Active ingredient: Domperidone (as domperidone maleate) 10 mg.
Excipients/Inactive Ingredients: Lactose monohydrate, maize starch, povidone K30, magnesium stearate, hypromellose, macrogol 6000, talc, titanium dioxide.
Naupastad 10 is indicated for the relief of the symptoms of nausea and vomiting in adults and adolescents 12 years of age and older and weighing 35 kg or more.
Naupastad 10 should no longer be used to treat other conditions such as bloating or heartburn.
Administration: It is recommended to take oral domperidone before meals. If taken after meals, absorption of the drug is somewhat delayed.
Dosage: Domperidone should be used at the lowest effective dose for the shortest duration and should not normally be used for longer than one week.
Patients should try to take each dose at the scheduled time. If a scheduled dose is missed, the missed dose should be omitted and the usual dosing schedule resumed. The dose should not be doubled to make up for a missed dose.
Usually, the maximum treatment duration should not exceed one week.
Adults and adolescents (12 years of age and older and weighing 35 kg or more): One 10 mg tablet up to three times per day with a maximum dose of 30 mg per day.
[Cross reference should be made to Precautions for further information.]
Hepatic impairment: Domperidone is contraindicated in moderate or severe hepatic impairment. Dose modification in mild hepatic impairment is however not needed.
Renal impairment: Since the elimination half-life of domperidone is prolonged in severe renal impairment, on repeated administration, the dosing frequency of domperidone should be reduced to once or twice daily depending on the severity of the impairment, and the dose may need to be reduced. Such patients on prolonged therapy should be reviewed regularly.
Paediatric population: The efficacy of domperidone in children less than 12 years of age has not been established.
The efficacy of domperidone in adolescents 12 years of age and older and weighing less than 35 kg has not been established.
Symptoms: Symptoms of over dosage may include agitation, altered consciousness, convulsions, disorientation, somnolence and extrapyramidal reactions.
Management: There is no specific antidote to domperidone, but in the event of overdose, standard symptomatic treatment should be given immediately. Gastric lavage as well as the administration of activated charcoal, may be useful. ECG monitoring should be undertaken, because of the possibility of QT interval prolongation. Close medical supervision and supportive therapy is recommended.
Anticholinergic, anti-parkinson drugs may be helpful in controlling the extrapyramidal reactions.
Domperidone is contraindicated in the following situations: Known hypersensitivity to domperidone or any of the excipients; Prolactin-releasing pituitary tumor (prolactinoma); When stimulation of the gastric motility could be harmful e.g. in patients with gastro-intestinal haemorrhage, mechanical obstruction or perforation; In patients with moderate or severe hepatic impairment; In patients who have known existing prolongation of cardiac conduction intervals, particularly QTc, patients with significant electrolyte disturbances or underlying cardiac diseases such as congestive heart failure; Co-administration with QT-prolonging drugs; Co-administration with potent CYP3A4 inhibitors (regardless of their QT prolonging effects).
Cardiovascular effects: Domperidone has been associated with prolongation of the QT interval on the electrocardiogram. During post-marketing surveillance, there have been very rare cases of QT prolongation and torsades de pointes in patients taking domperidone. These reports included patients with confounding risk factors, electrolyte abnormalities and concomitant treatment which may have been contributing factors.
Epidemiological studies showed that domperidone was associated with an increased risk of serious ventricular arrhythmias or sudden cardiac death. A higher risk was observed in patients older than 60 years, patients taking daily doses greater than 30 mg, and patients concurrently taking QT-prolonging drugs or CYP3A4 inhibitors.
Domperidone should be used at the lowest effective dose in adults and adolescents 12 years of age and older.
Domperidone is contraindicated in patients with known existing prolongation of cardiac conduction intervals, particularly QTc, in patients with significant electrolyte disturbances (hypokalaemia, hyperkalaemia, hypomagnesaemia), or bradycardia, or in patients with underlying cardiac diseases such as congestive heart failure due to increased risk of ventricular arrhythmia.
Electrolyte disturbances (hypokalaemia, hyperkalaemia, hypomagnesaemia) or bradycardia are known to be conditions increasing the proarrhythmic risk.
Treatment with domperidone should be stopped if signs or symptoms occur that may be associated with cardiac arrhythmia, and the patients should consult their physician.
Patients should be advised to promptly report any cardiac symptoms.
Use with apomorphine: Domperidone is contra-indicated with QT prolonging drugs including apomorphine, unless the benefit of the co-administration with apomorphine outweighs the risks, and only if the recommended precautions for co-administration mentioned in the apomorphine package insert are strictly fulfilled. Refer to the apomorphine package insert.
Renal impairment: The elimination half-life of domperidone is prolonged in severe renal impairment. For repeated administration, the dosing frequency of domperidone should be reduced to once or twice daily depending on the severity of the impairment. The dose may also need to be reduced.
Excipients: The film-coated tablets contain lactose. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Effects on ability to drive and use machines: Domperidone has no or negligible influence on the ability to drive and use machines.
Pregnancy: There are limited post-marketing data on the use of domperidone in pregnant women. Studies in animals have shown reproductive toxicity at maternally toxic doses. Domperidone should only be used during pregnancy when justified by the anticipated therapeutic benefit.
Lactation: Domperidone is excreted in human milk and breast-fed infants receive less than 0.1% of the maternal weight-adjusted dose. Occurrence of adverse effects, in particular cardiac effects cannot be excluded after exposure via breast milk. A decision should be made whether to discontinue breast-feeding or to discontinue/abstain from domperidone therapy taking into account the benefit of breast feeding for the child and the benefit of therapy for the woman. Caution should be exercised in case of QTc prolongation risk factors in breast-fed infants.
The following terms and frequencies are applied: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000), where frequency can not be estimated from clinical trials data, it is recorded as "Not known".
Immune system disorders: Not known: Anaphylactic reaction (including anaphylactic shock).
Psychiatric disorders: Uncommon: Loss of libido, anxiety.
Not known: Agitation, nervousness.
Nervous system disorders: Uncommon: Somnolence, headache.
Not known: Convulsion, extrapyramidal disorder.
Eye disorders: Not known: Oculogyric crisis.
Cardiac disorders: Not known: Ventricular arrhythmias, sudden cardiac death, QTc prolongation, Torsade de Pointes.
Gastrointestinal disorders: Common: Dry mouth.
Uncommon: Diarrhoea.
Skin and subcutaneous tissue disorders: Uncommon: Rash, pruritus.
Not known: Urticaria, angioedema.
Renal and urinary disorders: Not known: Urinary retention.
Reproductive system and breast disorders: Uncommon: Galactorrhoea, breast pain, breast tenderness.
Not known: Gynaecomastia, amenorrhoea.
General disorders and administration site conditions: Uncommon: Asthenia.
Investigations: Not known: Liver function test abnormal, blood prolactin increased.
The 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 of domperidone.
Increased risk of occurrence of QT-interval prolongation, due to pharmacodynamic and/or pharmacokinetic interactions.
Concomitant use of the following substances is contraindicated: QTc prolonging medicinal products: anti-arrhythmics class IA (e.g., disopyramide, hydroquinidine, quinidine); anti-arrhythmics class III (e.g., amiodarone, dofetilide, dronedarone, ibutilide, sotalol); certain anti-psychotics (e.g., haloperidol, pimozide, sertindole); certain anti-depressants (e.g., citalopram, escitalopram); certain antibiotics (e.g., erythromycin, levofloxacin, moxifloxacin, spiramycin); certain antifungal agents (e.g., pentamidine); certain antimalarial agents (in particular halofantrine, lumefantrine); certain gastro-intestinal medicines (e.g., cisapride, dolasetron, prucalopride); certain antihistaminics (e.g., mequitazine, mizolastine); certain medicines used in cancer (e.g., toremifene, vandetanib, vincamine); certain other medicines (e.g., bepridil, diphemanil, methadone); apomorphine, unless the benefit of the co-administration outweighs the risks, and only if the recommended precautions for co-administration are strictly fulfilled. Refer to the apomorphine package insert.
Potent CYP3A4 inhibitors (regardless of their QT prolonging effects), i.e.: protease inhibitors; systemic azole antifungals; some macrolides (erythromycin, clarithromycin, telithromycin).
Concomitant use of the following substances is not recommended: Moderate CYP3A4 inhibitors i.e. diltiazem, verapamil and some macrolides.
Concomitant use of the following substances requires caution in use: Caution with bradycardia and hypokalaemia-inducing drugs, as well as with the following macrolides involved in QT-interval prolongation: azithromycin and roxithromycin (clarithromycin is contra-indicated as it is a potent CYP3A4 inhibitor).
The previous list of substances is representative and not exhaustive.
Separate in vivo pharmacokinetic/pharmacodynamic interaction studies with oral ketoconazole or oral erythromycin in healthy subjects confirmed a marked inhibition of domperidone's CYP3A4 mediated first pass metabolism by these drugs.
With the combination of oral domperidone 10 mg four times daily and ketoconazole 200 mg twice daily, a mean QTc prolongation of 9.8 msec was seen over the observation period, with changes at individual time points ranging from 1.2 to 17.5 msec. With the combination of domperidone 10 mg four times daily and oral erythromycin 500 mg three times daily, mean QTc over the observation period was prolonged by 9.9 msec, with changes at individual time points ranging from 1.6 to 14.3 msec. Both the Cmax and AUC of domperidone at steady state were increased approximately three-fold in each of these interaction studies. In these studies domperidone monotherapy at 10 mg given orally four times daily resulted in increases in mean QTc of 1.6 msec (ketoconazole study) and 2.5 msec (erythromycin study), while ketoconazole monotherapy (200 mg twice daily) led to increases in QTc of 3.8 and 4.9 msec, respectively, over the observation period.
Store in a well-closed container, in a dry place. Do not store above 30°C.
A03FA03 - domperidone ; Belongs to the class of propulsives. Used in the treatment of functional gastrointestinal disorders.
Naupastad 10 FC tab 10 mg
10 × 10's
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