Domperidone; Indications, Dosage, Side Effects, Interactions ,Pregnancy

Domperidone

Domperidone is a specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.

Domperidone is a peripheral-specific antagonist of the dopamine receptor D2 (D2R), with antiemetic, gastrokinetic and galactagogue activities. Following administration, domperidone binds to D2R expressed by peripheral neurons; this inhibits dopamine binding and D2R-mediated signaling. Inhibition of peripheral D2R signaling prevents or relieves various gastrointestinal (GI) symptoms, such as nausea and vomiting, and may help relief reflux and symptoms of a variety of other upper GI disorders.

Domperidone is only found in individuals that have used or taken this drug. It is a specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms. Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which – among others – regulates nausea and vomiting

Mechanism of Action of Domperidone

Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which – among others – regulates nausea and vomiting

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Indications of Domperidone

Therapeutic Indications of Domperidone [FDA Level]

Contra indications of Domperidone

  • Triazole antifungal medications such as ketoconazole, itraconazole, fluconazole.
  • Macrolide antibiotics such as erythromycin and clarithromycin.
  • Grapefruit juice.
  • QT-prolonging drugs like amiodarone.
  • Prolactin secreting pituitary tumor (prolactinoma) or hyperprolactinemia.
  • Mechanical bowel disorders such as bowel obstruction, gastrointestinal haemorrhage or bowel perforation
  • Moderate hepatic impairment (liver disease).
  • Severe renal impairment (kidney disease).
  • Cardiac disease.

Dosage of Domperidone

Strengths: 10 mg ,

 Nausea, and vomiting /gastrointestinal abnormality

  • The usual dose for the treatment is 1 to 2 tablets taken 3 to 4 times a day before meals. Do not take more than 8 tablets (80mg) in 24 hours.
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Infants and Children

  • Children weighing less than 35kg (5 stone) should not take these tablets. The usual dose for the treatment is 0.25 0.5mg per kg bodyweight taken 3 to 4 times a day before meals. Your pharmacist may be able to help you if you are not sure.

Side Effects of Domperidone

Most common 

Common

Rare

Drug Interactions of Domperidone

Domperidone may interact with following drugs, supplyments, & may change the efficacy of drugs

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Pregnancy & Lactation of Domperidone

FDA  Pregnancy Category C 

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Breastfeeding

This medication passes into breast milk. If you are a breastfeeding mother and are taking domperidone, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children.


  1. References

    1. https://pubchem.ncbi.nlm.nih.gov

 

Domperidone