FORMULA
Each coated tablet contains:
Mosapride citrate dihydrate 5.293 mg (equivalent to Mosapride citrate 5.00 mg).
Simethicone (as 50% Simethicone 400mg(*)) 200mg.
Excipients: tricalcium phosphate 416.707 mg, microcrystalline cellulose 300.00 mg, sodium croscarmellose 36.000 mg, hydroxypropyl cellulose 30.000 mg, magnesium stearate 12.000 mg, dimethicone 208.00 mg, tricalcium phosphate 75.00 mg, magnesium carbonate 71.0 mg, colloidal silicon dioxide 25.0 mg, talc21.00mg,white Opadry (hydroxypropyl methylcellulose 23.652 mg, Polyethylene glycol 6.758 mg, Titanium dioxide 4.624 mg, Talc 0.534mg) 35.568 mg, yellow dye Nº10 lacquer 0.420 mg, yellow dye Nº6 lacquer 0.012 mg.
THERAPEUTIC ACTION
Antidyspeptic, antiflatulence, regulates digestive motility and accelerates gastric emptying.
ATC Code: A03FA.
INDICATIONS
Disorders associated with delayed gastric emptying (gastroparesis) associated with flatulence and meteorism.
PHARMACOLOGICAL PROPERTIES
Pharmacological action
Mosapride citrate
Mosapride citrate is a selective agonist of the serotonin 5-HT4 receptors present in the intrinsic nerves of the GI tract, and participates in the increased release of acetylcholine. For this reason it is thought to accelerate gastric emptying and modulate digestive motility both in the upper and lower intestinal tract.
Simethicone
Simethicone, a physiologically inert substance, has no pharmacological activity and acts by modifying thesurface tension of the gas bubbles causing their coalescence and facilitating their removal.
Pharmacokinetics
Mosapride citrate
This medication is given orally and before food intake. After oral administration of mosapride citrate, the peak concentration is reached 0.8 hours after ingestion, and its maximum concentration is 30.7 ng / ml (Cmax = 30.7 ng / ml). The half-life is 2 hours. Mosapride citrate binds to plasma proteins by 99%. It is metabolized in the liver by cytochrome P450, particularly CYP3A4. The unchanged active substance and its major metabolite are excreted in the urine and feces.
DOSAGE AND ADMINISTRATION
Adults
Give 1 tablet before meals, three times a day.
Geriatric patients
The dose may be reduced to 7.5 mg/day.
CONTRAINDICATIONS
Hypersensitivity to the active substance or any of its components.
Pregnancy. Lactation. Children.
PRECAUTIONS AND WARNINGS
The product should be used with caution in patients with hepatic and/or renal impairment.
A dosage adjustment should be considered in geriatric patients.
Mosapride citrate
If, despite the administration of medication, an improvement of the digestive symptoms that accompany chronic gastritis is not observed during a prolonged period (usually 2 weeks), the administration should not be continued.
Simethicone
There are clinical trials in a population between 2 and 92 years, with treatment duration of up to 2 years in a row with good tolerance; however, maximum treatment duration of 15 days in a row is recommended. If symptoms persist after this time, the clinical situation should be reviewed.
Drug interactions
Mosapride citrate
Caution with concomitant use By associating mosapride with erythromycin, the maximum plasma
concentration, the half-life and the AUC (area under the curve) of mosapride may increase, so caution should be exercised in this case.
Simethicone
Drug interactions have not been described. Carcinogenesis, mutagenesis and fertility disorders
Pregnancy
Assess the potential risk / benefit of the drug on pregnancy before using.
Mosapride citrate
In women who are or might be pregnant, administer only if the utility of treatment outweighs the risk of it. (Safety with respect to the administration during pregnancy is not confirmed).
Simethicone
Simethicone belongs to the FDA (Food and Drug Administration of the United States) category C.
There is no evidence of injury in pregnant women due to lack of digestive absorption of simethicone by the mother.
Lactation
Assess the potential risk / benefit of the drug before using.
Mosapride citrate
Avoid administration in women who are breastfeeding, but if the administration is essential, stop breastfeeding. In experimental animals (rats), the passage of the drug into breast milk was reported.
Simethicone
It is not known whether this drug is excreted in human milk; however, excretion is not expected due to a lack of digestive absorption of simethicone by the mother. Its use is generally accepted.
Pediatric use
Safety has not been studied in this population.
Mosapride citrate
Safety has not been established in administration to children. (There is no experience with its use).
Simethicone
The dosage must be individualized on the basis of the seriousness of the situation and on the surface of the patient rather than the weight.
Geriatric use
Mosapride citrate
As the physiological functions of kidney and liver are impaired in general in the elderly, administer medication cautiously observing the
patient’s condition. If side effects occur when used for digestive symptoms that accompany chronic gastritis, lower the dose (i.e. 7.5
mg per day) and take appropriate action.
ADVERSE REACTIONS
Mosapride citrate
The main adverse reactions were diarrhea, loose stools (1.8%), dry mouth (0.5%), and asthenia (0.3%). Abnormal changes were seen in clinical test values: eosinophilia (1.1%) neutral fats increase (1.0%), increased SGOT, SGPT, alkaline phosphatase and _-GT (each 0.4%) .
After marketing, according to research results for use and special investigations (investigations of long-term use), the following adverse reactions were observed: diarrhea, loose stools (0.8%), abdominal pain (0.4%), dry mouth (0.3%) (at the end of the re-research).
Significant adverse effects
Fulminant hepatitis, abnormal liver function, jaundice (all less than 0.1%). In fulminant hepatitis there is a severe impairment of liver function leading to a marked increase in GOT, GPT and _-GTP, in addition to jaundice, and even fatal cases, therefore, it is recommended to observe cautiously, and if any change is confirmed immediately suspend administration and take appropriate action.
The adverse effects of simethicone are usually mild and transient. The most characteristic adverse reaction is: rarely (<1%): moderate and transient constipation. Belching may occur which is the normal mechanism of removing the gases with this treatment.
OVERDOSE
Simethicone
Cases of untreated overdose have not yet been reported. Even if a much higher amount than that indicated is swallowed, it is highly unlikely that adverse effects appear due to the lack of digestive absorption of the drug. In case of accidental or deliberate overdose, treat the symptoms that
appear. No special procedure is recommended. Incase of a possible overdose, seek medical attention in the nearest hospital or toxicology center.
Storage
Store below 25 °C.
HOW SUPPLIED
Available in packs containing 30 coated tablets,
KEEP THIS AND ALL DRUGS OUT OF REACH OF CHILDREN.
NCDS Version number:01, version date. 18 May 2011
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