dose, skip it and continue your dosing regimen. Do not double the next dose to make up for a missed dose.

Use Domperidone during pregnancy

The use of Domperidone during pregnancy requires caution as data on its safety during this period are limited. Below are the main findings from the available research:

1. A study of pregnancy outcomes with domperidone found that taking this drug in the first trimester of pregnancy is not associated with an increased risk of spontaneous abortion, stillbirth, major birth defects, preterm birth, or low birth weight babies. However, additional research is needed to confirm these results in a larger sample (Pasternak et al., 2013).
2. EFEMERIS Database: Another study conducted as part of the EFEMERIS Database compared pregnancy outcomes between women exposed to domperidone and those not exposed to the drug. The findings indicate no significant difference in the incidence of birth defects between the groups, which also indicates the potential safety of the drug during pregnancy (Araujo et al., 2021).

Before using domperidone or other drugs during pregnancy, you should consult your doctor to evaluate all possible risks and benefits.

Contraindications

1. Allergic reaction: People with a known allergy to domperidone or any other ingredient in the drug should avoid taking it.
2. Heart problems: Domperidone may worsen heart problems or arrhythmias, so it is not generally recommended for patients with heart failure or other heart conditions.
3. Intestinal problems: People with intestinal bleeding, perforation, or mechanical obstructions in the stomach or intestines should avoid domperidone.
4. Liver problems: Patients with severe liver dysfunction or liver failure should use domperidone with caution as it may increase unwanted effects.
5. Kidney problems: People with severe kidney impairment or kidney failure may have limited use of domperidone.
6. Electrolyte Problems: Due to its effects on the gastrointestinal tract, domperidone can affect electrolyte levels in the body. People with electrolyte imbalances should be careful when using the drug.

Side effects Domperidone

1. Drowsiness: Some patients may feel sleepy or tired while taking domperidone.
2. Dizziness: This can also be a common side effect of domperidone.
3. Dry mouth: Some people may experience a feeling of dry mouth after taking domperidone.
4. Abdominal pain: Some patients may experience pain or discomfort in the abdomen.
5. Constipation: Some patients may experience constipation after taking domperidone.
6. Stomach problems menstrual cycle: Women may experience irregularities in their menstrual cycle.
7. Milky discharge from the breasts: Some women, especially after childbirth, may experience milky discharge from the breasts.
8. Extrapyramidal symptoms: In rare cases, extrapyramidal symptoms such as tremors, unusual body movements, or muscle cramps may occur with domperidone use.

Overdose

1. Dizziness and drowsiness.
2. Insomnia or other sleep disorders.
3. Anxiety or irritability.
4. Involuntary movements such as trembling or unusual body movements (dyskenesia).
5. Tachycardia (fast heart rate).
6. Convulsions.
7. Unusual changes in the electrocardiogram (ECG).

Interactions with other drugs

1. Drugs that prolong the QT interval: Domperidone may potentiate a prolonged QT interval on the ECG. Concomitant use with other drugs, such as antiarrhythmic drugs (eg, amidarone, sotalol) or antiarrhythmic antibiotics (eg, erythromycin, clarithromycin), may increase the risk of cardiac arrhythmias.
2. Drugs that depress the central nervous system: Concomitant use with other drugs, such as benzodiazepines, narcotic analgesics or hypnotics, may increase their sedative effect.
3. Drugs that enhance the effect of anticholinergic drugs: Concomitant use with anticholinergic drugs, such as antihistamines or antispasmodics, may increase the anticholinergic effects of domperidone.
4. Drugs that enhance antidopaminergic effects: Concomitant use with other antidopaminergic drugs, such as some antipsychotics or antiparkinsonian drugs, may increase their effect and lead to increased side effects.
5. Drugs that change gastric acidity: Drugs that reduce gastric acidity, such as antacids or proton pump inhibitors, may slow the absorption of domperidone from the gastrointestinal tract.
6. Drugs that increase the risk of extrapyramidal symptoms: Concomitant use with certain drugs, such as antipsychotics, may increase the risk of developing extrapyramidal symptoms.