Abstract
Dexlansoprazole MR, an enantiomer of lansoprazole, is a unique proton pump inhibitor with a duel release mechanism. This release mechanism produces two distinct peak concentrations that result in a prolonged mean residence time with increased duration of plasma concentrations and a greater percent time the pH is maintained above 4. The prolonged residence time allows dexlansoprazole MR to be administered throughout the day without regards to meals or the timing before a meal. In two trials of patients with erosive esophagitis, dexlansoprazole MR 60 mg and 90 mg demonstrated comparable healing rates to lansoprazole 30 mg. In patients with healed EE, dexlansoprazole MR 30 mg (75%) and 60 mg (83%) were superior to placebo (27%; p < 0.0025) in maintenance of healing. Dexlansoprazole MR 30 mg and 60 mg had a greater pecentage of heartburn-free days (91%-96%) and heartburn-free nights (96%-99%) than placebo (29%-72%) over the 6-month maintenance trial. Dexlansorpazole MR appears to be well tolerated with the safety profile being similar to lansoprazole with gastrointestinal adverse events being the most common. Dexlansoprazole MR provides a new treatment option for gastroesophageal reflux disease due to the flexible dosing, the unique release mechanisms and prologned pharmacodynamic effect.
Highlights
Pharmacotherapy with proton pump inhibitors (PPIs) as opposed to other acid suppressive agents has radically improved the treatment efficacy over histamine receptor antagonists in acid related disorders, such as gastroesophageal reflux disease (GERD).[1,2] The PPIs are potent blockers of acid secretion from parietal cells and significantly raise gastric pH compared to histamine receptor antagonists or antacids.[3]
Dexlansoprazole modified release (MR)’s dual release mechanism increases and prolongs the serum concentration that in turn allows for sustained gastric pH 4. It appears that dexlansoprazole MR, like other PPIs is equivalent in healing and symptom rate control for patients with mild to moderate erosive esophagitis (EE) (LA grades A and B), but is more effective than lansoprazole in moderate to severe EE (LA grades C and D) which would be consistent with a greater duration of acid suppression
Dexlansoprazole MR is a novel duel release PPI that results in prolonged serum concentrations and extensive acid suppression
Summary
Pharmacotherapy with proton pump inhibitors (PPIs) as opposed to other acid suppressive agents has radically improved the treatment efficacy over histamine receptor antagonists in acid related disorders, such as gastroesophageal reflux disease (GERD).[1,2] The PPIs are potent blockers of acid secretion from parietal cells and significantly raise gastric pH compared to histamine receptor antagonists or antacids.[3]. The PPIs have relatively short half lives at approximately 1–2 hours which suggests that they are unlikely to accumulate in the systemic circulation.[13] The AUCs are reported to correlate well with acid suppression.[15] The AUC for omeprazole 20 mg (0.2–1.2 μg⋅h/mL) and rabeprazole 20 mg (0.8 μg⋅h/mL) are much lower than the AUCs for pantoprazole 40 mg (2–5 μg⋅h/mL), omeprazole/sodium bicarbonate (1.665 μg⋅h/mL), lansoprazole (1.7–5 μg⋅h/mL), and esomeprazole (3.314 μg⋅h/mL) (Table 1).[13] The oral bioavailabilities of the proton pump inhibitors are all very different.
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