Domperidone (emetrol)

Feb 19, 2020

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Domperidone (emetrol)

Pharmacological action
An antagonist of central action dopamine receptors. Unlike methoklopramid, domperidone does not penetrate well through GHB. It blocks to a greater extent peripheral and to a lesser extent central (in the trigger zone of the vomiting center) dopamine receptors. Eliminates the inhibitory effect of dopamine on gastrointestinal motor function and increases the evacuation and motor activity of the stomach.

It has antiemetic effect, calms hiccups and eliminates nausea. It has no effect on the stomach secretion.

Increases the concentration of prolactin in blood serum.

Pharmacokinetics

After ingestion on an empty stomach Domperidone, absorption is fast. After a meal, the reduced acidity of gastric juice slows down and reduces absorption. Time to reach Cmax is 1 hour. Bioavailability – 15% due to the effect of “first pass” through the liver.

Distribution

Binding to plasma proteins is 90%. Penetrates into various tissues, badly passes through GB.

Doesn’t cumulate.

Metabolism

It is metabolized in liver and intestinal wall by hydroxylation and N-dezalkylation with participation of isoenzymes of cytochrome P450 system. It does not induce own metabolism.

Breeding .

T1/2 – 7-9 hours. It is excreted through the intestine – 66%, by kidneys – 33%, including 10% and 1% in unchanged form, respectively.

Pharmacokinetics in special clinical cases

In severe chronic renal failure, T1/2 elongates.

Readings

Domperidone (emetrol) - healthy

Nausea and vomiting of various genesis (including against the background of functional and organic diseases, infection, in toxaemia, radiation therapy, diet disorders, drug genesis – taking morphine, apomorphine, levodopa and bromocriptine; in endoscopic and X-ray gastrointestinal examination);
hiccups;
gastrointestinal atony (including postoperative);
necessity to speed up peristalsis during gastrointestinal x-ray examination;
dyspeptic symptoms against the background of delayed gastric emptying, gastroesophageal reflux and esophagitis: a feeling of overflow in epigastria, a feeling of bloating, flatulence, gastralgia, heartburn, burping with or without throwing the gastric content into the mouth.
Dosing mode
The drug is taken inside 15-20 minutes before meals Domperidone dosage

Adults and children over 5 years of age with chronic dyspeptic symptoms – 10 mg 3-4 times / day, including before bed if necessary.

In case of severe nausea and vomiting – 20 mg 3-4 times / day, the last meal – before bed.

The maximum daily dose is 80 mg.

For patients with renal insufficiency correction of the dose is necessary, the frequency of intake should not exceed 1-2 times/day.

Side effect

Digestive system: gastrointestinal disorders (transient bowel cramps).

Nervous system: extrapyramidal disorders (in children in persons with increased permeability of GBS, in adults – isolated cases). These phenomena are completely reversible and disappear after you stop taking the drug.

Allergic reactions: skin rash, hives.

Others: hyperprolactinemia (galactorrhea, gynecomastia, amenorrhea).

Domperidone (emetrol) - healthy

Contraindications for use
gastrointestinal bleeding;
mechanical intestinal obstruction;
stomach or intestine perforation;
prolactinoma;
lactation period;
childhood age under 5 years;
children with body weight up to 20 kg;
hypersensitivity to the drug components.
The preparation should be used with caution in case of marked renal and/or hepatic failure.

Application in pregnancy and lactation
There is not enough data on the use of domperidone in pregnancy. To date, there is no evidence of increased risk of malformations in humans. However, domperidone should only be prescribed during pregnancy when the expected therapeutic benefits to the mother exceed the potential risk to the fetus.

Domperidone (emetrol) - healthy

In women, the concentration of domperidone in breast milk ranges from 10% to 50% of the corresponding concentration in plasma and does not exceed 10 ng/ml. The total amount of domperidone excreted with breast milk is less than 7 µg/day when domperidone is used in the maximum doses allowed. It is not known whether domperidone in this concentration has adverse effects on infants. Therefore, when using domperidone during lactation, breastfeeding should be stopped.

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