What is Motilium
The active component of the drug is domperidone, a substance that can quickly suppress nausea, normalize peristalsis, stool, and relieve signs of indigestion. The product is produced in several pharmaceutical forms:
- film-coated tablets: white, biconvex, containing 10 mg of domperidone, packaged in blisters;
- non-coated sublingual tablets with mint flavor;
- syrup for children: a sweetish, thick, white, water-based liquid with a dosage of domperidone 1 mg per 1 ml, sold in glass bottles with a measuring syringe.
The tablet medicine contains auxiliary compounds: starch, povidone, stabilizers.
Motilium®
Anticholinergic drugs may counteract the effects of Motilium.
The bioavailability of Motilium when taken orally decreases after previous administration of cimetidine or sodium bicarbonate. You should not take antacid and antisecretory drugs simultaneously with Motilium, because they reduce its bioavailability.
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. Strong 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. (Drugs marked with an asterisk also prolong the QTc interval.)
In a number of studies of the pharmacokinetic and pharmacodynamic interactions of domperidone with oral ketoconazole and oral erythromycin in healthy volunteers, these drugs have been shown to significantly inhibit the primary metabolism of domperidone by the CYP3A4 isoenzyme.
With simultaneous administration of 10 mg of domperidone 4 times/day and 200 mg of ketoconazole 2 times/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) resulted in QTc interval prolongation by 1.6 ms (ketoconazole study) and 2.5 ms (erythromycin study), whereas 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, during the entire observation period.
In another multiple-dose study in healthy volunteers, there was no significant prolongation of the QTc interval during inpatient domperidone monotherapy (40 mg 4 times daily, total daily dose 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.
Theoretically (since the drug has a gastrokinetic effect), Motilium® could influence the absorption of concomitantly administered oral drugs, in particular, drugs with a delayed release of the active substance or enteric-coated drugs. However, the use of domperidone in patients taking paracetamol or digoxin did not affect the concentration 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.
For what diseases is Motilium needed?
The medicine helps restore well-being in the following pathologies:
- stomach ulcer;
- atonic bowel dysfunction;
- flatulence;
- hypokinetic dyskinesia of the gallbladder;
- epigastric pain;
- nausea, vomiting due to food or chemical intoxication;
- digestive disorders due to taking medications, radiation therapy;
- spontaneous constipation;
- frequent regurgitation in children.
The drug moderately stimulates intestinal peristalsis, normalizing gastric functions and eliminating signs of dyspepsia. Domperidone suppresses dopamine activity, producing a mild antipsychotic effect. But, unlike other drugs, it does not lead to autonomic disorders.
The medicine quickly penetrates the blood through the mucous membranes and interacts with its proteins. After administration, Motilium cleanses the stomach cavity, intestinal lumen, binds and neutralizes toxic substances. It is completely excreted from the body with intestinal contents after 12–24 hours, without accumulating in tissues.
MOTILIUM (suspension)
kov doctors and 3 from the emergency room.
On the 5th day, the child, who usually runs around with a temperature of 39.3 as if healthy, lay down with a cloth on the sofa. Then I decided to act tough. I quickly packed the bag for the hospital and called an ambulance. We were offered a Cerucal injection. Glory to this medicine! I finally achieved that the child began to retain fluid. On this day, my mother, a doctor, came to us from another city. She said: there is no point in sitting at home outside, it’s spring, we need to go for a walk. We went for a walk and walked about 1.5 km. My child trained 8 km. passes healthy, as if there is nothing to do. We came home. The child sat on the potty (sorry for the details), but about 0.6 liters of sour cream-like feces came out of him. Then I realized that the child had an obstruction. If it had taken another 1-2 days it would have been impossible to save him. My child has 2 terrible characteristics: he does not like to drink and poop (he always tries to restrain the urge so as not to be distracted from an interesting activity). This causes another problem: constipation and intoxication with one’s own feces. At the end of October, everything repeats itself. I have already told the doctors the story that happened in the spring. Doctors again do not undertake to diagnose anything. The child (4.5 years old) is still an artist, sometimes he lies down and rolls his eyes, sometimes he walks and staggers. That’s when we were prescribed Motilium along with Cerucal. We take it for three days. The child gradually began to recover. I began to eat and retain at least a quarter of my usual daily diet. Suddenly, on the evening of the third day, the child immediately began not just screaming, but screaming louder than women in labor during their last contraction, rushing from corner to corner, and covered in sweat. To all questions, he only answers: his butt hurts. In general, since he learned to speak from me, he knows that crying and screaming will not achieve anything. It is clear that the child is experiencing inhuman torment. I called an ambulance and quickly threw on a bag, preparing to be hospitalized. At the moment when the ambulance doctors arrived, the child suddenly rushes headlong onto the potty. The stool is not bulky, but smelly. Thanks to this, the emergency doctors were able to understand that it was an intestinal infection. When they found out that I was giving the child Motilium, they were so indignant (they just didn’t shoot me). They said that Motilium should not be prescribed for vomiting at all. They explained that if a child vomits, then the process of digestion does not come to pass, and improving digestion and intestinal movement on an empty stomach is a crime. Which leads to a very painful and often false (because there is simply nothing to do with it) urge to defecate. They said that they are repeatedly induced with such symptoms after Motilium against the background of vomiting.
After reading the instructions I was surprised. The instructions include indications for use in case of vomiting. Motilium was canceled for us. The next day we fought our way to the gastroenterologist without an appointment, arguing that we had an emergency rather than a chronic condition. The doctor confirmed the words of his ambulance colleagues and said that in our case Motilium should not be prescribed. Prescribed adequate treatment. After 2 days, the child was almost healthy.
To my question: what about all the indications in the instructions, he said that they were written in a streamlined manner and not correctly. And those who prescribe Motilium for vomiting and intestinal infections are not competent doctors. Motilium is intended to improve digestion and for frequent constipation.
I would like to note the miracle effect of Motilium. Despite the fact that the child took it for only three days, there have been no problems with bowel movements or constipation for a month now. Everything is like clockwork at the same time. The child developed a voracious appetite. He eats whatever you give him. Thanks to such an appetite, I finally taught him to eat salads from fresh vegetables every day. The child didn’t really like fruit either, and now he asks for an apple. Of course, the price of the product is not small; it cost us 721 rubles. If we had been prescribed it a couple of years ago, when problems with constipation had just begun, I think now my child would have a stronger immune system, since he would have an appetite and eat healthy foods, and would not poison himself with his own feces.
Therefore, I consider Motilium a very effective drug, especially if it is prescribed correctly.
How to take Motilium tablets
Adults are recommended to take 1 pill three times a day, 15–20 minutes before meals. The coated tablets are washed down with cool or warm water. Sublingual - placed under the tongue until completely dissolved. If necessary, the single dose is increased 2–3 times. The maximum number of tablets per day is 8 pcs. It is allowed to take the medicine before bedtime.
For children, treatment with Motilium in tablets is recommended from 6–7 years of age: 1 tablet 2–3 times a day. For body weights less than 35 kg, it is recommended to use a suspension of the drug.
Motilium lozenges 10 mg 10 pcs.
Anticholinergic drugs may counteract the effect of Motilium. The bioavailability of Motilium when taken orally decreases after previous administration of cimetidine or sodium bicarbonate. Antacids and antisecretory drugs should not be taken simultaneously with domperidone, as 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; - Antibiotics from the macrolide group, for example, clarithromycin and erythromycin; - HIV protease inhibitors, for example, 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 QT interval.) In a number of studies of the pharmacokinetic and pharmacodynamic interactions of domperidone with ketoconazole and erythromycin when taken 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, a prolongation of the QT interval was observed by an average of 9.8 ms during the entire observation period, at certain points the changes ranged 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 QT interval by an average of 9.9 ms during the entire observation period, at certain points the changes ranged from 1.6 to 14.3 ms. In each of these studies, the Cmax and AUC of domperidone were increased approximately threefold. It is currently unknown how elevated plasma concentrations of domperidone contribute to changes in the QT interval. In these studies, domperidone monotherapy (10 mg four times daily) resulted in QT interval prolongation of 1.6 ms (ketoconazole study) and 2.5 ms (erythromycin study), whereas ketoconazole monotherapy (200 mg twice daily) and erythromycin monotherapy (500 mg three times daily) resulted in a prolongation of the QT interval by 3.8 and 4.9 ms, respectively, during the entire observation period. In another multiple-dose study in healthy volunteers, there was no significant prolongation of the QT interval during inpatient domperidone monotherapy (40 mg four times daily for a 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. Theoretically, since Motilium has a gastrokinetic effect, it could affect the absorption of concomitantly administered oral drugs, in particular sustained-release or enteric-coated drugs. However, the use of domperidone in patients taking paracetamol or digoxin did not affect the blood levels of these drugs. Motilium can be taken simultaneously with: - antipsychotics, the effect of which it does not enhance; - with dopaminergic receptor agonists (bromocriptine, levodopa), since it inhibits their unwanted peripheral effects, such as digestive disorders, nausea and vomiting, without affecting their central effects.
Side effects of Motilium
The drug increases the synthesis of the hormone prolactin. In some cases, this can cause a short-term disruption of the menstrual cycle and provoke the development of gynemastia. Occasionally during treatment the following are possible:
- decreased appetite;
- dryness or unpleasant taste in the mouth;
- increased drowsiness;
- increased spasms in the intestines.
If any undesirable symptoms occur, you should consult your doctor.
When is Motilium contraindicated?
It is prohibited to use the medicine:
- in case of danger of perforation of a gastric ulcer, development of internal bleeding;
- in case of intestinal obstruction;
- in case of dysfunction, neoplasms in the pituitary gland;
- prolactinoma;
- severe kidney or liver damage;
- individual intolerance to any of the components of the drug.
If you are allergic to Motilium, itching, hyperemia, rash, lacrimation, and swelling of the mucous membranes are likely to occur. In such cases, discontinuation of therapy and replacement of the drug with another is required.
How does Motilium interact with other drugs?
During the period of using Motilium, it is advisable to stop using antacids and proton pump inhibitors - drugs that reduce the acidity of gastric juice. Simultaneous use slows down the action of Motilium and reduces its absorption.
Antimycotic drugs and drugs from the macrolide group inhibit the metabolism of domperidone. This is important to consider in cases of impaired renal and liver function.
When undergoing treatment with Ketoconazole, Azithromycin, Erythromycin and inhibitors of the CYP3A4 isoenzyme, Motilium should be discontinued. Otherwise, the risk of heart failure increases.
Motilium, 1 piece, 100 ml, 1 mg/ml, oral suspension
Domperidone is rapidly absorbed after oral administration on an empty stomach, the maximum plasma concentration (Cmax) is reached within 30-60 minutes. The low absolute bioavailability of domperidone when taken orally (approximately 15%) is associated with extensive first-pass metabolism in the intestinal wall and liver. Despite the fact that the bioavailability of domperidone in healthy people increases when taking the drug after meals, patients with complaints from the gastrointestinal tract (GIT) should take domperidone 15-30 minutes before meals. A decrease in gastric acidity leads to a decrease in the absorption of domperidone. Oral bioavailability is reduced by prior administration of cimetidine and sodium bicarbonate. When taking the drug after a meal, it takes longer to achieve maximum absorption and the area under the active substance concentration-time curve (AUC) increases slightly.
When taken orally, domperidone does not accumulate and does not induce its own metabolism; the maximum plasma concentration of 21 ng/ml at 90 minutes after 2 weeks of oral administration of the drug at a dose of 30 mg per day was almost the same as the maximum plasma concentration of 18 ng/ml after taking the first dose. Domperidone is 91-93% bound to plasma proteins. Distribution studies in animals using a radiolabeled drug have shown significant tissue distribution but low concentrations in the brain. Small amounts of the drug cross the placenta in rats.
Domperidone undergoes rapid and extensive metabolism in the liver by hydroxylation and N-dealkylation. In vitro metabolism studies using diagnostic inhibitors have shown that CYP3A4 is the main form of cytochrome P450 involved in the N-dealkylation of domperidone, while CYP3A4, CYP1A2 and CYP2E1 are involved in the aromatic hydroxylation of domperidone. Excretion in urine and feces is 31% and 66% of the oral dose, respectively. The proportion of the drug excreted unchanged is small (10% in feces and approximately 1% in urine). The plasma half-life after a single oral dose is 7-9 hours in healthy people, but increases in patients with severe renal impairment. In such patients (serum creatinine level >6 mg/100 ml, i.e. >0.6 mmol/L), the half-life of domperidone increases from 7.4 to 20.8 hours, but plasma concentrations of the drug are lower than in people with normal kidney function. A small amount of unchanged drug (about 1%) is excreted by the kidneys.
In patients with moderate hepatic impairment (Pugh score 7-9, Child-Pugh class B), the AUC and Cmax of domperidone are 2.9 and 1.5 times higher than in healthy individuals, respectively. The unbound fraction increases by 25% and the terminal half-life increases from 15 to 23 hours. In patients with mild hepatic impairment, systemic exposure is slightly reduced compared to healthy controls based on Cmax and AUC values, with no change in protein binding or terminal half-life. No data are available for patients with severe hepatic impairment. Pharmacokinetic data for children are not available.
How can I replace Motilium?
The most famous analogues and generics of the drug:
- Domrid;
- Domidon;
- Domperidone Hexal;
- Motinorm;
- Motoricum;
- Motilak;
- Peridonium.
You should not change the medicine to an alternative one on your own. In addition to differences in dosage, some of them have a wider list of contraindications; not all are approved for use in pediatrics.
