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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.

Animal studies and low concentrations of the drug found in the brain indicate a central effect of domperidone on dopamine receptors.

When administered orally, domperidone increases the duration of antral and duodenal contractions, accelerates gastric emptying and increases lower esophageal sphincter pressure in healthy people. Domperidone has no effect on gastric secretion.

Motilium Express lozenges 10 mg 30 pcs

pharmachologic effect

Antiemetic, dopamine receptor blocker central
ATC:

A.03.FA03 Domperidone

Pharmacodynamics:

Domperidone is a dopamine antagonist with antiemetic properties. However, domperidone does not penetrate the blood-brain barrier well. 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 of dopamine receptors in the chemoreceptor trigger zone. Animal studies and low concentrations of the drug found in the brain indicate a central effect of domperidone on dopamine receptors.

Pharmacokinetics:

Domperidone is rapidly absorbed after oral administration on an empty stomach, with peak plasma concentrations achieved within 30-60 minutes. The low absolute bioavailability of domperidone when taken orally (approximately 15%) is associated with intensive first-pass metabolism in the intestinal wall and liver.

Domperidone should be taken 15-30 minutes before meals. Reduced acidity in the stomach leads to impaired 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 pharmacokinetic curve (AUC) increases slightly.

When taken orally, domperidone does not accumulate and does not induce its own metabolism; the peak plasma concentration of 21 ng/mL at 90 minutes after 2 weeks of oral dosing at a dose of 30 mg per day was essentially the same as the peak plasma concentration of 18 ng/mL after the first dose. Domperidone is 91-93% bound to plasma proteins. Distribution studies with radiolabeled drug in animals showed significant drug distribution in tissues but low concentrations in the brain. Small amounts of the drug cross the placenta in rats.

Domperidone undergoes rapid and extensive metabolism by hydroxylation and N-dealkylation. In vitro metabolism studies with diagnostic inhibitors have shown that CYP3A4 is the major cytochrome P450 form 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 volunteers, but is increased in patients with severe renal impairment.

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 plasma concentrations of the drug are lower than in healthy volunteers . 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 B), the AUC and maximum plasma concentration (Cmax) of domperidone were 2.9 and 1.5 times higher than in healthy subjects volunteers accordingly. The unbound fraction increased by 25% and the half-life increased from 15 to 23 hours. In patients with mild hepatic impairment, slightly reduced systemic drug levels were observed compared with those in healthy volunteers based on Cmax and AUC, without changes in protein binding or half-life. Patients with severe hepatic impairment have not been studied.

Indications

a) A complex of dyspeptic symptoms, often associated with delayed gastric emptying, gastroesophageal: reflux, esophagitis:

- feeling of fullness in the epigastrium, feeling of bloating, pain in the upper abdomen;

- belching, flatulence;

- nausea, vomiting;

- heartburn, belching.

b) Nausea and vomiting of functional, organic, infectious origin, as well as caused by radiotherapy, drug therapy or diet disorders. A specific indication is nausea and vomiting caused by dopamine agonists when used in Parkinson's disease (such as levodopa and bromocriptine).

Contraindications

- established intolerance to the drug and its components;

- prolactin-secreting tumor of the pituitary gland (prolactinoma);

- simultaneous use of oral forms of ketoconazole, erythromycin or other potent inhibitors of the CYP3A4 isoenzyme that cause prolongation of the QT interval, such as fluconazole, voriconazole, clarithromycin, amiodarone and telithromycin (see section “Interactions”);

- gastrointestinal bleeding, mechanical obstruction or perforation (i.e. when stimulation of the motor function of the stomach can be dangerous);

- children under 5 years of age (for this dosage form);

- moderate to severe liver dysfunction;

- phenylketonuria.

Carefully:

- renal dysfunction;

- disturbances of cardiac rhythm and conduction, including prolongation of the QT interval, electrolyte imbalance, congestive heart failure.

Use during pregnancy and breastfeeding

Use during pregnancy

There is insufficient data on the use of domperidone during pregnancy. To date, there is no evidence of an increased risk of developmental defects in humans. However, Motilium® should be prescribed during pregnancy only if its use is justified by the expected therapeutic benefit.

Use during lactation

In women, the concentration of domperidone in breast milk ranges from 10 to 50% of the corresponding plasma concentration and does not exceed 10 ng/ml. The total amount of domperidone excreted into breast milk is less than 7 mcg per day when using the maximum allowable dose of domperidone. It is unknown whether this level has a negative effect on newborns. In this regard, when using the drug Motilium® during lactation, breastfeeding should be stopped.

special instructions

When using 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 Motilium®.

Use in children

Motilium® may in rare cases cause neurological side effects (see section "Side Effects"). The risk of neurological side effects is higher in young children because metabolic functions and the blood-brain barrier are not fully developed in the first months of life. In this regard, you should strictly adhere to the recommended dose (see section “Method of administration and dosage”). Neurological adverse effects can be caused by overdose of the drug in children, but other possible causes of such effects must be taken into account.

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 Motilium®, the frequency of use should be reduced to one or two 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 domperidone may be associated with an increased risk of serious ventricular arrhythmias or sudden death (see Adverse Effects section). 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. It is recommended to use domperidone in the lowest effective dose in adults and children.

If the medicine has become unusable or has expired, do not throw it into wastewater or onto the street! Place the medication in a bag and place it in the trash. These measures will help protect the environment!

Impact on the ability to drive vehicles. Wed and fur.:

Motilium® has no or negligible effects on the ability to drive a car and operate machinery.

Compound

Active substance (per 1 tablet): domperidone 10 mg.

Excipients (per 1 tablet): gelatin 5.513 mg, mannitol 4.136 mg, aspartame 0.750 mg, mint essence 0.300 mg, poloxamer 188 1.125 mg.

Directions for use and doses

Inside. It is recommended to take Motilium® tablets before meals; if taken after meals, the absorption of domperidone may slow down. The duration of continuous use of the drug without a doctor’s recommendation should not exceed 28 days.

Adults and children over 12 years of age and weighing 35 kg or more:

1-2 tablets of 10 mg 3-4 times a day. The maximum daily dose is 8 tablets (80 mg).

Children aged 5 to 12 years and weighing 35 kg or more:

1 tablet of 10 mg 3-4 times a day. The maximum daily dose of domperidone is no more than 8 tablets (80 mg).

Use in children Motilium® lozenges are indicated only for children weighing 35 kg or more; in pediatric practice, the Motilium® suspension should mainly be used. Use in patients with impaired renal function The frequency of taking Motilium® should be reduced to 1-2 times a day, depending on the severity of the impairment, a dose reduction may also be required. Such patients should be regularly examined (see section "Special instructions").

Use in patients with liver dysfunction

Do not use Motilium® if you have moderate or severe liver dysfunction. For mild liver dysfunction, no dose adjustment is required.

DIRECTIONS FOR USE

Since lozenges are quite fragile, they should not be pressed through the foil to avoid damage. In order to remove a tablet from the blister, you need the following:

- take the foil by the edge and completely remove it from the cell in which the tablet is located;

- press gently 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 and can be swallowed with saliva without washing it down with water.

Side effects

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 mammary glands, menstrual irregularities and amenorrhea, lactation disorders, asthenia.

Adverse reactions observed in <1% of patients taking Motilium®: hypersensitivity, urticaria, swelling and discharge from the mammary glands.

According to spontaneous reports of adverse events

The following undesirable effects were classified as follows: very common (≥ 10%), common (≥ 1% but < 10%), uncommon (≥ 0.1% but < 1%), rare (≥ 0.01%, But

Immune system disorders. Very rare: anaphylactic reactions, including anaphylactic shock.

Mental disorders. Very rare: agitation, nervousness (mainly in newborns and children).

Nervous system disorders. Very rare: extrapyramidal disorders, seizures (mainly in newborns and children).

Disorders of the cardiovascular system. Very rare: QT prolongation, ventricular arrhythmia*, sudden coronary death*.

Disorders of the skin and subcutaneous tissues. Very rare: Quincke's edema, urticaria.

Renal and urinary tract disorders. Very rare: urinary retention.

Laboratory and instrumental data. Very rare: abnormalities in laboratory tests of liver function, increased blood prolactin levels.

*Some epidemiological studies have suggested that domperidone 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.

Drug interactions

Anticholinergic drugs may neutralize 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 (see section "Special Instructions").

— 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 [see Contraindications section]).

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 (see section "Contraindications").

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 influence 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:

- neuroleptics, 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.

Overdose

Symptoms

Symptoms of overdose occur most often in infants and children and may include: agitation, altered consciousness, seizures, confusion, somnolence and extrapyramidal disturbances.

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. Anticholinergics and antiparkinsonian drugs can be used to correct extrapyramidal manifestations.

Storage conditions

Store in a dry place at a temperature not exceeding 25 °C.

Keep out of the reach of children. Store in original packaging.

Best before date

2 years. Do not use after expiration date.

Conditions for dispensing from pharmacies Dispensed with a doctor's prescription

Possible product names

Motilium express lozenges 10 mg 30 pcs.

Indications for use

a complex of dyspeptic symptoms, often associated with delayed gastric emptying, gastroesophageal reflux, esophagitis (a feeling of fullness in the epigastrium, a feeling of bloating, pain in the upper abdomen, belching, flatulence, nausea, vomiting, heartburn);
nausea and vomiting of functional, organic, infectious origin, as well as caused by drug therapy or diet disorders;
nausea and vomiting caused by dopamine agonists when used in Parkinson's disease (such as levodopa and bromocriptine).

Directions for use and doses

Inside. Since lozenges are quite fragile, they should not be pressed through the foil to avoid damage. In order to remove a tablet from the blister, you need the following:

take the foil by the edge and completely remove it from the cell in which the tablet is located
press gently 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 and can be swallowed with saliva without washing it down with water.

It is recommended to take Motilium tablets before meals; if taken after meals, the absorption of domperidone may slow down. The duration of continuous use of the drug without a doctor’s recommendation should not exceed 28 days.

Adults and children over 12 years old and weighing 35 kg or more: 1-2 tablets of 10 mg 3-4 times a day. The maximum daily dose is 8 tablets (80 mg).

Children aged 5 to 12 years and weighing 35 kg or more: 1 tablet of 10 mg 3-4 times a day. The maximum daily dose of domperidone is no more than 8 tablets (80 mg).

Use in children Motilium lozenges are indicated only for children weighing 35 kg or more; in pediatric practice, Motilium suspension should mainly be used.

Motilium®Express

— 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 [see Contraindications section]).

It is currently unknown how elevated plasma concentrations of domperidone contribute to changes in the QT interval.

Motilium® can be taken simultaneously with:

- neuroleptics, the effect of which it does not enhance;

Contraindications

prolactin-secreting tumor of the pituitary gland (prolactinoma);
simultaneous use of oral forms of ketoconazole, erythromycin or other potent inhibitors of the CYP3A4 isoenzyme that cause prolongation of the QT interval, such as fluconazole, voriconazole, clarithromycin, amiodarone and telithromycin;
gastrointestinal bleeding, mechanical obstruction or perforation (when stimulation of gastric motility may be dangerous);
moderate to severe liver dysfunction;
phenylketonuria;
children under 5 years of age (for this dosage form);
hypersensitivity to the components of the drug.

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, that is, they should not be taken simultaneously with the drug Motilium.

During long-term therapy, patients should be monitored regularly.

Motilium may in rare cases cause neurological side effects. In this regard, you should strictly adhere to the recommended dose. Neurological adverse effects can be caused by overdose of the drug in children, but other possible causes of such effects must be taken into account.

Motilium

Anticholinergic drugs may neutralize the effect 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 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. 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; Telithromycin. (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 orally administered 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 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.