Domet - instructions for use, doses, side effects, contraindications

Excipients: cellulose microcrystalline, lactose, corn starch, silicon dioxide colloid, magnesium stearate, talc, corn pregelatinized starch, dye-yellow, methyl parahydroxybenzoate, propyl parahydroxybenzoate, sodium carboxymethyl starch.

Description:

Round, slightly biconcave tablets, without a pinkish-orange shell, with a risk on one side. Allowed a slight marbling.

Pharmacotherapeutic group:antiemetics - dopamine receptor blocker central

ATX: & nbsp

A.03.F.A.03 Domperidone

Pharmacodynamics:

Antiemetic means. It blocks central and peripheral dopamine receptors, eliminates the inhibitory effect of dopamine on the motor function of the gastrointestinal tract, stimulates the motor and evacuation activity of the stomach. Has antiemetic effect, soothes hiccups, eliminates nausea.

Pharmacokinetics:

Suction

After oral administration, fasting is rapidly absorbed from the gastrointestinal tract. The maximum concentration is reached in 30-60 minutes. Low bioavailability of domperidone (about 15%) is due to intensive metabolism at the first passage in the liver and intestinal wall.When taken after meals, the absorption of the drug is slightly slowed down, and the area under the "active substance concentration-time" (AUC) curve increases. Reduced acidity of gastric contents reduces the absorption of domperidone.

Has no effect on gastric secretion. Domperidone poorly penetrates the blood-brain barrier (BBB), so its use is rarely accompanied by extrapyramidal side effects, especially in adults; stimulates the secretion of prolactin by the pituitary gland located outside the BBB.

Distribution

Domperidone is well distributed in the tissues of the body. Concentration in brain tissues is not high. The degree of binding to plasma proteins is 91-93%.

Metabolism

It is subject to intensive metabolism in the liver by hydroxylation and N-dealkylation.

Excretion

The half-life is 7-9 hours. Domperidone is excreted mainly through the intestine (66%) and kidneys (33%). In an unnamed form, only a small percentage of domperidone is excreted (10% through the intestine and 1% by the kidneys).

Pharmacokinetics in special clinical cases

With severe renal failure, the elimination half-life increases.In patients with severe renal failure (serum creatinine> 6 mg / 100 ml), the elimination half-life increases from 7.4 to 20.8 hours.

Indications:

Dyspeptic syndrome, often associated with delayed emptying of the stomach, gastroesophageal reflux, esophagitis: a feeling of overfilling in the epigastrium, a feeling of bloating, pain in the upper abdomen, belching, flatulence, heartburn with or without casting the contents of the stomach into the mouth; nausea and vomiting of various origin, including functional, organic, infectious origin, caused by radiotherapy, drug therapy, intoxication or a violation of diet; nausea and vomiting caused by treatment with dopamine agonists (levodopa, bromocriptine).

Contraindications:

Hypersensitivity to domperidone, prolactin-secreting pituitary tumor (prolactinoma), gastrointestinal bleeding, mechanical obstruction or intestinal perforation.

In the form of tablets are not prescribed for children under 5 years old and weighing up to 20 kg.

Carefully:

Application for liver failure: domperidone actively it is metabolized in the liver, therefore administration of the drug to patients with hepatic insufficiency is not recommended.

Application for renal failure: with severe renal failure (serum creatinine> 6 mg / 100 mL) period half-dilution of domperidone increases from 7.4 to 20.8 hours. Depending on the degree of severity, it is recommended to correct the dose of the drug, as well as reduce the frequency of taking the drug to 1-2 times a day. If long-term treatment is needed, this group of patients needs careful monitoring of the level of domperidone in the blood.

Pregnancy and lactation:

The use of domperidone during pregnancy is possible only if the expected benefit to the mother exceeds the potential risk to the fetus.

If it is necessary to prescribe the drug during lactation, the question of stopping breastfeeding should be resolved.

Dosing and Administration:

Inside, for 15-20 min, before meals and, if necessary, before going to bed. The course of treatment is usually four weeks, after which the need to continue and stop treatment with the drug is considered.

Adults and children over 5 years old and weighing over 20 kg:

- for chronic dyspepsia prescribe 10 mg 3 times a day; with insufficient effect, this dose is doubled;

- in acute and subacute conditions, especially with nausea and vomiting appoint 20 mg 3-4 times a day.

The maximum daily dose is 80 mg.

With renal insufficiency:

Depending on the degree of severity, it is recommended to correct the dose of the drug, as well as reduce the frequency of taking the drug to 1 - 2 times a day.

Side effects:

From the central nervous system: *rarely: extrapyramidal disorders (in children and in persons with increased permeability of the BBB).

From the gastrointestinal tract: * rarely: transient intestinal spasms.

Allergic reactions: * very rarely: urticaria, skin rash.

Other: "rarely hyperprolactinemia (galactorrhea, gynecomastia, amenorrhea).

* frequency of side effects: very often - ≥ 10%; often from ≥ 1% to <10%; sometimes from ≥ 0.1% to <1%; rarely from ≥ 0.01% to <0.1%; very rarely <0.01%.

Overdose:

Symptoms - drowsiness, disorientation, extrapyramidal disorders, especially in children.

Treatment - gastric lavage, the appointment of activated charcoal. Anticholinergics, drugs used to treat parkinsonism, or antihistamines may be effective in the occurrence of extrapyramidal reactions.

Interaction:

The main pathway of metabolic transformations of domperidone occurs with the participation of an isoenzyme CYP3A4 systems of cytochrome P450. Based research in vitro it can be assumed that a joint intake with drugs that inhibit this enzyme causes an increase in the level of domperidone in the blood plasma. Examples of isoenzyme inhibitors CYP3A4 are the following medicines: antifungal agents of the azole group, antibiotics of the macrolide group, HIV protease inhibitors, nefazodone.

Antisecretory drugs can reduce the bioavailability of domperidone, so they should be taken after meals, i.e. they should not be taken concomitantly with domperidone.

With simultaneous use of anticholinergic and antacid preparations can neutralize the effect of domperidone.

Domperidone is compatible with the administration of neuroleptics, dopaminergic receptor agonists (bromocriptine, levodopa).

The use of domperidone against the background of treatment with paracetamol or digoxin does not affect the level of these drugs in the blood.

Effect on the ability to drive transp. cf. and fur:

Domperidone does not interfere with the speed of psychomotor reactions.

Form release / dosage:Tablets, 10 mg.

Packaging:

For 10 tablets in a contour mesh PVC / aluminum package (blister); 1, 3 or 10 contour squares (blisters) in a pack of cardboard, complete with instructions for medical use in Russian.

Packing of 100 tablets is intended for hospital supplies.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LSR-007711/08

Date of registration:25.09.2008

The owner of the registration certificate:Protek Biosystems Pvt. Ltd.Protek Biosystems Pvt. Ltd. India

Manufacturer: & nbsp

PROTECH BIOSYSTEMS, PVT. Ltd. India

Representation: & nbspProtekh Biosystems Pvt.LtdProtekh Biosystems Pvt.LtdRussia

Information update date: & nbsp19.01.2016

Illustrated instructions

Instructions

Domet (Domet)