Motilium pills 10mg, 30pcs

Composition

Active ingredient: domperidone 10 mg; Excipients: lactose monohydrate 54.2 mg, corn starch 20 mg, microcrystalline cellulose 10 mg, pregelatinized starch 3 mg, povidone K 90 1.5 mg, magnesium stearate 0.6 mg, hydrogenated cotton seed oil 0.5 mg, sodium lauryl sulfate 0.15 mg. Film coating: hypromellose 2910 5 mpax 2.2 mg, sodium lauryl sulfate 0.05 mg.

Clinical Pharmacology

Pharmacodynamics : Domperidone is a dopamine antagonist with antiemetic properties. Domperidone does not penetrate well through the blood-brain barrier. The use of domperidone is rarely accompanied by extrapyramidal side effects, especially in adults, but domperidone stimulates the release of prolactin from the pituitary gland. Its antiemetic effect may be due to a combination of peripheral (gastrokinetic) action and antagonism to dopamine receptors in the chemoreceptor trigger zone, which is located outside the blood-brain barrier. Animal studies and low concentrations of the drug detected in the brain indicate a predominantly peripheral effect of domperidone on dopamine receptors. When used orally, domperidone increases the duration of antral and duodenal contractions, accelerates gastric emptying and increases the pressure of the sphincter of the lower esophagus. Domperidone has no effect on gastric secretion. Pharmacokinetics: When taken on an empty stomach, domperidone is rapidly absorbed after oral use, with peak plasma concentrations reached within 30 to 60 minutes. The low absolute oral bioavailability of domperidone (approximately 15%) is associated with intensive presystemic metabolism in the intestinal wall and liver. Domperidone should be taken 15 to 30 minutes before meals. A decrease in acidity in the stomach leads to a deterioration in the absorption of domperidone. Oral bioavailability is reduced with prior use of cimetidine and sodium bicarbonate. When taking the drug after a meal, it takes longer to achieve maximum absorption, and the area under the pharmacokinetic curve (AUC) slightly increases. When taken orally, domperidone does not accumulate and does not induce its own metabolism; the peak plasma level of 21 ng / ml 90 minutes after 2 weeks of oral use at a dose of 30 mg per day was almost the same as the level of 18 ng / ml after the first dose. Domperidone binds to plasma proteins by 91-93%. Studies of the distribution of the drug with a radioactive label in animals showed its wide distribution in tissues, but low concentrations in the brain. Small amounts of the drug pass through the placenta in rats. Domperidone undergoes rapid and intensive metabolism by hydroxylation and N-dealkylation. In vitro metabolism studies with diagnostic inhibitors have shown that the CYP3A4 isoenzyme is the main form of cytochrome P450 involved in the N-dealkylation of domperidone, while the CYP3A4, CYP1A2, and CYP2E1 isoenzymes are involved in the aromatic hydroxylation of domperidone. Excretion by the kidneys and intestines is 31% and 66% of the oral dose, respectively. The proportion of the drug released unchanged is small (10% is excreted by the intestines and approximately 1% by the kidneys). The plasma half-life after a single oral dose is 7 to 9 hours in healthy volunteers, but increases in patients with severe renal insufficiency. In such patients (serum creatinine > 6 mg/100 ml, i. e. >> 0.6 mmol/L), the half-life of domperidone increases from 7.4 to 20.8 hours, but the drug concentrations in plasma are lower than in patients with normal renal function. A small amount of the unchanged drug (about 1%) is excreted by the kidneys. In patients with moderate hepatic impairment (Child – Pugh score 7-9), the AUC and Cmax of domperidone were 2.9 and 1.5 times higher than in healthy volunteers, respectively. The proportion of the unbound fraction increased by 25% and the elimination half-life increased from 15 to 23 hours. Patients with mild hepatic impairment showed slightly reduced systemic levels of the drug compared to those in healthy volunteers based on Cmax and AUC, without changes in protein binding or half-life. Patients with severe hepatic impairment were not studied.

Indications

To relieve symptoms of nausea and vomiting.

Use during pregnancy and lactation

MOTILIUM® is contraindicated for use during pregnancy and lactation.

Contraindications

– hypersensitivity to domperidone or any other component of the drug;- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;- a prolactinoma;- simultaneous use of oral ketoconazole, erythromycin or other drugs that increase the QT interval or potent inhibitors of isoenzyme CYP34A, such as fluconazole, voriconazole, clarithromycin, amiodarone, telithromycin etc. (see “Special instructions”, “Interaction with other medicines”);- severe electrolyte disorders or heart diseases, such as chronic heart failure;- bleeding from the gastrointestinal tract, mechanical intestinal obstruction, perforation of the stomach or intestines; – moderate to severe liver failure;- body weight less than 35 kg; – children under 12 years of age with a body weight of less than 35 kg; – pregnancy; – breast-feeding period.

Side effects

According to clinical studiesnotable reactions observed in ≥ 1% of patients taking MOTILIUM: depression, anxiety, decreased or no libido, headache, drowsiness, akathisia, diarrhea, rash, pruritus, breast enlargement/gynecomastia, breast pain and sensitivity, galactorrhea, menstrual disorders and amenorrhea, lactation disorders, asthenia. Adverse reactions observed in patients with The following adverse effects were classified as very common (≥ 10%), common (≥ 1%, but < 10%), uncommon (≥ 0.1%, but < 1%), rare (≥ 0.01%, but < 0.1%), and very rare (Based on spontaneous reports of adverse events. Immune system disorders. Very rare: anaphylactic reactions, including anaphylactic shock. Mental disorders. Very rare: increased excitability, nervousness, irritability. Nervous system disorders. Very rare: drowsiness, headache, dizziness, extrapyramidal disorders and seizures. Disorders of the cardiovascular system. Frequency unknown: ventricular arrhythmia*, pirouette-type ventricular tachycardia, sudden coronary death*. Skin and subcutaneous tissue disorders. Very rare: urticaria, angioedema. Disorders of the kidneys and urinary tract. Very rare: urinary retention. Laboratory and instrumental data. Very rare: abnormalities in laboratory parameters of liver function, hyperprolactinemia. Adverse reactions identified in post-marketing clinical trials Immune system disorders. Frequency unknown:   anaphylactic reactions, including anaphylactic shock. Mental disorders. Infrequently:   increased excitability, nervousness. Nervous system disorders. Common: dizziness. Rare: convulsions. Frequency unknown:  extrapyramidal disorders. Disorders of the cardiovascular system. Frequency unknown: ventricular arrhythmia*, pirouette-type ventricular tachycardia, sudden coronary death*. Disorders of the gastrointestinal tract. Frequency unknown: dry mouth. Skin and subcutaneous tissue disorders. Frequency unknown: angioedema. Disorders of the kidneys and urinary tract. Infrequently: urinary retention. Laboratory and instrumental data. Infrequently: abnormalities in laboratory parameters of liver function. Rare: hyperprolactinemia. * Some epidemiological studies have shown that domperidone use may be associated with an increased risk of serious ventricular arrhythmias or sudden death. The risk of these events is more likely in patients over 60 years of age and in patients taking the drug in a daily dose of more than 30 mg. It is recommended to use domperidone in the lowest effective dose in adults and children.

Interaction

Interaction with the following medications may increase the risk of prolongation of the QT interval. Contraindicated combinations: drugs that increase the QT interval: Class IA antiarrhythmic drugs (for example, disopyramide, hydroquinidine, quinidine), Class III antiarrhythmic drugs (for example, amiodarone, dofetidil, dronedarone, ibutilide, sotalol), antipsychotics (for example, haloperidol, pimozide, sertindol), antidepressants (for example, citalopram, escitalopram), antibiotics (erythromycin, levofloxacin, moxifloxacin, spiramycin), antifungal medications (for example, pentamidine), antimalarials (in particular, halofantrin, lumefantrin), gastrointestinal medications (for example, cisapride, dolasetron, prucalopride), antihistamines (for example, mechitazine, mizolastine), antitumor drugs (for example, toremifen, vandetanib, vincamine), other drugs (for example, bepridil, difemanil methylsulfate, methadone), powerful CYP3A4 inhibitors (protease inhibitors, azole-type antifungal agents, some macrolide antibiotics (erythromycin, clarithromycin, telithromycin). Not recommended combinations: moderate CYP3A4 inhibitors (diltiazem, verapamil, some macrolide antibiotics). Combinations that should be used with caution: drugs that cause bradycardia and hypokalemia, as well as azithromycin and roxithromycin. Cimetidine, sodium bicarbonate, and other antacids and antisecretory drugs reduce the bioavailability of domperidone. Increase the concentration of domperidone in blood plasma: azole antifungal agents, macrolide antibiotics, HIV protease inhibitors, nefazodone. It is compatible with the use of antipsychotic drugs (neuroleptics), dopaminergic receptor agonists (bromocriptine, levodopa). Concomitant use with paracetamol and digoxin does not affect the concentration of these drugs in the blood.

How to take, course of use and dosage

Inside. It is recommended to take MOTILIUM tablets 15-30 minutes before meals, if you take the drug after a meal, the absorption of domperidone may slow down. Adults and children over 12 years of age with a body weight of 35 kg or more. 1 tablet (10 mg) 3 times a day, the maximum daily dose is 3 tablets (30 mg). Children under 12 years of age and weighing 35 kg or more. 1 tablet (10 mg) 3 times a day, the maximum daily dose is 3 tablets (30 mg). In children’s practice, MOTILIUM®suspension should mainly be used. Continuous use of MOTILIUM® without consulting a doctor should not exceed 7 days in duration. If necessary, the doctor can extend the course of treatment. Use in patients with renal insufficiency. Since the elimination half-life of domperidone in severe renal insufficiency (with serum creatinine levels greater than 6 mg/10 ml, i. e. more than 0.6 mmol/l) increases, the frequency of use.

Overdose

Overdose symptoms are most common in children and children. Signs of overdose include agitation, altered consciousness, seizures, disorientation, drowsiness, and extrapyramidal reactions. Treatment of overdose: Symptomatic, no specific antidote. Gastric lavage, taking activated charcoal, if extrapyramidal reactions occur-anticholinergic, antiparkinsonian agents. Because of the possible increase in the QT interval, an electrocardiogram (ECG) should be monitored.

Description

Round biconvex film-coated tablets, white to pale cream in color, with the inscription “JANSSEN” on one side of the tablet and M/10 on the other. On the cross-section, the tablet core is white.

Special instructions

Domperidone is not recommended for the prevention of nausea and vomiting after anesthesia. During long-term therapy with the drug, patients should be under regular medical supervision. Domperidone may cause prolongation of the QT interval on the ECG. In the course of post-marketing studies in patients taking domperidone, in rare cases, an increase in the QT interval and the occurrence of ventricular tachycardia of the “pirouette”type were noted. These adverse reactions were observed mainly in patients with risk factors, with severe electrolyte disturbances, or taking concomitant medications that increase the QT interval. Some studies have shown that the use of domperidone can lead to an increased risk of ventricular arrhythmia or sudden coronary death (especially in patients over 60 years of age or with a single dose of more than 30 mg, as well as in patients simultaneously taking drugs that increase the QT interval, or CYP3A4 inhibitors). The use of domperidone and other drugs that can cause prolongation of the QT interval in patients with severe electrolyte disorders (hypo – and hyperkalemia, hypomagnesemia) or in patients with heart diseases, such as chronic heart failure. It has been shown that the presence of electrolyte disturbances (hypo – and hyperkalemia, hypomagnesemia) and bradycardia in a patient can increase the risk of arrhythmia. Domperidone should be discontinued if any symptoms that may be associated with cardiac arrhythmia occur. In this case, you should consult your doctor. When used simultaneously, domperidone enhances the effect of neuroleptics. When used concomitantly with dopaminergic receptor agonists (bromocriptine, levodopa), domperidone inhibits undesirable peripheral effects of the latter, such as digestive disorders, nausea and vomiting, without affecting their central effects. The drug is recommended to be taken at the minimum effective dose. If the medicine has become unusable or the expiration date has expired, do not throw it into the sewage system or on the street! Place the medicine in a plastic bag and put it in the trash can. These measures will help protect the environment!

Form of production

Film-coated tablets

Storage conditions

Store at a temperature of 15 to 30° C. Keep out of the reach of children.

Shelf life

3 years

Active ingredient

Domperidone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children as prescribed by a doctor, Pregnant women as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Flatulence, Gastrointestinal motility disorders, Reflux Esophagitis, Intestinal infections