Composition, form of production and packaging
? Tablets chewing white or white with a creamy shade of color, round, flat-cylindrical, with a risk.
domperidone 10 mg
Excipients: aspartame, lactitol, xylitol, magnesium stearate, menthol.
4 things. - packings of cellular contour (1, 2, 3, 4, 5) - packs cardboard.
6 pcs. - packings of cellular contour (1, 2, 3, 4, 5) - packs cardboard.
10 pieces. - packings of cellular contour (1, 2, 3, 4, 5) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
The drug has a prokinetic, antiemetic effect, normalizes the function of the digestive system. Blocker of dopamine D 2 receptors. Prokinetic properties are associated with blockade of peripheral dopamine receptors and elimination of the inhibitory effect of dopamine on the function of the gastrointestinal tract. 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, eliminates the development of nausea and vomiting.
Domperidone weakly penetrates through the BBB, therefore, the use of domperidone is rarely accompanied by extrapyramidal side effects, especially in adults, but domperidone 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 the dopamine receptors in the chemoreceptor trigger zone. Domperidone has no effect on gastric secretion.
After taking the drug inside, domperidone is rapidly absorbed. It has low bioavailability (about 15%). Reducing the acidity of gastric juice reduces the absorption of domperidone. C max in plasma is achieved after 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%), unchanged - 10% and 1% of the dose, respectively. T 1/2 is 7-9 hours.
Pharmacokinetics in special clinical cases
With severe renal failure, T 1/2 is lengthened.
1) Complex of dyspeptic symptoms, often associated with delayed emptying of the stomach, gastroesophageal reflux, esophagitis:
- a feeling of overflow in the epigastrium, a sensation of bloating, pain in the upper abdomen;
- belching, flatulence;
- Heartburn with casting or without casting the contents of the stomach into the mouth.
2) Nausea and vomiting of a functional, organic, infectious origin caused by radiotherapy, drug therapy or a diet disorder, as well as the use of dopamine agonists in Parkinson's disease (such as levodopa and bromocriptine).
The drug is taken preferably, preferably before meals. When taking the drug after a meal, absorption is somewhat slowed down.
Adults appoint 10 mg (1 tab.) 3 times / day, 15-30 minutes before meals and, if necessary, before bed.
Children older than 5 years - 2.5 mg per 10 kg body weight 3 times / day, before meals and, if necessary, before bed.
If necessary, the indicated dose can be doubled.
Acute and subacute conditions (primarily nausea and vomiting)
Adults appoint 20 mg (2 tablets) 3-4 times / day, before meals and at bedtime.
Children older than 5 years - 5 mg per 10 kg body weight, 3-4 times / day, before meals and at bedtime.
With renal failure , a reduction in the frequency of taking the drug is recommended. In patients with severe renal insufficiency (serum creatinine> 6 mg / 100 ml, i.e.> 0.6 mmol / l), T 1/2 domperidone increased from 7.4 to 20.8 h, but plasma concentrations were lower than in healthy volunteers. Because a very small percentage of the drug is excreted by the kidneys unchanged, then it is hardly necessary to correct a single dose in patients with renal insufficiency. However, with a re-appointment, the frequency of administration should be reduced to 1-2 times / day, depending on the severity of renal failure, and a dose reduction may also be necessary. With prolonged therapy, patients should be under regular supervision.
Given the metabolism of domperidone in the liver, caution should be given to patients with hepatic insufficiency .
Side effects are rare.
Allergic reactions: rarely - a rash, hives.
From the digestive system: there were exceptional cases of transient intestinal spasms.
From the side of the nervous system: in children and with increased permeability of the BBB, extrapyramidal reactions are noted, which are completely reversible and spontaneously disappear after discontinuation of treatment.
On the part of the endocrine system: the drug can induce an increase in the level of prolactin in the plasma (because the pituitary gland is outside the BBB). In rare cases, hyperprolactinemia can stimulate the appearance of galactorrhea, gynecomastia and dysmenorrhea.
- established intolerance to the drug;
- Prolactin-secreting pituitary tumor (prolactinoma);
- Children under 5 years.
Do not use Passage, when stimulation of the motor function of the stomach can be dangerous, incl. with gastrointestinal bleeding, mechanical obstruction or perforation.
PREGNANCY AND LACTATION
When administered to animals in doses up to 160 mg / kg / day, domperidone did not have a teratogenic effect. However, like most drugs, the drug should be given in the first trimester of pregnancy only if its use is justified by the expected therapeutic benefit. To date, there is no evidence of an increased risk of developmental malformations in humans.
In women, concentrations of domperidone in breast milk are 4 times lower than the corresponding concentrations in plasma. It is not known whether this level has a negative effect on newborns. Therefore, if the mother accepts Passage, breast-feeding is not recommended, except when the expected benefit justifies the potential risk.
APPLICATION FOR FUNCTIONS OF THE LIVER
Because a very small percentage of the drug is excreted by the kidneys unchanged, then it is hardly necessary to correct a single dose in patients with renal insufficiency. However, with a re-appointment, the frequency of administration should be reduced to 1-2 times / day, depending on the severity of the insufficiency, it may also be necessary to reduce the dose.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Given the metabolism of domperidone in the liver, caution should be used to administer the drug to patients with hepatic insufficiency.
APPLICATION FOR CHILDREN
Contraindicated in children under the age of 5 years.
With the combined use of the drug Passagex with antacid or antisecretory drugs, the latter should be taken after meals, and not before meals, i.e. they should not be taken concomitantly with the drug Passagex.
Impact on the ability to drive vehicles and manage mechanisms
Domperidone does not disrupt the speed of psychomotor reactions.
Symptoms: drowsiness, disorientation and extrapyramidal reactions, especially in children.
Treatment: recommended the use of activated carbon and careful observation. Anticholinergics, drugs used to treat parkinsonism, or antihistamines may be effective in the occurrence of extrapyramidal reactions.
With simultaneous use of anticholinergic drugs can neutralize the effect of the drug Passagex.
With simultaneous use with the drug Passage antacid and antisecretory drugs reduce its bioavailability.
On the basis of in vitro studies, it can be assumed that, while using medicines that significantly inhibit CYP3A4 (antifungals of the azole group, antibiotics from the macrolide group, HIV protease inhibitors, nefazodone antidepressant) with Passagex, an increase in the concentration of domperidone in plasma can be observed.
The drug does not affect the concentration of paracetamol and digoxin in the blood.
It is possible that Passagex can influence the absorption of concomitantly administered drugs with sustained release of the active substance or coated with an enteric coating.
TERMS OF RELEASE FROM PHARMACY
The drug is approved for use as a means of OTC.
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 - 2 years.