Domperidone pills 10mg, 30pcs

Composition

Per tablet:

Active ingredient:  domperidone – 10.00 mg.

Auxiliary substances:  lactose monohydrate (milk sugar) – 53.10 mg, corn starch-20.00 mg, microcrystalline cellulose-10.00 mg, povidone-K 25-3.00 mg, magnesium stearate-0.70 mg, sodium lauryl sulfate-0.20 mg.

Shell composition:  hypromellose – 1.15 mg, macrogol-4000-0.30 mg, titanium dioxide-0.55 mg

Pharmacological action

Domperidone is a dopamine antagonist with antiemetic properties. However, domperidone does not penetrate well through the blood-brain barrier. 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. Animal studies and low concentrations of the drug found in the brain indicate a central effect of domperidone on dopamine receptors.

When used orally, domperidone increases the duration of antral and duodenal contractions, accelerates gastric emptying and increases the pressure of the lower esophageal sphincter in healthy people. Domperidone has no effect on gastric secretion.

Pharmacokinetics:

When taken on an empty stomach, domperidone is rapidly absorbed after oral use, peak plasma concentrations are reached within 30-60 minutes.

The low absolute oral bioavailability of domperidone (approximately 15%) is associated with intensive first-pass metabolism in the intestinal wall and liver. Domperidone should be taken 15-30 minutes before meals. Reduced acidity in the stomach leads to impaired absorption of domperidone.

Oral bioavailability is reduced with prior use of cimetidine and sodium bicarbonate. When taking the drug after a meal, it takes longer to achieve maximum absorption and the area under the pharmacokinetic curve (AUC) slightly increases.

When taken orally, domperidone does not accumulate and does not induce its own metabolism; the peak plasma level of 21 ng / ml 90 minutes after 2 weeks of oral use at a dose of 30 mg per day was almost the same as the level of 18 ng / ml after the first dose.

Domperidone binds to plasma proteins by 91-93%.

Distribution studies with a radiolabeled drug in animals showed a significant distribution of the drug in tissues but low concentrations in the brain. Small amounts of the drug pass through the placenta in rats.

Domperidone undergoes rapid and intensive metabolism by hydroxylation and N-dealkylation. In vitro metabolism studies with diagnostic inhibitors have shown that the CYP3A4 isoenzyme is the main form of cytochrome P 450 involved in the N-dealkylation of domperidone, while the CYP3A4 isoenzymes CYP1A2 and CYP2E1 are involved in the aromatic hydroxylation of domperidone.

Renal and intestinal excretion is 31% and 66% of the oral dose, respectively. The proportion of the drug released unchanged is small (10% – through the intestines and approximately 1% – through the kidneys). The plasma half-life after a single oral dose is 7-9 hours in healthy volunteers, but increases in patients with severe renal insufficiency.

In such patients (serum creatinine 6 mg/100 ml, i. e. > 06 mmol/L), the half-life of domperidone increases from 74 to 208 hours, but the drug concentrations in plasma are lower than in healthy volunteers. A small amount of the unchanged drug (about 1%) is excreted by the kidneys.

In patients with moderate hepatic impairment (Child – Pugh score 7 – 9 points), the AUC and Cmax of domperidone were 29 and 15 times higher than in healthy volunteers, respectively. The unbound fraction was increased by 25% and the elimination half-life was increased from 15 to 23 hours.

In patients with mild hepatic insufficiency, the systemic exposure is lower than in healthy patients. Pharmacokinetics have not been studied in patients with severe hepatic insufficiency.

Indications

To relieve symptoms of nausea and vomiting.

Use during pregnancy and lactation

There are insufficient data on the use of domperidone during pregnancy. The use of the drug during pregnancy is contraindicated.

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. children who are breastfed may develop adverse reactions from the cardiovascular system.

In this regard, when using domperidone during breastfeeding, you should stop breastfeeding.

Contraindications

– Hypersensitivity to domperidone or any other component of the drug;

– lactose intolerance lactase deficiency, glucose-galactose malabsorption;

– denominated electrolyte disorders, or heart disease such as congestive heart failure;

– children’s age up to 12 years weighing at least 35 kg;

– simultaneous use of oral ketoconazole or erythromycin other medicines which increase the QT interval or potent inhibitors of CYP3A4 such as fluconazole voriconazole clarithromycin, amiodarone, telithromycin, etc. ;

– bleeding from the gastrointestinal tract, mechanical intestinal obstruction, perforation of the stomach or intestines;

– hepatic insufficiency moderate and severe degrees of severity;

– a prolactinoma;

– pregnancy and lactation.

With caution: Kidney failure.

Side effects

According to clinical studies

Adverse reactions observed in ≥ 1% of patients taking domperidone: depression anxiety decreased or no libido headache drowsiness akathisia dry mouth diarrhea rash pruritus galactorrhea gynecomastia breast pain and sensitivity menstrual disorders and amenorrhea lactation disorders asthenia.

Adverse reactions observed in

According spontaneous reports of adverse events

Frequency of adverse reactions listed below were determined according to the following (classification of the world health organization): very common > 1/10 often from > 1/100 to < 1/10 from uncommon > 1/1000 to < From 1/100 rare > 1/10,000 sec to < 1/1000 very rare from < 1/10000, including individual messages.

Immune system disorders

Very rare: allergic reactions including anaphylaxis anaphylactic shock anaphylactic reactions angioedema.

Disorders of the gastrointestinal tract

Rare: gastrointestinal including transient intestinal cramps; very rare: diarrhea.

Nervous system disorders

Very rare: extrapyramidal disorders convulsions increased excitability and irritability drowsiness headache.

Disorders of the cardiovascular system

Very rare: prolongation of the QT interval; frequency unknown: ventricular tachyarrhythmia of the “pirouette” type * sudden coronary death*.

Skin and subcutaneous tissue disorders

Very rare: angioedema pruritus of the skin urticaria.

Kidney and urinary tract disorders

Very rare: urinary retention.

Other services

Very rare: changes in liver function tests.

Rare: hyperprolactinemia galactorrhea gynecomastia amenorrhea.

*Some epidemiological studies have shown that the use of domperidone may be associated with an increased risk of serious ventricular arrhythmias or sudden death. The risk of these events is more likely in patients over 60 years of age and in patients taking the drug in a daily dose of more than 30 mg. It is recommended to use domperidone in the lowest effective dose in adults and children.

Interaction

Interaction with the following medications may increase the risk of prolongation of the QT interval:

Contraindicated combinations: drugs that increase the QT interval: Class IA antiarrhythmic drugs (for example, disopyramide hydroquinidine quinidine) Class III antiarrhythmic drugs (for example, amiodarone dofetilide dronedarone ibutilide sotalol) antipsychotics (e. g. haloperidol pimozide sertindol) antidepressants (e. g. citalopram escitalopram) antibiotics (erythromycin levofloxacin moxifloxacin spiramycin) antifungal medications (e. g. pentamidine) antimalarials (e. g. halofantrin lumefantrin) gastrointestinal medications (e. g. cisapride dolasetron prucalopride) antihistamines (e. g. mechitazine mizolastine) antitumor drugs (e. g. toremifene vandetanib vincamine) other drugs (e. g. bepridil difemanil methylsulfate methadone) potent CYP3A4 inhibitors (protease inhibitors azole antifungal agents some macrolide antibiotics (erythromycin clarithromycin telithromycin)).

Not recommended combinations:  moderate CYP3A4 inhibitors (diltiazem verapamil some macrolide antibiotics).

Combinations that should be used with caution: drugs that cause bradycardia and hypokalemia, as well as azithromycin and roxithromycin.

Cimetidine sodium bicarbonate other antacids and antisecretory drugs reduce the bioavailability of domperidone.

Increase the concentration of domperidone in blood plasma: azole antifungal agents macrolide antibiotics HIV protease inhibitors nefazodone.

It is compatible with the use of antipsychotic drugs (neuroleptics) with dopaminergic receptor agonists (bromocriptine levodopa).

Concomitant use with paracetamol and digoxin does not affect the concentration of these drugs in the blood.

How to take, course of use and dosage

Inside.

It is recommended to take film-coated tablets before meals if they are taken after meals, the absorption of domperidone may slow down.

Adults and children over 12 years of age with a body weight of 35 kg or more:

1 tablet (10 mg) 3 times a day. The maximum daily dose is 3 tablets (30 mg).

Usually, the duration of the course of treatment does not exceed one week.

Use in children

Domperidone film-coated tablets are indicated only for adults and children over 12 years of age with a body weight of 35 kg or more in children’s practice, domperidone should mainly be used in a different dosage form.

Use in patients with renal insufficiency

In patients with renal insufficiency, a single dose adjustment is not required. With repeated use, the frequency of taking the drug should be reduced to 1-2 times a day, depending on the severity of the disorders. You may also need to reduce the dose. These patients should be regularly evaluated (see section “Special instructions”).

Use in patients with hepatic insufficiency

No dose adjustment is required in patients with mild hepatic insufficiency. The drug is contraindicated in patients with moderate to severe hepatic insufficiency.

Overdose

Overdose symptoms are most common in children. Signs of overdose include agitation altered consciousness convulsions disorientation drowsiness and extrapyramidal reactions.

Treatment of overdose: symptomatic there is no specific antidote. Gastric lavage taking activated charcoal in case of extrapyramidal reactions – anticholinergic antiparkinsonian agents. Because of the possible increase in the QT interval, an electrocardiogram (ECG) should be monitored.

Special instructions

It is not recommended to use Domperidone for the prevention of nausea and vomiting after anesthesia.

During long-term therapy with the drug, patients should be under regular medical supervision.

Domperidone may cause prolongation of the QT interval on the ECG. In the course of post-marketing studies in patients taking domperidone, in rare cases, an increase in the QT interval and the occurrence of ventricular tachycardia of the “pirouette”type were noted. These adverse reactions were observed mainly in patients with risk factors with severe electrolyte disturbances or taking concomitant medications that increase the QT interval.

Some studies have shown that the use of domperidone can lead to an increased risk of ventricular arrhythmia or sudden coronary death (especially in patients over 60 years of age or with a single dose of more than 30 mg, as well as in patients taking concomitant drugs that increase the QT interval or CYP3A4 inhibitors).

The use of Domperidone and other drugs that can cause prolongation of the QT interval is contraindicated in patients who have an elongation of the cardiac conduction intervals, especially the QT interval in patients with severe electrolyte disorders (hypo-and hyperkalemia hypomagnesemia) or in patients with heart diseases such as chronic heart failure.

It has been shown that the presence of electrolyte disturbances (hypo – and hyperkalemia hypomagnesemia) and bradycardia in a patient may increase the risk of arrhythmia. The drug should be discontinued if you experience any symptoms that may be associated with cardiac arrhythmia. In this case, you should consult your doctor.

The drug Domperidone enhances the effect of neuroleptics when used simultaneously.

When Domperidone is co-administered with dopaminergic receptor agonists (bromocriptine levodopa), it inhibits undesirable peripheral effects, such as digestive disorders, nausea and vomiting, without affecting their central effects.

The drug is recommended to be taken at the minimum effective dose.

Influence on the ability to drive vehicles and mechanisms:

Caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions due to the risk of side effects that may affect these abilities.

Storage conditions

Store in a dark place at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf

life is 3 years.

Active ingredient

Domperidone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets