Motilac, 10 mg 30 pcs.

Motilac is an antiemetic.

Prokinetic. It increases duration of peristaltic contractions of the antral part of the stomach and duodenum, improves stomach function by accelerating its emptying if this process is slowed down, increases tone of the lower esophageal sphincter, eliminates development of nausea and vomiting.

Domperidone poorly penetrates through the GEB, so the use of domperidone is rarely accompanied by extrapyramidal side effects, especially in adults, but domperidone stimulates prolactin release from the pituitary gland. Its antiemetic effect is probably due to a combination of peripheral (gastrokinetic) action and antagonism to dopamine receptors in the chemoreceptor trigger zone. Domperidone has no effect on gastric secretion.

Pharmacokinetics

Absorption

After oral administration it is rapidly absorbed from the GI tract. It has low bioavailability (about 15%). Decreased acidity of gastric contents decreases absorption of domperidone.C_max in plasma is reached after 1 hour.

Distribution

Domperidone is widely distributed in tissues, its concentration is low in brain tissues. Binding to plasma proteins is 91-93%.

Metabolism

It is subjected to intensive metabolism in the intestinal wall and the liver.

Extracted

Extracted through the intestine (66%) and the kidneys (33%), unchanged, respectively, 10 and 1% of the dose value. T_1/2 is 7-9 h (in severe renal failure it is prolonged).

Indications

The complex of dyspeptic symptoms, often associated with delayed gastric emptying, gastroesophageal reflux, esophagitis;

Nausea and vomiting of functional, organic, infectious origin, caused by radiotherapy, drug therapy or dietary disorder.

A specific indication is nausea and vomiting caused by dopamine agonists when used in Parkinson’s disease (such as L-dopa and bromocriptine).

Active ingredient

Composition

1 tablet contains:

Active substance:

domperidone 10 mg;

Supplementary substances:

Potato starch;

Lactose;

MCC;

How to take, the dosage

Overly, 15-20 minutes before a meal.

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

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

In patients with significant renal dysfunction, when repeated administration, the number of times a day should not exceed 1 to 2; the drug dose may need to be decreased (depending on the severity of the failure).

Interaction

Anticholinergic drugs neutralize the effect, antacids and antisecretory drugs decrease bioavailability, cytochrome P450 CYP3A4 isoenzyme inhibitors (azole antifungal drugs, macrolide antibiotics, HIV protease inhibitors, nefazodone) increase plasma levels.

The effect on absorption of concomitantly used drugs with delayed release of the active substance is not excluded.

Domperidone does not affect the blood levels of paracetamol and digoxin.

Special Instructions

When Motilac is used in combination with antacids or antisecretory drugs, the latter should be taken after meals, not before meals, i.e. they should not be taken simultaneously with Motilac.

Contraindications

Motilac is contraindicated in patients with a known intolerance to the drug.

Motilac should not be used when stimulation of gastric motility may be dangerous, i.e. in cases of gastrointestinal bleeding, mechanical obstruction or perforation.

Motilac is also contraindicated in patients with a prolactin-secreting pituitary tumor (prolactinoma).

Side effects

Side effects are rare. There have been exceptional cases of transient intestinal spasms.

Extrapyramidal phenomena are rarely seen in children and are the exception in adults. These phenomena are completely reversible and disappear spontaneously after discontinuation of treatment.

Since the pituitary gland is outside the BBB, Motilac may induce elevated plasma prolactin levels. In rare cases, this hyperprolactinemia may stimulate the appearance of galactorrhea and gynecomastia.

Rare allergic reactions such as rash and urticaria have been noted.

Overdose

Symptoms: drowsiness, disorientation, extrapyramidal reactions (mainly in children).

Treatment: In case of overdose, activated charcoal and close monitoring is recommended. Anticholinergic agents, drugs used to treat parkinsonism, or antihistamines may be effective if extrapyramidal reactions occur.

Pregnancy use

When administered to animals in doses up to 160 mg/kg/day there is no teratogenic effect.

The use in the first trimester of pregnancy is possible if the expected effect of therapy exceeds the potential risk to the fetus. There are currently no data on increased risk of malformations in humans.

In women, concentrations of domperidone in breast milk are 4 times lower than the corresponding concentrations in plasma. It is not known whether this level has an adverse effect on newborns.

Hence, if the mother is taking Motilac, breastfeeding is not recommended unless the expected benefit justifies the potential risk.

Similarities