Omeprazole

What is Omeprazole?

• Omeprazole (Prilosec; Prilosec OTC) is a proton pump inhibitor (PPI) widely used in the therapy of gastroesophageal reflux and peptic ulcer disease.

Omeprazole

Omeprazole enantiomers

What are the uses of this medicine?

Omeprazole (Prilosec; Prilosec OTC) used in adults:

• for up to 8 weeks for the healing of duodenal ulcers. The duodenal area is the area where food passes when it leaves the stomach.
• with certain antibiotics for 10 to 14 days to treat an infection caused by bacteria called H. pylori. If needed, your doctor may decide to prescribe another 14 to 18 days of omeprazole delayed-release capsules by itself after the antibiotics. Sometimes H. pylori bacteria can cause duodenal ulcers. The infection needs to be treated to prevent the ulcers from coming back.
• for up to 8 weeks for healing stomach ulcers.
• for up to 4 weeks to treat heartburn and other symptoms that happen with gastroesophageal reflux disease (GERD).
• GERD happens when acid in your stomach backs up into the tube (esophagus) that connects your mouth to your stomach. This may cause a burning feeling in your chest or throat, sour taste, or burping.
• for up to 8 weeks to heal acid-related damage to the lining of the esophagus (called erosive esophagitis or EE). If needed, your doctor may decide to prescribe another 4 weeks of omeprazole delayed-release capsules.
• to maintain healing of the esophagus. It is not known if omeprazole delayed-release capsules are safe and effective when used for longer than 12 months (1 year) for this purpose.
• for the long-term treatment of conditions where your stomach makes too much acid. This includes a rare condition called Zollinger-Ellison Syndrome.

For children 2 to 16 years of age, omeprazole delayed-release capsules are used:

• for up to 4 weeks to treat heartburn and other symptoms that happen with gastroesophageal reflux disease (GERD).
• for up to 8 weeks to treat gastroesophageal reflux disease (GERD) with acid-related damage to the lining of the esophagus [called erosive esophagitis (or EE) due to acid-mediated GERD].
• to maintain healing of the esophagus. It is not known if omeprazole delayed-release capsules are safe and effective when used longer than 12 months (1 year) for this purpose.

How does this medicine work?

Omeprazole Mechanism V1

• Omeprazole (oh mep' ra zole), like other PPIs, inhibits gastric acid production by binding to and inactivating the H+/K+-ATPase of gastric parietal cells, causing inhibition of the proton pump that transports H+ into the gastric lumen, the common final step in gastric acid production.
• Omeprazole is a prodrug and is converted to the active form (sulfenic acid) in the acidic secretory canaliculi of parietal cells.
• Because the inhibition is irreversible, acid secretion is suppressed for 24 to 48 hours, until new proton pump molecules have been synthesized and transported to the cell membrane.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• known hypersensitivity reactions including anaphylaxis to the formulation.
• in patients receiving rilpivirine-containing products.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• anticoagulants ('blood thinners') such as warfarin (Jantoven), atazanavir (Reyataz, in Evotaz), cilostazol, citalopram (Celexa), clopidogrel (Plavix), cyclosporine (Gengraf, Neoral, Sandimmune), dasatinib (Sprycel), diazepam (Valium, Valtoco), digoxin ( Lanoxin), disulfiram, diuretics ('water pills'), erlotinib (Tarceva), iron supplements, itraconazole (Sporanox, Tolsura), ketoconazole, methotrexate (Trexall, Xatmep), mycophenolate mofetil (Cellcept, Myfortic), nelfinavir (Viracept), nilotinib (Tasigna), phenytoin (Dilantin, Phenytek), rifampin (Rifadin, Rimactane), ritonavir (Norvir, in Kaletra), saquinavir (Invirase), tacrolimus (Astagraf, Envarsus, Prograf), voriconazole (Vfend), St. John's wort and rilpivirine (Edurant, in Cabenuva, Complera, Odefsey).

Is this medicine FDA approved?

• Omeprazole was the first PPI approved for use in the United States (1989), initially only for the indication of severe peptic ulcer disease and Zollinger-Ellison syndrome.
• Subsequently, the indications for its use have broadened to routine peptic ulcer disease, gastroesophageal reflux disease and prevention of stress ulcers.
• Omeprazole and esomeprazole are two of the most widely used medications in clinical practice with more than 20 million prescriptions filled yearly in the United States alone.
• Omeprazole is available in multiple forms including 10, 20 and 40 mg standard and delayed release capsules and powder for oral suspension in generic forms and under the brand name of Prilosec.

How should this medicine be used?

Recommended dosage: In Adults:

For Treatment of Active Duodenal Ulcer:

• 20 mg once daily upto 4 weeks.

For Helicobacter pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence:

Triple Therapy:

• Omeprazole 20 mg Amoxicillin 1000 mg Clarithromycin 500 mg.
• Take all three drugs twice daily for 10 days.
• In patients with an ulcer present at the time of initiation of therapy, continue omeprazole 20 mg once daily for an additional 18 days for ulcer healing and symptom relief.

Dual Therapy:

• Omeprazole 40 mg once daily Clarithromycin 500 mg three times daily for 14 days.
• In patients with an ulcer present at the time of initiation of therapy, an additional 14 days of omeprazole 20 mg once daily is recommended for ulcer healing and symptom relief.

For Active Benign Gastric Ulcer:

• 40 mg once daily upto 4 to 8 weeks.

For Treatment of Symptomatic GERD:

• 20 mg once daily Up to 4 weeks.

For Treatment of EE due to Acid-Mediated GERD:

• 20 mg once daily upto 4 to 8 weeks.

Maintenance of Healing of EE due to Acid-Mediated GERD:

• 20 mg once daily.
• Controlled studies do not extend beyond 12 months.

Pathological Hypersecretory Conditions:

• Starting dose is 60 mg once daily; adjust to patient needs
• Daily dosages of greater than 80 mg should be administered in divided doses.
• Dosages up to 120 mg three times daily have been administered as long as clinically indicated.
• Some patients with Zollinger-Ellison syndrome have been treated continuously for more than 5 years.

In pediatric patients (2 to 16 years):

Treatment of Symptomatic GERD:

• 10 to less than 20 kg: 10 mg Once daily for up to 4 weeks.
• 20 kg and greater: 20 mg Once daily for up to 4 weeks.

Treatment of EE due to Acid-Mediated GERD:

• 10 to less than 20 kg: 10 mg once daily for 4 to 8 weeks.
• 20 kg and greater: 20 mg once daily for 4 to 8 weeks.

Maintenance of Healing of EE due to Acid-Mediated GERD:

• 10 to less than 20 kg: 10 mg Once daily. Controlled studies do not extend beyond 12 months
• 20 kg and greater: 20 mg

Administration:

• Prescription omeprazole comes as a delayed-release capsule, and packets of delayed-release granules for suspension to take by mouth or give through a feeding tube. Nonprescription (over-the-counter) omeprazole comes as a delayed-release tablet to take by mouth.
• Prescription omeprazole is usually taken once a day before a meal but may be taken twice a day when used with other medications to eliminate H. pylori, or up to three times a day, before meals when used to treat conditions in which the stomach produces too much acid.
• The nonprescription delayed-release tablets are usually taken once a day in the morning at least 1 hour before eating for 14 days in a row.
• If needed, additional 14-day treatments may be repeated, not more often than once every 4 months.
• Take omeprazole delayed-release capsules before meals.
• Antacids may be used concomitantly with omeprazole delayed-release capsules.
• If a dose is missed, administer as soon as possible. However, if the next scheduled dose is due, do not take the missed dose, and take the next dose on time. Do not take two doses at one time to make up for a missed dose.

omeprazole delayed-release capsules:

• Swallow omeprazole delayed-release capsules whole; do not chew.
• For patients unable to swallow an intact capsule, omeprazole delayed-release capsules can be opened and administered as follows:
• Place one tablespoon of applesauce into a clean container (e.g., empty bowl). The applesauce used should not be hot and should be soft enough to be swallowed without chewing.
• Open the capsule.
• Carefully empty all of the pellets inside the capsule on the applesauce.
• Mix the pellets with the applesauce.
• Swallow applesauce and pellets immediately with a glass of cool water to ensure complete swallowing of the pellets. Do not chew or crush the pellets. Do not save the applesauce and pellets for future use.

Omeprazole Granules for oral suspension:

• If you are taking the granules for oral suspension, you will need to mix it with water before use.
• If you are using the 2.5-mg packet, place 1 teaspoonful (5 mL) of water in a container.
• If you are using the 10-mg packet, place 1 tablespoonful (15 mL) of water in a container.
• Add the contents of the powder packet and stir.
• Wait 2 to 3 minutes to allow the mixture to thicken, and stir the mixture again.
• Drink the entire mixture within 30 minutes.
• If any of the mixture is stuck to the container, pour more water into the container, stir and drink all the mixture immediately.
• The granules for oral suspension can be given through a feeding tube.
• If you have a feeding tube, ask your doctor how you should take the medication.
• Follow the directions carefully.

• Do not take nonprescription omeprazole for immediate relief of heartburn symptoms.
• It may take 1 to 4 days for you to feel the full benefit of the medication.
• Call your doctor if your symptoms get worse or do not improve after 14 days or if your symptoms return sooner than 4 months after you finish your treatment.
• Do not take nonprescription omeprazole for longer than 14 days or treat yourself with omeprazole more often than once every 4 months without talking to your doctor.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As a delayed-release capsule, and packets of delayed-release granules for suspension

This medicine is available in fallowing brand namesː

• Prilosec; Prilosec OTC

What side effects can this medication cause?

The most common side effects of this medicine may include:

• Headache
• Nausea
• vomiting
• stomach pain
• diarrhea
• gas

In addition to the side effects listed above, the most common side effects in children 1 to 16 years of age include:

• respiratory system event
• fever

Other side effects:

• Serious allergic reactions
• rash
• throat tightness
• face swelling
• difficulty breathing

Omeprazole delayed-release capsules can cause serious side effects, including:

• acute tubulointerstitial nephritis
• Diarrhea
• Bone fractures
• Certain types of lupus erythematosus
• Vitamin B-12 deficiency
• Low magnesium levels in your body
• fundic gland polyps
• Severe skin reactions

What special precautions should I follow?

• In adults, symptomatic response does not preclude the presence of gastric malignancy. Consider additional follow-up and diagnostic testing.
• Acute tubulointerstitial nephritis (TIN) has been observed in patients taking PPIs and may occur at any point during PPI therapy. Discontinue omeprazole delayed-release capsules and evaluate patients with suspected acute TIN.
• PPI therapy like omeprazole may be associated with an increased risk of Clostridium difficile-associated diarrhea, especially in hospitalized patients. Patients should use the lowest dose and shortest duration of PPI therapy appropriate to the condition being treated.
• Proton pump inhibitor (PPI) therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist, or spine. Patients at risk for osteoporosis-related fractures should be managed according to established treatment guidelines.
• Severe cutaneous adverse reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), drug reaction with eosinophilia and systemic symptoms (DRESS), and acute generalized exanthematous pustulosis (AGEP) have been reported in association with the use of PPIs. Discontinue omeprazole at the first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and consider further evaluation.
• Cutaneous lupus erythematosus (CLE) and systemic lupus erythematosus (SLE) have been reported in patients taking PPIs, including omeprazole. Avoid administration of PPIs for longer than medically indicated. If signs or symptoms consistent with CLE or SLE are noted in patients receiving omeprazole, discontinue the drug and refer the patient to the appropriate specialist for evaluation.
• Avoid concomitant use of omeprazole with clopidogrel. Clopidogrel is a prodrug.
• Daily treatment with any acid-suppressing medications over a long period of time (e.g., longer than 3 years) may lead to malabsorption of cyanocobalamin (vitamin B-12) caused by hypo- or achlorhydria.
• Hypomagnesemia, symptomatic and asymptomatic, has been reported rarely in patients treated with PPIs for at least three months, in most cases after a year of therapy. Consider monitoring magnesium and calcium levels prior to initiation of omeprazole and periodically while on treatment in patients with a preexisting risk of hypocalcemia (e.g., hypoparathyroidism). Supplement with magnesium and/or calcium, as necessary. If hypocalcemia is refractory to treatment, consider discontinuing the PPI.
• Avoid concomitant use of omeprazole with St. John’s Wort or rifampin.
• Serum chromogranin A (CgA) levels increase secondary to drug-induced decreases in gastric acidity. The increased CgA level may cause false positive results in diagnostic investigations for neuroendocrine tumors.
• Concomitant use of PPIs with methotrexate (primarily at high dose) may elevate and prolong serum levels of methotrexate and/or its metabolite, possibly leading to methotrexate toxicities.
• PPI use is associated with an increased risk of fundic gland polyps that increases with long-term use, especially beyond one year. Use the shortest duration of PPI therapy appropriate to the condition being treated.
• Omeprazole passes into your breast milk. Talk to your doctor about the best way to feed your baby if you take omeprazole delayed-release capsules.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• confusion, drowsiness, blurred vision, tachycardia, nausea, vomiting, diaphoresis, flushing, headache, dry mouth.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• No specific antidote for omeprazole overdosage is known.
• Omeprazole is extensively protein bound and is, therefore, not readily dialyzable.
• In the event of overdosage, treatment should be symptomatic and supportive.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies with omeprazole in pregnant women.
• Available epidemiologic data fail to demonstrate an increased risk of major congenital malformations or other adverse pregnancy outcomes with first trimester omeprazole use.
• It is not known if omeprazole delayed-release capsules will harm your unborn baby.

Can this medicine be used in children?

• The safety and effectiveness of omeprazole delayed-release capsules have been established in pediatric patients 2 to 16 years for the treatment of symptomatic GERD, treatment of EE due to acid-mediated GERD, and maintenance of healing of EE due to acid-mediated GERD.

The safety and effectiveness of omeprazole have not been established in: patients less than 1 year of age for:

• Treatment of symptomatic GERD
• Maintenance of healing of EE due to acid-mediated GERD

pediatric patients for:

• Treatment of active duodenal ulcer
• H. pylori eradication to reduce the risk of duodenal ulcer recurrence
• Treatment of active benign gastric ulcer
• Pathological hypersecretory conditions

• Patients less than 1 month of age for any indication.

What are the active and inactive ingredients in this medicine?

• Active ingredient: Omeprazole

• Inactive ingredients: The 10 mg and 20 mg capsule contains the following inactive ingredients: anhydrous lactose, low-substituted hydroxypropyl cellulose, magnesium oxide, magnesium stearate, microcrystalline cellulose, methacrylic acid copolymer dispersion type C, polysorbate 80, povidone and talc, triethyl citrate. The capsule shells for the 10 mg have the following inactive ingredients: black iron oxide, gelatin, red iron oxide, titanium dioxide and yellow iron oxide. The capsule shells for the 20 mg have the following inactive ingredients: gelatin and titanium dioxide. The ink used for printing contains: black iron oxide, propylene glycol and shellac.

• The 40 mg capsule contains the following inactive ingredients: acetone, anhydrous lactose, croscarmellose sodium, dehydrated alcohol, dibutyl sebacate, hypromellose phthalate, low-substituted hydroxypropyl cellulose, microcrystalline cellulose, polysorbate 80, povidone and talc. The capsule shells for the 40 mg have the following inactive ingredients: hypromellose, red iron oxide, titanium dioxide, and yellow iron oxide. In addition, the capsule shells may also contains black iron oxide, carrageenan, and potassium chloride. The ink used for printing contains black iron oxide.

Who manufactures and distributes this medicine?

Manufactured by:

• Lek Pharmaceuticals d.d., Ljubljana, Slovenia for
• Sandoz Inc., Princeton, NJ

What should I know about storage and disposal of this medication?

• Store omeprazole delayed-release capsules at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep the container of omeprazole delayed-release capsules closed tightly.
• Keep the container of omeprazole delayed-release capsules dry and away from light.

The antiulcer agents in clinical use

Proton Pump Inhibitors

• Dexlansoprazole
• Esomeprazole
• Lansoprazole
• Omeprazole
• Pantoprazole
• Rabeprazole

Selective Histamine Type 2 Receptor Antagonists or H2 Blockers

• Cimetidine
• Famotidine
• Nizatidine
• Ranitidine

• Dailymed label info on Omeprazole
• FDA Omeprazole

Omeprazole Resources
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