Dexlansoprazole

• GERD (Gastroesophageal Reflux Disease)
• Erosive Esophagitis
• Heartburn
• Acid Reflux

Dexlansoprazole is a proton pump inhibitor (PPI) with a dual delayed-release formulation used for the treatment of gastroesophageal reflux disease (GERD) and erosive esophagitis. This medication offers extended acid suppression through a unique delivery system that provides two separate releases of the drug.

Mechanism of Action

Dexlansoprazole is the R-enantiomer of lansoprazole and a proton pump inhibitor that suppresses gastric acid secretion by specifically inhibiting the hydrogen-potassium ATPase enzyme system (the proton pump) at the secretory surface of gastric parietal cells. This enzyme is the final step in gastric acid production. Dexlansoprazole binds to the proton pump and blocks it irreversibly, reducing both basal and stimulated acid secretion regardless of the stimulus. The medication's dual delayed-release formulation releases drug at two different pH levels in the gastrointestinal tract, providing an initial release in the proximal duodenum and a second release in the more distal small intestine.

Available Formulations

Dexlansoprazole is available as delayed-release capsules in 30 mg and 60 mg strengths. The capsules can be swallowed whole or opened and the granules sprinkled on applesauce or mixed with water for patients who have difficulty swallowing. The capsules can be taken without regard to food, unlike some other PPIs that are recommended before meals. An orally disintegrating tablet is also available.

Medical Uses

Dexlansoprazole is FDA-approved for healing of all grades of erosive esophagitis (EE) for up to 8 weeks, maintaining healing of EE for up to 6 months, treatment of heartburn associated with symptomatic non-erosive GERD for 4 weeks, and treatment of heartburn associated with symptomatic non-erosive GERD in patients 12-17 years old for 4 weeks. The dual-release formulation provides extended duration of acid suppression compared to single-release PPIs.

Dosing Guidelines

For healing erosive esophagitis, the dose is 60 mg once daily for up to 8 weeks. For maintaining healing of EE, 30 mg once daily is used. For symptomatic non-erosive GERD, 30 mg once daily for 4 weeks is recommended. The medication can be taken at any time of day without regard to meals, offering flexibility compared to other PPIs. For patients with moderate hepatic impairment, doses should not exceed 30 mg daily. The orally disintegrating tablet should be allowed to dissolve on the tongue without water.

Important Safety Information

Long-term PPI use has been associated with increased risk of Clostridioides difficile-associated diarrhea, bone fractures (hip, wrist, spine), fundic gland polyps, hypomagnesemia, vitamin B12 deficiency, and acute interstitial nephritis. Patients should use the lowest effective dose for the shortest duration. PPIs may reduce the effectiveness of clopidogrel through CYP2C19 inhibition; alternative antiplatelet strategies should be considered. Acute interstitial nephritis can occur at any time during PPI therapy.

Drug Interactions

Dexlansoprazole is metabolized by CYP2C19 and CYP3A4. It may reduce the absorption of drugs dependent on gastric pH for bioavailability (ketoconazole, itraconazole, ampicillin esters, iron salts, mycophenolate mofetil). Increased levels of drugs metabolized by CYP2C19 (diazepam, phenytoin) may occur. Concomitant use with methotrexate may increase methotrexate toxicity. Warfarin anticoagulation should be monitored when starting or stopping dexlansoprazole. Use with atazanavir should be avoided.

Special Populations

There are no adequate studies in pregnant women; animal studies showed no harm, but use during pregnancy only if clearly needed. It is unknown whether dexlansoprazole is excreted in human breast milk. Safety and efficacy have been established in adolescents 12-17 years for symptomatic GERD. Elderly patients do not require dose adjustment. Patients with moderate hepatic impairment should not exceed 30 mg daily; the medication has not been studied in severe hepatic impairment. No dose adjustment is needed for renal impairment.