Domperidone + Omeprazole (Domperidonum + Omeprazolum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Proton pump inhibitors

Antiemetic drugs

Included in the formulation
  • Omez® D
    capsules inwards 
    Torrent Pharmaceuticals Co., Ltd.     India
  • Omega® JEM
    capsules inwards 
    Dr. Reddy's Laboratories Ltd.     India
    • АТХ:

    A.02.B.X   Other antiulcer drugs

    Pharmacodynamics:

    Domperidone. Increases the duration of peristaltic contractions of the antral part of the stomach and duodenum, accelerates the emptying of the stomach in case of slowing down of this process, increases the tone of the lower esophageal sphincter, prevents the development of nausea and vomiting. Stimulates the release of prolactin from the pituitary gland. The antiemetic effect may be due to a combination of peripheral (gastrokinetic) action and antagonism to dopamine receptors in the trigger zone of the brain. Domperidone has no effect on gastric secretion. Poorly penetrates the blood-brain barrier, so the use of domperidone is rarely accompanied by the development of extrapyramidal side effects, especially in adults.

    Omeprazole. Inhibits the enzyme H+-TO+-ATPase (proton pump) in parietal cells of the stomach and thereby blocks the final stage of the synthesis of hydrochloric acid.This leads to a decrease in the level of basal and stimulated secretion, regardless of the nature of the stimulus. After a single intake of the drug, omeprazole acts within the first hour and lasts for 24 hours, the maximum effect is achieved after 2 hours. After discontinuation of the drug secretory activity is completely restored after 3-5 days.

    Pharmacodynamic justification of the combination. Omeprazole suppresses the secretion of hydrochloric acid, domperidone increases the tone of the lower esophageal sphincter and accelerates the emptying of the stomach, thereby reducing the activity of aggressive gastric juice factors and throwing up gastric contents into the esophagus.

    Pharmacokinetics:

    Domperidone

    After oral administration domperidone quickly absorbed. It has low bioavailability (about 15%). The decreased acidity of the gastric contents reduces the absorption of domperidone. Tmax in plasma - 1 hour.

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

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

    It is excreted through the intestine (66%) and kidneys (33%), in unchanged form, respectively 10% and 1% of the dose value. The half-life is 7-9 hours, with pronounced renal failure - lengthening.

    Omeprazole

    Omeprazole is rapidly absorbed from the digestive tract, Tmax in plasma - 0,5-1 hours Bioavailability is 30-40%. Binding to plasma proteins is about 90%. Omeprazole almost completely metabolized in the liver. It is an inhibitor of the enzyme system CYP2C19. Half-life - 0.5-1 h. It is excreted by the kidneys (70-80%) and with bile (20-30%). In chronic renal failure, excretion decreases in proportion to a decrease in creatinine clearance. In elderly patients excretion decreases, bioavailability increases. With hepatic failure, bioavailability is 100%, half-life - 3 hours

    Indications:

    Treatment of dyspepsia and gastroesophageal reflux, poorly amenable to monotherapy with proton pump inhibitors or antagonists H2receptors.

    ICD-10

    XI.K20-K31.K21   Gastroesophageal reflux

    XI.K20-K31.K30   Dyspepsia

    Contraindications:

    Hypersensitivity; gastrointestinal bleeding; mechanical obstruction of the gastrointestinal tract; perforation of the stomach or intestines; prolactinoma; lactation period; childhood.

    Carefully:

    Renal and / or liver failure; pregnancy.

    Pregnancy and lactation:

    Caution should be used during pregnancy.

    Contraindicated use of the drug during lactation (breastfeeding).

    Dosing and Administration:

    Inside, washed down with a small amount of water, 1 capsule 2 times a day, 15-20 minutes before meals.

    Side effects:

    Domperidone

    From the digestive system: transient intestinal spasms.

    From the nervous system: extrapyramidal disorders (in children and people with increased permeability of the blood-brain barrier).

    Allergic reactions: skin rash, hives.

    Other: hyperprolactinemia (galactorrhea, gynecomastia).

    Omeprazole

    On the part of the digestive system: diarrhea or constipation, nausea, vomiting, flatulence, abdominal pain, dry mouth, taste disorders, stomatitis, transient increase in hepatic enzyme activity in plasma; in patients with a previous severe liver disease - hepatitis (including jaundice), a violation of liver function.

    From the nervous system: headache, dizziness, agitation, drowsiness, insomnia, paresthesia, depression,hallucinations; in patients with severe concomitant somatic diseases, patients with previous severe liver disease - encephalopathy.

    From the musculoskeletal system: muscle weakness, myalgia, arthralgia.

    On the part of the hematopoiesis system: leukopenia, thrombocytopenia; in some cases - agranulocytosis, pancytopenia.

    From the skin: itching, skin rash; in some cases - photosensitivity, multiforme exudative erythema, alopecia.

    Allergic reactions: urticaria, angioedema, bronchospasm, interstitial nephritis, anaphylactic shock, fever.

    Other: impaired vision, peripheral edema, increased sweating, gynecomastia; rarely - the formation of gastric glandular cysts during long-term treatment (the consequence of inhibition of the secretion of hydrochloric acid, is benign, reversible).

    Overdose:

    Domperidone. Symptoms: drowsiness, disorientation and extrapyramidal reactions. Treatment: reception of activated carbon; when extrapyramidal reactions occur - anticholinergic, anti-Parkinsonian, antihistamines.

    Omeprazole. Symptoms: impaired vision, drowsiness, agitation, confusion, headache, increased sweating, dry mouth, nausea, arrhythmia. Treatment: symptomatic. There is no specific antidote. Hemodialysis is not effective enough.

    Interaction:

    Omeprazole (in combination domperidone + omeprazole) can reduce the absorption of esters, itraconazole, iron salts, ketoconazole, ampicillin (omeprazole increases the pH in the stomach).

    Omeprazole, being an inhibitor of cytochrome P450, can increase the concentration and reduce the excretion of diazepam and phenytoin (metabolized in the liver with the participation of cytochrome CUR2C19), which in some cases may require a reduction in its dose.

    Omeprazole enhances the inhibitory effect on the hemopoietic system of other drugs.

    Sodium bicarbonate, cimetidine, other antacid and antisecretory drugs reduce the bioavailability of domperidone.

    Anticholinergic drugs neutralize the action of domperidone.

    Increase the concentration of domperidone in plasma: antifungal agents of the azole series, antibiotics from the macrolide group, HIV protease inhibitors, nefazodone.

    Special instructions:

    Before the beginning of therapy it is necessary to exclude the presence of malignant process in the digestive tract, as treatment, masking the symptoms, can delay the establishment of the correct diagnosis.

    Instructions
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