Molax/Molax-M

MOLAX-M: White, round and biconvex film coated tablet with "m" on one side and "
Click on icon to see table/diagram/image
" on the other.
Each tablet contains Domperidone maleate equivalent to Domperidone 10 mg.
MOLAX: White suspension.
Each 1 mL contains Domperidone 1 mg.

Pharmacology: Pharmacodynamics: Domperidone is a dopamine antagonists (both D₁ receptors - facilitates gastrointestinal smooth muscle activity; and D₂ receptors - inhibit the release of neural acetylcholine), structurally related to the benzimidazole. It has peripheral anticholinergic properties relating to gastroprokinetics properties; it facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. It also has antiemetic properties relating to dopaminergic blocking activity at both the chemoreceptor trigger zone (in the brainstem) and at the gastric level. It also elevates serum prolactin concentrations. It has no effect on the receptors of the brain (not readily crosses the blood-brain barriers), so that psychotropic or neurologic effects are practically absent.
Pharmacokinetics: Domperidone can be absorbed rapidly after oral doses. The absorption is decreased by the prior administration of cimetidine or sodium bicarbonate. The systemic bioavailability of Domperidone is only about 15% in fasting subjects given an oral dose; this is increased when domperidone is given 90 minutes after food. The low availability is thought to be due to first-pass hepatic and intestinal metabolism. It is more than 90% bound to plasma proteins and has a terminal elimination half-life of about 7.5 hours (prolonged to 21 hours in patients with severe renal dysfunction; serum creatinine greater than 530 mmol/L). It does not accumulate upon repeated administration. It undergoes rapid and extensive hepatic metabolism. The main metabolic pathways are N-dealkylation by cytochrome P450 isoenzyme CYP3A4, and aromatic alkylation by CYP3A4, CYP1A2, and CYP2E1; yielding 2 inactive metabolites. About 30% of an oral dose is excreted in urine within 4 days, almost entirely as metabolites; the remainder of a dose is excreted in faeces over several days, about 10% as unchanged drug. It does not readily cross the blood-brain barrier. Small amounts of the drug are distributed into breast milk; concentrations are 10-50% of those in maternal serum.

For treatment symptoms associated with upper gastrointestinal motility disorders or dyspepsia: upper abdominal pain, feeling of abdominal distension, bloating, flatulence, nausea; caused by gastritis, diabetic gastroparesis, or drug therapy such as dopaminergic agents.
Short-term treatment of nausea and vomiting from various origins.

Recommended dose: Adult dose and adolescents (over 12 years old and weighing 35 kg or more): For the treatment of nausea and vomiting: 10 to 20 mg, 3 or 4 times daily; 15-30 minutes before meals and, if necessary, before bed.
For the symptomatic treatment of dyspepsia: 10 to 20 mg 4 times daily; 15-30 minutes before meals and before bed.
The maximum daily dose is 80 mg.
Pediatric dose: Use MOLAX SUSPENSION 0.25 to 0.5 mg/kg, 3 or 4 times daily; 15-30 minutes before meals and, if necessary, before bed.
The maximum daily pediatric dose is 2.4 mg/kg, and does not exceed 80 mg.
Administration: It is recommended to take the drug before meals to avoid absorption delay.
Concomitant antacids or antisecretory agents can be taken together with MOLAX-M TABLET.
However, MOLAX SUSPENSION should not be taken simultaneously as the oral availability will be lowered.
Hepatic impairment: Domperidone is highly metabolized in liver. Patients with mild hepatic impairment have a lower systemic exposure than healthy subjects with no change in protein binding and terminal elimination half-life. Patients with moderate impairment, however, have higher drug levels than healthy subjects, with prolonged terminal half-life, and increased unbound fraction. There are no studies in patients with severe impairment. Therefore, it is recommended to use caution in patients with mild hepatic impairment. The use in patients with moderate and severe hepatic impairment is contraindicated.
Renal impairment: Dosage adjustment of single acute administration in patients with renal dysfunction is not necessary since renal clearance is small compared to total plasma clearance. On repeated administration, however, the dosing frequency should be reduced to once or twice daily because of the increased elimination half-life, depending on the severity of the impairment; and the dose may need to be reduced. The patients on prolonged therapy should also be reviewed regularly.

The symptom includes arrhythmia, drowsiness, disorientation, extrapyramidal reactions, hypotension; they are self limiting and usually disappear within 24 hours. Close observation and supportive therapy are recommended.
There is no specific antidote for the overdose. However, anticholinergic agents, antiparkinsonian medications, or antihistamines with anticholinergics properties may be useful in controlling the extrapyramidal reactions associated with Domperidone toxicity.
Gastric lavage as well as the administration of activated charcoal may be useful in facilitating the elimination of Domperidone.

Sensitivity to Domperidone; Moderate or severe hepatic impairment; Gastrointestinal hemorrhage, mechanical obstruction or perforation (or whenever stimulation of gastric motility might be dangerous); Prolactinoma.

According to Notification of the Ministry of Public Health: Avoid usage in patient with moderate to severe hepatic impairment.
Avoid usage in patient with QT prolongation and with a history of QT prolongation and on patient with concomitant use of drug-induced QT prolongation such as cisapride, erythromycin and ketoconazole.
Avoid usage in patient with hypokalemia and hypomagnesemia.
Avoid concomitant usage with CYP3A4 inhibitors such as ketoconazole, erythromycin, cimetidine and omeprazole, due to the elevation of plasma domperidone.

Use in Children: Use caution, determine the dose accurately and follow strictly in neonates, infants, and small children. Because the risk of neurological side effects, though rarely occur, is higher in young children, as metabolic function and the blood-brain barrier are not fully developed in the 1^st month of life.

Safe use of the medicine during pregnancy has not been established; therefore it should be used during pregnancy only when the potential benefit justifies the possible risks to the fetus.
Low concentrations of Domperidone are found in the breast milk, but the long-term potential for adverse effects in the nursing infant have not been determined. Therefore it is not recommended in nursing mothers including to increase milk production, due to the unknown risks to the nursing infant. A decision should be made whether to discontinue nursing or the drug.

Frequencies are classified as: Very Common (10% and above), Common (1% and above but less than 10%), Uncommon (0.1% and above but less than 1%), Rare (0.01% and above but less than 0.1%), and Very rare (less than 0.01% including isolated reports).
Gastrointestinal disorders: Common: Dry mouth.
Uncommon: Diarrhoea.
Reproductive system and breast disorders: Uncommon: Galactorrhoea, breast pain, breast tenderness.
Rare: Gynaecomastia, amenorrhoea.
Psychiatric disorders: Uncommon: Loss of libido, anxiety.
Very rare: Agitation, nervousness.
Nervous system disorders: Uncommon: Somnolence, headache.
Very rare: Extrapyramidal disorders, convulsion.
Skin and subcutaneous tissue disorders: Uncommon: Rash, pruritus.
Very rare: Angioedema, urticaria.
General disorders and administration site conditions: Uncommon: Asthenia.
Immune system disorders: Very rare: Anaphylactic shock reaction.
Cardiac disorders: Very rare: Sudden cardiac death, serious ventricular arrhythmias.
Renal and urinary disorders: Very rare: Urinary retention.
Investigation: Very rare: Liver function test abnormal, blood prolactin increased.

Antacids and antisecretory drugs: These drugs lower the oral availability of MOLAX SUSPENSION.
Opioid analgesics and antimuscarinics: The prokinetic effects of Domperidone may be antagonized by such drugs.
Potent CYP3A4 inhibitors: These drugs may increase the plasma concentration of Domperidone. Potent CYP3A4 includes Azole antifungals e.g., fluconazole, itraconazole, ketoconazole, voriconazole; macrolide antibiotics e.g., clarithromycin and erythromycin, HIV protease inhibitors e.g., amprenavir, atazanavir, fosamprenavir, indinavir, nelfinavir, ritonavir and saquinavir; calcium antagonists e.g., diltiazem and verapamil; amiodarone, aprepitant, nefazodone, telithromycin.
Some potent CYP3A4 inhibitors: Fluconazole, ketoconazole, voriconazole, clarithromycin, erythromycin, amiodarone, telithromycin; produce an associated slight prolongation in QT interval. Concomitant use with Domperidone is not recommended.
Dopaminergic agonists: Domperidone may antagonize the hypoprolactinaemia effect of bromocriptine. It also may suppress the unwanted peripheral effect of bromocriptine and L-dopa e.g., digestive disorders, nausea and vomiting, without counteracting their central properties.
Sustained-release and enteric-coated formulations of drugs: Domperidone enhances gastric and small intestinal motive, it may accelerate absorption of drugs from the small bowel with slowing absorption of drugs taken up from stomach, particularly those with sustained-release or enteric-coated formulations.

MOLAX-M: Store below 30°C.
MOLAX: Store below 30°C, protect from light.

GIT Regulators, Antiflatulents & Anti-Inflammatories / Antiemetics

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

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