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Domperidone

When taken on an empty stomach, domperidone is rapidly absorbed after oral administration, 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 level 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 level 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 showed that the CYP3A4 isoenzyme is the main form of cytochrome P450 involved in the N-dealkylation of domperidone, while the CYP3A4, CYP1A2 and CYP2E1 isoenzymes are involved in the aromatic hydroxylation of domperidone.

Excretion through the kidneys and through the intestines is 31% and 66% of the oral dose, respectively. The proportion of the drug excreted unchanged is small (10% through the intestines and approximately 1% through the kidneys). 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 (Child-Pugh B score 7-9), the AUC and Cmax of domperidone were 2.9 and 1.5 times higher than in healthy volunteers, respectively. The unbound fraction increased by 25% and the half-life increased from 15 to 23 hours. In patients with mild hepatic impairment, systemic exposure is lower than in healthy patients. Pharmacokinetics have not been studied in patients with severe hepatic impairment.

Pharmacological properties of the drug Domperidone

Dopamine receptor antagonist, prokinetic. Practically does not penetrate the BBB. Increases the duration of peristaltic contractions of the antrum of the stomach and duodenum, accelerates gastric emptying, and increases the tone of the lower esophageal sphincter. Does not affect gastric secretion. It has an antiemetic effect due to a combination of gastrokinetic effect and antagonism to dopamine receptors in the chemoreceptor trigger zone, which is located outside the BBB. After oral administration, it is quickly absorbed. It is subjected to intensive metabolism in the intestinal wall and liver, and has low bioavailability (about 15%). The maximum concentration in blood plasma is achieved 1 hour after administration. Reduced gastric acidity reduces the absorption of domperidone. Binds to plasma proteins by 91–93%. Excreted in feces (66%) and urine (33%). The half-life is 7–9 hours, and in cases of severe renal failure it is prolonged.

Domperidone

Domperidone

(lat.
domperidonum
, English
domperidone
) - a drug for the treatment of functional intestinal disorders, prokinetic, antiemetic.
Chemical compound
: 5-chloro-1-[1-[3-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)propyl]-4-piperidinyl]-1,3-dihydro-2H- benzimidazole-2-OH.
Empirical formula: C22H24Cl N5O2. Domperidone is the international nonproprietary name (INN) of the drug.
According to the pharmacological index, it belongs to the group “Gastrointestinal motility stimulants, including emetics.” According to ATC, it belongs to the group “Gastrointestinal motility stimulants” and has code A03FA03. Domperidone blocks dopamine D2 receptors and thus eliminates dopamine inhibition of the motor activity of the digestive system. Increases the duration of gastric antrum and duodenal peristalsis, prevents slow gastric emptying, and increases the tone of the lower esophageal sphincter. The antiemetic effect of domperidone is due to a combination of gastrokinetic action and blockade of chemoreceptors of the trigger zone of the vomiting center. Domperidone prevents the development or reduces the severity of vomiting and nausea.

The mechanism of the prokinetic action of domperidone (Maev I.V. et al.)

Domperidone increases the level of prolactin in the blood.
After oral administration, domperidone is rapidly absorbed from the gastrointestinal tract. Food or low acidity of gastric juice slows down and reduces absorption. The maximum concentration of domperidone in the blood is reached after 0.5–1 hour. Found in small quantities in breast milk. It is subjected to intensive metabolism in the intestinal wall and liver (by hydroxylation and N-dealkylation) with the formation of hydroxydomperidone and 2,3-dihydro-2-oxo-1-H-benzimidazole-1-propionic acid, respectively. The half-life after a single dose is 7 hours and increases in chronic renal failure. 31% is excreted by the kidneys, of which 1% is excreted unchanged and 66% is excreted by the intestines (10% unchanged). Domperidone may accumulate in patients with liver disease.

Domperidone belongs to the second generation gastrokinetics and, unlike metoclopramide (trade names Cerucal , Reglan

etc.), does not penetrate the blood-brain barrier (BBB) and does not cause extrapyramidal disorders characteristic of metoclopramide: spasm of the facial muscles, trismus, rhythmic protrusion of the tongue, bulbar type of speech, spasm of the extraocular muscles, spasmodic torticollis, opisthotonus, muscle hypertonicity, etc. . Also, unlike metoclopramide, domperidone does not cause parkinsonism: hyperkinesis, muscle rigidity. When taking domperidone, side effects of metoclopramide such as drowsiness, fatigue, tiredness, weakness, headaches, increased anxiety, confusion, and tinnitus are less common and less pronounced.

Also, while inferior in terms of its effect on gastrointestinal motility to the more effective prokinetic agent cisapride, domperidone does not have its serious side effects (ventricular arrhythmias, cardiac arrest, and even sudden death due to long QT syndrome). Therefore, domperidone is a more preferable prokinetic agent than metoclopramide and cisapride.

In case of overdose

With domperidone, the above extrapyramidal disorders and sedative effects are possible.
In this case, the use of activated carbon, anticholinergics or antihistamines is indicated. Indications for use
.
Nausea and vomiting, including in the presence of infections, with toxemia, radiation therapy, diet disorders, during endoscopic and radiopaque studies of the digestive tract, hiccups, postoperative or other atony of the stomach and intestines.
Feelings of bloating, fullness in the epigastrium, pain in the upper abdominal cavity, belching, flatulence, heartburn, reflux of gastric contents into the oral cavity. At the Department of Children's Diseases No. 2 of the Russian State Medical University, at the Russian Children's Clinical Hospital and the Moscow Research Institute of Pediatrics and Pediatric Surgery, studies were carried out in which it was found that taking domperidone (as opposed to mebeverine) leads to an increase in the rhythmicity coefficient of contractions of the gastrointestinal tract parts studied using electrogastroenterography compared to basal ones. values.

At the same time, there are studies showing that the prescription of dompidone as a prokinetic drug in the complex treatment of GERD in patients with diabetes mellitus is less effective in a number of parameters, such as the intensity of the reduction of esophageal symptoms (heartburn, regurgitation, dysphagia, odynophagia), in the normalization of pH-metry and peripheral electrogastroenterography compared with itopride (Fedorchenko Yu.L.).

Contraindications.

Hypersensitivity to domperidone, bleeding in the stomach or intestines, perforation of the stomach or intestines, mechanical intestinal obstruction, hyperprolactinemia, prolactinoma, pregnancy.
For children under 5 years of age and weighing less than 20 kg, taking domperidone tablets is not recommended. Part of domperidone passes into breast milk, so it is not recommended during breastfeeding (the Russian Ministry of Health* proposed to amend the instructions for film-coated tablets, 10 mg, in particular, the list of contraindications for use has been added: moderate and severe liver failure, pregnancy , breastfeeding period, children under 12 years of age or body weight up to 35 kg, simultaneous use of drugs that increase the QT interval and inhibitors of the CYP34A
).

Dosage forms

:
preparations containing domperidone are available in the form of an oral suspension, tablets, lozenges, film-coated tablets.
Side effects.

Digestive system:
spasm of smooth muscles of the gastrointestinal tract, dry mouth, stomatitis, thirst, heartburn, changes in appetite, constipation or diarrhea. Nervous system and sensory organs:
extrapyramidal disorders in overdose, headache, asthenia, irritability, nervousness, drowsiness, leg cramps, lethargy, conjunctivitis.
Allergic reactions:
skin rash, itching, urticaria, swelling.
Urinary system:
change in frequency of urination, burning, difficulty and pain when urinating.
Others:
increased levels of prolactin in the blood plasma, galactorrhea, gynecomastia, menstrual irregularities, mastalgia, palpitations.
( The letter* has added the list of side effects for film-coated tablets, 10 mg: very rarely - urticaria, anaphylactic shock, angioedema shock, convulsions, increased excitability and irritability, drowsiness, headache, changes in liver function tests; frequency unknown - ventricular tachycardia of the “pirouette” type, sudden coronary death.
)

Interaction.

Antacids and antisecretory drugs reduce bioavailability. Anticholinergics weaken the effect of domperidone. Antifungal drugs of the azole group, antibiotics of the macrolide group, and HIV protease inhibitors can block the metabolism of domperidone and increase its plasma level, so their combined use with domperidone requires caution. Concomitant use with monoamine oxidase inhibitors also requires caution. Domperidone does not affect the level of digoxin and paracetamol in the blood.

Trade names of drugs with active ingredients

domperidone: Damelium, Domet, Domperidone, Domperidone Hexal, Domstal, Motilak, Motilium, Motinorm, Motonium, Passazhiks.

Ukraine: Domrid, Domrid SR.

Domperidone is not approved by the FDA for use in the United States. Unlike the USA, in Canada, Japan, China, Israel, Great Britain and most European countries it has such permission.

Medicines with the complex active ingredient domperidone + omeprazole: Omez D and Omez DSR.

All drugs containing domperidone as an active ingredient, including combination drugs, have been transferred from over-the-counter to prescription

.**

Patient materials in English

(for UK, pdf):

"Patient Information Leaflet for Domperidone Stomach Discomfort Relief Tablets (Domperidone 10 mg)", May 2012.
"Domperidone 1 mg/ml Oral Suspension. Patient Information Leaflet", 05.11.2012
"Package Leaflet: Information for the User. Domperidone 10 mg Tablets. Domperidone maleate"

* Letter from the Director of the Department of State Regulation of Medicines of the Ministry of Health of the Russian Federation A.G. Tsyndymeev No. 20-3/162 dated 03/05/2015 ** Letter from the Director of the Department of State Regulation of Medicines of the Ministry of Health of the Russian Federation A.G. Tsyndymeev No. 20-3/100 dated January 31, 2017

Resources for healthcare professionals regarding the use of domperidone

Printed publications

Alekseeva E.V., Fominykh V.P., Tropinskaya N.S., Popova T.S. Use of the prokinetic drug domperidone in patients in the early postoperative period // Surgery. - No. 3. – pp. 62–69. – 2010.
Ponomareva A.P., Rachkova N.S., Belmer S.V., Khavkin A.I. Peripheral electrogastroenteromyography in pediatric gastroenterology / M.: 2007, 48 p.
Rebrov V.G., Loginov A.F., Kalinin A.V. Changes in the electrical activity of the stomach and intestines under the influence of motilium / Russian Journal of Gastroenterology, Hepatology, Coloproctology. —1997. - No. 4. - With. 42–45.
Starostin B.D., Starostina G.A. Clinical and economic effectiveness of motilak in gastroesophageal reflux disease // News of Universities. North Caucasus region. Natural Sciences. Special issue. - 2005. - p. 51–52.
Arkhipov V.V., Serebrova S.Yu. Safety of the use of prokinetics in the practice of a therapist using the example of domperidone (Motilac) // Russian Medical Journal. - 2007. - Volume 15. - No. 16. - p. 1218.
Maev I.V., Dicheva D.T., Andreev D.N. Possibilities of using Domperidone in the complex therapy of GERD // Medical Council. 2012. No. 12. pp. 56–60.
Fedorchenko Yu.L. Comparative characteristics of prokinetics in the treatment of gastroesophageal reflux disease in patients with diabetes // Experimental and clinical gastroenterology. 2013. No. 5. pp. 42–58.
Kosenko P.M., Rudnev A.F., Mikhailenko P.A., Matveeva E.A. Electrophysiological assessment of the influence of prokinetics on the motility of the gastrointestinal tract // Young scientist. — 2021. — No. 17 (151). — pp. 125-127.

On the website GastroScan.ru in the “Literature” section there is a subsection “Prokinetics”, containing articles on the use of prokinetics in the treatment of diseases of the gastrointestinal tract.

Video

Still from video: Shavkuta G.V. Combined functional disorders of the esophagus and stomach: actual clinical practice and modern recommendations for patient management

Still from the video (with simultaneous translation into Russian): Serhat Bor (Turkey).
Diagnosis and treatment of GERD: what's new? On the website GastroScan.ru in the “Video” section there is a subsection for patients “Popular Gastroenterology” and a subsection “For Doctors”, containing video recordings of reports, lectures, webinars in various areas of gastroenterology for healthcare professionals.
Domperidone has contraindications, side effects and application features; consultation with a specialist is necessary. Back to section

Domperidone overdose, symptoms and treatment

Symptoms of overdose may include drowsiness, disorientation and extrapyramidal disorders, especially in children. In case of overdose, gastric lavage, intake of activated charcoal and medical supervision are recommended. To eliminate extrapyramidal symptoms, anticholinergic drugs, drugs for the treatment of parkinsonism, or antihistamines with anticholinergic effects are used.

List of pharmacies where you can buy Domperidone:

Moscow
Saint Petersburg

Domperidone-Edvansd

Absorption

When taken on an empty stomach, domperidone is rapidly absorbed after oral administration, the maximum concentration (Cmax) in the blood plasma is reached 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 poor absorption of domperidone. Oral bioavailability is reduced by prior administration of cimetidine and sodium bicarbonate. When taking domperidone after food, it takes longer to achieve maximum absorption and the area under the concentration-time curve (AUC) is slightly increased.

When taken orally, domperidone does not accumulate and does not induce its own metabolism; Cmax in blood plasma - 21 ng/ml 90 minutes after 2 weeks of taking the drug orally at a dose of 30 mg per day was almost the same as the concentration - 18 ng/ml after taking the first dose.

Distribution

Domperidone is 91-93% bound to plasma proteins. Distribution studies of radiolabeled domperidone in animals have shown a wide tissue distribution but low concentrations in the brain. Small amounts of domperidone cross the placenta in rats.

Metabolism

Domperidone undergoes rapid and extensive metabolism by hydroxylation and N-dealkylation. In vitro metabolism studies with diagnostic inhibitors have shown that the CYP3A4 isoenzyme is the main cytochrome P450 form involved in the N-dealkylation of domperidone, while the CYP3A4, CYP1A2 and CYP2E1 isoenzymes are involved in the aromatic hydroxylation of domperidone. Excretion by the kidneys and intestines accounts for 31% and 66% of the oral dose, respectively. The proportion of domperidone excreted unchanged is small (10% is excreted by the intestines and approximately 1% by the kidneys).

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 2 mmol/L), the half-life of domperidone increases from 7.4 to 20.8 hours, but plasma domperidone concentrations are lower than in patients with normal renal function. A small amount of unchanged domperidone (about 1%) is excreted by the kidneys.

Special patient groups

In patients with moderate hepatic impairment (Child-Pugh score 7-9), the AUC and Cmax of domperidone were 2.9 and 1.5 times higher than in healthy volunteers, respectively. The proportion of 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, with no changes in protein binding or half-life. The pharmacokinetics of domperidone in patients with severe hepatic impairment have not been studied.

Indications for use of the drug Domperidone

A complex of dyspeptic symptoms associated with delayed gastric emptying, gastroesophageal reflux, esophagitis (a feeling of fullness of the stomach, heaviness in the epigastric region, a feeling of bloating, pain in the upper abdomen, belching, flatulence, nausea, vomiting, heartburn with regurgitation of gastric contents) ; nausea and vomiting of functional, organic, infectious or nutritional origin, as well as caused by radiation or emetogenic chemotherapy; nausea and vomiting caused by dopamine agonists (levodopa, bromocriptine).