Motilak

pharmachologic effect

The structure of the active component domperidone is similar to antipsychotics, and its effectiveness is comparable to metoclopramide . The active substance has virtually no effect on the severity of gastric secretion and is not capable of causing extrapyramidal disorders .

By increasing the contraction time of the walls of the duodenum and stomach, the medication has a positive effect on the motility of the gastrointestinal tract. The drug accelerates gastric emptying without retaining the bolus.

By increasing the tone of the gastroesophageal sphincter, an antiemetic effect is achieved.

Use during pregnancy and breastfeeding

When administered to animals in doses up to 160 mg/kg/day, it has no teratogenic effect. Use in the first trimester of pregnancy is possible if the expected effect of therapy exceeds the potential risk to the fetus. There is currently no evidence of an increased risk of developmental defects in humans. In women, concentrations of domperidone in breast milk are 4 times lower than the corresponding concentrations in plasma. It is unknown whether this level has a negative effect on newborns. Therefore, if the mother is taking Motilac, breastfeeding is not recommended unless the expected benefit justifies the potential risk.

Pharmacodynamics and pharmacokinetics

The active substance is rapidly absorbed after oral administration. Bioavailability about 15% (low). With reduced acidity of gastric juice, absorption of the active ingredient is reduced. Peak concentration is recorded after 60 minutes. The binding to plasma proteins is 93%.

The drug penetrates into all tissues of the body, a small concentration is also recorded in the brain. In the liver and intestinal walls, the drug undergoes intensive metabolism . The half-life is 7-9 hours.

Pharmacokinetics

Suction

After oral administration, it is quickly absorbed from the gastrointestinal tract. It has low bioavailability (about 15%). Reduced acidity of gastric contents reduces the absorption of domperidone. Cmax in plasma is reached after 1 hour.

Distribution

Domperidone is widely distributed in tissues; its concentration in brain tissue is low. Plasma protein binding is 91–93%.

Metabolism

Subject to intensive metabolism in the intestinal wall and liver.

Removal

Excreted through the intestines (66%) and kidneys (33%), unchanged, 10 and 1% of the dose, respectively. T1/2 - 7–9 hours (with severe renal failure it is prolonged).

Indications for use of Motilak

What is Motilak for? The medication is actively prescribed for:

• reflux esophagitis;
• belching;
• heartburn.

What domperidone can be prescribed for:

• increased gas formation;
• epigastric pain.

Indications for use in patients with Parkinson's disease : nausea while taking Levodopa and Bromocriptine .

Indications for the drug Motilak®

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;

- heartburn with or without reflux of stomach contents into the oral cavity.

Nausea and vomiting of functional, organic, infectious origin, 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 L-dopa and bromocriptine).

Instructions for use of Motilak (Method and dosage)

How to prescribe the medicine Motilak?

Instructions for use: daily dose – 30 mg; single dose – 10 mg. It is recommended to take the medication 30 minutes before meals. Lozenges must be kept in the mouth until completely dissolved; The coated tablets must not be broken, divided or chewed. In isolated cases, the daily amount of medication can be increased to 60 mg.

Children (weight 20-30 kg) are prescribed ½ tablet 2 times a day. If you weigh more than 30 kg, take 1 tablet twice a day.

Composition and release form

in a blister pack 10 pcs.; in a cardboard pack 1 or 3 packs.

in a blister pack 10 pcs.; in a cardboard pack 1 or 3 packs.

Motilak analogues (structural substitutes)

Level 4 ATX code matches:
Passazhix

Motinorm

Domrid

Motilium

Itomed

Metoclopramide

Domperidone

Ganaton

Cerucal

Motinorm , Motorix , Peridon , Motoricum . Analogues of Motilak are produced in Russia and abroad.

Side effects

Side effects are rare. Exceptional cases of transient intestinal cramps have been reported.

Extrapyramidal effects are rarely observed in children and are an exception in adults. These phenomena are completely reversible and disappear spontaneously after cessation of treatment.

Since the pituitary gland is located outside the BBB, Motilac can induce an increase in plasma prolactin levels. In rare cases, this hyperprolactinemia can stimulate the appearance of galactorrhea and gynecomastia.

Rare allergic reactions such as rash and hives have been reported.

Interaction

Anticholinergic drugs neutralize the effect, antacid and antisecretory drugs reduce bioavailability, inhibitors of the cytochrome P450 CYP3A4 isoenzyme (antifungals of the azole group, antibiotics of the macrolide group, HIV protease inhibitors, nefazodone) increase plasma levels. It is possible that concomitantly used drugs with sustained release of the active substance may have an effect on absorption. Domperidone does not affect the level of paracetamol and digoxin in the blood.

Directions for use and doses

Inside, 15–20 minutes before meals.

Adults in cases of acute nausea or vomiting: 20 mg 3-4 times a day and before bedtime.

For chronic dyspeptic symptoms: 10 mg (1 tablet) 3-4 times a day and, if necessary, before bedtime. If necessary, the indicated dose is doubled.

For patients with severe renal impairment, when re-prescribed, the frequency of administration should not exceed 1-2 times a day; it may be necessary to reduce the dose of the drug (depending on the severity of the deficiency).

Motilak

Motilak (pharmacologically active substance - domperidone) is an antiemetic drug, an antagonist of central dopamine receptors of the chemoreceptor trigger zone. It is used for various dyspeptic disorders associated with slower transport of gastric contents, gastroesophageal reflux, esophagitis, as well as nausea and vomiting of a wide variety of etiologies. In recent years, so-called prokinetics - drugs that stimulate the motility of the upper digestive tract - have become increasingly popular. This is due to the widespread prevalence of diseases associated with weakened tone and impaired peristalsis of the esophagus, stomach and duodenum. Drugs belonging to different pharmacological groups can stimulate the motility of the digestive tract, but in reality only dopamine receptor antagonists, including domperidone (Motilac), are used as prokinetics. This drug is used today in more than 60 countries around the world. The experience of using motilak is reflected in many articles and reviews. The surge in interest in the drug in recent years comes as the US Food and Drug Administration has approved its use to treat gastrointestinal diseases that are resistant to other drugs. The bioavailability of motilac is quite low and amounts to no more than 18%, which is explained by the severity of first-pass metabolism. The peak concentration of the active substance in the blood is observed after 30–60 minutes. The half-life of the drug is 7.5 hours (longer in patients with renal failure). The advantage of motilak over its “comrade” in the pharmacological group metoclopramide is the lack of the ability to penetrate the blood-brain barrier, thereby affecting the central nervous system. Unlike metoclopramide, which blocks both central and peripheral dopamine receptors, motilac affects mainly the receptors of the stomach and duodenum.

The drug increases the tone of the lower esophageal sphincter, enhances the ability of the stomach to contract and prevents atony, accelerates the transport of stomach contents. Without affecting the central nervous system, motilak nevertheless acts on the chemoreceptors of the trigger zone, thereby realizing its antiemetic effect. Motilak does not affect gastric secretion.

Motilak is available in two dosage forms: regular tablets and lozenges. For chronic dyspepsia, adults take 10 mg 3 times a day and, if indicated, additionally before bedtime. If the therapeutic response is weak, the dose is doubled. For children over 5 years of age, the dose is calculated based on the ratio of 2.5 mg for every 10 kg of body weight in 3 doses during the day and, if indicated, additionally before bedtime. For nausea, vomiting and other acute conditions, adults are recommended to take 20 mg 3-4 times a day and, as needed, before going to bed. For children over 5 years of age, the dose is calculated based on the ratio of 5 mg for every 10 kg of body weight for 3-4 doses during the day and, if the situation requires it, additionally before bedtime. If you combine Motilak with food, the absorption of the drug in the digestive tract will slow down somewhat. With long-term use of Motilac (for example, for the treatment of any chronic conditions), the optimal time to take the drug is 15-30 minutes before meals. Patients suffering from renal failure should take Motilak less often than usual - 1-2 times a day. Considering the fact that the metabolism of motilac takes place in the liver, the drug is prescribed to persons with liver failure with extreme caution. Patients with insufficient renal function do not require dose adjustment (only a small amount of the drug is excreted unchanged by the kidneys), however, with repeated drug courses, the frequency of dosing should also be reduced. Motilak is not combined with antacid or antisecretory drugs (they reduce the already low bioavailability of the drug).

Precautionary measures

Given the metabolism of domperidone in the liver, Motilak should be prescribed with caution to patients with liver failure.

In patients with severe renal failure (serum creatinine > 6 mg/100 ml, i.e. > 0.6 mmol/l), T1/2 of domperidone increased from 7.4 to 20.8 hours, but plasma concentrations of the drug were lower than in healthy volunteers. Since a very small percentage of the drug is excreted unchanged by the kidneys, single dose adjustment is unlikely to be necessary in patients with renal failure. However, when re-prescribed, the frequency of administration should be reduced to 1-2 times a day, depending on the severity of the deficiency, and it may also be necessary to reduce the dose. During long-term therapy, patients should be monitored regularly.