COMPOSITION

Noburn TM tablet: Each tablet contains Domperidone maleate BP equivalent to Domperidone 10 mg.

PHARMACOLOGICAL INFORMATION

Pharmacological Action

Noburn is a peripheral dopamine D 2 – receptor antagonist with gastrokinetic and anti-emetic properties. It is used in the treatment of symptoms of nausea and vomiting of variable origin.. Noburn effectively increases esophageal peristalsis and lower esophageal sphincter pressure (LESP), increases gastric motility and peristalsis, enhances gastroduodenal coordination and consequently facilitates gastric emptying and decreases small bowel transit time.

Mechanism of Action

The gastroprokinetic properties of Domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis. The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level.

Pharmacokinetics

The systemic bioavailability of domperidone is only about 15% in fasting subjects given a dose by mouth, although this is increased when domperidone is given after food. The low bioavailability is thought to be due to first-pass hepatic and intestinal metabolism.

Domperidone is more than 90% bound to plasma proteins, and has a terminal elimination half-life of about 7.5 hours. It is chiefly cleared from the blood by extensive metabolism. About 30% of an oral dose is excreted in urine within 24 hours, almost entirely as metabolites; the remainder of a dose is excreted in faeces over several days, about 10% as unchanged drug. It does not readily cross the blood-brain barrier.

Small amounts of domperidone are distributed into breast milk, reaching concentrations about one-quarter of those in maternal serum.

CLINICAL INFORMATIONS

Therapeutic Indications

Dosage and Administration

The recommended oral dose for

Adults: 10-20 mg every 4-8 hours daily.

Children: 0.2-0.4 mg/kg body weight every 4-8 hours daily.

Domperidone should be taken 15-30 minutes before a meal. For acute vomiting and nausea, maximum period of treatment is 12 weeks. Use in children is restricted to nausea and vomiting following cytotoxics or radiotherapy. 

Use in Pregnancy and Lactation

Pregnant women: The safety of domperidone has not been proven and it is therefore not recommended during pregnancy. Animal studies have not demonstrated teratogenic effect in the fetus.

Lactating mother: Domperidone may precipitate galactorrhea and improve post-natal lactation. It is secreted in breast milk but in very small quantities insufficient to be considered harmful.

Use in Patient with Impaired Hepatic Function

Since domperidone is highly metabolised in the liver, Noburn TM should be used with caution in patients with hepatic impairment.

Use in Patient with Impaired Renal Function

It is unlikely that the dose needs to be adjusted for single administration in patients with renal insufficiency. However, on repeated administration the dosing frequency will need to be reduced to once or twice daily depending on the severity of the impairment . The dose may also need to be reduced. Generally, patients on prolonged therapy should be reviewed regularly.

Side Effects

Domperidone may produce hyperprolactinemia (1.3%). This may result in galactorrhea, breast enlargement, and soreness and reduced libido. Dry mouth (1%), thirst, headache (1.2%), nervousness, drowsiness (0.4%), diarrhea (0.2%), skin rash and itching (0.1%) may occur during treatment with domperidone. Extra-pyramidal reactions are seen in 0.05% of patients in clinical studies.

Contraindications

Domperidone is contraindicated to patients having known hypersensitivity to this drug and in case of neonates. It is also contraindicated in patients with prolactin releasing pituitary tumor (prolactinoma). Domperidone should not be used whenever gastro-intestinal stimulation might be dangerous i.e. gastrointestinal hemorrhage, mechanical obstruction or perforation.

Precautions

Domperidone should be used with caution in case of children because there may be increased risk of extra-pyramidal reactions in young children because of an incompletely developed blood-brain barrier. Since domperidone is highly metabolized in liver, it should be used with caution in patient with hepatic impairment. Domperidone is not recommended for chronic use or for the routine prophylaxis of postoperative nausea and vomiting.

Drug Interactions

Domperidone may antagonise the hypoprolactinaemic effect of drugs such as bromocriptine. In addition, the prokinetic effects of domperidone may alter the absorption of some drugs. Opioid analgesics and antimuscarinics may antagonise the prokinetic effects of domperidone.

Overdosage

Symptoms: Symptoms of overdosage may include drowsiness, disorientation and extrapyramidal reactions.

Treatment: There is no specific antidote to domperidone, but in the event of overdose, gastric lavage as well as the administration of activated charcoal, may be useful. Close medical supervision and supportive therapy is recommended.

Anticholinergic, anti-parkinson drugs may be helpful in controlling the extrapyramidal reactions.

PHARMACEUTICAL INFORMATION

Storage Conditions

Store in a cool and dry place and protect from light and moisture. Keep this medication out of the reach of children.

Presentation & Packaging

Noburn TM tablet : Each commercial box contains 100 tablets in alu-pvc blister packs.