Motilium Express lozenges 10 mg N30

Dosage forms and composition

Motilium contains the active dose of the substance domperidone. It is a strong dopamine receptor blocker. Several types of the drug are available for oral administration:

1. Regular film-coated tablets: white, convex, engraved “10M”. Each contains 10 mg of domperidone, lactose, MCC, hydrogenated vegetable fat, starch, polyvidone and other auxiliary components. The package contains 1–3 blisters.
2. Lingual lozenges with a similar dosage, slightly minty taste. The active substance in them is supplemented with gelatin, menthol, aspartame and mannitol. Packed in 10–30 pieces.
3. Suspension for children. White, syrupy, sweetish liquid containing 1 mg of domperidone per 100 ml. Packaged in dark glass bottles with a screw cap. The drug also contains sodium saccharinate, water, sorbitol, polysorbate and stabilizers. Each package of the product has a special syringe for precise dosing.

When is it best to take Motilium?

Many people know what nausea is and what troubles and consequences vomiting brings. This is a constant anxious state of the body, unpleasant abdominal pain, restless and anxious sleep. It is very important to know which medications will best help relieve unpleasant and disturbing symptoms without harming the body. Motilium is an effective and fast-acting remedy that copes well with a complex task. It relieves dyspeptic symptoms that are caused by problems with gastric emptying, esophagitis and gastroesophageal reflux. Basically, the medicine is prescribed when:

Therapeutic effect

Motilium has the ability to eliminate nausea, stop vomiting, and gently activate intestinal motility. The active component of the drug, domperidone, exhibits some properties of an antipsychotic, suppressing sensitivity to dopamine. Unlike other inhibitors, it is more neutral: it does not cause dystonia, tremor, or nervous tics.

The drug increases the tone of muscle fibers and enhances contractions of the esophageal sphincter in its lower part. Thanks to this, the evacuation function of the stomach is normalized, signs of dyspepsia, indigestion, and other motility disorders and diseases of the gastrointestinal tract are eliminated.

The drug is absorbed by the mucous membranes within a few minutes and actively binds to blood proteins. Transformed by liver cells. It is excreted from the body by the kidneys and with intestinal contents within 0.5–1 days after administration.

Domperidone stimulates the release of prolactin. The secretion of gastric juice and its acidity are not affected. When consumed during or immediately after a meal, the effect of Motilium may slow down somewhat.

Motilium Express lozenges No. 30

A country

UK, UK, France
Country of origin may vary depending on product batch. Please check with the operator for detailed information when confirming your order.

Compound

1 tablet contains: domperidone 10 mg. Excipients: gelatin - 5.513 mg, mannitol - 4.136 mg, aspartame - 0.75 mg, mint essence - 0.3 mg, poloxamer 188 - 1.125 mg. Lozenges are white or almost white, round.

pharmachologic effect

Domperidone is a dopamine antagonist with antiemetic properties. Domperidone does not penetrate the blood-brain barrier well. Domperidone is rarely associated with 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 of dopamine receptors in the chemoreceptor trigger zone, which is located outside the BBB. Animal studies and low concentrations of the drug detected in the brain indicate a predominantly peripheral effect of domperidone on dopamine receptors. When administered orally, domperidone increases the duration of antral and duodenal contractions, accelerates gastric emptying and increases sphincter pressure of the lower esophagus. Domperidone has no effect on gastric secretion.

Mode of application

The drug is taken orally. It is recommended to take Motilium before meals; if the drug is taken after meals, the absorption of domperidone may slow down. In patients of all age groups, usually for the treatment of acute nausea and vomiting, the maximum duration of continuous use of the drug should not exceed 1 week. If nausea and vomiting continues for more than 1 week, the patient should reconsult with their doctor. For other indications, the duration of therapy is 4 weeks. If symptoms do not disappear within 4 weeks, it is necessary to re-examine the patient and assess the need for continued therapy. Lozenges Adults and children over 12 years old and weighing ≥35 kg - 10 mg (1 tablet) 3 times a day. The maximum daily dose is 30 mg (3 tablets). Children under 12 years of age and weighing ≥35 kg - 10 mg (1 tablet) 3 times a day. The maximum daily dose is no more than 30 mg (3 tablets). In pediatric practice, Motilium suspension should mainly be used. Directions for use Since lozenges are quite fragile, they should not be pressed through the foil to avoid damage. To remove the tablet from the blister the following is necessary: ​​- take the foil by the edge and completely remove it from the cell in which the tablet is located; - gently press from below; - remove the tablet from the package. Place the tablet on your tongue. Within a few seconds it will disintegrate on the surface of the tongue, it can be swallowed with saliva, without drinking water. Special groups of patients Since T1/2 of domperidone in severe renal failure (with serum creatinine level > 6 mg/100 ml, i.e. > 0.6 mmol/l) increases, the frequency of taking Motilium should be reduced to 1 or 2 times a day, depending on the severity of the deficiency. It is necessary to conduct regular examination of patients with severe renal failure. The use of the drug is contraindicated in patients with moderate (7-9 points according to the Child-Pugh classification) or severe (> 9 points according to the Child-Pugh classification) liver failure. In patients with mild (5–6 points according to the Child-Pugh classification) liver failure, dosage adjustment of the drug is not required.

Interaction

Anticholinergic drugs can neutralize the effect of the drug Motilium. The bioavailability of the drug Motilium when taken orally decreases after previous administration of cimetidine or sodium bicarbonate. You should not take antacid and antisecretory drugs simultaneously with domperidone, because they reduce its bioavailability after oral administration. The main role in the metabolism of domperidone is played by the CYP3A4 isoenzyme. In vitro studies and clinical experience indicate that concomitant use of drugs that significantly inhibit this isoenzyme may cause increased plasma concentrations of domperidone. Potent CYP3A4 inhibitors include azole antifungals (such as fluconazole*, itraconazole, ketoconazole* and voriconazole*), macrolide antibiotics (such as clarithromycin* and erythromycin*), HIV protease inhibitors (such as amprenavir, atazanavir, fosamprenavir, indinavir, nelfinavir, ritonavir and saquinavir), calcium antagonists (such as diltiazem and verapamil), amiodarone*, aprepitant, nefazodone, telithromycin*. (Drugs marked with an asterisk also prolong the QTc interval.) In a number of pharmacokinetic and pharmacodynamic interaction studies of domperidone with ketoconazole and erythromycin administered orally in healthy volunteers, these drugs have been shown to significantly inhibit first-pass metabolism via the CYP3A4 isoenzyme. With simultaneous administration of 10 mg of domperidone 4 times a day and 200 mg of ketoconazole 2 times a day, there was an increase in the QTc interval by an average of 9.8 ms during the entire observation period, at certain points the changes varied from 1.2 to 17.5 ms. With simultaneous administration of 10 mg of domperidone 4 times a day and 500 mg of erythromycin 3 times a day, there was an increase in the QTc interval by an average of 9.9 ms during the entire observation period, at certain points the changes varied from 1.6 to 14.3 ms. In each of these studies, the Cmax and AUC of domperidone were increased approximately 3-fold. It is currently unknown how elevated plasma concentrations of domperidone contribute to changes in the QTc interval. In these studies, domperidone monotherapy (10 mg 4 times / day) led to a prolongation QTc interval by 1.6 ms (ketoconazole study) and 2.5 ms (erythromycin study), while ketoconazole monotherapy (200 mg 2 times / day) and erythromycin monotherapy (500 mg 3 times / day) led to a prolongation of the QTc interval by 3.8 and 4.9 ms, respectively, throughout the observation period. In another study using multiple doses in healthy volunteers, no significant prolongation of the QTc interval was found during inpatient monotherapy with domperidone (40 mg 4 times / day, total daily dose of 160 mg, which is 2 times the recommended maximum daily dose). However, plasma concentrations of domperidone were similar to those in studies of the interaction of domperidone with other drugs. The combined use of anticholinergic drugs (for example, dextromethorphan, diphenhydramine) may interfere with the development of the antidyspeptic effects of Motilium. Theoretically, since Motilium has a gastrokinetic effect, it could influence absorption of concomitantly administered oral drugs, in particular drugs with prolonged release of the active substance or enteric-coated drugs. However, the use of domperidone in patients taking paracetamol or digoxin did not affect the level of these drugs in the blood. Motilium can be taken simultaneously with antipsychotics, the effect of which it does not enhance; dopamine receptor agonists (bromocriptine, levodopa), the undesirable peripheral effects of which, such as digestive disorders, nausea, vomiting, it suppresses without affecting their central effects.

Side effect

According to clinical studies, Adverse reactions observed in ? 1% of patients taking Motilium: depression, anxiety, decreased or absent libido, headache, drowsiness, akathisia, dry mouth, diarrhea, rash, itching, galactorrhea, gynecomastia, pain and tenderness in the area of ​​the mammary glands, menstrual irregularities and amenorrhea, lactation disorders, asthenia. Adverse reactions observed in Contraindications - hypersensitivity to domperidone or any of the components of the drug; - prolactinoma; - simultaneous use of oral forms of ketoconazole, erythromycin or other drugs that increase the interval QT, or potent inhibitors of the CYP3A4 isoenzyme, such as fluconazole, voriconazole, clarithromycin, amiodarone, telithromycin and others (see sections "Special instructions" and "Drug interactions"); - severe electrolyte disturbances or heart disease, such as chronic heart failure; - bleeding from the gastrointestinal tract, mechanical intestinal obstruction, perforation of the stomach or intestines; - liver failure of moderate and severe severity; - body weight less than 35 kg (for lozenges); - children under 12 years of age with a body weight less than 35 kg (for lozenges);—pregnancy;—breastfeeding period. The drug should be used with caution in case of impaired renal function, cardiac rhythm and conduction disturbances (incl. prolongation of the QT interval), electrolyte imbalance, congestive heart failure. Pregnancy and lactation Pregnancy There is insufficient data on the use of domperidone during pregnancy. To date, there is no evidence of an increased risk of malformations in humans. However, the drug should be prescribed during pregnancy only in cases where its use is justified by the expected therapeutic benefit. Lactation The amount of domperidone that can enter the child's body through breast milk is small. The maximum relative dose for infants (%) is estimated at about 0.1% of the dose taken by the mother based on body weight. It is unknown whether this level has a negative effect on newborns. In this regard, when using the drug during lactation, it is recommended to stop breastfeeding. Use in elderly patients The use of domperidone may be associated with an increased risk of serious ventricular arrhythmias or sudden death. The risk may be more likely in patients over 60 years of age.

Overdose

Symptoms of overdose occur most often in infants and children and may include agitation, impaired consciousness, convulsions, disorientation, somnolence and extrapyramidal disorders. Treatment: There is no specific antidote for domperidone. In case of overdose, gastric lavage and administration of activated charcoal, careful observation and supportive care are recommended. To correct extrapyramidal manifestations, anticholinergics, antiparkinsonian drugs, or antihistamines can be used.

special instructions

When using the drug Motilium in combination with antacid or antisecretory drugs, the latter should be taken after meals and not before meals, i.e. they should not be taken simultaneously with the drug Motilium. Use for kidney diseases. Since a very small percentage of the drug is excreted unchanged by the kidneys, single dose adjustment is not required in patients with renal failure. However, when re-prescribing the drug Motilium, the frequency of use should be reduced to 1-2 times a day, depending on the severity of renal dysfunction, and it may also be necessary to reduce the dose. During long-term therapy, patients should be monitored regularly. Effects on the cardiovascular system Some epidemiological studies have shown that the use of domperidone may be associated with an increased risk of serious ventricular arrhythmias or sudden death. The risk may be more likely in patients over 60 years of age and in patients taking the drug in daily doses of more than 30 mg. The use of domperidone in the lowest effective dose is recommended in adults and children. The use of domperidone and other drugs that lead to prolongation of the QTc interval is not recommended in patients with existing conduction disorders, in particular, prolongation of the QTc interval, and in patients with severe electrolyte imbalance (hypokalemia , hyperkalemia, hypomagnesemia) or with bradycardia, or in patients with underlying cardiac disease such as congestive heart failure. As is known, against the background of electrolyte imbalance and bradycardia, the risk of arrhythmias increases. If signs or symptoms appear that may be associated with cardiac arrhythmia, therapy with Motilium should be discontinued and a doctor should be consulted. Potential for drug interactions The main route of metabolism of domperidone is via CYP3A4. In vitro data and human studies indicate that concomitant use of drugs that significantly inhibit this enzyme may be associated with increased plasma concentrations of domperidone. The combined use of domperidone with strong CYP3A4 inhibitors, which have been shown to cause QT prolongation, is contraindicated. Caution should be exercised when co-administering domperidone with strong CYP3A4 inhibitors that do not cause QT prolongation, such as indinavir; Patients should be closely monitored for signs or symptoms of adverse reactions. Caution is advised when coadministering domperidone with drugs known to prolong the QT interval; Patients should be closely monitored for signs or symptoms of cardiovascular adverse reactions. Examples of such drugs include: - Class IA antiarrhythmics (eg, disopyramide, quinidine); - Class III antiarrhythmics (eg, amiodarone, dofetilide, dronedarone, ibutilide, sotalol); - certain antipsychotics (for example, haloperidol, pimozide, sertindole); - certain antidepressants (for example, citalopram, escitalopram); - certain antibiotics (for example, levofloxacin, moxifloxacin); - certain antifungals (for example, pentamidine); - certain antimalarials (eg, halofantrine); - certain gastrointestinal medicines (eg, dolasetron); - certain anticancer medicines (eg, toremifene, vandetanib); - certain other medicines (eg, bepridil, methadone). Excipients Motilium suspension for oral administration contains sorbitol and is not recommended for use in patients with sorbitol intolerance. Motilium EXPRESS lozenges contain aspartame, so they should not be used in patients with hyperphenylalaninemia. Disposal of the drug If the drug has become unusable or has expired, do not throw it away. sewage or outside. It is necessary to place the medicine in a bag and place it in the trash container. These measures will help protect the environment. Pediatric use Motilium may cause neurological side effects in rare cases. The risk of neurological side effects is higher in young children because Metabolic functions and the BBB are not fully developed in the first months of life. In this regard, you should strictly adhere to the recommended dose. Neurological side effects can be caused in children by an overdose of the drug, but other possible causes of such effects must be taken into account. Impact on the ability to drive vehicles and operate machinery. Care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration. and speed of psychomotor reactions due to the risk of developing adverse reactions that may affect these abilities.

Dispensing conditions in pharmacies

On prescription

Indications and doses

Treatment with Motilium includes a wide range of gastrointestinal pathologies:

• peptic ulcer - as part of complex therapy;
• intestinal atony;
• symptoms of delayed gastric emptying: heaviness, feeling of fullness, nausea;
• flatulence, intestinal cramps;
• hypokinetic cholecystitis;
• epigastric pain, heartburn, vomiting, belching and other symptoms of esophagitis;
• attacks of vomiting caused by intoxication, functional disorders, drug or radiotherapy.

Motilium is prescribed for quick cleansing of the stomach cavity and intestinal lumen in preparation for ultrasound and radiographic examinations, and other medical procedures.

For children, the drug is indicated for profuse vomiting, pathological regurgitation, signs of esophageal reflux, flatulence, and bloating.

It is recommended to use the product on an empty stomach, 30–40 minutes before. before meals. In some cases - before bed.

1. Children under 5 years of age are given a suspension at the rate of 2.5 ml for every 10 kg of body weight. Infants are administered Motilium from a special syringe or pipette 3-4 times a day. The bottle is shaken several times before using the mixture. The special syringe dispenser is washed with water after each set of medication.
2. Children over 1 year of age are allowed to double the dosage.
3. At the age of 5–12 years, 10–20 ml of suspension per dose or 1–2 tablets of the drug up to 4 times a day are allowed.

Adults can take the medicine 1-2 tablets as many times a day as necessary. The maximum recommended dose is 80 mg. With reduced liver function, the dosage should be reduced by 1.5–2 times. The drug does not harm those suffering from renal failure and is approved for use, since metabolites are excreted in the urine in an insignificant amount. No dose adjustment is required in such cases.

Pharmacokinetic properties of the drug

The medicine is best taken before meals, on an empty stomach. Thus, its rapid absorption from the gastrointestinal tract occurs. After taking Motilium orally, the drug can be detected in the blood plasma after half an hour or an hour. Domperidone has low bioavailability as a result of extensive primary metabolism in the liver and intestinal walls. Although it is noted that if a healthy person takes the medicine after a meal, the bioavailability of the drug increases.

Motilium. Help for the stomach

For a sick person, it is recommended to take the medicine only a few minutes or half an hour before meals. If the acidity of gastric juice is reduced then the absorption of domperidone is reduced. A decrease in the bioavailability of the drug was also observed in the case of prior administration of certain medications such as sodium bicarbonate or cimetinide.

When taking medicine, you need to remember that greater results are achieved if you take it before meals than after meals. Conducted animal studies regarding the binding of domperidone to plasma proteins show that the drug is distributed in high concentrations in the tissues; slightly less of it can be found in the brain.

Studies on rats have shown that the smallest percentage of the drug is able to penetrate the placenta barrier. Motilium is excreted from the body in feces and urine.

Side effects and interactions

When treating with Motilium, caution should be exercised when using antacids and agents that reduce secretory activity. It is recommended to separate them by time.

The simultaneous use of antifungal drugs, some drugs against HIV infection and macrolides contributes to the prolonged presence of Motilium in the blood. This is important to consider for people with impaired liver and endocrine system functions.

Most patients tolerate therapy well. In rare cases, the drug may cause menstrual irregularities or gynemastia due to changes in prolactin levels in women.

In case of an overdose, spasms in the intestinal area, loss of appetite, drowsiness, and an unpleasant taste in the mouth are likely to occur.

Pharmacological qualities of the drug

Motilium. Lozenges

Motilium refers to medications that are aimed at stimulating intestinal motility and suppressing the urge to vomit. The main effect of the drug is provided by domperidone, which acts like some antipsychotics and metoclopramide, which are antagonists of dopapine.

This type of medication causes virtually no side effects, since it has poor permeability through the blood-brain barrier. However, sometimes children may experience unwanted side effects of the drug. Thanks to the main, active substance, prolactin is released from the pituitary cells.

The drug copes well with gastric emptying and helps increase the duration of duodenal and antral contractions.

When the medicine is taken orally in an adult, the evacuation of solid and liquid food from the stomach is much easier, while in sick patients, when the evacuation of solid food is slowed down, this process is much faster and better. Taking the medicine in a healthy person normalizes the tone and pressure in the esophageal sphincter area. However, the medicine does not have a negative effect on the secretion of gastric juice.

Side effects caused by taking Motilium. Contraindications

Motilium. Release form - tablets

It is very rare to find medications that do not cause side effects. Even drugs that have a natural base are not suitable for everyone. Therefore, Motilium is no exception. Side effects can be severe or moderate, sometimes even unnoticed. The most common side effects are:

1. in the endocrine system. In this case, gynecomastia, galactorrhea, and hyperprolactinemia develop;
2. in the central nervous system. In this case, extrapyramidal disorders are observed, which disappear as soon as you stop taking the suspension or tablets;
3. in the digestive system. In this case, a disorder of the gastrointestinal tract is very rarely observed, and spasmodic contraction of the intestine is very rarely observed.

After examining the patient and child, the doctor will tell you whether Motilium can be taken as a remedy. Thus, in case of perforation of the stomach or intestines or its obstruction as a result of a mechanical disorder, it is better to replace the drug with another more suitable medicine. It is also contraindicated for people who suffer from prolactinoma. If they have gastrointestinal bleeding, their body cannot tolerate one of the components of this drug.