Passage - instructions for use, dose, side effects, contraindications

Excipients: [silicon dioxide colloid (aerosil), povidone (polyvinylpyrrolidone low molecular weight or kollidon 30), potato starch, sodium dodecyl sulfate (sodium lauryl sulfate), lactose monohydrate (sugar milk), calcium stearate];

excipients for the shell: [giprolose (klucel), polysorbate - 80 (tween 80), titanium dioxide].

Description:The tablets covered with a cover of white or almost white color, round, biconcave. Two layers are visible on the cross-section.

Pharmacotherapeutic group:Antiemetics - dopamine receptor blocker central

ATX: & nbsp

A.03.F.A.03 Domperidone

Pharmacodynamics:

Domperidone, a dopamine receptor antagonist, possesses antiemetic properties similar to metoclopramide and some neuroleptics. However, unlike these drugs (LS), domperidone poorly penetrates the blood-brain barrier (BBB). 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.Its antiemetic effect may be due to a combination of peripheral (gastrokinetic) action and antagonism to dopamine receptors in the chemoreceptor trigger zone. Primarily blocks peripheral dopamine receptors, to a lesser extent - central.

When administered orally domperidone prolongs the duration of antral and duodenal contractions, accelerates the emptying of the stomach - the yield of liquid and semi-solid fractions in healthy people and solid fractions in patients in whom this process has been slowed and increases the pressure of the sphincter of the lower esophagus in healthy people. Domperidone has no effect on gastric secretion.

Pharmacokinetics:

Suction

After taking the drug inside domperidone quickly absorbed.

It has low bioavailability (about 15%). Reducing the acidity of gastric juice reduces the absorption of domperidone. The maximum concentration in plasma (C_max) is achieved after 1 hour.

Distribution

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

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

Excretion
It is excreted through the intestine (66%) and kidneys (33%), in unchanged form, respectively, 10% and 1% of the value of the dose taken. The half-life (T_½) is 7-9 hours, with pronounced renal failure, it lengthens.

Indications:

- A complex of dyspeptic symptoms, often associated with delayed emptying of the stomach, gastroesophageal reflux, esophagitis:

- a feeling of overfilling in the epigastrium ("heaviness" in the stomach), 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.

- Nausea and vomiting of a functional, organic, infectious origin caused by radiotherapy, drug therapy or a diet disorder, and against dopamine agonists when used in Parkinson's disease (such as levodopa and bromocriptine).

Contraindications:

- An established intolerance to the drug and its components;

- Prolactin-secreting pituitary tumor (prolactinoma);

- children under 5 years old and weighing up to 20 kg;

- gastrointestinal bleeding, mechanical obstruction or perforation (ie, when stimulation of gastric motility may be dangerous);

- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Carefully:Pronounced renal and / or hepatic insufficiency.

Pregnancy and lactation:It is not recommended to use the drug Passage during pregnancy (due to insufficient data). If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside, 15-20 minutes before meals.

Adults and children over 5 years of age with chronic dyspeptic phenomena - 10 mg (1 tablet) 3 times a day and, if necessary, before bedtime. With severe nausea and vomiting - 20 mg 3-4 times a day. The maximum daily intake for adults is 80 mg (8 tablets). The maximum daily dose for children should not exceed 10 mg (1 tablet, film-coated) per 10 kg of body weight.

Notes.

It is recommended that oral use of Passage before meals. When taking the drug after a meal, absorption is somewhat slowed down.

With renal failure, dose adjustment is necessary, the frequency of administration should not exceed 1-2 times during the day.

Side effects:

From the digestive system: transient intestinal spasms.

From the central nervous system (CNS): extrapyramidal phenomena are observed in children and with increased permeability of the BBB. These phenomena are completely reversible and spontaneously disappear after discontinuation of treatment.

From the endocrine system: Passage can induce an increase in the concentration of prolactin in the plasma, since the pituitary gland is outside the BBB. In rare cases, this hyperprolactinemia can stimulate the appearance of galactorrhea, gynecomastia and dysmenorrhea.

Allergic reactions: a rash, hives.

Overdose:

Symptoms: Symptoms of overdose can be drowsiness, disorientation and extrapyramidal reactions, especially in children.

Treatment: In case of an overdose, the use of activated carbon and careful observation are recommended. Anticholinergics, drugs used to treat parkinsonism or antihistamines may be effective in the occurrence of extrapyramidal reactions.

Interaction:

With simultaneous use of anticholinergic drugs can neutralize the effect of domperidone.With simultaneous application with domperidone antacid preparations reduce its bioavailability. Based on research in vitro it can be assumed that, when used simultaneously with domperidone LS, significantly inhibiting isoenzyme CYP3A4 (antifungal preparations of the azole group, antibiotics from the macrolide group, HIV protease inhibitors, nefazodone antidepressant), an increase in the concentration of domperidone in plasma can be observed. The drug does not affect the concentrations of paracetamol and digoxin in the blood. It is possible that domperidone can affect the absorption of concomitantly administered drugs with sustained release of the active substance or coated with an enteric coating.

Special instructions:

With the combined use of the drug Passagex with antacid or antisecretory (M-cholinolytics, H₂-gastamine blockers, proton pump inhibitors), drugs should be taken after meals, not before meals, i.e. they should not be taken concomitantly with the drug Passagex.

Application for liver diseases

Given the metabolism of domperidone in the liver, caution should be given to the drug Passage to patients with hepatic insufficiency.

Application in diseases of the kidneys

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 hours, but plasma concentrations of the drug were lower than in healthy volunteers. Since a very small percentage of the drug is excreted by the kidneys unchanged, it is hardly necessary to correct a single dose in patients with renal insufficiency. However, with a repeated appointment, the frequency of reception should not exceed 1-2 times during the day, depending on the severity of the insufficiency, and there may also be a need to reduce the dose. With prolonged therapy, patients should be under regular supervision.

Effect on the ability to drive transp. cf. and fur:Domperidone does not affect the ability to drive vehicles and engage in other, potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated 10 mg.

Packaging:

For 10 or 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 2, 3 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:In a dry, dark place, at a temperature of no higher than 25 FROM.

Keep out of the reach of children.

Shelf life:3 years. Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:P N003305 / 01

Date of registration:18.08.2009

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp09.08.2017

Illustrated instructions

Instructions

Passenger (Passagix)