Composition, form of production and packaging
The tablets covered with a film membrane of white or almost white color, round, biconcave; on the cross-section - the inner layer of white or white with a creamy shade of color.
1 tab.
domperidone 10 mg
Auxiliary substances: microcrystalline cellulose - 60 mg, pregelatinized starch - 19.46 mg, silicon dioxide colloid (aerosil) - 90 Ојg, magnesium stearate - 450 Ојg, polyvinyl alcohol - 1.44 mg, macrogol (polyethylene glycol) - 730 Ојg, talc - 530 Ојg, titanium dioxide - 900 mcg.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (4) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
An antiemetic drug, a central action antagonist of dopamine receptors. Unlike metoclopramide, domperidone does not penetrate poorly through the BBB. It blocks the peripheral and to a lesser extent the central (in the trigger zone of the vomiting center) dopamine receptors. Eliminates the inhibitory effect of dopamine on the motor function of the gastrointestinal tract and increases the evacuation and motor activity of the stomach.
Has antiemetic effect, soothes hiccups and eliminates nausea. Has no effect on gastric secretion.
Increases the concentration of prolactin in the blood serum.
PHARMACOKINETICS
Suction
After ingestion on an empty stomach - absorption is fast. Admission after meals, reduced acidity of gastric juice slow down and reduce absorption. The time to reach Cmax is 1 hour. Bioavailability is 15% due to the effect of "first passage" through the liver.
Distribution
Binding to plasma proteins - 90%. Penetrates into various tissues, it does not pass well through GEB.
Do not cumulate.
Metabolism
Metabolized in the liver and in the intestinal wall by hydroxylation and N-dealkylation with the participation of cytochrome P450 isoenzymes. Does not induce its own metabolism.
Excretion
T 1/2 - 7-9 h. It is excreted through the intestine - 66%, kidneys - 33%, incl. in unchanged form - 10% and 1%, respectively.
Pharmacokinetics in special clinical cases
With pronounced chronic renal failure, T 1/2 lengthens.
INDICATIONS
- nausea and vomiting of various genesis (including on the background of functional and organic diseases, infection, toxemia, radiation therapy, diet disorders, drug origin - morphine, apomorphine, levodopa and bromocriptine, endoscopic and radiocontrast studies of the gastrointestinal tract) ;
- hiccough;
- atony of the gastrointestinal tract (including postoperative);
- the need to accelerate peristalsis in radiocontrast studies of the gastrointestinal tract;
- dyspeptic symptoms on the background of delayed emptying of the stomach, gastroesophageal reflux and esophagitis: a feeling of overfilling in the epigastrium, a sensation of bloating, flatulence, gastralgia, heartburn, belching with or without casting gastric contents into the oral cavity.
DOSING MODE
The drug is taken orally 15-20 minutes before meals.
Adults and children over 5 years with chronic dyspeptic symptoms - 10 mg 3-4 times / day, incl. and before bedtime if necessary.
With severe nausea and vomiting - 20 mg 3-4 times / day, the last reception - before bedtime.
The maximum daily dose is 80 mg.
For patients with renal insufficiency , dose adjustment is necessary, the frequency of administration should not exceed 1-2 times / day.
SIDE EFFECT
From the digestive system: gastrointestinal disorders (transient intestinal spasms).
From the side of the nervous system: extrapyramidal disorders (in children in individuals with increased permeability of the BBB, in adults - single cases). These phenomena are completely reversible and disappear after discontinuation of the drug.
Allergic reactions: skin rash, hives.
Other: hyperprolactinemia (galactorrhea, gynecomastia, amenorrhea).
CONTRAINDICATIONS
bleeding from the gastrointestinal tract;
- mechanical intestinal obstruction;
- perforation of the stomach or intestines;
- prolactinoma;
- lactation period;
- Children's age till 5 years;
- Children weighing up to 20 kg;
- Hypersensitivity to the components of the drug.
With caution , use the drug with severe renal and / or liver failure.
PREGNANCY AND LACTATION
Data on the use of domperidone in pregnancy is not enough. To date, there is no evidence of an increased risk of malformations in humans. However, prescribe domperidone during pregnancy should be only in case the expected therapeutic benefit for the mother exceeds the potential risk to the fetus.
In women, the concentration of domperidone in breast milk is from 10% to 50% of the corresponding plasma concentration and does not exceed 10 ng / ml. The total amount of domperidone excreted in breast milk is less than 7 Ојg / day when domperidone is administered in the maximum admissible doses. It is not known whether domperidone in this concentration has a negative effect on infants. In this regard, when using domperidona during lactation should stop breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be applied to the drug with severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution , use the drug with severe hepatic insufficiency.
APPLICATION FOR CHILDREN
Contraindicated in children under 5 years, as well as in children weighing up to 20 kg.
SPECIAL INSTRUCTIONS
Domperidone and antacid preparations or drugs that reduce gastric secretion should not be taken together at the same time. When taking domperidone before meals, these medications should be taken after meals.
OVERDOSE
Symptoms: drowsiness, disorientation, extrapyramidal disorders (especially in children).
Treatment: reception of activated charcoal, with extrapyramidal disorders - m-holinoblokatory, antiparkinsonian drugs or antihistamines with anticholinergic properties.
DRUG INTERACTION
Cimetidine, sodium hydrogen carbonate reduce the bioavailability of domperidone.
M-cholinoblockers and antacid drugs neutralize the action of domperidone.
The concentration of domperidone in plasma increases with simultaneous use with inhibitors of the isoenzyme CYP3A4: antifungal azole agents, antibiotics of the macrolide group, HIV protease inhibitors, nefazodone (antidepressant). When combined with ketoconazole, approximately a threefold increase in C max domperidone in plasma is achieved.
With simultaneous admission with paracetamol and digoxin, the concentrations of these drugs in the blood do not change.
Domperidone is compatible with antipsychotic drugs (neuroleptics) and with dopamine receptor agonists (bromocriptine, levodopa).
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 В° C. Shelf life - 3 years.
