Domperidone-Teva tablets 10 mg 30 pcs

Domperidone – dopamine receptor blocker having antiemetic action

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action due to a combination of peripheral (gastrokinetic) action and inhibition of dopamine receptors in the brain trigger zone of chemoreceptors located outside the blood-brain barrier in areapostrema.

When administered domperidone increases the pressure in the esophagus, antroduodenalnuyu improves motility and accelerates gastric emptying without causing effects on gastric secretion.

Domperidone increases prolactin secretion from the pituitary gland.

pharmacokinetics

When administered on an empty stomach, domperidone is rapidly absorbed and its Cmax in plasma are reached within 30-60 minutes. Low absolute bioavailability after oral administration (about 15%) due to the effect of “first pass” through the liver. While in healthy volunteers increased the bioavailability of domperidone when administered to a meal, patients with complaints on the part of the gastrointestinal tract should take domperidone 15-30 minutes before a meal. By reducing gastric acidity observed violation of absorption of domperidone. Preliminary receiving cimetidine and sodium bicarbonate reduces the bioavailability of domperidone. If ingestion after eating some more time is required to achieve maximum absorption.

When administered domperidone does not accumulates and does not induce its own metabolism. Domperidone is 91-93% bound to plasma proteins. Domperidone is distributed in various tissues of the body, it is found in breast milk, but does not penetrate the blood-brain barrier. Concentration of domperidone in breast milk is 10-50% of the plasma concentration.

domperidone metabolism occurs in the liver and in the intestinal wall by hydroxylation and N-dealkylation involving isozymes CYP3A4, CYP1A2 and CYP2E1.

Domperidone appears intestine (66%) and kidneys (33%), including: in unmodified form (10% and 1%, respectively). T1 / 2 of 7-9 hours.

Pharmacokinetics in special clinical situations

In patients with serum creatinine concentrations of more than 0.6 mmol / L T1 / 2 is from 7.4 to 20.8 hours, the domperidone plasma concentration lowered.

Active substance:
Domperidone

Manufacturer

Teva Pharmaceutical Enterprise Co., Ltd., Israel

Composition

1 tablet contains:

Active ingredient: 10 mg of domperidone;

Excipients: Microcrystalline cellulose – 60.00 mg pregelatinized starch – 19.46 mg Colloidal silicon dioxide (Aerosil) – 0.09 mg magnesium stearate – 0.45 mg Polyvinyl alcohol – 1,44mg, macrogol (polyethylene glycol) – 0.73 mg talc – 0.53 mg titanium dioxide – 0.90 mg

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Indications

dyspeptic symptoms, such as:

• Nausea, vomiting.


• Fullness in the epigastric region.


• Discomfort in the upper abdomen.


• regurgitation of gastric contents.

Contraindications

• Hypersensitivity to domperidone or any other component of the product.


• prolactin secreting pituitary tumor (prolactinoma).


• Gastrointestinal bleeding.


• The perforation of the gastrointestinal tract.


• Mechanical bowel obstruction.


• The hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption.


• The period of breastfeeding.


• Children weighing less than 35 kg.

Caution:

• Pregnancy.


• Liver failure.


• Kidney failure.

Side effects

From the digestive system: Gastrointestinal disorders (transient intestinal cramps)

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From the nervous system: extrapyramidal disorder (in children and patients with increased permeability of the BBB, in adults – single cases); these effects are completely reversible and disappear after discontinuation of the drug.

Allergic reactions: skin rash, urticaria

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Other: hyperprolactinemia (galactorrhea, gynecomastia, amenorrhea)

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How to accept, acceptance rate and dosage

Inside before eating, drinking plenty of water.

• Adults and children weighing more than 35 kg 1-2 tablets 3-4 times a day. The maximum dose is 80 mg per day. Course duration – 4 weeks. Further the drug is possible after consultation with a doctor.

Patients with renal failure decrease recommended dosing frequency of 1-2 times per day.

Storage conditions

In a dry, dark place at a temperature below 25 ° C

Active substance

Domperidone

Interaction

cimetidine, sodium bicarbonate reduces the bioavailability of domperidone.

M-holinoblokatory and antacid drugs neutralize domperidone.

domperidone increases the concentration in plasma isozyme inhibitors of CYP3A4: antifungal azole drugs, macrolide antibiotics, HIV protease inhibitors, nefazodone (antidepressant). When co-administered with ketoconazole achieved approximately threefold increase in the maximum concentration of domperidone.

Simultaneous treatment with paracetamol and digoxin had no effect on the concentration of these drugs in the blood.

Compatible with antipsychotic drugs (neuroleptics) and dopamine receptor agonists (bromocriptine, levodopa).

Special conditions

cimetidine, sodium bicarbonate reduces the bioavailability of domperidone.

M-holinoblokatory and antacid drugs neutralize domperidone.

domperidone increases the concentration in plasma isozyme inhibitors of CYP3A4: antifungal azole drugs, macrolide antibiotics, HIV protease inhibitors, nefazodone (antidepressant). When co-administered with ketoconazole achieved approximately threefold increase in the maximum concentration of domperidone.

Simultaneous treatment with paracetamol and digoxin had no effect on the concentration of these drugs in the blood.

Compatible with antipsychotic drugs (neuroleptics) and dopamine receptor agonists (bromocriptine, levodopa).

Pregnancy and lactation

Teva-Domperidone is contraindicated in pregnancy, breast-feeding and children under the age of 1 year.

Overdose

Symptoms: drowsiness, disorientation, extrapyramidal disorder (especially in children)

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Treatment: administration of activated charcoal, with extrapyramidal disorders –
m-holinoblokatory, antiparkinsonian drugs or antihistamines with anticholinergic properties.