Canada-Approved Medicine

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.


Ther. Class.

gastric stimulant

Pharm. Class.


dopamine antagonists


  • 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.

Unlabeled Use(s):

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.

Therapeutic Effect(s):

  • 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.


POunknown30 min (blood levels)6–8 hr


Contraindicated in:

  • Known hypersensitivity/intolerance;
  • Concurrent use of ketoconazole;
  • Prolactinoma;
  • Conditions where GI stimulation is dangerous including GI hemorrhage/mechanical obstruction/perforation;
  • Lactation: Breastfeeding 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 flashes, 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 times daily;  Nausea/vomiting due to dopamine agonist antiparkinson agents: 10 mg 3 times daily; higher doses may be required during dose titration.

Renal Impairment 
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.


  • Use lowest effective dose.
  • Administer 3 times daily, 15–30 min before meals and at bedtime.

Patient/Family Teaching

  • 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.
  • Rep:  Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Evaluation/Desired Outcomes

  • Prevention or relief of nausea and vomiting.
  • Decreased symptoms of gastric stasis.