Motogastrik - Instructions For Use, Reviews, Price, Tablet Analogs

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

Motogastric

Motogastric: 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. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Motogastric

ATX code: A03FA03

Active ingredient: domperidone (Domperidone)

Manufacturer: JSC "ALSI Pharma" (Russia)

Description and photo update: 09.10.2019

Motogastric - antiemetic; central blocker of dopamine receptors.

Release form and composition

Dosage form - film-coated tablets: biconvex, round, shell color - white or almost white; the cross-section shows the inner layer of white or almost white color [in a contoured cell package made of varnished printed aluminum foil and PVC film (polyvinyl chloride) 10 tablets; in a cardboard box together with instructions for use Motogastric 1, 2, 3, 4 or 5 packs].

Composition of one film-coated tablet:

• active ingredient: domperidone - 10 mg;
• additional ingredients: MCC (microcrystalline cellulose) - 60 mg; pregelatinized starch - 19.46 mg; magnesium stearate - 0.45 mg; aerosil (colloidal silicon dioxide) - 0.09 mg;
• film shell: Opadray II (series 85) [polyvinyl alcohol - 1.44 mg; titanium dioxide - 0.9 mg; polyethylene glycol (macrogol) - 0.73 mg; talc - 0.53 mg] - 3.6 mg.

Pharmacological properties

Pharmacodynamics

The active substance of Motogastric, domperidone, is a selective antagonist of D ₂ -dopamine receptors, which has an antiemetic effect.

Domperidone stimulates the release of prolactin from the pituitary gland, while its use rarely causes the development of extrapyramidal side effects, especially in adults. Poorly penetrates the blood-brain barrier.

The antiemetic effect of Motogastric may be due to a combination of gastrokinetic (blocking peripheral dopamine D2 receptors) action and antagonism to dopamine receptors in the chemoreceptor trigger zone outside the blood-brain barrier.

The predominantly peripheral effect of domperidone on dopamine receptors has been confirmed by animal studies and low concentrations of the drug found in the brain.

When domperidone is taken orally, the duration of duodenal and antral contractions increases, gastric emptying is accelerated and the sphincter pressure of the lower esophagus increases. Motogastric has no effect on gastric secretion.

Pharmacokinetics

The main pharmacokinetic characteristics of domperidone:

• absorption: after oral administration on an empty stomach, it is rapidly absorbed, reaching a maximum concentration (C _max) in the blood plasma within 0.5-1 h. Due to intensive first-pass metabolism in the liver and intestinal wall, domperidone, when taken orally, has a low absolute bioavailability (~ 15%) … It is necessary to take the remedy 0.25-0.5 hours before meals; due to a decrease in acidity in the stomach, the absorption of domperidone worsens. Pre-intake of sodium bicarbonate and cimetidine reduces the bioavailability of domperidone. Food intake increases T _Cmax(time to reach the maximum concentration), while the AUC (area under the pharmacokinetic curve "concentration - time") also slightly increases. When taken orally, domperidone does not induce its own metabolism, it does not accumulate in the body. When using Motogastric for 14 days at a daily dose of 30 mg, C _max in blood plasma 1.5 hours after administration was 21 ng / ml and did not differ significantly from that after taking the first dose (18 ng / ml);
• distribution: the connection of domperidone with plasma proteins is 91-93%. Animal studies on the distribution of radioactively labeled domperidone have shown that the substance is widely distributed in tissues, but in the brain it is found in low concentrations. In rats, a small amount of domperidone crossed the placenta;
• metabolism: the fast and intense metabolism of domperidone occurs through hydroxylation and N-dealkylation. In studies of metabolism in vitro with diagnostic inhibitors, it was shown that the main form of cytochrome P ₄₅₀ involved in the N-dealkylation of domperidone is the isoenzyme CYP3A4, while the isoenzymes CYP2E1, CYP1A2 and CYP3A4 are responsible for aromatic hydroxylation of the substance;
• excretion: carried out with feces and urine and is, respectively, 66% and 31% of the dose taken orally. Only a small part is excreted unchanged: through the intestines - 10%, by the kidneys - about 1%. In healthy volunteers, T _1/2 (half-life) from plasma after a single oral administration is from 7 to 9 hours, in the presence of severe renal failure [serum creatinine> 6 mg / 100 ml (> 0.6 mmol / L)] may increase from 7.4 to 20.8 hours. At the same time, the concentration of domperidone in plasma in patients with severe renal failure is lower than in patients with normal renal function.

Pharmacokinetics of Motogastric in patients with impaired liver function:

• impaired hepatic function of mild severity: systemic concentrations of domperidone, determined on the basis of AUC and C _max, were slightly reduced compared with that in healthy volunteers; changes in the degree of binding to proteins or T _{1/2 were} not observed;
• impaired liver function of moderate severity (7-9 points on the Child-Pugh scale): C _max and AUC of domperidone were 1.5 and 2.9 times higher, respectively, than in healthy volunteers. The proportion of unbound fraction increased by 25%, and T _1/2 increased from 15 to 23 hours;
• severe hepatic dysfunction: the pharmacokinetics of domperidone have not been studied.

Indications for use

Taking Motogastric tablets is indicated in the following cases:

• the need to alleviate the symptoms of nausea and vomiting of various etiologies, which manifest themselves against the background of functional / organic diseases, various kinds of infections, toxinemia, radiation therapy, drug intoxication (morphine, apomorphine, levodopa, bromocriptine), as well as in case of dietary disorders;
• endoscopic and X-ray contrast studies of the gastrointestinal tract (GIT);
• gastrointestinal atony (including postoperative);
• hiccups;
• the need to accelerate peristalsis in the process of conducting X-ray contrast studies of the gastrointestinal tract;
• dyspepsia as a result of delayed gastric emptying, esophagitis, gastroesophageal reflux (feeling of fullness in the epigastrium, bloating, heartburn, flatulence, gastralgia, belching with / without reflux of gastric contents into the oral cavity).

Contraindications

Absolute:

• moderate and severe hepatic dysfunction;
• bleeding from the gastrointestinal tract, perforation of the stomach or intestines, mechanical intestinal obstruction;
• prolactinoma (prolactin-secreting pituitary tumor);
• impaired cardiac conduction, especially prolongation of the QTc interval, severe electrolyte disturbances or heart disease, for example, CHF (chronic heart failure);
• concomitant administration with drugs that prolong the QT interval, with the exception of apomorphine;
• simultaneous administration of oral forms of erythromycin, ketoconazole, as well as other strong inhibitors of the CYP3A4 isoenzyme - clarithromycin, itraconazole, fluconazole, posaconazole, voriconazole, ritonavir, saquinavir, amiodarone, telithromycin, telaprevir;
• body weight less than 35 kg;
• children under 12 years of age with a body weight of less than 35 kg;
• period of pregnancy;
• breast-feeding;
• glucose-galactose malabsorption, lactase deficiency, lactose intolerance;
• hypersensitivity to domperidone or any of the components that make up the drug.

Relative (Motogastric tablets should be taken with precautions):

• impaired renal function;
• children's age from 12 to 18 years;
• simultaneous administration of drugs causing hypokalemia and bradycardia, as well as roxithromycin and azithromycin;
• combined use with apomorphine.

Motogastric, instructions for use: method and dosage

Motogastric tablets are taken orally 0.25–0.5 hours before meals; if the drug is taken after meals, the absorption of domperidone may slow down.

The recommended dosage regimen of Motogastric: adults and children over 12 years old with a body weight of 35 kg or more - 10 mg (1 pc.) 3 times a day. The maximum daily dose is 30 mg (3 pcs.).

The course of treatment should not exceed 7 days.

Treatment of special patient groups:

• impaired renal function: depending on the severity of renal failure, the frequency of taking Motogastric is recommended to be reduced to 1 or 2 times a day (in patients with severe renal impairment, T _{1/2 of} domperidone increases). Such patients are indicated for regular examination;
• hepatic impairment: patients with moderate (7–9 points according to the Child-Pugh classification) or severe (≥ 9 points according to the Child-Pugh classification) hepatic impairment use domperidone is contraindicated. In case of mild impairment (5-6 points according to the Child-Pugh classification), the dose of Motogastric does not need to be adjusted.

For pediatric patients, domperidone is preferably administered as a suspension.

Side effects

The incidence of adverse reactions is classified according to the recommendations of the WHO (World Health Organization): very often - more than 1/10; often less than 1/100 and more than 1/10; infrequently - less than 1/1000 and more than 1/100; rarely - less than 1/10 000 and more than 1/1000; very rarely - less than 1/10 000; with an unknown frequency - the frequency of occurrence cannot be determined from the available information.

According to data obtained in the course of clinical studies, the following side effects were recorded while taking Motogastric:

• digestive system: often - diarrhea, dry mouth;
• nervous system: often - drowsiness, headache;
• psyche: often - asthenia, akathisia, anxiety, depression;
• genitals and mammary glands: often - decreased / lack of libido, pain and sensitivity in the area of the mammary glands, gynecomastia, galactorrhea, impaired lactation, menstrual irregularities and amenorrhea; infrequently - swelling and discharge from the mammary glands;
• skin and subcutaneous tissues: often - itching, rash; infrequently - urticaria, hypersensitivity.

Disturbances from systems and organs according to spontaneous reports of adverse reactions:

• nervous system: very rarely - extrapyramidal disorders, dizziness, convulsions;
• psyche: very rarely - increased excitability (agitation), irritability, nervousness;
• cardiovascular system: with unknown frequency - pirouette-type ventricular tachycardia (TdP - Torsades de pointes), ventricular arrhythmia *, sudden coronary death *;
• immune system: very rarely - anaphylactic reactions, including anaphylactic shock;
• skin and subcutaneous tissues: very rarely - Quincke's edema (angioedema), urticaria;
• kidneys and urinary tract: very rarely - urinary retention;
• laboratory and instrumental studies: very rarely - an increase in the concentration of prolactin in the blood, deviations of laboratory parameters of liver function.

* Some epidemiological studies have shown that domperidone may increase the risk of severe ventricular arrhythmias or sudden death. The risk of these pathologies is more likely in elderly patients (over 60 years old) and in patients taking Motogastric in a daily dose of over 30 mg. The use of the drug in the lowest effective dose in adults and children is recommended.

Overdose

With an overdose of domperidone, drowsiness, hyperexcitability, convulsions, disorientation and extrapyramidal reactions are possible (observed mainly in children).

If an overdose of Motogastric is suspected, symptomatic treatment is performed. Prescribe gastric lavage, intake of activated carbon, in the event of extrapyramidal reactions - anticholinergic, antiparkinsonian drugs. Due to the risk of a possible increase in the QT interval, ECG (electrocardiogram) monitoring is necessary. There is no specific antidote.

special instructions

If, against the background of Motogastric therapy, it becomes necessary to take antacids or antisecretory agents, the latter should be taken after meals, and not before meals, avoiding their simultaneous intake with domperidone.

There is no need to adjust a single dose in patients with renal insufficiency, since only a small percentage of domperidone is excreted unchanged in the urine. However, when re-taking Motogastric, the frequency of use should be reduced to 1–2 times a day (depending on the severity of renal dysfunction), in addition, it may be necessary to reduce the dose. Patients on long-term therapy with domperidone should be monitored regularly.

When taking Motogastric, the QT interval on the ECG may be lengthened. In post-registration studies conducted in patients taking domperidone, rare cases of polymorphic ventricular tachycardia of the "pirouette" type and an increase in the QT interval were recorded. These adverse events were predominantly observed in patients with risk factors, severe electrolyte disturbances, or concurrently taking medications that increase the QT interval.

Joint administration of Motogastric with drugs that prolong the QT interval (except for apomorphine) is contraindicated.

Combined use with apomorphine is possible only if the benefits of such a combination significantly outweigh the risk, and only with strict adherence to the recommended precautions for joint therapy with drugs listed in the instructions for medical use of apomorphine.

Some studies have shown that the use of domperidone may increase the risk of severe ventricular arrhythmias / sudden coronary death. The risk is especially high in patients who are simultaneously taking inhibitors of the isoenzyme CYP3A4 or drugs that increase the QT interval, in elderly patients (over 60 years old), and also in those taking domperidone in daily doses of more than 30 mg.

Both adults and pediatric patients (over 12 years old) are recommended to use Motogastric in the lowest effective dose.

If signs or symptoms appear associated with cardiac arrhythmias, drug therapy should be interrupted and immediately seek medical advice.

Patients should immediately report any cardiac problems to their doctor.

In rare cases, taking Motogastric can cause neurological adverse reactions. The risk of such manifestations in young children is higher, since the blood-brain barrier and metabolic functions are not fully developed in the first months of life. For this reason, it is important to strictly adhere to the recommended dose. Neurological adverse reactions can develop in children against the background of an overdose of the drug, but other possible causes of their occurrence must be taken into account.

Influence on the ability to drive vehicles and complex mechanisms

Due to the risk of adverse reactions, such as drowsiness and dizziness, patients taking Motogastrik should be careful when driving and engaging in other potentially hazardous activities that require a high concentration of attention and speed of psychomotor reactions.

Application during pregnancy and lactation

For pregnant and breastfeeding women, drug therapy is contraindicated.

Pediatric use

Children under 12 years old with a body weight of less than 35 kg Motogastric is not prescribed.

Adolescents aged 12 to 18 years should be careful when taking this medicine.

With impaired renal function

Renal dysfunction is a relative contraindication to taking Motogastric (caution should be exercised during therapy).

For violations of liver function

The drug is contraindicated in moderate and severe hepatic dysfunction.

Use in the elderly

Elderly patients (over 60 years) should be aware that domperidone may increase their risk of developing serious ventricular arrhythmias or sudden death.

Drug interactions

Possible interactions of domperidone with drugs / substances used simultaneously:

• anticholinergic drugs: can neutralize the effect of domperidone;
• sodium bicarbonate, cimetidine (with the previous administration): reduce the oral bioavailability of domperidone;
• antacid and antisecretory drugs: reduce the bioavailability of domperidone;
• levodopa: it is possible to increase the concentration of levodopa in blood plasma (30-40%); dose adjustment is not required.

Combinations that increase the risk of QTc interval prolongation

Contraindicated combinations:

• established drugs that prolong the QTc interval: antipsychotics (pimozide, haloperidol, sertindole), antidepressants (escitalopram, citalopram), gastrointestinal drugs (dolasetron, cisapride, prucaloprid), antibiotics (moxifloxacin, antibiotics, spiramistin mizolastine, mechitazine), antimalarials (lumefantrine, halofantrine), antifungal agents (pentamidine), antineoplastic drugs (vandetanib, toremifene, vincamine), class IA antiarrhythmics (quinidine, disopyramide), dopamine class III antiarrhythmics (dodarone), sotalol, ibutilide), some other drugs (diphemanil methyl sulfate, bepridil, methadone);
• strong inhibitors of the isoenzyme CYP3A4: macrolide antibiotics (erythromycin, clarithromycin, telithromycin), azole antifungal drugs (itraconazole, fluconazole, ketoconazole, posaconazole, voriconazole). According to the results of in vitro studies and accumulated clinical experience of use, since the metabolism of domperidone is mainly carried out through the isoenzyme CYP3A4, concomitant therapy with drugs that significantly inhibit this isoenzyme may be accompanied by an increase in plasma concentrations of domperidone.

Simultaneous administration of domperidone 4 times / day at 10 mg and erythromycin 3 times / day at 500 mg led to an extension of the QTc interval by an average of 9.9 ms throughout the observation period, at some moments the changes varied from 1.6 to 14.3 ms.

Simultaneous administration of domperidone 4 times / day, 10 mg and ketoconazole 2 times / day, 200 mg led to an extension of the QTc interval by an average of 9.8 ms throughout the observation period, at some moments the changes varied from 1.2 to 17.5 ms.

In each of these studies, the AUC and C _{max of} domperidone increased approximately 3-fold. In addition, monotherapy with domperidone 4 times / day at 10 mg led to an increase in the mean QTc interval of 2.5 ms (study of erythromycin) and 1.6 ms (study of ketoconazole), while monotherapy with erythromycin 3 times / day at 500 mg and monotherapy with ketoconazole 2 times / day at 200 mg led to an increase in the QTc interval of 4.9 and 3.8 ms, respectively, during the observation period.

Combinations not recommended:

• some antibiotics from the macrolide group (erythromycin, clarithromycin, telithromycin);
• calcium antagonists (verapamil and diltiazem).

Combinations to be used with caution:

• drugs that cause bradycardia and hypokalemia;
• some antibiotics of the macrolide group (roxithromycin, azithromycin);
• apomorphine *.

* Domperidone is contraindicated when taken together with drugs that prolong the QT interval, with the exception of apomorphine. Therapy with domperidone in combination with apomorphine is possible, provided that its benefits exceed the risks and with strict adherence to the recommended precautions for joint use of drugs.

Analogs

Motogastric analogs are Domet, Domperidone, Domperidon-Teva, Domridon, Domstal, Motijekt, Motilak, Motilium, Motilium Express, Motinorm, Motonium, Passages, etc.

Terms and conditions of storage

Keep out of the reach of children.

Store in its original packaging at a temperature not exceeding 25 ° C.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Motogastrika

Currently, there are isolated reviews of Motogastrik, which do not allow a reasonable assessment of the safety and effectiveness of its use. Most often, patients note that the drug has the declared clinical effect. A case of using the drug after chemotherapy is described; as a result of treatment, severe attacks of nausea were stopped. Concomitant diarrhea may have been a reaction to Motogastric and may be due to chemotherapy.

The price of Motogastric in pharmacies

Prices for Motogastric, film-coated tablets, 10 mg, in the pharmacy chain vary between 135-162 rubles. for a package containing 10 pcs., and 175-250 rubles. per package containing 30 pcs.

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!