Tuesday, February 5, 2013

OMEPRAZOLE

             


Omeprazole is a proton pump inhibitor used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD), laryngopharyngeal reflux (LPR) and Zollinger–Ellison syndrome. Omeprazole is one of the most widely prescribed drugs internationally and is available over the counter in some countries.
Used to treat GERD (gastroesophageal reflux disease), gastric and duodenum ulceration and gastritis.

Helicobacter pylori eradication
Omeprazole is combined with the antibiotics clarithromycin and amoxicillin (or metronidazole in penicillin-hypersensitive patients) in the 7–14 day eradication triple therapy for Helicobacter pylori. Infection by H. pylori is the causative factor in the majority of peptic ulcers.
Mechanism of action  :   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.
Pharmacokinetics  : The absorption of omeprazole takes place in the small intestine and is usually completed within 3–6 hours. The systemic bioavailability of omeprazole after repeated dose is about 60%.
Omeprazole bioavailability is significantly impaired by the presence of food and, therefore, patients should be advised to take omeprazole with a glass of water on an empty stomach (i.e., fast for at least 60 minutes before taking omeprazole). Additionally, most sources recommend that after taking omeprazole at least 30 minutes should be allowed to elapse before eating (at least 60 minutes for immediate-release omeprazole plus sodium bicarbonate products, such as Zegerid), though some sources say that with delayed-release forms of omeprazole it is not necessary to wait before eating after taking the medication. Plasma protein binding is about 95%.
Omeprazole is completely metabolized by the cytochrome P450 system, mainly in the liver. Identified metabolites are the sulfone, the sulfide and hydroxy-omeprazole, which exert no significant effect on acid secretion. About 80% of an orally given dose is excreted as metabolites in the urine and the remainder is found in the feces, primarily originating from bile secretion.



(RS)-5-methoxy-2-((4-methoxy-3,5-dimethylpyridin-2-yl) methylsulfinyl)-1H-benzo[d]imidazole

WHY IS THIS MEDICATION PRESCRIBED ?
Prescription omeprazole is used alone or with other medications to treat gastroesophageal reflux disease (GERD), a condition in which backward flow of acid from the stomach causes heartburn and possible injury of the esophagus (the tube between the throat and stomach). Prescription omeprazole is used to treat the symptoms of GERD, allow the esophagus to heal, and prevent further damage to the esophagus. Prescription omeprazole is also used to treat conditions in which the stomach produces too much acid such as Zollinger-Ellison syndrome. Prescription omeprazole is also used to treat ulcers (sores in the lining of the stomach or intestine) and it is also used with other medications to treat and prevent the return of ulcers caused by a certain type of bacteria (H. pylori). Nonprescription (over-the-counter) omeprazole is used to treat frequent heartburn (heartburn that occurs at least 2 or more days a week). Omeprazole is in a class of medications called proton-pump inhibitors. It works by decreasing the amount of acid made in the stomach.

How should this medicine be used?

Prescription omeprazole comes as a delayed-release capsule, and packets of delayed-release (long-acting) granules for suspension (to be mixed with liquid) to take by mouth. Nonprescription (over-the-counter) omeprazole comes as a delayed-release capsule or tablet to take by mouth. The delayed-release capsules and the granules should be taken at least 1 hour before a meal. They are 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 when used to treat conditions in which the stomach produces too much acid. The nonprescription delayed-release tablets or capsules are usually taken once a day in the morning at least 1 hour before eating for 14 days in a row. Additional 14-day treatments may be repeated once every 4 months if needed. To help you remember to take omeprazole, take it at around the same time(s) every day. Follow the directions on your prescription label or the package label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take omeprazole exactly as directed. Do not take more or less of it or take it more often or for a longer period of time than prescribed by your doctor or stated on the package. Tell your doctor if you have taken nonprescription omeprazole for a longer period of time than stated on the package.
If you are taking the delayed-release tablets, swallow them whole with a full glass of water. Do not split, chew, or crush them or crush and mix them into food.
Swallow the delayed-release capsules whole. If you have difficulty swallowing the delayed-release capsules, place one tablespoon of soft, cool applesauce in an empty bowl. Open the delayed-release capsule and carefully empty all the granules inside the capsule onto the applesauce. Mix the granules with the applesauce and swallow the mixture immediately with a glass of cool water. Do not chew or crush the granules. Do not store the applesauce/granule mixture for future use.
If you are taking the powder 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 powder and the contents of the prescription delayed-release capsules can both 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.
Continue to take omeprazole even if you feel well. Do not stop taking prescription omeprazole without talking to your doctor. If your condition does not improve or gets worse, call your doctor.
Ask your pharmacist or doctor for a copy of the manufacturer's information for the patient.

Other uses for this medicine

This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

What special precautions should I follow?

Before taking omeprazole,

  • tell your doctor and pharmacist if you are allergic to omeprazole, dexlansoprazole (Dexilant), esomeprazole (Nexium), lansoprazole (Prevacid), pantoprazole (Protonix), rabeprazole (Aciphex), any other medications, or any of the ingredients in the omeprazole product you will be taking. Ask your pharmacist or check the package label for a list of the ingredients.
  • tell your doctor and pharmacist what 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: certain antibiotics, including ampicillin (Principen, in Unasyn);anticoagulants ('blood thinners') such as warfarin (Coumadin); atazanavir (Reyataz); benzodiazepines such as diazepam (Valium); cilostazol (Pletal); clopidogrel (Plavix); cyclosporine (Neoral, Sandimmune); digoxin (Lanoxicaps, Lanoxin) disulfiram (Antabuse); diuretics ('water pills'); iron supplements; ketoconazole (Nizoral); methotrexate (Rheumatrex, Trexall), nelfinavir (Viracept); phenytoin (Dilantin); saquinavir (Invirase); tacrolimus (Prograf); and voriconazole (Vfend) and other prescription antifungal or anti-yeast medications. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • if you plan to take nonprescription omeprazole, tell your doctor if your heartburn has lasted 3 months or longer or if you have experienced any of the following symptoms: lightheadedness, sweating, or dizziness along with your heartburn; chest pain or shoulder pain; shortness of breath or wheezing; pain that spreads to your arms, neck, or shoulders; unexplained weight loss; nausea; vomiting, especially if the vomit is bloody; stomach pain; difficulty swallowing food or pain when you swallow food; or black or bloody stools. You may have a more serious condition that cannot be treated with nonprescription medication.
  • tell your doctor if you are of Asian descent and if you have or have ever had a low level of magnesium in your blood or liver disease.
  • if you are 50 years of age or older, ask your doctor if it is safe for you to take nonprescription or prescription omeprazole. The risk that you may develop a severe form of diarrhea caused by bacteria or that you may fracture your wrist, hip, or spine may be higher if you are an older adult.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking omeprazole, call your doctor.

What special dietary instructions should I follow?

Unless your doctor tells you otherwise, continue your normal diet.

What should I do if I forget a dose?

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

What side effects can this medication cause?

Omeprazole may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • constipation
  • gas
  • nausea
  • vomiting
  • headache

Some side effects can be serious. If you experience any of these symptoms, call your doctor immediately, or get emergency medical help: Rash,   hives,     itching   ,  swelling of the face, throat,  tongue, lips, eyes, hands, feet, ankles, or lower legs  ,         difficulty breathing or swallowing,       hoarseness       irregular, fast, or pounding heartbeat    ,    excessive tiredness     ,     dizziness   ,   lightheadedness   ,   muscle spasms,         uncontrollable shaking of a part of the body     ,     seizures  ,       diarrhea with watery stools    ,   stomach pain    ,     fever.


People who take proton pump inhibitors such as omeprazole may be more likely to fracture their wrists, hips, or spine than people who do not take one of these medications. The risk is highest in people who take high doses of one of these medications or take them for one year or longer.
Some people who take omeprazole for a long time may develop weakening of the stomach lining.
Talk to your doctor about the risks of taking omeprazole.
Omeprazole may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.
If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online [at http://www.fda.gov/Safety/MedWatch] or by phone [1-800-332-1088].

What storage conditions are needed for this medicine?

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from light, excess heat, and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.

In case of emergency/overdose

In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.

Symptoms of overdose may include the following:  confusion   ,     drowsiness ,  blurred vision,   fast or pounding heartbeat ,     nausea   ,    vomiting   ,      sweating  ,   flushing (feeling of warmth)     ,    headache  ,  dry mouth



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