Genodom

Genodom

domperidone

Manufacturer:

Geno

Distributor:

Nebula

Marketer:

Mascots
Full Prescribing Info
Contents
Domperidone.
Description
Each ml contains: Domperidone BP 1 mg.
Flavoured Syrupy Base qs.
GENODOM is white coloured suspension with a sweet and flavoured taste.
Domperidone BP 1mg as Anti-emetic preparation.
Excipients/Inactive Ingredients: GENODOM also contains following inactive ingredients: Sorbitol Solution 70% (Non Crystallising) BP, Glycerol BP, Polysorbate-80 NF, Methyl Hydroxy Benzoate BP, Propyl Hydroxy Benzoate BP, Sodium Saccharin BP, Xanthan Gum BP, Lemon Flavour Co.Sp., Purified Water BP.
Action
Pharmacology: Pharmacodynamics: Mechanism of Action: Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which - among others - regulates nausea and vomiting.
Pharmacokinetics: DOMPERIDONE: Absorption: In fasting subjects, Domperidone is rapidly absorbed after oral administration, with peak plasma concentrations at 30 to 60 minutes. The low absolute bioavailability of oral Domperidone (approximately 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 gastro-intestinal complaints should take Domperidone 15-30 minutes before a meal. Reduced gastric acidity impairs the absorption of Domperidone. Oral bioavailability is decreased by prior concomitant administration of cimetidine and 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 induce its own metabolism; a peak plasma level after 90 minutes of 21 ng/ml after two weeks oral administration of 30 mg per day was almost the same as that of 18 ng/ml after the first dose. Domperidone is 91-93% bound to plasma proteins. Distribution studies with radiolabelled drug in animals have shown wide tissue distribution, but low brain concentration. Small amounts of 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 faecal excretions amount to 31 and 66% of the oral dose respectively. The proportion of the drug excreted unchanged is small (10% of faecal excretion and approximately 1% of urinary excretion). The plasma half-life after a single oral dose is 7-9 hours in healthy subjects but is prolonged in patients with severe renal insufficiency.
Toxicology: Preclinical Safety Data: Electrophysiological in vitro and in vivo studies indicate an overall moderate risk of Domperidone to prolong the QT interval in humans. In in vitro experiments on isolated cells transfected with HERG and on isolated guinea pig myocytes, ratios were about 10, based on IC50 values inhibiting currents through ion channels in comparison to the free plasma concentrations in humans after administration of the maximum daily dose of 20mg (q.i.d.). However, safety margins in in vitro experiments on isolated cardiac tissues in in vivo models (dog, guinea pig, rabbits sensitised for torsades de pointes) exceeded the free plasma concentrations in humans at maximum daily dose (20mg q.i.d.) by more than 50-fold. In the presence of inhibition of the metabolism via CYP3A4 free plasma concentrations of Domperidone can rise up to 10-fold.
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.
Indications/Uses
The relief of the symptoms of nausea and vomiting.
Dosage/Direction for Use
0.3 mg/Kg per dose.
Method of Administrations: Oral Route of Administration.
Overdosage
Overdose has been reported primarily in infants and children. Symptoms of overdosage may include agitation, altered consciousness, convulsions, disorientation, somnolence and extrapyramidal reactions.
Treatment: There is no specific antidote to domperidone, but in the event of overdose, gastric lavage as well as the administration of activated charcoal, may be useful. Close medical supervision and supportive therapy is recommended.
Anticholinergic, anti-parkinson drugs may be helpful in controlling the extrapyramidal reactions.
Contraindications
In patients with known hypersensitivity to Domperidone or nany of the contents of the Suspension.
Special Precautions
Dosage adjustment may be necessary in patients who are receiving Domperidone concomitantly with Cimetidine.
Effects on Ability to Drive and Use Machines: NONE.
Use In Pregnancy & Lactation
Usage in PREGNANCY: Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
In 2nd & 3rd trimesters: Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Usage in LACTATION: According to the U.S. Food and Drug Administration (FDA), Domperidone is not approved for enhanced lactation in any country.
The hormone prolactin stimulates lactation in humans, and its release is inhibited by the dopamine secreted by the hypothalamus. Domperidone, by acting as an anti-dopaminergic, results in increased prolactin secretion, and thus promotes lactation.
Adverse Reactions
Domperidone has been reported to show allergic reactions, such as rash or urticaria, have been reported. Abdominal cramps have been reported. Dystonic reactions (extrapyramidal phenomena) may occur.
Reversible raised serum prolactin levels have been observed which may lead to galactorrhoea and gynaecomastia. Hypertensive crises in patients with phaeochromocytoma may occur with administration of Domperidone. Where the blood brain barrier is not fully developed (mainly in young babies) or is impaired, the possible occurrence of neurological side-effects cannot be totally excluded.
Drug Interactions
Domperidone: Concomitant administration of anti-cholinergic drugs may inhibit the anti-dyspeptic effects of Domperidone. Anti-muscarinic agents and opioid analgesics may antagonise the effect of Domperidone. Domperidone suppresses the peripheral effects (digestive disorders, nausea and vomiting) of dopaminergic agonists. Since Domperidone has gastro-kinetic effects, it could influence the absorption of concomitant orally administered medicines, particularly those with sustained release or enteric coated formulations. As Domperidone interferes with serum prolactin levels, it may interfere with other hypoprolactinaemic agents and with some diagnostic tests.
Antacids and anti-secretory agents lower the oral bioavailability of Domperidone. They should be taken after meals and not before meals, i.e. they should not be taken simultaneously with Domperidone.
Reduced gastric acidity impairs the absorption of Domperidone.
Oral bioavailability is decreased by prior administration of cimetidine or sodium bicarbonate.
The main metabolic pathway of Domperidone is through CYP3A4. In vitro data suggests that concomitant use of drugs that significantly inhibit this enzyme may result in increased plasma levels of Domperidone. Examples of CYP3A4 inhibitors include the following: Azole antifungals, Macrolide antibiotics, HIV protease inhibitors, Nefazodone.
Caution For Usage
Instructions for Use, Handling and Disposal: For Internal use only.
Incompatibilities: None.
Storage
Keep the cap tightly closed. Store at a temperature not exceeding 30°C in a dark & dry place. Shake well before use.
Shelf Life: 36 Months from the date of Manufacturing.
ATC Classification
A03FA03 - domperidone ; Belongs to the class of propulsives. Used in the treatment of functional gastrointestinal disorders.
Presentation/Packing
Oral susp 1 mg/mL (white coloured) x 30 mL x 1's.
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