Xelopes40 mg

Gastroesophageal Reflux Disease (GERD)

Xelopes is FDA-approved for the treatment of symptomatic GERD and for the treatment and maintenance of healing of erosive esophagitis.

Duodenal Ulcer

Xelopes is FDA-approved for short-term treatment (typically 4 weeks) of active duodenal ulcer, and, in combination with antibacterial regimens, for Helicobacter pylori eradication to reduce the risk of duodenal ulcer recurrence.

Gastric Ulcer

Xelopes is FDA-approved for short-term treatment (4-8 weeks) of active benign gastric ulcer.

NSAID-Associated Ulcer

Xelopes is FDA-approved for risk reduction of NSAID-associated gastric ulcer in patients requiring continued NSAID use, and for healing of NSAID-associated ulcers.

Helicobacter pylori Eradication

Xelopes is FDA-approved as part of combination regimens (with antibiotics such as clarithromycin and amoxicillin) for H. pylori eradication; it is not effective as monotherapy for this indication and requires combination therapy.

Pathological Hypersecretory Conditions

Xelopes is FDA-approved for long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome, multiple endocrine adenomas, and systemic mastocytosis.

Prevention of Acid Aspiration / Stress Ulcer Prophylaxis (Adjunct, Guideline/Practice-Supported Use)

Xelopes is also used, based on clinical practice and guideline support rather than a specific FDA-labeled indication in every case, for prophylaxis of acid aspiration during general anesthesia and for stress ulcer prophylaxis in select critically ill patients; such use should be directed by a physician.

Each dose contains Omeprazole as the active ingredient, typically formulated as enteric-coated (delayed-release) granules to protect the drug from degradation by gastric acid. In Bangladesh, Omeprazole is available as 10 mg, 20 mg, and 40 mg enteric-coated capsules and tablets, oral powder sachets (20 mg, 40 mg) for suspension, and a 40 mg/vial injection for intravenous use.

Xelopes is a proton pump inhibitor (PPI) used to reduce the amount of acid produced in the stomach. It is widely prescribed for conditions such as gastroesophageal reflux disease (GERD), peptic ulcer disease, and, in combination with antibiotics, for the eradication of Helicobacter pylori infection. Xelopes works by irreversibly blocking the hydrogen-potassium-adenosine triphosphatase (H+/K+-ATPase) enzyme system, often called the gastric proton pump, in the parietal cells of the stomach lining, which is the final step in gastric acid secretion. Xelopes is available in oral delayed-release capsule, tablet, and oral suspension forms, as well as an intravenous injection for patients who cannot take medication by mouth. Xelopes is not an antibiotic and has no direct antibacterial activity on its own.

Proton Pump Inhibitor (PPI)

Omeprazole is a substituted benzimidazole that is acid-labile and is therefore formulated as enteric-coated granules to allow absorption in the small intestine after passing through the acidic stomach. After oral administration, Omeprazole is absorbed rapidly, with peak plasma concentrations reached within 0.5 to 3.5 hours; bioavailability increases from about 35% after a single dose to approximately 60% with once-daily repeated dosing. Omeprazole is a prodrug that accumulates in the acidic environment of the parietal cell canaliculi, where it is converted to its active sulfenamide form, which irreversibly binds to and inhibits the H+/K+-ATPase enzyme, blocking the final common pathway of gastric acid secretion regardless of the stimulus. The onset of the antisecretory effect occurs within one hour, with the maximum effect within two hours, and the inhibitory effect on acid secretion can last up to 72 hours because new enzyme synthesis is required to restore acid secretion. Omeprazole is extensively metabolized in the liver, primarily by the CYP2C19 and, to a lesser extent, CYP3A4 enzyme pathways, with a plasma elimination half-life of about 0.5 to 1 hour in patients with normal hepatic function; metabolites are excreted mainly in the urine, with the remainder eliminated in the feces.

• Take Xelopes before eating, ideally in the morning before breakfast.
• Swallow delayed-release capsules or tablets whole with water; do not crush or chew them, as this destroys the enteric coating that protects the drug from stomach acid.
• For patients unable to swallow capsules whole, the capsule may be opened and the intact granules mixed with a small amount of soft, non-hot, mildly acidic food such as applesauce, and swallowed immediately without chewing, only as directed by a physician or pharmacist.
• The oral suspension/sachet formulation of Xelopes should be prepared and taken exactly as instructed on the product label or by a pharmacist.
• Do not stop Xelopes abruptly after prolonged use without medical advice, as this may cause rebound acid hypersecretion; a physician may recommend tapering.
• If a dose is missed, take it as soon as remembered unless it is almost time for the next dose; do not double the dose.

• Clopidogrel: Xelopes inhibits the CYP2C19 enzyme required to convert clopidogrel to its active metabolite, reducing clopidogrel's antiplatelet effect and potentially increasing the risk of cardiovascular events in patients relying on clopidogrel; concomitant use should be avoided, and an alternative strategy should be discussed with a physician.
• Methotrexate (high-dose): concomitant use with Xelopes may elevate and prolong methotrexate and/or its metabolite levels, increasing the risk of methotrexate toxicity; temporary withdrawal of Xelopes may be considered in patients receiving high-dose methotrexate.
• Drugs dependent on gastric pH for absorption (e.g., ketoconazole, itraconazole, atazanavir, iron salts): by raising gastric pH, Xelopes can significantly reduce the absorption and effectiveness of these drugs.
• Warfarin: Xelopes can increase warfarin plasma levels and prothrombin time/INR, raising bleeding risk; INR should be monitored more closely when Xelopes is started or stopped.
• Diazepam and phenytoin: Xelopes inhibits their hepatic metabolism (via CYP2C19), which can increase plasma levels of these drugs; dose adjustment or monitoring may be needed.
• Clarithromycin: when used together (as in H. pylori regimens), plasma levels of both Xelopes and clarithromycin increase; this is generally accounted for in combination regimen dosing.
• St. John's Wort and rifampin: these CYP enzyme inducers can substantially decrease Xelopes plasma levels and reduce its efficacy.

Common Side Effects

The most common side effects reported with Xelopes include the following:

• Headache
• Abdominal pain
• Nausea and vomiting
• Diarrhea
• Constipation
• Flatulence

Serious Side Effects (Seek Medical Attention)

• Signs of a severe allergic reaction: rash, hives, facial or throat swelling, difficulty breathing, or anaphylaxis
• Severe, watery, or bloody diarrhea that does not improve, which may indicate Clostridioides difficile-associated diarrhea (see Precautions and Warnings)
• Signs of low magnesium: seizures, abnormal or fast heart rhythm, tremors, muscle spasms, or persistent muscle cramps (see Precautions and Warnings)
• New or worsening joint pain with a rash on the cheeks or arms that worsens in sunlight, which may indicate cutaneous or systemic lupus erythematosus
• Yellowing of the skin or eyes, dark urine, or severe stomach pain, which may indicate liver problems
• Severe skin reactions such as blistering or peeling skin (Stevens-Johnson syndrome/toxic epidermal necrolysis)
• Signs of a low blood cell count: unusual bruising, bleeding, fever, or infections that do not go away

Pregnancy

Data from multiple epidemiological studies and case series have not shown a clear increase in the risk of major birth defects, miscarriage, or other adverse fetal outcomes with Xelopes use during pregnancy. However, Xelopes should be used during pregnancy only if clearly needed and if the potential benefit to the mother justifies the potential risk to the fetus; a physician should always be consulted before using Xelopes during pregnancy.

Breastfeeding

Xelopes passes into breast milk in small amounts. Because of the theoretical possibility of adverse effects in the nursing infant, a decision to continue or discontinue breastfeeding, or to continue or discontinue Xelopes, should be made in consultation with a physician, weighing the benefits of breastfeeding against the mother's clinical need for Xelopes.

• Gastric malignancy: symptomatic response to Xelopes does not exclude the presence of gastric malignancy; the possibility of gastric cancer should be considered, particularly in patients with alarm symptoms (e.g., weight loss, recurrent vomiting) or new-onset symptoms after age 50, before starting treatment.
• Clostridioides difficile-associated diarrhea: proton pump inhibitors including Xelopes may increase the risk of C. difficile-associated diarrhea; patients should seek medical care for persistent diarrhea that does not improve.
• Bone fracture risk: long-term (particularly more than one year) or high-dose Xelopes use has been associated with an increased risk of osteoporosis-related fractures of the hip, wrist, or spine; the lowest effective dose for the shortest duration appropriate to the condition should be used, and adequate calcium/vitamin D intake and bone health monitoring may be considered for long-term users.
• Hypomagnesemia: prolonged Xelopes use (generally more than three months) can cause low blood magnesium, which may present with tetany, seizures, arrhythmia, or muscle spasm; magnesium levels may be checked before starting long-term therapy and periodically during treatment, especially in patients also taking digoxin or diuretics.
• Vitamin B12 deficiency: long-term Xelopes use (typically more than 3 years) may reduce absorption of vitamin B12, potentially leading to deficiency.
• Interaction with clopidogrel: concomitant use should be avoided; see Interaction.
• Cutaneous and systemic lupus erythematosus: proton pump inhibitors including Xelopes may cause new-onset or exacerbation of existing lupus erythematosus; new symptoms should be evaluated promptly, and discontinuation with referral considered if lupus is diagnosed.
• Rebound acid hypersecretion: stopping Xelopes after prolonged use may cause a temporary increase in acid-related symptoms; gradual dose tapering may be advised by a physician.
• Fundic gland polyps: long-term use of Xelopes, especially beyond one year, is associated with an increased risk of benign fundic gland polyps.

Reported overdoses of Xelopes (including doses far exceeding the usual therapeutic dose) have generally caused mild, transient symptoms such as confusion, drowsiness, blurred vision, rapid heartbeat, nausea, vomiting, sweating, flushing, headache, and dry mouth, with no serious long-term consequences reported. There is no specific antidote for Xelopes overdose. If an overdose of Xelopes is suspected, seek immediate medical attention or contact a poison control center right away; treatment is symptomatic and supportive, and Xelopes is not effectively removed by dialysis due to extensive protein binding.

Store Xelopes at room temperature, below 30°C, protected from light and moisture, and keep the container tightly closed. Keep out of reach of children.

• Hepatic impairment: Xelopes is extensively metabolized by the liver; dose reduction should be considered in patients with significant hepatic impairment, and such patients should be monitored closely.
• Renal impairment: no dose adjustment is generally required for renal impairment, as Xelopes and its metabolites are not significantly affected by kidney function.
• Elderly patients: no dose adjustment is generally required based on age alone, although elimination of Xelopes may be somewhat reduced; elderly patients are also at higher risk of the long-term risks described in Precautions and Warnings (e.g., fracture, hypomagnesemia).
• Patients of Asian descent: because of genetic differences in CYP2C19 metabolism, Asian patients may have higher Xelopes plasma levels than others at the same dose; dose adjustment may be considered by the prescribing physician.
• Pediatric patients: see Pediatric Uses.
• Pregnant and breastfeeding women: see Pregnancy and Lactation.

The duration of Xelopes treatment depends on the indication: most ulcer-healing and GERD/erosive esophagitis treatment courses run 4 to 8 weeks, H. pylori eradication regimens run 10 to 14 days, and NSAID-associated ulcer risk-reduction or maintenance therapy for erosive esophagitis may continue for longer periods as directed by a physician. Pathological hypersecretory conditions such as Zollinger-Ellison syndrome may require long-term, individually titrated Xelopes therapy for as long as clinically indicated. Because long-term use of Xelopes carries risks described in Precautions and Warnings, treatment should be used for the shortest duration that achieves the treatment goal, and the ongoing need for Xelopes should be periodically reassessed by a physician.

Xelopes for injection (40 mg/vial) is a lyophilized powder that must be reconstituted before intravenous use, strictly following the manufacturer's instructions and by a qualified healthcare professional. It is typically reconstituted with the diluent supplied, or with 0.9% Sodium Chloride Injection or 5% Dextrose Injection as specified in the product's prescribing information, and administered slowly by intravenous injection or infusion; the reconstituted solution of Xelopes should be used within the time window specified on the product labeling and should not be mixed with other medications in the same line.

Proton Pump Inhibitor (PPI); substituted benzimidazole class

Omeprazole works by irreversibly binding to and inhibiting the hydrogen-potassium-adenosine triphosphatase (H+/K+-ATPase) enzyme system located in the secretory surface of the gastric parietal cells. This enzyme, commonly called the gastric proton pump, represents the final common step in gastric acid secretion, regardless of the stimulus (histamine, acetylcholine, or gastrin). By blocking this pump, Omeprazole suppresses both basal and stimulated gastric acid secretion, and because the inhibition is irreversible, new enzyme must be synthesized before acid secretion capacity is restored, giving Omeprazole a duration of action that outlasts its plasma half-life.

C (legacy FDA pregnancy category from older labeling; current U.S. prescribing information for Xelopes uses a narrative pregnancy risk summary rather than a letter category)

Xelopes is FDA-approved for the treatment of GERD and erosive esophagitis in children 1 year of age and older, with dosing based on body weight (see Dosage). Safety and efficacy of Xelopes in infants younger than 1 year of age have not been established, and Xelopes should be used in this age group only under close medical supervision if a physician determines it is necessary. Xelopes is not FDA-approved in children for H. pylori eradication or pathological hypersecretory conditions, and its use for these indications in pediatric patients would be an off-label decision made by a physician based on individual clinical judgment.