Itopraz

Uses

Itopride is an acetylcholine esterase inhibitor and dopamine D2 receptor antagonist used to treat symptoms of functional dyspepsia such as nausea and vomiting.

Investigated for use/treatment in gastrointestinal diseases and disorders (miscellaneous).

Short-term treatment in healing and symptomatic relief of duodenal ulcers and erosive or ulcerative Gastroesophageal Reflux Disease (GERD).

Maintaining healing and reducing relapse rates of heartburn symptoms in patients with GERD.

Treatment of daytime and night time heartburn and other symptoms associated with GERD.

Long-term treatment of pathological hypersecretory conditions, including Zollinger Ellison Syndrome.

In combination with Amoxicillin and Clarithromycin to eradicate Helicobacter pylori.

Itopraz is also used to associated treatment for these conditions: Abdominal Pain, Dyspepsia, Functional Dyspepsia, Gastroenteritis, Loss of Appetite, Nausea, Nausea and vomiting, Vomiting, Abdominal bloating, Pyrosis, Stomach discomfortDuodenal Ulcer, Gastric Ulcer, Gastro-esophageal Reflux Disease (GERD), Heartburn, Helicobacter Pylori Infection, NSAID Associated Gastric Ulcers, Non-erosive Reflux Esophagitis Disease (NERD), Vomiting, Zollinger-Ellison Syndrome, Erosive reflux esophagitis

How Itopraz works

Itopride has anticholinesterase (AchE) activity as well as dopamine D2 receptor antagonistic activity. It is well established that M3 receptors exist on the smooth muscle layer throughout the gut and acetylcholine (ACh) released from enteric nerve endings stimulates the contraction of smooth muscle through M3 receptors. The enzyme AChE hydrolyses the released ACh, inactivates it and thus inhibits the gastric motility leading to various digestive disorders. Besides ACh, dopamine is present in significant amounts in the gastrointestinal tract and has several inhibitory effects on gastrointestinal motility, including reduction of lower esophageal sphincter and intragastric pressure. These effects appear to result from suppression of ACh release from the myenteric motor neurons and are mediated by the D2 subtype of dopamine receptors. Itopride, by virtue of its dopamine D2 receptor antagonism, removes the inhibitory effects on Ach release. It also inhibits the enzyme AchE which prevents the degradation of ACh. The net effect is an increase in ACh concentration, which in turn, promotes gastric motility, increases the lower esophageal sphincter pressure, accelerates gastric emptying and improves gastro-duodenal coordination. This dual mode of action of Itopride is unique and different from the actions of other prokinetic agents available in the market.

Rabeprazole belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but suppress gastric acid secretion by inhibiting the gastric H⁺/K⁺ATPase (hydrogen-potassium adenosine triphosphatase) at the secretory surface of the gastric parietal cell. Because this enzyme is regarded as the acid (proton) pump within the parietal cell, rabeprazole has been characterized as a gastric proton-pump inhibitor. Rabeprazole blocks the final step of gastric acid secretion. In gastric parietal cells, rabeprazole is protonated, accumulates, and is transformed to an active sulfenamide. When studied in vitro, rabeprazole is chemically activated at pH 1.2 with a half-life of 78 seconds.

Dosage

Itopraz dosage

Healing of Erosive or Ulcerative Gastroesophageal Reflux Disease (GERD): 20 mg to be taken once daily for 4 to 8 weeks. For those patients who have not healed after 8 weeks of treatment, an additional 8 week course may be considered.

Maintenance of Healing of Erosive or Ulcerative Gastroesophageal Reflux Disease (GERD Maintenance): The recommended adult oral dose is 20 mg once daily.

Treatment of Symptomatic Gastroesophageal Reflux Disease (GERD):The recommended adult oral dose is 20 mg once daily for 4 weeks. If symptoms do not resolve completely after 4 weeks, an additional course of treatment may be considered.

Healing of Duodenal Ulcers:The recommended adult oral dose is 20 mg once daily after the morning meal for a period up to four weeks. Most patients with duodenal ulcer heal within four weeks. A few patients may require additional therapy to achieve healing.

Helicobacter pylori Eradication:To Reduce the Risk of Duodenal Ulcer Recurrence-

• Rabeprazole Sodium 20 mg Twice Daily for 7 Days
• Amoxicillin 1000 mg Twice Daily for 7 Days
• Clarithromycin 500 mg Twice Daily for 7 Days

All three medications should be taken twice daily with the morning and evening meals. It is important that patients comply with the full 7-day regimen.

Treatment of Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome: The dosage of Rabeprazole Sodium in patients with pathologic hypersecretory conditions varies with the individual patient. The recommended adult oral starting dose is 60 mg once a day. Doses should be adjusted to individual patient needs and should continue for as long as clinically indicated. Some patients may require divided doses. Doses up to 100 mg QD and 60 mg BID have been administered. Some patients with Zollinger-Ellision syndrome have been treated continuously with Rabeprazole Sodium for up to one year.

Side Effects

Rabeprazole Sodium may sometimes cause headache, diarrhoea, abdominal pain, vomiting, constipation, dry mouth, increased or decreased appetite, muscle pain, drowsiness and dizziness.

Precaution

Administration of Rabeprazole Sodium to patients with mild to moderate liver impairment resulted in increased exposure and decreased elimination. Caution should be exercised in patients with severe hepatic impairment.

Interaction

Rabeprazole is metabolized by the Cytochrome P-450 (CYP-450) drug metabolizing enzyme system. Rabeprazole does not have clinically significant interactions with other drugs metabolized by the CYP-450 system,such as Warfarin and Theophylline given as single oral dose, Diazepam as a single intravenous dose, and Phenytoin given as a single intravenous dose. In normal subjects, co-administration of Rabeprazole 20 mg QD resulted in an approximately 30% decrease in the bioavailability of Ketoconazole and increase in the AUC and Cmax for digoxin of 90% and 29% respectively.

Elimination Route

Absolute bioavailability is approximately 52%.

Half Life

1-2 hours (in plasma)

Elimination Route

Following a single 20 mg oral dose of 14C-labeled rabeprazole, approximately 90% of the drug was eliminated in the urine, primarily as thioether carboxylic acid; its glucuronide, and mercapturic acid metabolites.

Pregnancy & Breastfeeding use

Rabeprazole is FDA Pregnancy Category B. No data is available on administration of Rabeprazole to pregnant women. However this drug should be used during pregnancy, only if clearly needed. There are no data on the excretion of Rabeprazole into the breast milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the benefit of the drug to the mother.

Contraindication

Rabeprazole Sodium is contraindicated in patient with known hypersensitivity to Rabeprazole or to any component in the product.

Special Warning

Use in pediatric patients: The safety and effectiveness of Rabeprazole in pediatric patients have not been established.

Acute Overdose

There has been no experience with large overdoses with Rabeprazole. No specific antidote for Rabeprazole is known. Rabeprazole is extensively protein bound and is not readily dialyzable. In the event of overdosage, treatment should be symptomatic and supportive.

Storage Condition

Store below 25°C, protected from light and moisture. Keep all medicines out of the reach of the children.

Innovators Monograph

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