Orpra 20 mg Capsule (Delayed Release)

Uses

Each film coated MUPS tablet contains 20 mg Orpra 20 mg Capsule (Delayed Release) enteric coated micro pellets

Orpra 20 mg Capsule (Delayed Release) (Multiple-Unit Pellet System) is indixated in-

• Duodenal and Gastric ulcers
• NSAID-induced gastric and duodenal ulcers
• Reflux Oesophagitis
• GERD (Gastroesophageal Reflux Disease)
• Eradication of H. pylori with appropriate antibiotics
• Zollinger-Ellison Syndrome

MUPS is abbreviation for Multiple-Unit Pellet System. However, from pharmaceutical industry and research perspective, the term in general refers to MUPS compacted into tablets. Thus, the resulting tablets prepared by compaction of modified release coated multiparticulates or pellets are called as MUPS. It is the more recent and challenging technology that combines the advantages of both tablets and pellet filled capsules in one dosage form.

MUPS ensure rapid and uniform gastric emptying and subsequently uniform drug dissolution of pellets in the gastrointestinal tract due to their small size and larger surface, uniform drug absorption is facilitated which results in consistent and controlled pharmacological action.

A further reduction in inter- and intra-subject variability in drug absorption and clinical response is facilitated since the number of pellets per MUPS dosage form is much more than a conventional pellet-filled capsule and possibility of dose dumping(in stomach) and incomplete drug release is further minimized.

Orpra 20 mg Capsule (Delayed Release) is also used to associated treatment for these conditions: Ankylosing Spondylitis (AS), Duodenal Ulcer, Erosive Esophagitis, Gastric Ulcer, Gastro-esophageal Reflux Disease (GERD), Healing, Heartburn, Helicobacter Pylori Infection, NSAID Associated Gastric Ulcers, Osteoarthritis (OA), Rheumatoid Arthritis, Zollinger-Ellison Syndrome, Hypersecretory conditions, Multiple endocrine adenomas

How Orpra 20 mg Capsule (Delayed Release) works

Hydrochloric acid (HCl) secretion into the gastric lumen is a process regulated mainly by the H(+)/K(+)-ATPase of the proton pump , expressed in high quantities by the parietal cells of the stomach. ATPase is an enzyme on the parietal cell membrane that facilitates hydrogen and potassium exchange through the cell, which normally results in the extrusion of potassium and formation of HCl (gastric acid) .

Orpra 20 mg Capsule (Delayed Release) is a member of a class of antisecretory compounds, the substituted benzimidazoles, that stop gastric acid secretion by selective inhibition of the H+/K+ ATPase enzyme system. Proton-pump inhibitors such as omeprazole bind covalently to cysteine residues via disulfide bridges on the alpha subunit of the H+/K+ ATPase pump, inhibiting gastric acid secretion for up to 36 hours . This antisecretory effect is dose-related and leads to the inhibition of both basal and stimulated acid secretion, regardless of the stimulus .

Mechanism of H. pylori eradication

Peptic ulcer disease (PUD) is frequently associated with Helicobacter pylori bacterial infection (NSAIDs) . The treatment of H. pylori infection may include the addition of omeprazole or other proton pump inhibitors as part of the treatment regimen , . H. pylori replicates most effectively at a neutral pH . Acid inhibition in H. pylori eradication therapy, including proton-pump inhibitors such as omeprazole, raises gastric pH, discouraging the growth of H.pylori . It is generally believed that proton pump inhibitors inhibit the urease enzyme, which increases the pathogenesis of H. pylori in gastric-acid related conditions .

Dosage

Orpra 20 mg Capsule (Delayed Release) dosage

Adult:

• GERD (Gastroesophageal Reflux Disease):20 mg Once daily for 4 weeks
• Gastric ulcer:20 mg Once daily for 4-8 weeks; in severe cases Twice daily
• Duodenal ulcer:20 mg Once daily for 2-4 weeks; in severe cases Twice daily
• NSAID-induced ulceration:20 mg Once daily for 4-8 weeks
• Reflux esophagitis:20 mg Once daily for 4-8 weeks; in severe cases Twice daily
• H. pylori eradication (Orpra 20 mg Capsule (Delayed Release) MUPS tablet with Amoxicillin and Clarithromycin or Metronidazole):20 mg Twice daily for 1 week
• Zollinger-Ellison Syndrome:60 mg Once daily; Usual maintenance, 20-120mg daily

Children:

• Acid regurgitation in GERD (Gastroesophageal Reflux Disease):20 mg Once daily for 2-4 week
• Reflux esophagitis:20 mg Once daily for 4-8 weeks

Swallow the tablet whole with a glass of water. The tablet must not be chewed or crushed. OR

If the patients have trouble swallowing the tablets, put the tablet into a glass of water (Do not use other liquids). Stir the preparation until the tablets disintegrate. Then drink the liquid within 30 minutes. Stir the mixture just always before drinking.

Toxicity

Oral acute (LD50): 4000 mg/kg (mouse), 2210 mg/kg (rat) .

Overdose

Symptoms of overdose include confusion, drowsiness, blurred vision, tachycardia, nausea, diaphoresis, flushing, headache, and dry mouth.

Carcinogenesis and mutagenesis

In 24-month studies in rats, a dose-related significant increase in gastric carcinoid tumors and ECL cell hyperplasia was seen in male and female animals. Carcinoid tumors have also been found in rats treated with a fundectomy or long-term treatment with other proton pump inhibitors, or high doses of H2-receptor antagonists .

Orpra 20 mg Capsule (Delayed Release) showed positive clastogenic effects in an in vitro human lymphocyte chromosomal aberration study, in one of two in vivo mouse micronucleus tests, and in an in vivo bone marrow cell chromosomal aberration test. Orpra 20 mg Capsule (Delayed Release) tested negative in the in vitro Ames test, an in vitro mouse lymphoma cell forward mutation assay, and an in vivo rat liver DNA damage assay .

The use in breastfeeding

Limited data indicate that omeprazole may be present in human milk. There is currently no information on the effects of omeprazole on the breastfed infant or production of milk. The benefits of breastfeeding should be considered along with the level of need for omeprazole and any potential adverse effects on the breastfed infant from omeprazole .

Effects on fertility

Effects of omeprazole at oral doses up to 138 mg/kg/day in rats (about 34 times an oral human dose) was found to have no impact on fertility and reproductive performance .

Precaution

Orpra 20 mg Capsule (Delayed Release) tablet should be used carefully if the patient has severe liver dysfunction and severe renal impairment.

Interaction

Orpra 20 mg Capsule (Delayed Release) is metabolized through CYP2C19 . When starting or stopping treatment with Orpra 20 mg Capsule (Delayed Release) should be taken into account potential interactions with medicines which are CYP2C19 metabolized.

Food Interaction

• Take before a meal. Allow 30-60 minutes before a meal.

Orpra 20 mg Capsule (Delayed Release) Drug Interaction

Moderate: atorvastatin, levothyroxine, alprazolamMinor: aspirin, aspirin, duloxetine, cyanocobalaminUnknown: diphenhydramine, omega-3 polyunsaturated fatty acids, fluticasone nasal, pregabalin, metoprolol, metoprolol, acetaminophen, albuterol, montelukast, acetaminophen, ascorbic acid, cholecalciferol, cetirizine

Orpra 20 mg Capsule (Delayed Release) Disease Interaction

Major: C. diffModerate: bone fractures, hypomagnesemia

Volume of Distribution

Approximately 0.3 L/kg, corresponding to the volume of extracellular water .

Elimination Route

Orpra 20 mg Capsule (Delayed Release) delayed-release capsules contain an enteric-coated granule formulation of omeprazole (because omeprazole is acid-labile), so that absorption of omeprazole begins only after the granules exit the stomach .

Absorption of omeprazole occurs rapidly, with peak plasma concentrations of omeprazole achieved within 0.5-3.5 hours .

Absolute bioavailability (compared with intravenous administration) is approximately 30-40% at doses of 20-40 mg, largely due to pre-systemic metabolism. The bioavailability of omeprazole increases slightly upon repeated administration of omeprazole delayed-release capsules .

Half Life

0.5-1 hour (healthy subjects, delayed-release capsule)
Approximately 3 hours (hepatic impairment)

Clearance

Healthy subject (delayed release capsule), total body clearance 500 - 600 mL/min

Geriatric plasma clearance: 250 mL/min

Hepatic impairment plasma clearance: 70 mL/min

Elimination Route

After a single dose oral dose of a buffered solution of omeprazole, negligible (if any) amounts of unchanged drug were excreted in urine. Most of the dose (about 77%) was eliminated in urine as at least six different metabolites. Two metabolites were identified as hydroxyomeprazole and the corresponding carboxylic acid. The remainder of the dose was found in the feces. This suggests significant biliary excretion of omeprazole metabolites. Three metabolites have been identified in the plasma, the sulfide and sulfone derivatives of omeprazole, and hydroxyomeprazole. These metabolites possess minimal or no antisecretory activity .

Pregnancy & Breastfeeding use

Not known to be harmful. Orpra 20 mg Capsule (Delayed Release) can be used during pregnancy. Orpra 20 mg Capsule (Delayed Release) is excreted in breast milk but is not likely to influence the child when therapeutic doses are used.

Contraindication

Orpra 20 mg Capsule (Delayed Release) is contraindicated in those patients who have known hypersensitivity to any other components of the formulation.

Storage Condition

Store in a cool (below 30° C) and dry place, protected from light and moisture.

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