This monograph describes a medication approved for use in Canada by the Therapeutic Products Directorate, a division of Health Canada’s Health Products and Food Branch. The medication is not approved by the United States Food and Drug Administration; however, a similar formulation carrying a different generic or brand name might be available in the US.
- Management of symptoms associated with GI motility disorders including subacute/chronic gastritis and diabetic gastroparesis.
- Treatment of nausea/vomiting associated with dopamine agonist antiparkinson therapy.
To stimulate lactation.
- Acts as a peripheral dopamine receptor blocker.
- Increases GI motility, peristalsis, and lower esophageal sphincter pressure.
- Facilitates gastric emptying and decreases small bowel transit time.
- Also increases prolactin levels.
- Improved GI motility.
- Decreased nausea/vomiting associated with dopamine agonist antiparkinson therapy.
Absorption: Well absorbed following oral administration.
Distribution: Does not cross the blood-brain barrier; enters breast milk in low concentrations.
Metabolism and Excretion: Undergoes extensive first-pass hepatic metabolism; much via the CYP3A4 enzyme system. 31% excreted in urine, 66% in feces.
Half-life: 7 hr.
|PO||unknown||30 min (blood levels)||6–8 hr|
- Known hypersensitivity/intolerance;
- Concurrent use of ketoconazole;
- Conditions where GI stimulation is dangerous including GI hemorrhage/mechanical obstruction/perforation;
- Lactation: Breast feeding is not recommended unless potential benefits outweigh potential risks.
Use Cautiously in:
- History of breast cancer;
- Hepatic impairment;
- Severe renal impairment (dose adjustment may be necessary during chronic therapy);
- OB: Use only if expected benefit outweighs potential hazard;
- Pedi: Safety and effectiveness not established.
Adverse Reactions/Side Effects
CNS: headache, insomnia
GI: dry mouth
GU: amenorrhea, impotence
Derm: hot flushes, rash
Endo: galactorrhea, gynecomastia, hyperprolactinemia
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
Ketoconazole ↑ levels and the risk of cardiovascular toxicity; concurrent use contraindicated; other azole antifungals, macrolide anti-infectives, and protease inhibitors may have similar effects.
- Risk of adverse cardiovascular reactions may be ↑ by concurrent use of drugs known to ↑ QT interval including antiarrhythmics, some fluoroquinolones, antipsychotics, beta-2 adrenergic agonists, antimalarials, SSRIs, tri/tetracyclic antidepressants, and nefazodone and should be undertaken cautiously, especially if other risk factors for torsade de pointes exists.
- Effectiveness may be ↓ by concurrent use of anticholingerics.
- Due to effects on gastric motility, absorption of drugs from the small intestine may be accelerated, while absorption of drugs from the stomach may be slowed, especially sustained-release or enteric-coated formulations.
- Concurrent use with MAOIs should be undertaken with caution.
Grapefruit juice may ↑ levels.
PO (Adults): Upper GI motility disorders– 10 mg 3–4 times daily; may be ↑ to 20 mg 3–4 times daily; Nausea/vomiting due to dopamine agonist antiparkinson agents– 20 mg 3–4 times daily, higher doses may be required during dose titration.
PO (Adults): Depending on degree of impairment, dosing during chronic therapy should be reduced to once or twice daily.
Tablets: 10 mg
- Assess for nausea, vomiting, abdominal distention, and bowel sounds before and after administration.
- Monitor BP (sitting, standing, lying down) and pulse before and periodically during therapy. May cause prolonged QT interval, tachycardia, and orthostatic hypotension, especially in patients older than 60 yr or taking >30 mg/day.
- Monitor for symptoms related to hyperprolactinemia (menstrual abnormalities, galactorrhea, sexual dysfunction).
Lab Test Considerations:
May cause ↑ serum ALT, AST, and cholesterol.
- Monitor serum prolactin prior to and periodically during therapy. May cause ↑ serum prolactin levels.
- Imbalanced nutrition: less than body requirements
- Risk for injury(side effects)
- Use lowest effective dose.
- Administer 3–4 times daily, 15–30 min before meals and at bedtime.
- Instruct patient to take as directed. Advise patient to avoid grapefruit juice during therapy.
- Advise patient to notify health care professional if galactorrhea (excessive or spontaneous flow of breast milk), gynecomastia (excessive development of male mammary gland), menstrual irregularities (spotting or delayed periods), palpitations, irregular heartbeat (arrhythmia), dizziness, or fainting occur.
- Advise female patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.
- Prevention or relief of nausea and vomiting.
- Decreased symptoms of gastric stasis.