MOTILIUM Domperidone 1mg / mL Suspension 100mL
NONRXDRUG-DR-X8545
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
The dyspeptic symptom complex that is often associated with delayed gastric emptying, gastroesophageal reflux and esophagitis: Epigastric sense of fullness, early satiety, feeling of abdominal distension, upper abdominal pain; bloating, eructation, flatulence; nausea and vomiting; heartburn with or without regurgitations of gastric contents in the mouth. Nausea and vomiting of functional organic, infectious or dietetic origin or induced by radiotherapy or drug therapy. A specific indication is nausea and vomiting induced by dopamine agonists used in the treatment of Parkinson's disease (eg, L-dopa and bromocriptine).
Dosage/Direction for Use
It is recommended to take oral domperidone (Motilium) 15-30 minutes before meals. If taken after meals, absorption of the drug is somewhat delayed. When domperidone (Motilium) is used under medical supervision, the following dosing information applies: Adults and adolescents ≥ 12 years of age and weighing ≥ 35 kg, and children < 12 years of age and weighing ≥ 35 kg: The dose of domperidone (Motilium) should be the lowest effective dose for the individual situation (typically 30 mg/day) and can be increased if necessary to a maximum daily oral dose of 40 mg. Usually, the maximum treatment duration should not exceed one week for the treatment of acute nausea and vomiting. If nausea and vomiting persist for longer than one week, patients should consult their physician. For other indications, the initial duration of treatment is up to four weeks. If treatment exceeds four weeks, patients should be reevaluated and the need for continued treatment reassessed. (See Table 1.)
Adults and adolescents (≥ 12 years of age) weighing < 35 kg: The dose of domperidone (Motilium) should be the lowest effective dose. The total daily dose is dependent on body weight (see Table 2). Usually, the maximum treatment duration should not exceed one week for the treatment of acute nausea and vomiting. For other indications, the initial duration of treatment is up to four weeks. If treatment exceeds four weeks, patients should be reevaluated and the need for continued treatment reassessed. Film-coated tablets and orodispersible tablets are unsuitable for use in adults and adolescents weighing less than 35 kg. (See Table 2.)
Infants and children < 12 years of age and weighing < 35 kg: The efficacy of Motilium has not been established in infants and children < 12 years of age and weighing < 35 kg.
When domperidone (Motilium) is not prescribed by a doctor and is used over-the-counter, the following dosing information applies:
Adults and adolescents 12-60 years of age and weighing ≥ 35 kg: Domperidone (Motilium) can be taken as 10 mg administered up to 3 times a day to a maximum daily dose of 30 mg.
Continuous use of domperidone (Motilium) without medical consultation should not exceed 7 days for the treatment of acute nausea and vomiting and 14 days for dyspeptic symptom complex.
Adults > 60 years of age: Patients older than 60 years of age should consult their physician before taking Domperidone (Motilium).
Infants and children <12 years old: Domperidone (Motilium) should not be administered to children <12 years old and weighing ≥ 35 kg unless prescribed for use. The efficacy of Motilium has not been established in infants and children < 12 years of age and weighing < 35 kg.
Prescription and Non-prescription Use: Renal impairment: Since the elimination half-life of domperidone is prolonged in severe renal impairment (serum creatinine > 6 mg/100 mL, i.e. > 0.6 mmol/L), the dosing frequency of domperidone (Motilium) should be reduced to once or twice daily, depending on the severity of the impairment, and the dose may need to be reduced. Patients with severe renal impairment should be reviewed regularly (see Pharmacology: Pharmacokinetics under Actions).
Hepatic impairment: Domperidone (Motilium) is contraindicated for patients with moderate (Child-Pugh 7 to 9) or severe (Child-Pugh >9) hepatic impairment (see Contraindications). Dose adjustment is not required for patients with mild (Child-Pugh 5 to 6) hepatic impairment (see Pharmacology: Pharmacokinetics under Actions).
When domperidone (Motilium) is not prescribed by a doctor and is used over-the-counter, the following dosing information applies:
Adults and adolescents 12-60 years of age and weighing ≥ 35 kg: Domperidone (Motilium) can be taken as 10 mg administered up to 3 times a day to a maximum daily dose of 30 mg.
Continuous use of domperidone (Motilium) without medical consultation should not exceed 7 days for the treatment of acute nausea and vomiting and 14 days for dyspeptic symptom complex.
Adults > 60 years of age: Patients older than 60 years of age should consult their physician before taking Domperidone (Motilium).
Infants and children <12 years old: Domperidone (Motilium) should not be administered to children <12 years old and weighing ≥ 35 kg unless prescribed for use. The efficacy of Motilium has not been established in infants and children < 12 years of age and weighing < 35 kg.
Prescription and Non-prescription Use: Renal impairment: Since the elimination half-life of domperidone is prolonged in severe renal impairment (serum creatinine > 6 mg/100 mL, i.e. > 0.6 mmol/L), the dosing frequency of domperidone (Motilium) should be reduced to once or twice daily, depending on the severity of the impairment, and the dose may need to be reduced. Patients with severe renal impairment should be reviewed regularly (see Pharmacology: Pharmacokinetics under Actions).
Hepatic impairment: Domperidone (Motilium) is contraindicated for patients with moderate (Child-Pugh 7 to 9) or severe (Child-Pugh >9) hepatic impairment (see Contraindications). Dose adjustment is not required for patients with mild (Child-Pugh 5 to 6) hepatic impairment (see Pharmacology: Pharmacokinetics under Actions).
Overdosage
Symptoms: Drowsiness, disorientation and extrapyramidal reactions, especially in children.
Treatment: Anticholinergic, antiparkinson drugs or antihistamines with anticholinergic properties may be helpful in controlling the extrapyramidal reactions.
In case of overdosage, gastric lavage as well as the administration of activated charcoal may be useful. Close medical supervision and supportive therapy is recommended.
Treatment: Anticholinergic, antiparkinson drugs or antihistamines with anticholinergic properties may be helpful in controlling the extrapyramidal reactions.
In case of overdosage, gastric lavage as well as the administration of activated charcoal may be useful. Close medical supervision and supportive therapy is recommended.
Administration
Should be taken on an empty stomach: Take 15-30 min before meals.
Contraindications
Patients with known intolerance to domperidone. Motilium should not be used whenever stimulation of gastric motility might be dangerous eg, in the presence of GI hemorrhage, mechanical obstruction or perforation.
Patients with a prolactin-releasing pituitary tumor (prolactinoma).
Patients with a prolactin-releasing pituitary tumor (prolactinoma).
Special Precautions
When antacids or antisecretory agents are used concomitantly, they should be taken after meals and not before meals ie, they should not be taken simultaneously with Motilium tablets and suspension.
The film-coated tablets contain lactose and may be unsuitable for patients with lactose intolerance, galactosemia or glucose/galactose malabsorption.
Liver Disorders: Since domperidone is highly metabolized in the liver, Motilium should be used with caution in patients with hepatic impairment.
Kidney Disorders: In patients with severe renal insufficiency (serum creatinine >6 mg/100 mL ie, >0.6 mmol/L), the elimination half-life of domperidone was increased from 7.4 to 20.8 hrs, but plasma drug levels were lower than in healthy volunteers. Since very little unchanged drug is excreted via the kidneys, it is unlikely that the dose of a single acute administration needs to be adjusted in patients with renal insufficiency. However, on 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 reduced. Patients on prolonged therapy should be reviewed regularly.
Use in Pregnancy: Domperidone given to animals at doses up to 160 mg/kg/day did not produce teratogenic effects.
However, as with most medicines, Motilium should only be used during the 1st trimester of pregnancy, if this is justified by the anticipated therapeutic benefit.
Up to now, there has been no evidence of any increase in the risk of malformations in humans.
Use in Lactation: Motilium is excreted in breast milk of lactating rats (mostly as metabolites: Peak concentrations of 40 and 800 ng/mL after oral and IV administration of 2.5 mg/kg, respectively). In women, domperidone concentrations in breast milk are 4 times lower than corresponding plasma concentrations. It is not known whether this is harmful to the newborn. Therefore, nursing is not recommended for mothers who are taking Motilium, unless the expected benefits outweigh any potential risk.
Use in Children: Infants: Because the metabolic and blood-brain barrier functions are not fully developed during the first months of life, any drug should only be given to infants with great caution and under close medical supervision.
Since the typical absence of neurological side effects with Motilium is mainly due to its poor penetration through the blood-brain barrier, the possible occurrence of such effects cannot be totally excluded in infants <1 year.
The film-coated tablets contain lactose and may be unsuitable for patients with lactose intolerance, galactosemia or glucose/galactose malabsorption.
Liver Disorders: Since domperidone is highly metabolized in the liver, Motilium should be used with caution in patients with hepatic impairment.
Kidney Disorders: In patients with severe renal insufficiency (serum creatinine >6 mg/100 mL ie, >0.6 mmol/L), the elimination half-life of domperidone was increased from 7.4 to 20.8 hrs, but plasma drug levels were lower than in healthy volunteers. Since very little unchanged drug is excreted via the kidneys, it is unlikely that the dose of a single acute administration needs to be adjusted in patients with renal insufficiency. However, on 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 reduced. Patients on prolonged therapy should be reviewed regularly.
Use in Pregnancy: Domperidone given to animals at doses up to 160 mg/kg/day did not produce teratogenic effects.
However, as with most medicines, Motilium should only be used during the 1st trimester of pregnancy, if this is justified by the anticipated therapeutic benefit.
Up to now, there has been no evidence of any increase in the risk of malformations in humans.
Use in Lactation: Motilium is excreted in breast milk of lactating rats (mostly as metabolites: Peak concentrations of 40 and 800 ng/mL after oral and IV administration of 2.5 mg/kg, respectively). In women, domperidone concentrations in breast milk are 4 times lower than corresponding plasma concentrations. It is not known whether this is harmful to the newborn. Therefore, nursing is not recommended for mothers who are taking Motilium, unless the expected benefits outweigh any potential risk.
Use in Children: Infants: Because the metabolic and blood-brain barrier functions are not fully developed during the first months of life, any drug should only be given to infants with great caution and under close medical supervision.
Since the typical absence of neurological side effects with Motilium is mainly due to its poor penetration through the blood-brain barrier, the possible occurrence of such effects cannot be totally excluded in infants <1 year.
Adverse Reactions
Increased prolactin levels. GI disorders. Transient intestinal cramps. Galactorrhea. Gynecomastia. Amenorrhea.
Drug Interactions
Concomitant administration of anticholinergic drugs may antagonize the antidyspeptic effect of Motilium.
Antacids and antisecretory drugs should not be given simultaneously with Motilium as they lower its bioavailability (see Precautions).
Theoretically, since Motilium has gastrokinetic effects, it could influence the absorption of concomitantly orally administered drugs, particularly those with sustained-release or enteric-coated formulations. However, in patients already stabilized on digoxin or paracetamol, concomitant administration of domperidone did not influence the blood levels of these drugs.
Main metabolic pathway of domperidone is through CYP3A4. In vitro data suggest that the concomitant use of drugs that significantly inhibit this enzyme may result in increased plasma levels. Examples of CYP3A4 inhibitors: Azole antifungals, macrolide antibiotics, HIV protease antibiotics and nefazodone.
Motilium may also be associated with: Neuroleptics, the action of which it does not potentiate; dopaminergic agonists (bromocriptine, L-dopa), whose unwanted peripheral effects eg, digestive disorders, nausea and vomiting, it suppresses without counteracting its central properties.
Antacids and antisecretory drugs should not be given simultaneously with Motilium as they lower its bioavailability (see Precautions).
Theoretically, since Motilium has gastrokinetic effects, it could influence the absorption of concomitantly orally administered drugs, particularly those with sustained-release or enteric-coated formulations. However, in patients already stabilized on digoxin or paracetamol, concomitant administration of domperidone did not influence the blood levels of these drugs.
Main metabolic pathway of domperidone is through CYP3A4. In vitro data suggest that the concomitant use of drugs that significantly inhibit this enzyme may result in increased plasma levels. Examples of CYP3A4 inhibitors: Azole antifungals, macrolide antibiotics, HIV protease antibiotics and nefazodone.
Motilium may also be associated with: Neuroleptics, the action of which it does not potentiate; dopaminergic agonists (bromocriptine, L-dopa), whose unwanted peripheral effects eg, digestive disorders, nausea and vomiting, it suppresses without counteracting its central properties.
Storage
Store between 15°C and 30°C.
Action
Synthetic gastrokinetic and antinauseant for oral use.
Pharmacology: Domperidone is a dopamine antagonist with antiemetic properties similar to those of metoclopramide and certain neuroleptic drugs. Unlike these other drugs, however, domperidone does not readily cross the blood-brain barrier. In domperidone users, especially in adults, extrapyramidal side effects are very rare, but domperidone promotes the release of prolactin from the pituitary. Its antiemetic effect may be due to a combination of peripheral (gastrokinetic) effects and antagonism of dopamine receptors in the chemoreceptor trigger zone, which lies outside the blood-brain barrier in the area postrema. Animal studies, together with the low concentrations found in the brain, indicate a predominantly peripheral effect of domperidone on dopamine receptors.
Studies in man have shown oral domperidone to increase the duration of antral and duodenal contractions, to increase the gastric emptying of liquids and semisolids in healthy subjects and of solids in patients in whom it was delayed, and to increase lower esophageal sphincter pressure in healthy subjects. It has no effect on gastric secretion.
Pharmacokinetics: Absorption: In fasting subjects, domperidone is rapidly absorbed after oral administration, with peak plasma concentrations at approximately 1 hr. The low absolute bioavailability of oral domperidone (~15%) is due to an extensive first-pass metabolism in the gut wall and liver. Although domperidone's bioavailability is enhanced in normal subjects when taken after a meal, patients with GI complaints should take domperidone 15-30 min before a meal. Reduced gastric acidity impairs the absorption of domperidone. Oral bioavailability is decreased by prior administration of cimetidine or sodium bicarbonate. The time of peak absorption is slightly delayed and the AUC somewhat increased when the oral drug is taken after a meal.
Distribution: Oral domperidone does not appear to accumulate or to induce its own metabolism; a peak plasma level after 90 min of 21 ng/mL after 2 weeks oral administration of 30 mg/day was almost the same as that of 18 ng/mL after the 1st dose. Domperidone is 91-93% bound to plasma protein. Distribution studies with radiolabeled drug have shown wide tissue distribution, but low brain concentrations. Small amounts of the drug cross the placenta in rats.
Metabolism: Domperidone undergoes rapid and extensive hepatic metabolism by hydroxylation and N-dealkylation. In vitro metabolism experiments with diagnostic inhibitors revealed that CYP3A4 is a major form of cytochrome P-450 involved in the N-dealkylation of domperidone, whereas CYP3A4, CYP1A2 and CYP2E1 are involved in domperidone aromatic hydroxylation.
Excretion: Urinary and fecal excretions amount to 31% and 66% of the oral dose, respectively. The proportion of the drug excreted unchanged is small (10% of fecal excretion and approximately 1% of urinary excretion). The plasma half-life is prolonged in patients with severe renal insufficiency.
Toxicology: Preclinical Safety Data: At a high, maternally toxic dose (more than 40 times the recommended human dose), teratogenic effects were seen in the rat. No teratogenicity was observed in mice and rabbits.
Electrophysiological in vitro and in vivo studies have shown that domperidone, at high concentrations, may prolong the QTc interval.
Pharmacology: Domperidone is a dopamine antagonist with antiemetic properties similar to those of metoclopramide and certain neuroleptic drugs. Unlike these other drugs, however, domperidone does not readily cross the blood-brain barrier. In domperidone users, especially in adults, extrapyramidal side effects are very rare, but domperidone promotes the release of prolactin from the pituitary. Its antiemetic effect may be due to a combination of peripheral (gastrokinetic) effects and antagonism of dopamine receptors in the chemoreceptor trigger zone, which lies outside the blood-brain barrier in the area postrema. Animal studies, together with the low concentrations found in the brain, indicate a predominantly peripheral effect of domperidone on dopamine receptors.
Studies in man have shown oral domperidone to increase the duration of antral and duodenal contractions, to increase the gastric emptying of liquids and semisolids in healthy subjects and of solids in patients in whom it was delayed, and to increase lower esophageal sphincter pressure in healthy subjects. It has no effect on gastric secretion.
Pharmacokinetics: Absorption: In fasting subjects, domperidone is rapidly absorbed after oral administration, with peak plasma concentrations at approximately 1 hr. The low absolute bioavailability of oral domperidone (~15%) is due to an extensive first-pass metabolism in the gut wall and liver. Although domperidone's bioavailability is enhanced in normal subjects when taken after a meal, patients with GI complaints should take domperidone 15-30 min before a meal. Reduced gastric acidity impairs the absorption of domperidone. Oral bioavailability is decreased by prior administration of cimetidine or sodium bicarbonate. The time of peak absorption is slightly delayed and the AUC somewhat increased when the oral drug is taken after a meal.
Distribution: Oral domperidone does not appear to accumulate or to induce its own metabolism; a peak plasma level after 90 min of 21 ng/mL after 2 weeks oral administration of 30 mg/day was almost the same as that of 18 ng/mL after the 1st dose. Domperidone is 91-93% bound to plasma protein. Distribution studies with radiolabeled drug have shown wide tissue distribution, but low brain concentrations. Small amounts of the drug cross the placenta in rats.
Metabolism: Domperidone undergoes rapid and extensive hepatic metabolism by hydroxylation and N-dealkylation. In vitro metabolism experiments with diagnostic inhibitors revealed that CYP3A4 is a major form of cytochrome P-450 involved in the N-dealkylation of domperidone, whereas CYP3A4, CYP1A2 and CYP2E1 are involved in domperidone aromatic hydroxylation.
Excretion: Urinary and fecal excretions amount to 31% and 66% of the oral dose, respectively. The proportion of the drug excreted unchanged is small (10% of fecal excretion and approximately 1% of urinary excretion). The plasma half-life is prolonged in patients with severe renal insufficiency.
Toxicology: Preclinical Safety Data: At a high, maternally toxic dose (more than 40 times the recommended human dose), teratogenic effects were seen in the rat. No teratogenicity was observed in mice and rabbits.
Electrophysiological in vitro and in vivo studies have shown that domperidone, at high concentrations, may prolong the QTc interval.
MedsGo Class
GIT Regulators, Antiflatulents & Anti-Inflammatories / Antiemetics
Features
Brand
Motilium
Full Details
Dosage Strength
1 mg / ml
Drug Ingredients
- Domperidone
Drug Packaging
Suspension 100ml
Generic Name
Domperidone
Dosage Form
Suspension
Registration Number
DR-X8545
Drug Classification
Over-The-Counter (OTC)
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