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Generic Dexilant ( Dexlansoprazole )
Dexilant (dexlansoprazole) is a proton pump inhibitor (PPI) indicated for the treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD), the healing of all grades of erosive esophagitis (EE), and the maintenance of healed erosive esophagitis and relief of heartburn in adults. Dexilant is the R-enantiomer of lansoprazole and works by irreversibly inhibiting the hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase) enzyme system, known as the proton pump, on the secretory surface of gastric parietal cells, thereby suppressing both basal and stimulated gastric acid secretion. Dexilant features a proprietary dual delayed-release (DDR) formulation that provides two distinct releases of the active drug at separate pH thresholds, resulting in an extended plasma concentration-time profile and prolonged acid suppression compared to single-release PPIs.
Usual adult dose: For the healing of erosive esophagitis, the recommended dose is 60 mg once daily for up to 8 weeks. For the maintenance of healed erosive esophagitis and relief of associated heartburn, the recommended dose is 30 mg once daily for up to 6 months. For the symptomatic treatment of non-erosive GERD causing heartburn, the recommended dose is 30 mg once daily for 4 weeks. Dexilant capsules may be taken with or without food. Alternatively, the capsule may be opened and the intact granules sprinkled on one tablespoon of applesauce and swallowed immediately without chewing. The granules must not be crushed or chewed, as this would disrupt the dual delayed-release delivery system. No dosage adjustment is required for elderly patients or those with mild to moderate renal impairment. In patients with moderate hepatic impairment (Child-Pugh Class B), the maximum recommended dose is 30 mg daily.
Dosage form: Dual delayed-release capsules: 30 mg (opaque blue and grey hard gelatin capsule) and 60 mg (opaque blue hard gelatin capsule). Each capsule contains a mixture of two types of enteric-coated granules that release dexlansoprazole at different pH values, with the first release occurring in the proximal small intestine at pH 5.5 and the second release in the distal small intestine at pH 6.75, providing an extended duration of acid suppression.
Onset of action: Following oral administration, dexlansoprazole exhibits a dual-peak plasma concentration profile. The first peak concentration occurs approximately 1 to 2 hours after dosing, corresponding to release from the first group of granules. The second peak occurs approximately 4 to 5 hours after dosing, corresponding to release from the second group of granules in the distal small intestine. Pharmacodynamic effects on gastric acid secretion begin within approximately 1 hour of the first dose. Symptomatic relief of heartburn is typically observed within the first week of daily treatment, while complete healing of erosive esophagitis generally requires 4 to 8 weeks of continuous therapy.
Duration of action: The dual delayed-release formulation extends the duration of pharmacodynamic effect, maintaining intragastric pH above 4 for a mean of 71% of a 24-hour period with the 60 mg dose, which is significantly longer than that provided by single-release PPIs. The elimination half-life of dexlansoprazole in plasma is approximately 1 to 2 hours, but the therapeutic effect persists for more than 24 hours due to irreversible inactivation of the proton pump and the prolonged release profile. This extended coverage supports true once-daily dosing for all indications.
Alcohol recommendation: No clinically significant pharmacokinetic or pharmacodynamic interaction has been identified between Dexilant and alcohol. Alcohol does not directly alter the acid-suppressive efficacy of the medication. However, excessive alcohol consumption can independently irritate the gastric and esophageal mucosa, worsen symptoms of GERD, increase the risk of erosive esophagitis, and counteract the therapeutic benefits of proton pump inhibitor treatment. Patients undergoing therapy for GERD or erosive esophagitis are advised to minimize or avoid alcohol intake in accordance with established dietary and lifestyle modifications for gastroesophageal reflux disease.
Most common side effects: Diarrhea, abdominal pain, nausea, upper respiratory tract infection, vomiting, and flatulence. Headache has also been reported in clinical trials. Most adverse reactions are mild to moderate in intensity and transient in nature. Prolonged use of proton pump inhibitors has been associated with an increased risk of Clostridium difficile-associated diarrhea, osteoporosis-related fractures of the hip, wrist, or spine with long-term and high-dose therapy, hypomagnesemia (which may be symptomatic and require magnesium supplementation and discontinuation), vitamin B12 malabsorption due to hypochlorhydria, and fundic gland polyps. Patients on extended maintenance therapy should be periodically reassessed to determine the ongoing necessity of treatment.
Would you like to learn more about Dexilant (Dexlansoprazole) for the management of GERD and erosive esophagitis?
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