Draspazol^® (Tablets) Instructions for Use

Marketing Authorization Holder

Artelar, LLC (Russia)

Manufactured By

Avva Rus, JSC (Russia)

ATC Code

A03FA03 (Domperidone)

Active Substance

Domperidone (Rec.INN registered by WHO)

Dosage Form

Draspazol®

Film-coated tablets, 10 mg: 10, 20, 30, 40, or 50 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white in color, round, biconvex; the core is white on the cross-section.

Excipients: lactose monohydrate – 49 mg, microcrystalline cellulose 102 – 10 mg, povidone K17 – 10 mg, magnesium stearate – 1 mg, corn starch – up to a core tablet weight of – 100 mg.

Coating composition: hypromellose – 1.74 mg, macrogol 6000 – 0.26 mg.

10 pcs. – blister packs (1) – cardboard packs.
10 pcs. – blister packs (2) – cardboard packs.
10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (4) – cardboard packs.
10 pcs. – blister packs (5) – cardboard packs.

Clinical-Pharmacological Group

Centrally acting antiemetic drug blocking dopamine receptors

Pharmacotherapeutic Group

Means for the treatment of functional disorders of the gastrointestinal tract; gastrointestinal motility stimulants

Pharmacological Action

Antiemetic agent. It has an antiemetic effect, soothes hiccups and in some cases eliminates nausea. The action is due to the blockade of central dopamine receptors. This eliminates the inhibitory effect of dopamine on the motor function of the gastrointestinal tract and increases the evacuation and motor activity of the stomach.

Pharmacokinetics

Absorption after oral administration, on an empty stomach, is rapid (administration after meals, reduced gastric acidity slow down and reduce absorption). C_max is reached in 1 h. Bioavailability is 15% (first-pass effect through the liver). Plasma protein binding is 90%. It penetrates into various tissues, poorly passes through the blood-brain barrier. It is metabolized in the liver and in the intestinal wall (by hydroxylation and N-dealkylation). It is excreted through the intestine 66%, by the kidneys – 33%, including unchanged – 10% and 1%, respectively. T_1/2 is 7-9 h, in severe chronic renal failure it is prolonged.

Indications

Nausea, vomiting, hiccups of various origins (in toxemia, radiation therapy, dietary violations, intake of certain drugs /morphine/, endoscopic and radiopaque studies, in the postoperative period). Postoperative hypotension and atony of the stomach and intestines, biliary dyskinesia, flatulence, reflux esophagitis, cholecystitis, cholangitis, various types of dyspepsia. Nausea and vomiting caused by the intake of dopamine mimetics.

ICD codes

Dosage Regimen

Administer orally.

Determine the dose individually based on age and clinical presentation.

For adults and adolescents 12 years and older (with body weight of 35 kg or more), the usual dose is 10 mg (one tablet) taken three to four times daily.

Take the tablet 15-30 minutes before meals.

Do not exceed a maximum daily dose of 30 mg (three tablets).

The duration of treatment should not exceed one week without medical reassessment.

For patients with severe renal impairment (serum creatinine level exceeding 6 mg/100 ml), reduce the dosing frequency to once or twice daily.

In cases of moderate to severe hepatic impairment, exercise caution and consider dose reduction due to decreased first-pass metabolism.

This drug is contraindicated in children under 12 years of age and in children with a body weight less than 35 kg.

Adverse Reactions

From the central nervous system rarely – increased excitability and/or extrapyramidal disorders, headache.

From the digestive system smooth muscle spasms of the gastrointestinal tract organs, dry mouth, thirst.

Allergic reactions itching, rash, urticaria.

Other increased plasma prolactin level, galactorrhea, gynecomastia.

Contraindications

Gastrointestinal bleeding, mechanical intestinal obstruction, perforation of the stomach or intestine, prolactinoma, pregnancy, lactation period (breastfeeding), hypersensitivity to domperidone; children under 12 years of age and body weight less than 35 kg (for tablets).

Use in Pregnancy and Lactation

Domperidone is contraindicated for use during pregnancy and lactation.

Use in Hepatic Impairment

Should be used with caution in liver function disorders.

Use in Renal Impairment

Should be used with caution in renal function disorders. In renal failure, the frequency of administration should be reduced.

Pediatric Use

Contraindicated in children under 1 year of age (under 5 years and children with body weight under 20 kg – for tablets).

Special Precautions

Should be used with caution in liver and kidney function disorders.

Drugs containing Domperidone should be administered to children in dosage forms intended for the appropriate age.

Drug Interactions

With simultaneous use with antacids, antisecretory drugs (including cimetidine, sodium bicarbonate) the bioavailability of domperidone decreases.

With simultaneous use with anticholinergic drugs, the effect of domperidone is suppressed.

Since Domperidone is metabolized mainly with the participation of the CYP3A4 isoenzyme, it is believed that with the simultaneous use of domperidone and inhibitors of this isoenzyme (including azole group antifungal drugs, macrolide group antibiotics, HIV protease inhibitors, nefazodone), an increase in the plasma level of domperidone is possible.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.