Domperidone

Oral
Nausea and vomiting

Dose and frequency reduction may be required.

Moderate or severe: Contraindicated.

Should be taken on an empty stomach. Take 15-30 min before meals.

Prolactin-releasing pituitary tumour (prolactinoma), conditions where stimulation of gastric motility may be harmful (e.g. gastrointestinal haemorrhage, mechanical obstruction or perforation), known existing prolongation of cardiac conduction intervals (particularly QTc), underlying cardiac disease (e.g. CHF), significant electrolyte disturbances (e.g. hypokalaemia, hypomagnesaemia, hyperkalaemia). Moderate or severe hepatic impairment. Concomitant use with QT-prolonging drugs or potent CYP3A4 inhibitors (e.g. azole antifungals, macrolides, protease inhibitors, nefazodone).

Patient with personal or family history of breast cancer, risk factors for sudden cardiac arrest (e.g. family history of coronary artery disease, high blood pressure, obesity, hypercholesterolaemia, diabetes, alcoholism, smoking). Renal and mild hepatic impairment. Children and elderly. Pregnancy and lactation.

Significant: Increased prolactin levels (dose-dependent). Very rarely, QT prolongation.
Eye disorders: Oculogyric crisis.
Gastrointestinal disorders: Dry mouth, diarrhoea.
General disorders and administration site conditions: Asthenia.
Immune system disorders: Very rarely, anaphylactic reaction (including anaphylactic shock).
Investigations: Very rarely, abnormal LFT.
Nervous system disorders: Headache, somnolence. Very rarely, convulsion, extrapyramidal disorder.
Psychiatric disorders: Anxiety, loss of libido. Very rarely, agitation, nervousness.
Renal and urinary disorders: Very rarely, urinary retention.
Reproductive system and breast disorders: Breast pain and tenderness, galactorrhoea. Rarely, amenorrhoea, gynaecomastia.
Skin and subcutaneous tissue disorders: Rash, pruritus. Very rarely, angioedema, urticaria.
Potentially Fatal: Very rarely, ventricular arrhythmias, Torsade de Pointes, sudden cardiac death.

Monitor renal function. Obtain ECG at baseline then periodically during treatment.

Symptoms: Altered consciousness, agitation, convulsions, disorientation, extrapyramidal reactions, and somnolence. Management: Supportive and symptomatic treatment. Perform gastric lavage and administer activated charcoal. Monitor ECG for the possibility of QT interval prolongation. May administer anticholinergics or anti-Parkinsonian agents to control extrapyramidal reactions.

Decreased bioavailability with antacids or antisecretory agents; avoid concurrent use. Anticholinergic agents (e.g. dextromethorphan, diphenhydramine) may antagonise the anti-dyspeptic effect of domperidone.
Potentially Fatal: Increased risk of serious ventricular arrhythmias or sudden cardiac death with QT-prolonging drugs (e.g. disopyramide, amiodarone, haloperidol, citalopram, erythromycin, pentamidine, halofantrine, cisapride, mizolastine, toremifene, aprepitant, bepridil, methadone) or potent CYP3A4 inhibitors (e.g. clarithromycin, ketoconazole, ritonavir, nefazodone).

May increase serum concentrations with grapefruit juice.

Description:
Mechanism of Action: Domperidone is a dopamine antagonist with antiemetic properties. Its effect may be attributed to a combination of peripheral (gastrokinetic) effects and antagonism of dopamine receptors in the chemoreceptor trigger zone (located in the area postrema). It increases oesophageal peristalsis, pressure in the lower oesophageal sphincter, gastric motility and peristalsis, and improves gastroduodenal coordination, thus facilitating gastric emptying and reducing small bowel transit time.
Pharmacokinetics:
Absorption: Rapidly absorbed. Bioavailability: Approx 15%. Time to peak plasma concentration: Approx 30-60 minutes.
Distribution: Enters breast milk (small amounts). Plasma protein binding: 91-93%.
Metabolism: Rapidly and extensively metabolised in the liver by CYP3A4 isoenzyme via N-dealkylation and by CYP3A4, CYP1A2, and CYP2E1 isoenzymes via hydroxylation. Undergoes extensive first-pass metabolism.
Excretion: Via urine (31%; approx 1% as unchanged drug); faeces (66%; 10% as unchanged drug). Elimination half-life: 7-9 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3151, Domperidone. https://pubchem.ncbi.nlm.nih.gov/compound/Domperidone. Accessed Mar. 29, 2022.

Store between 15-30°C. Protect from moisture and light.

Antiemetics

A03FA03 - domperidone ; Belongs to the class of propulsives. Used in the treatment of functional gastrointestinal disorders.

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