Indications of Apuldon 10 mg

Dyspeptic symptom complex, often linked with delayed gastric emptying, gastroesophageal reflux, and esophagitis, may include:

1. Epigastric sensation of fullness
2. Abdominal distension
3. Upper abdominal pain
4. Belching
5. Flatulence
6. Early satiety
7. Nausea and vomiting
8. Heartburn, with or without regurgitation of gastric contents into the mouth

These symptoms can occur in various conditions, such as non-ulcer dyspepsia, acute nausea and vomiting of functional, organic, infectious, dietetic origin, or induced by radiotherapy, drug therapy, or migraine. Additionally, in Parkinson's disease, it can manifest as dopamine-agonist induced nausea and vomiting. For radiological studies, it can be used to speed up barium transit in follow-through radiological examinations.

Theropeutic Class

Motility Stimulants, Motility stimulants/Dopamine antagonist, Prokinetic drugs

Pharmacology

Apuldon 10 mg functions as a dopamine receptor antagonist. It exerts gastroprokinetic action by inhibiting dopamine receptors found in the chemoreceptor trigger zone (CTZ) and the stomach. Its limited ability to cross the blood-brain barrier means it has minimal impact on dopaminergic receptors in the brain, thus avoiding psychotropic and neurological side effects.

Dosage and Administration of Apuldon 10 mg

For adults, the recommended dosage is 10-20 mg every 4-8 hours daily. Children should take 0.2-0.4 mg/kg every 4-8 hours daily. When used for acute nausea and vomiting, the maximum treatment duration should not exceed 12 weeks. It is advisable to take this medication 15-30 minutes before a meal.

Dosage of Apuldon 10 mg

Apuldon 10 mg should be taken 15-30 minutes before meals, and if needed, before bedtime. The typical recommended oral dosage of Domperidone is as follows:

For Adults:

1. 10-20 mg (1-2 tablets or 10-20 ml suspension) every 6-8 hours daily.
2. The maximum daily dose of Domperidone is 80 mg.

For Children:

1. 2-4 ml of suspension per 10 kg of body weight or 0.4-0.8 ml of pediatric drops per 10 kg of body weight, every 6-8 hours daily.

In cases of dyspeptic symptoms: For Adults:

1. 10-20 mg (1-2 tablets or 10-20 ml suspension) every 6-8 hours daily.

For Children:

1. 0.2-0.4 mg/kg (2-4 ml of suspension per 10 kg or 0.4-0.8 ml of pediatric drops per 10 kg of body weight) every 6-8 hours daily.

For acute and sub-acute conditions, especially in cases of acute nausea and vomiting: For Adults:

1. 20 mg (2 tablets or 20 ml suspension) every 6-8 hours daily.

For Children:

1. 0.2-0.4 mg/kg (2-4 ml of suspension per 10 kg or 0.4-0.8 ml of pediatric drops per 10 kg of body weight) every 6-8 hours daily.

When administered rectally in the form of suppositories: For Adults (including elderly):

1. 30-60 mg every 4-8 hours.

For Children:

1. The maximum daily rectal dose for children weighing between 10 to 25 kg is 30 mg. The dose may be divided throughout the day if necessary.

Please note that the maximum treatment period for acute nausea and vomiting is 12 weeks.

Interaction of Apuldon 10 mg

The simultaneous use of anticholinergic drugs may counteract the antidyspeptic effects of domperidone. It's important to note that antacids and antisecretory drugs should not be administered concurrently with domperidone as they can reduce its oral bioavailability. Domperidone primarily undergoes metabolism through the CYP3A4 enzyme. In vitro data suggest that coadministration with drugs significantly inhibiting this enzyme may lead to elevated plasma levels of domperidone. Examples of CYP3A4 inhibitors include azole antifungals, macrolide antibiotics, HIV protease inhibitors, nefazodone, and others.

Theoretically, as domperidone has gastro-kinetic effects, it could potentially impact the absorption of concurrently orally administered drugs, especially those with sustained release or enteric-coated formulations. However, in patients already stabilized on medications like digoxin or paracetamol, the concurrent use of domperidone did not affect the blood levels of these drugs. Domperidone does not potentiate the action of neuroleptics, and it suppresses the unwanted peripheral effects such as digestive disorders, nausea, and vomiting caused by dopaminergic agonists like bromocriptine and L-dopa without counteracting their central properties.

Contraindications

Apuldon 10 mg is not to be used by patients with a known hypersensitivity to this medication or in the case of neonates. It should also be avoided in situations where gastrointestinal stimulation could be unsafe, such as in cases of gastrointestinal hemorrhage, mechanical obstruction, or perforation. Additionally, it is contraindicated in patients with a prolactin-releasing pituitary tumor (prolactinoma).

Side Effects of Apuldon 10 mg

Side effects are uncommon, with occasional reports of transient intestinal cramps. Extrapyramidal symptoms are rare among young children and exceptionally rare in adults. These symptoms typically resolve spontaneously and completely upon discontinuing the treatment. Since the pituitary gland is situated outside the blood-brain barrier, domperidone may lead to an increase in plasma prolactin levels. In rare cases, this hyperprolactinemia can result in neuroendocrinological effects like galactorrhea and gynecomastia. In situations where the blood-brain barrier is immature (as in infants) or compromised, the possibility of neurological side effects cannot be entirely ruled out. Additionally, there have been occasional reports of rare allergic reactions, including rash and urticaria.

Pregnancy and Lactation

The safety of using Apuldon 10 mg during pregnancy has not been established; hence, its use is not recommended during pregnancy. Animal studies have not shown any teratogenic effects on the fetus. Domperidone may induce galactorrhea and enhance post-natal lactation. It is excreted in breast milk in minimal quantities, which are insufficient to be considered harmful.

Precautions and Warnings

Apuldon 10 mg should be employed with utmost care in children due to the potential for an increased risk of extrapyramidal reactions, which can be more pronounced in young children with an incompletely developed blood-brain barrier. Additionally, considering that domperidone undergoes extensive metabolism in the liver, it should also be used cautiously in patients with hepatic impairment.

Overdose Effects of Apuldon 10 mg

Signs of an overdose can manifest as drowsiness, disorientation, and extrapyramidal reactions, particularly in children. If an overdose occurs, it is advisable to administer activated charcoal and closely monitor the patient. The use of anticholinergic drugs, antiparkinson drugs, or antihistamines with anticholinergic properties may be beneficial in managing extrapyramidal reactions.

Storage Conditions

Store below 30°C, Protected from light and moisture. Keep out of children's reach.

Drug Classes

Motility Stimulants, Motility stimulants/Dopamine antagonist, Prokinetic drugs

Mode Of Action

Apuldon 10 mg acts as a dopamine antagonist, primarily by blocking dopamine receptors located in the Chemoreceptor Trigger Zone (CTZ) and the stomach. Its gastroprokinetic effect is achieved by inhibiting dopamine receptors that influence the motility of the gastrointestinal tract. Because it has limited ability to penetrate the blood-brain barrier, Domperidone has minimal impact on dopaminergic receptors in the brain, thus avoiding psychotropic and neurological side effects. Domperidone restores normal motility and tone in the upper gastrointestinal tract, promotes gastric emptying, enhances antral and duodenal peristalsis, and regulates pylorus contraction. Additionally, it increases esophageal peristalsis and lowers esophageal sphincter pressure, preventing the regurgitation of gastric contents.

Pediatric Uses

Use in infants: Given that the metabolic and blood-brain barrier functions are not fully developed during the first months of life, any medication should be administered to infants with great caution and under close medical supervision. Although the typical absence of neurological side effects with domperidone is primarily due to its limited penetration through the blood-brain barrier, the potential occurrence of such effects cannot be entirely ruled out in infants under 1 year of age.

Use in liver disorders: Because domperidone undergoes extensive metabolism in the liver, it should be employed cautiously in patients with hepatic impairment.

Use in kidney disorders: In individuals with severe renal insufficiency (serum creatinine andgt;6 mg/100ml, i.e., andgt;0.6 mmol/l), the elimination half-life of domperidone increases from 7.4 to 20.8 hours, although plasma drug levels remain lower than in healthy volunteers. Since very little unchanged drug is excreted through the kidneys, it is unlikely that the dose of a single acute administration needs to be adjusted in patients with renal insufficiency. However, for repeated administration, the dosing frequency should be reduced to once or twice daily, depending on the severity of the impairment, and the dose may need to be lowered. In general, patients on prolonged therapy should undergo regular reviews.