Motilium Express - Instructions For The Use Of Tablets, Reviews, Price

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Motilium Express

Motilium Express: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Motilium Express

ATX code: A03FA03

Active ingredient: domperidone (Domperidone)

Producer: Catalent UK Swindon Zydis (Great Britain)

Description and photo update: 2019-08-07

Prices in pharmacies: from 350 rubles.

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Motilium Express is an antiemetic drug.

Release form and composition

Dosage form - tablets for resorption: white or almost white, round in shape (in a cardboard box 1 or 3 blisters of 10 tablets and instructions for the use of Motilium Express).

Composition of 1 tablet:

• active substance: domperidone - 10 mg;
• auxiliary components: poloxamer 188 - 1.125 mg; mint essence - 0.3 mg; mannitol - 4.136 mg; gelatin - 5.513 mg; aspartame - 0.75 mg.

Pharmacological properties

Pharmacodynamics

The active substance of Motilium Express, domperidone, is a dopamine antagonist with antiemetic properties. The substance penetrates poorly through the blood-brain barrier.

Domperidone therapy is accompanied by extrapyramidal side effects, especially in adults, in rare cases, the substance stimulates the production of prolactin from the pituitary gland. The antiemetic effect is probably associated with a combination of gastrokinetic (peripheral) action and antagonism towards dopamine receptors in the chemoreceptor trigger zone outside the blood-brain barrier.

The predominantly peripheral effect of domperidone on dopamine receptors is evidenced by animal studies and the low concentration of the drug detected in the brain.

Domperidone, when taken orally, has the following effects:

• an increase in the duration of duodenal and antral contractions;
• acceleration of gastric emptying;
• increased sphincter pressure of the lower esophagus.

The substance does not affect gastric secretion.

Pharmacokinetics

After oral administration on an empty stomach, domperidone is rapidly absorbed. C _max (maximum concentration of the substance) in blood plasma is reached in approximately 30-60 minutes. It has a low bioavailability (about 15%), which is associated with intense first-pass metabolism in the liver and intestinal wall.

Motilium Express should be taken 15-30 minutes before meals. With a decrease in acidity in the stomach, a malabsorption of the substance occurs.

With the preliminary administration of sodium bicarbonate and cimetidine, oral bioavailability decreases. In the case of application of Motilium Express after meals, it takes more time to reach C _max, while AUC (area under the concentration-time curve) slightly increases.

Domperidone, when taken orally, does not accumulate and does not induce its own metabolism. After applying Motilium Express for two weeks at a daily dose of 30 mg, the C _max value in the blood plasma after 90 minutes is 21 ng / ml, which only slightly differs from the C _max value after taking the first dose (18 ng / ml).

Plasma protein binding ranges from 91 to 93%.

When conducting a study in animals of the distribution of domperidone with a radioactive label, its wide distribution in tissues was established, while low concentrations were recorded in the brain. In rats, a small amount of the substance penetrated the placental barrier.

The metabolic process of domperidone is fast and intense, it is provided by hydroxylation and N-dealkylation. In studies of metabolism with diagnostic inhibitors, it was shown that the main form of cytochrome P ₄₅₀, which is involved in the N-dealkylation of domperidone, is the isoenzyme CYP3A4; CYP1A2, CYP3A4 and CYP2E1 are involved in the aromatic hydroxylation of the substance.

Excretion of domperidone by the intestines and kidneys is 66 and 31%, respectively. A small dose of the drug is excreted in the form of an unchanged substance: with feces - 10%, with urine - approximately 1%. Plasma T _1/2 (half-life) after a single oral dose in healthy volunteers is 7-9 hours. In patients with severe renal insufficiency, the value of this indicator increases.

T _{1/2 of} domperidone in severe renal failure (in patients with serum creatinine> 6 mg / 100 ml, i.e.> 0.6 mmol / l) increases from 7.4 to 20.8 hours, while the plasma concentration of the substance lower than in patients with no renal impairment. A small amount of the original substance (approximately 1%) is excreted by the kidneys.

The AUC and C _max values of domperidone in patients with moderate hepatic dysfunction (on the Child - Pugh scale - from 7 to 9 points) are 2.9 and 1.5 times higher than those in healthy volunteers, respectively. The part of the unbound fraction increases by 25%, the T _1/2 value increases from 15 to 23 hours. In mild hepatic impairment, slightly reduced systemic levels of domperidone are observed compared to those in healthy volunteers based on AUC and C _max, while T _1/2 and protein binding are unchanged. The safety profile of the drug in patients with severe hepatic impairment has not been studied.

Indications for use

• a complex of dyspepsia symptoms, which is often associated with such disorders as delayed gastric emptying, gastroesophageal reflux, esophagitis (manifested as a feeling of bloating, epigastric overflow, pain in the upper abdomen, belching with / without gastric contents, vomiting, nausea, flatulence, heartburn);
• vomiting and nausea of various etiologies (functional, organic, infectious), as well as those associated with radiotherapy, drug therapy or dietary disorders;
• vomiting and nausea, the development of which is caused by dopamine agonists (levodopa, bromocriptine) when used by patients with Parkinson's disease.

Contraindications

Absolute:

• moderate and severe liver failure;
• prolactinoma;
• heart disease (eg, chronic heart failure), severe electrolyte disturbances;
• mechanical intestinal obstruction, bleeding from the gastrointestinal tract, intestinal or stomach perforation;
• combination therapy with oral forms of ketoconazole, erythromycin or other drugs that increase the QT interval, or with potent inhibitors of the CYP3A4 isoenzyme (including voriconazole, amiodarone, fluconazole, clarithromycin, telithromycin, and others);
• weight less than 35 kg;
• age up to 12 years with a weight of up to 35 kg;
• pregnancy and lactation;
• individual intolerance to the components of the drug.

Relative (Motilium Express tablets are prescribed under medical supervision):

• impaired renal function;
• congestive heart failure;
• electrolyte imbalance;
• violations of conduction and heart rhythm (including prolongation of the QT interval).

Motilium Express, instructions for use: method and dosage

Motilium Express tablets are intended for oral administration. The drug is recommended to be taken before meals, since the absorption of domperidone, if taken after meals, may slow down.

The maximum duration of continuous reception of Motilium Express in patients of all age categories for the treatment of acute nausea and vomiting usually does not exceed 7 days. If at the end of this period the symptoms persist, you should consult your doctor again.

When using Motilium Express for other indications, the duration of treatment is 4 weeks. If at the end of this period the symptoms persist, the patient should be re-examined and the effectiveness of treatment evaluated.

The recommended dosing regimen for adults and children over 12 years of age weighing ≥ 35 kg: 3 times a day, 1 tablet. The maximum daily dose is 30 mg (3 tablets).

The lozenges are rather fragile to avoid damage, it is not recommended to push them through the foil (it is necessary to completely remove the foil from the cell by grasping its edge).

After removing from the blister, the tablet must be put on the tongue. On its surface, the tablet disintegrates in a few seconds, after which it can be swallowed with saliva without drinking water.

The frequency of application of Motilium Express in patients with severe renal insufficiency should be reduced to 1-2 times a day. During the period of therapy, the patient's condition should be monitored regularly.

Side effects

According to the data of clinical studies, adverse reactions that were observed in ≥ 1% of cases during therapy with Motilium Express were: anxiety, depression, drowsiness, headache, akathisia, diarrhea, dry mouth, asthenia, lack / decrease in libido, itching, gynecomastia, galactorrhea, rash, violation of lactation, tenderness and pain in the area of the mammary glands, amenorrhea and menstrual irregularities.

Less than 1% of patients with Motilium Express developed urticaria, hypersensitivity, swelling and discharge from the mammary glands.

Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare; with an unknown frequency - it is impossible to establish the frequency of occurrence adverse reactions based on available data), recorded based on spontaneous reports during post-marketing use:

• kidneys and urinary tract: very rarely - urinary retention;
• immune system: very rarely - angioedema, anaphylactic reactions (including anaphylactic shock), urticaria;
• cardiovascular system: very rarely - ventricular arrhythmia *, prolongation of the QT interval, sudden coronary death *;
• nervous system: very rarely - extrapyramidal disorders, dizziness, convulsions (mainly in newborns and children);
• laboratory indicators: very rarely - an increase in the level of prolactin in the blood, deviations of laboratory indicators of hepatic function;
• psyche: very rarely - agitation, nervousness (mainly in newborns and children).

Adverse reactions registered during post-registration clinical trials of Motilium Express:

• psyche: infrequently - increased excitability (mainly in newborns and children), nervousness;
• kidneys and urinary tract: infrequently - urinary retention;
• cardiovascular system: with an unknown frequency - serious ventricular arrhythmias *, prolongation of the QT interval, sudden coronary death *;
• nervous system: often - dizziness; rarely - convulsions (mainly in newborns and children); with an unknown frequency - extrapyramidal disorders (mainly in newborns and children);
• laboratory data: infrequently - deviations of laboratory parameters of hepatic function; rarely - an increase in the level of prolactin in the blood;
• allergic reactions: with an unknown frequency - anaphylactic reactions (including anaphylactic shock), angioedema.

* Some epidemiological studies have found that domperidone therapy may be associated with an increased likelihood of severe ventricular arrhythmias or sudden death. The risk of these side effects is more likely in patients over 60 years of age and in patients who exceed the daily dose (30 mg). Adults and children are advised to take Motilium Express at the lowest effective dose.

Overdose

The most common symptoms of overdose occur in infants and children, they can include disorders such as agitation, disorientation, seizures, impaired consciousness, extrapyramidal disorders and drowsiness.

Therapy: gastric lavage and intake of activated charcoal are recommended, careful monitoring of the patient's condition should be established, supportive treatment is indicated. In order to correct extrapyramidal manifestations, it is possible to use anticholinergics, antiparkinsonian or antihistamines. There is no specific antidote.

special instructions

With the combined use of Motilium Express with antisecretory or antacid drugs, the latter should be taken not before, but after meals, that is, simultaneous administration is not recommended.

In patients with renal insufficiency, a single dose adjustment is not required. In this case, in the case of repeated use of Motilium Express, the frequency of its intake should be reduced to 1-2 times a day (depending on the severity of renal dysfunction). In addition, there may be a need for dose reduction. Long-term therapy should take place under regular medical supervision.

Some epidemiological studies have shown that therapy with Motilium Express may be associated with an increased risk of developing serious ventricular arrhythmias or sudden death. The risk is more likely in patients over 60 years of age, as well as when using the drug in a daily dose that exceeds the recommended one.

Application Motilium Express and other drugs that lead to a lengthening of the interval QT _c, is not recommended for patients with the following disorders:

• severe electrolyte imbalance (hyperkalemia, hypokalemia, hypomagnesemia);
• conduction disorders (for example, with prolongation of the QT interval _c);
• concomitant heart disease (such as congestive heart failure);
• bradycardia.

In cases of the appearance of symptoms or signs that may indicate the development of cardiac arrhythmia, you should stop taking Motilium Express and consult your doctor.

The main metabolic pathway of domperidone is via CYP3A4. According to human studies, concomitant use of drugs that significantly inhibit this enzyme may occur with an increase in the plasma concentration of domperidone. The combination of domperidone with potent CYP3A4 inhibitors, which cause prolongation of the QT interval, is contraindicated.

With the simultaneous use of domperidone with potent CYP3A4 inhibitors that do not cause prolongation of the QT interval (for example, with indinavir), caution is required. Patients should be carefully monitored to detect symptoms or signs of adverse reactions.

With the combined use of Motilium Express with drugs that cause prolongation of the QT interval, care must be taken. Monitoring is necessary to identify adverse reactions from the cardiovascular system.

This warning applies in particular to the following medicines:

• haloperidol, pimozide, sertindole (antipsychotics);
• disopyramide, quinidine, ibutilide, amiodarone, dronedarone, dofetilide, sotalol (class IA and III antiarrhythmics);
• levofloxacin, moxifloxacin (antibiotics);
• citalopram, escitalopram (antidepressants);
• halofantrine (antimalarial drugs);
• pentamidine (antifungal drugs);
• toremifene, vandetanib (anticancer drugs);
• dolasetron (gastrointestinal drugs);
• bepridil, methadone (some other drugs).

Aspartame is a part of Motilium Express, therefore the drug is not prescribed for patients with hyperphenylalaninemia.

Influence on the ability to drive vehicles and complex mechanisms

During the period of application of Motilium Express, care should be taken when driving a motor vehicle, which is associated with the likelihood of adverse reactions that may affect the ability to concentrate and the speed of psychomotor reactions.

Application during pregnancy and lactation

Motilium Express is not prescribed during pregnancy / lactation.

There is not enough information on the use of domperidone during pregnancy. And although there is no information on the increased risk of malformations in humans, the appointment of Motilium Express is not recommended for pregnant women.

Only a small amount of domperidone can enter the child's body with mother's milk. The maximum relative dose for infants (%) is estimated at about 0.1% of the dose taken by the mother based on body weight. Whether this level of the substance has a negative effect on newborns is unknown. In this regard, Motilium Express is not prescribed for women who are breastfeeding, or, if such therapy is necessary, it is recommended to interrupt breastfeeding.

Pediatric use

Patients under 12 years of age weighing up to 35 kg are not prescribed the drug. In pediatric practice, the use of Motilium in the form of a suspension is recommended.

With impaired renal function

Motilium Express for impaired renal function should be used under medical supervision.

For violations of liver function

The drug is not prescribed for patients with moderate and severe liver dysfunctions.

Drug interactions

• anticholinergic drugs: the action of Motilium Express when used in combination can be neutralized;
• cimetidine, sodium bicarbonate: if domperidone is taken after these agents, its bioavailability may decrease; you should not take antisecretory and antacid drugs simultaneously with Motilium Express;
• itraconazole, fluconazole, ketoconazole, voriconazole (azole antifungal drugs), clarithromycin, erythromycin (macrolide antibiotics), ritonavir, amprenavir, nelfinavir, atazanavir, indinavir, fosamprenavir, calcium vurapinavir inhibitors (HIV), sakvinavir calcium inhibitors, HIV) as well as other potent inhibitors of CYP3A4, including amiodarone, nefazodone, aprepitant, telithromycin: the plasma concentration of domperidone may increase;
• anticholinergic drugs (including dextromethorphan, diphenhydramine): the severity of the antidispeptic effects of Motilium Express may decrease.

When conducting some studies of the pharmacodynamic and pharmacokinetic interaction of domperidone and ketoconazole / erythromycin in healthy volunteers, it was shown that these drugs significantly inhibit the first pass metabolism, carried out by the isoenzyme CYP3A4. When combined reception domperidone (4 times a day by 10 mg) and ketoconazole (2 times a day, 200 mg) was observed lengthening the interval QT _c on average 9.8 ms over the entire period of observation, at some point changes were in the range 1, 2-17.5 ms. With the combined administration of domperidone in the same daily dose and erythromycin (3 times a day, 500 mg each), a similar effect was observed (on average, prolongation of the QT interval _cwas 9.9 ms, at some moments the changes were in the range of 1.6–14.3 ms). At the same time, the values of C _max and AUC of domperidone increased approximately 3 times in each of these studies.

What contribution to the change in the QT _c interval is made by the increased plasma concentration of domperidone is currently unknown.

Monotherapy with domperidone in these studies led to an extension of the QT interval _c by 1.6 and 2.5 ms (in studies with ketoconazole and erythromycin, respectively), while monotherapy with ketoconazole and erythromycin - by 3.8 and 4.9 ms, respectively, throughout observation period.

In another study where healthy volunteers were used multiple doses during the stationary domperidone monotherapy significant lengthening of the interval the QT _c were found. At the same time, the plasma concentration of domperidone was similar to that in studies of the interaction of domperidone and other drugs.

Analogs

Analogues of Motilium Express are: Domperidone, Domed, Motiject, Domstal, Motilak, Motilium, Motogastric, Passage, Motonium, Motoinorm, etc.

Terms and conditions of storage

Store in a place protected from moisture at temperatures up to 25 ° C in its original packaging. Keep out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews of Motilium Express

Reviews of Motilium Express are mostly positive. It is considered an effective and fast-acting drug. Also, the advantages include a pleasant taste and a convenient form of release. The cost is assessed as high.

Price for Motilium Express in pharmacies

The approximate price of Motilium Express (30 tablets) is 635 rubles.

Motilium Express: prices in online pharmacies

Drug name Price Pharmacy

Motilium Express 10 mg lozenges 10 pcs. RUB 350 Buy

Motilium Express 10 mg lozenges 30 pcs. RUB 400 Buy

Motilium express tablets for rassas. 10mg 30 pcs. 652 r Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!