Omeprazole is a medication used in the treatment of gastroesophageal reflux disease, peptic ulcer disease, and Zollinger–Ellison syndrome. It is also used to prevent upper gastrointestinal bleeding in people who are at high risk. It can be taken by mouth or injected into a vein.
Mechanism of Action of Omeprazole
Omeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. By acting specifically on the proton pump, omeprazole blocks the final step in acid production, thus reducing gastric acidity. Omeprazole is a selective and irreversible proton pump inhibitor. It suppresses stomach acid secretion by specific inhibition of the H+/K+-ATPase system found at the secretory surface of gastric parietal cells. Because this enzyme system is regarded as the acid (proton, or H+) pump within the gastric mucosa, omeprazole inhibits the final step of acid production. Omeprazole also inhibits both basal and stimulated acid secretion irrespective of the stimulus. The inhibitory effect of omeprazole occurs within 1 hour after oral administration. The maximum effect occurs within 2 hours. The duration of inhibition is up to 72 hours. When omeprazole is stopped, baseline stomach acid secretory activity returns after 3 to 5 days. The inhibitory effect of omeprazole on acid secretion will plateau after 4 days of repeated daily dosing.
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Indications of Omeprazole
Omeprazole is used to treat conditions caused by too much acid production in the stomach, such as
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Omeprazole is indicated for the treatment of duodenal ulcers, benign gastric ulcers, gastroesophageal reflux disease (GERD), heartburn and other symptoms associated with GERD, and long-term treatment of pathological hypersecretory conditions like Zollinger-Ellison syndrome, multiple endocrine adenomas, and systemic mastocytosis.
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Duodenal ulcers, gastric ulcers, NSAID-associated ulcers, Helicobacter pylori eradication in peptic ulcer disease, reflux oesophagitis, and symptomatic gastro-oesophageal reflux disease and for the treatment of Zollinger-Ellison syndrome.
- To treat symptoms of GORD such as heartburn and acid regurgitation
- Gastroesophageal reflux disease (GERD)
- Erosive esophagitis (acid-related damage to the esophagus, the tube that connects your mouth to your stomach)
- Gastric (stomach) ulcers or duodenal ulcers. Duodenal ulcers occur in your duodenum. This is the first part of your small intestine. It is the part connected to your stomach.
- Conditions where your stomach makes too much acid, such as Zollinger-Ellison Syndrome
- Stomach infections caused by Helicobacter pylori bacteria.
- Ulcers in the upper part of the intestine (duodenal ulcer) or stomach (gastric ulcer).
- Ulcers which are infected with bacteria called ‘Helicobacter pylori’. If you have this condition, your doctor may also prescribe antibiotics to treat the infection and allow the ulcer to heal.
- Ulcers caused by medicines called NSAIDs (Non-Steroidal Anti-Inflammatory Drugs). omeprazole 20 mg capsules can also be used to stop ulcers from forming if you are taking NSAIDs.
- Too much acid in the stomach caused by a growth in the pancreas (Zollinger-Ellison syndrome).
- Treatment of duodenal ulcers
- Benign gastric ulcers
- Gastroesophageal reflux disease (GERD),
- Heartburn and other symptoms associated with GERD,
- Erosive esophagitis, and long-term treatment of pathological hypersecretory conditions
- Multiple endocrine adenomas,
- Systemic mastocytosis
Therapeutic Indications of Omeprazole
- Anti-Ulcer Agents; Enzyme Inhibitors
- Omeprazole is indicated for the treatment of a complex of symptoms which may be caused by any of the conditions where a reduction of gastric acid secretion is required (e.g., duodenal ulcer, gastric ulcer, nonsteroidal anti-inflammatory drugs associated gastric and duodenal ulcer, reflux esophagitis, gastroesophageal reflex disease) or when no identifiable organic cause is found (i.e., functional dyspepsia).
- Omeprazole is indicated for the treatment of heartburn and other symptoms associated with gastroesophageal reflux disease.
- Omeprazole is indicated for the short-term treatment of erosive esophagitis (associated with gastroesophageal reflux disease) that has been diagnosed by endoscopy. Omeprazole also is indicated to maintain healing of erosive esophagitis.
- Omeprazole is indicated for the long-term treatment of pathologic gastric hypersecretion associated with Zollinger-Ellison syndrome (alone or as part of multiple endocrine neoplasia Type-1), systemic mastocytosis, and multiple endocrine adenomas.
- Omeprazole is indicated in the short-term treatment of active duodenal ulcer and active benign gastric ulcer.
- Omeprazole is indicated in combination with clarithromycin (and amoxicillin or metronidazole for the treatment of duodenal and gastric ulcer associated with Helicobacter pylori infections. Eradication of H. pylori has been shown to reduce the risk of ulcer recurrence.
- Omeprazole is indicated for the treatment of duodenal or gastric ulcers associated with the use of nonsteroidal anti-inflammatory drugs (NSAIDs).
- Despite treatment with supra-physiological doses of pancreatic enzyme supplements, residual steatorrhoea is a common problem in patients with cystic fibrosis (CF) and pancreatic insufficiency.
- Strategies to enhance the activity of pancreatic enzymes include decreasing duodenal acidity. The aim of this study was to evaluate the effect of omeprazole, on fat absorption in CF patients with residual steatorrhoea despite high dose pancreatic enzyme supplements (> or =10,000 U lipase/kg per day).
- Omeprazole improves fat digestion and absorption in cystic fibrosis patients with the residual fecal fat loss despite maximal pancreatic enzyme substitution.
Contra-Indications of Omeprazole
- People with a known hypersensitivity to PPI, substituted benzimidazoles or any other component of the capsule formulation (e.g. certain dyes)
- Pregnancy
- Breastfeeding women
- People with known hypersensitivity (allergy) to PPI or any of the ingredients in the medication.
- Clostridium difficile infection
- Inadequate Vitamin B12
- Low amount of magnesium in the blood
- Liver problems
- Interstitial Nephritis
- Subacute cutaneous lupus erythematosus
- Systemic Lupus Erythematosus
- Osteoporosis
- Broken Bone
- Allergies to Proton Pump Inhibitors
Taking a proton pump inhibitor such as omeprazole may increase your risk of bone fracture in the hip, wrist, or spine. This effect has occurred mostly in people who have taken the medication long term or at high doses, and in those who are age 50 and older. It is not clear whether omeprazole is the actual cause of an increased risk of fracture.
Dosage of Omeprazole
Strengths: 2.5 mg; 2 mg/mL; 10 mg;20 mg, 40 mg; 20, 40 mg I.V
Gastroesophageal Reflux Disease
- 20 mg orally once a day
- Duration of therapy: Up to 4 weeks
Dyspepsia
Over-the-Counter (OTC) formulations
- Recommended dose: 20 mg orally once a day in the morning
- Duration of therapy: 14 days
Duodenal Ulcer
- 20 mg orally once a day
- Duration of therapy: 4 weeks
Gastric Ulcer
- 40 mg orally once a day
- Duration of therapy: 4 to 8 weeks
Erosive Esophagitis
- Treatment: 20 mg orally once a day
- Duration of therapy: 4 to 8 weeks
- Maintenance: 20 mg orally once a day
Zollinger-Ellison Syndrome
- Initial dose: 60 mg orally once a day
- Maximum dose: 360 mg/day (as 120 mg orally 3 times a day)
Helicobacter pylori Infection
- Dual therapy: 40 mg orally once a day, taken concomitantly with clarithromycin
- Duration of therapy: 14 days
- Triple therapy: 20 mg orally 2 times a day, taken concomitantly with amoxicillin and clarithromycin
- Duration of therapy: 10 days
Pediatric, Gastroesophageal Reflux Disease
1 to 16 years
- 5 to less than 10 kg: 5 mg orally once a day
- 10 to less than 20 kg: 10 mg orally once a day
- 20 kg and greater: 20 mg orally once a day
- Duration of therapy: Up to 4 weeks
- 16 to 18 years: 20 mg orally once a day
- Duration of therapy: Up to 4 weeks
Side Effects of Omeprazole
The most common
- Disturbances of the gut such as diarrhea, constipation, nausea, vomiting or abdominal pain.
- Drowsiness and lightheadedness
- Nausea and vomiting
- joint pain
- Nausea and vomiting
- Severe stomach ache
- Severe diarrhea
- Vaginal thrush
- Skin rash
- A headache
- Chest pain
- Diarrhea or loose stools
- Difficulty with breathing
- Dizziness
- Heartburn
- Muscle pain
More common
- Abdominal or stomach pain,
- Chills or fever
- A headache,
- Joint or back pain
- Muscle aching or cramping
- Muscle pains or stiffness
- Chest pressure or squeezing pain in the chest
- Excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- Constipation
- Diarrhea
- Loss of muscle coordination
- Sleepiness or unusual drowsiness
- Clumsiness or unsteadiness
- Drowsiness
Rare
- Anxiety
- change in vision
- seizures
- abnormal or fast heart rate
- tremors
- weight loss
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- a headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- muscle pains or stiffness
- chest pressure or squeezing pain in the chest
- discomfort in arms, shoulders, neck or upper back
Drug Interactions of Omeprazole
Omeprazole may interact with following drugs, supplements, & may change the efficacy of the drug
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- bisphosphonates (e.g., alendronate, etidronate)
- carbamazepine
- carvedilol
- celecoxib
- certain tyrosine kinase inhibitors (e.g. dasatinib, nilotinib)
- chlorpropamide
- cilostazol
- citalopram
- clobazam
- clopidogrel
- clozapine
- cyclosporine
- diazepam
- escitalopram
- fluoxetine
- iron salts (e.g., ferrous fumarate, ferrous sulfate)
- losartan
- methotrexate
- montelukast
- multivitamins with iron, folate
- mycophenolate
- phenobarbital
- phenytoin
- other proton pump inhibitors (e.g., esomeprazole, lansoprazole)
- “statin” anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
- tizanidine
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- trimethoprim
- warfarin
- zafirlukast
Pregnancy Catagory of Omeprazole
FDA Pregnancy Category C
Pregnancy
If you are pregnant or breastfeeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine.
Lactation
Omeprazole is excreted in breast milk but is not likely to influence the child when therapeutic doses are used. Your doctor will decide whether you can take Omeprazole 20mg Capsules if you are breastfeeding.
Before taking this medicine
You should not use this medicine if you are allergic to omeprazole or to any benzimidazole medicine such as albendazole or mebendazole. Heartburn is often confused with the first symptoms of a heart attack. Seek emergency medical attention if you have chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, and a general ill feeling.
Ask a doctor or pharmacist if it is safe for you to use omeprazole if you have other medical conditions, especially
- liver disease;
- low levels of magnesium in your blood; or
- osteoporosis or low bone mineral density (osteopenia).
Do not use over-the-counter omeprazole without the advice of a doctor if you have:
- trouble or pain with swallowing;
- bloody or black stools, vomit that looks like blood or coffee grounds;
- heartburn that has lasted for over 3 months;
- frequent chest pain, heartburn with wheezing;
- unexplained weight loss; or
- nausea or vomiting, stomach pain.he
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