Overview
11 DESCRIPTION The active ingredient in omeprazole delayed-release capsules, USP is a substituted benzimidazole, 5-methoxy-2-[[(4-methoxy-3, 5-dimethyl-2-pyridinyl) methyl] sulfinyl]-1H-benzimidazole, a compound that inhibits gastric acid secretion. Its empirical formula is C 17 H 19 N 3 O 3 S, with a molecular weight of 345.42.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Omeprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the gastric mucosa, omeprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus. 12.
Indications
- 1 INDICATIONS AND USAGE Omeprazole is a proton pump inhibitor (PPI) indicated for the: • Treatment of active duodenal ulcer in adults (1.1) • Eradication of Helicobacter pylori to reduce the risk of duodenal ulcer recurrence in adults (1.2) • Treatment of active benign gastric ulcer in adults (1.3) • Treatment of symptomatic gastroesophageal reflux disease (GERD) in patients 2 years of age and older (1.4) • Maintenance of healing of EE due to acid-mediated GERD in patients 2 years of age and older (1.6) • Pathologic hypersecretory conditions in adults (1.7) 1.
Common Doses
- 20 mg
- 1000 mg
- 500 mg
- 40 mg
Dosage
2 DOSAGE AND ADMINISTRATION Indication Recommended Adult (2.1) and Pediatric Dosage (2.2) Treatment of Active Duodenal Ulcer 20 mg once daily for 4 weeks; some patients may require an additional 4 weeks (2.1) H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence Triple Therapy: Omeprazole delayed-release capsules Amoxicillin Clarithromycin 20 mg 1000 mg 500 mg Each drug twice daily for 10 days (2.1) * Dual Therapy: Omeprazole delayed-release capsules Clarithromycin 40 mg once daily for 14 days** 500 mg three times daily for 14 days (2.
Contraindications
- 4 CONTRAINDICATIONS • Omeprazole delayed-release capsules are contraindicated in patients with known hypersensitivity reactions including anaphylaxis to the formulation or any substituted benzimidazole. Hypersensitivity reactions may include anaphylaxis, anaphylactic shock, angioedema, bronchospasm, acute tubulointerstitial nephritis, and urticaria [see Warnings and Precautions ( 5.2 ), Adverse Reactions (6) ]. • Proton pump inhibitors (PPIs), including omeprazole, are contraindicated in patients receiving rilpivirine-containing products [see Drug Interactions (7) ].
Side Effects
- 6 ADVERSE REACTIONS The following serious adverse reactions are described below and elsewhere in labeling: • Acute Tubulointerstitial Nephritis [see Warnings and Precautions (5.2) ] • Clostridium difficile -Associated Diarrhea [see Warnings and Precautions (5.3) ] • Bone Fracture [see Warnings and Precautions (5.4) ] • Cutaneous and Systemic Lupus Erythematosus [see Warnings and Precautions (5.6) ] • Cyanocobalamin (Vitamin B-12) Deficiency [see Warnings and Precautions (5.8) ] • Hypomagnesemia and Mineral Metabolism [see Warnings and Precautions (5.
Interactions
- 7 DRUG INTERACTIONS Tables 3 and 4 include drugs with clinically important drug interactions and interaction with diagnostics when administered concomitantly with omeprazole and instructions for preventing or managing them. Consult the labeling of concomitantly used drugs to obtain further information about interactions with PPIs. Table 3: Clinically Relevant Interactions Affecting Drugs Co-Administered with Omeprazole and Interaction with Diagnostics Antiretrovirals Clinical Impact: The effect of PPIs on antiretroviral drugs is variable.