Esomeprazole dosing

Comparable daily doses of PPIs are omeprazole 20 mg = esomeprazole 20 mg = lansoprazole 30 mg = rabeprazole 20 mg = pantoprazole 40 mg. The PPIs degrade in acidic environments and are therefore formulated in delayed-release capsules or tablets.16 Lansoprazole, esomeprazole, and omeprazole contain enteric-coated (pH-sensitive) granules in a capsule form. For patients unable to swallow the capsule or in pediatric patients, the contents of the capsule can be mixed in applesauce or placed in orange juice. If a patient has a nasogastric tube, the contents of an omeprazole capsule can be... 

Most patients require standard doses to prevent relapses. H2RAs may be an effective maintenance therapy in patients with mild disease. The PPIs are the drugs of choice for maintenance treatment of moderate to severe esophagitis. Usual once-daily doses are omeprazole 20 mg, lansoprazole 30 mg, rabeprazole 20 mg, or esomeprazole 20 mg. Lower doses of a PPI or alternate-day regimens may be effective in some patients with less severe disease. 

IV-The recommended adult dose is esomeprazole 20 or 40 mg given once daily by IV injection (no less than 3 minutes) or IV infusion (10 to 30 minutes). 

Esomeprazole (Nexium) [Gastric Acid Inhibitor/Proton Pump Inhibitor] Uses Short-term (4-8 wk) for erosive esophagitis/GERD H. pylori Infxn in combo w/ antibiotics Action Proton pump inhibitor, gastric acid Dose Adults. GERD/erosive gastritis 20 0 mg/d PO x 4-8 wk 20 0 mg IV 10-30 min inf or >3 min IV push, 10 d max Maint 20 mg/d... 

AstraZeneca (formerly Astra) has launched the proton-pump inhibitor esomeprazole (19) (as Nexium) as a treatment for peptic ulcer, gastroesophageal reflux disease, duodenal ulcer, and esophagitis. Esomeprazole is the (S)-enantiomer of omeprazole and was developed as a result of its improved pharmokinetic profile and better potency after oral dosing than (f )-form of omeprazole or the racemate. The dosage is higher than would be expected for a simple chiral switch. The stereogenic center is at sulfur. Detailed accounts of the development of the process have been published.189190... 

A given oral dose of esomeprazole appears to result in an approximately two-fold higher AUC than the same dose of omeprazole. 

The inter-individual variation in AUC is significantly less for esomeprazole than for the same dose of omeprazole [48]. 

MOCLOBEMIDE PROTON PUMP INHIBITORS -OMEPRAZOLE/ ESOMEPRAZOLE Possible t efficacy and adverse effects of modobemide Inhibition of CYP2C19 Monitor more closely effect only seen in extensive CYP2C19 metabolizers. Dose i may be required... 

BZDs PROTON PUMP INHIBITORS -OMEPRAZOLE/ ESOMEPRAZOLE T efficacy and adverse effects, e.g. prolonged sedation Inhibition of metabolism via CYP4S0 (some show competitive inhibition via CYP2C19) Monitor for t side-effects, and 1 dose as necessaiy. Likely to delay recovery after procedures for which BZDs have been used. Consider alternative proton pump inhibitor, e.g. lansoprazole or pantoprazole... 

ANTICOAGULANTS - ORAL H2 RECEPTOR BLOCKERS t anticoagulant effect with cimetidine and possibly famotidine Inhibition of metabolism via CYP1A2, CYP2C9 and CYP2C19 Use alternative acid suppression, e.g. other H2 antagonist or protein pump inhibitor (not esomeprazole, lansoprazole or omeprazole) or monitor INR more closely 1 dose may be required. Take acid suppression regularly not PRN if affects INR control... 

ANTICOAGULANTS-ORAL PROTON PUMP INHIBITORS Possibly t anticoagulant effect when esomeprazole, lansoprazole or omeprazole is added to warfarin Uncertain at present. Omeprazole and lansoprazole are known to induce CYP1A2, which plays a role in activation of coumarins Monitor INR more closely. 1 dose may be required. If 10%, 20% or 30% over range, omit dose for 1, 2 or 3 days respectively consider i maintenance dose by 10%. Regular dosing of a proton pump inhibitor is preferable if affects INR significantly. Not reported with pantoprazole or rabeprazole... 

Omeprazole carries a higher risk for interactions as it has a high affinity for CYP2C19 and a somewhat lower affinity for CYP3A4. Pantoprazole (which is further metabolized by non-saturable phase II reactions after initial metabolism by CYP isoenzymes) has a lower potential for interaction associated with CYP450 inhibition, It is also likely that, despite the limited information, esomeprazole, lansoprazole and rabeprazole also have weaker potential for interaction compared with omeprazole. Pantoprazole has been reported to be used without dose adjustments in critical care patients with organ dysfunction. 

PROTON PUMP INHIBITORS SAQUINAVIR Significantly t plasma concentrations of saquinavir during concomitant treatment with esomeprazole. t risk of toxic effects of saquinavir Uncertain FDA in April 2009 recommended that patients should be monitored for toxic effects of saquinavir and that L dose of saquinavir may be required... 

Esomeprazole is the 5-isomer of omeprazole. The pharmacology, pharmacokinetics, efficacy, and safety of esomeprazole have been reviewed (1). Esomeprazole produces acid control comparable to that of currently available proton pump inhibitors. It undergoes less hepatic metabolism than omeprazole, has an oral availability of 89% at a dose of 40 mg, and a half-life of 1.5 hours. Esomeprazole is well tolerated its common adverse effects are diarrhea, headache, nausea, abdominal pain, respiratory infection, and sinusitis. 

To assess symptom control, esomeprazole 20 mg on demand has been compared with placebo on demand (maximum of one dose a day) for 6 months in a multicenter, double-blind study in 342 endoscopy-negative patients with gastro-esophageal reflux disease (2). There was complete resolution of heartburn after 4 weeks of daily esomeprazole therapy. On-demand therapy with esomeprazole was significantly more effective than placebo in controlling symptoms. The frequencies of adverse effects and laboratory profiles were similar in the two groups when adjusted for the time spent in the study. 

To examine the pharmacokinetics and pharmacodynamics of esomeprazole, 12 healthy men took once-daily esomeprazole 5, 10, or 20 mg, or omeprazole 20 mg for 5 days in a crossover study (3). The pharmacokinetics of esomeprazole were time- and dose-dependent. There was greater acid inhibition with esomeprazole than with omeprazole. 

To assess acid control, esomeprazole 20 or 40 mg/day has been compared with omeprazole 20 mg/day for 5 days in a double-blind, crossover study in 38 patients with symptoms of gastro-esophageal reflux disease (10). Pharmacokinetic variables and 24-hour intragastric pH were measured on day 5 of each dosing period. 

Esomeprazole 20 or 40 mg/day and omeprazole 20 mg/ day for 8 weeks have been compared in the treatment of gastro-esophageal reflux disease in a multicenter, randomized, double-blind trial in 1960 patients (11). Symptom control and healing rates were significantly better with either dose of esomeprazole than with omeprazole. There was no significant difference in reported adverse events between the treatment groups. The most commonly reported were headache, abdominal pain, and diarrhea. 

The effects of omeprazole 40 mg/day and esomeprazole 40 mg/day for 5 days on intragastric acidity have been compared in an open, crossover study in 130 patients with symptoms of gastro-esophageal reflux (20). Esomeprazole provided more effective acid control than twice the standard dose of omeprazole. Adverse effects were similar with the two drugs, and the most commonly reported were headache, nausea, and abdominal pain. 

Preliminary placebo-controlled studies with esomeprazole indicate that maintenance of erosive esophagitis healing occurs in 54% to 94% of patients after 6 months of 10-mg to 40-mg doses of esomperazole. Doses of 20 mg to 40 mg were superior to the 10-mg dose. Studies are needed comparing esomeprazole to the other proton pump inhibitors in maintenance therapy for GERD. 

The PPIs (omeprazole, esomeprazole, lansoprazole, rabeprazole, and pantoprazole) dose-dependently inhibit basal and stimulated gastric acid secretion. When PPI therapy is initiated, the degree of acid suppression increases over the first 3 to 4 days of therapy, as more and more proton pumps are inhibited. Upon discontinuation of therapy, full restoration of acid secretion takes 3 to 5 days. Because PPIs inhibit only those proton pumps that are actively secreting acid, they are most effective when taken 15 to 30 minutes before meals. ... 

Sostek MB, Chen Y, Skammer W, et al. Esomeprazole administered through a nasogastric tube provides bioavailability similar to oral dosing. Aliment Pharmacol Ther 2003 18 581-586. 

Prilosec, Rapinex, Zegerid) and its S-isomer, esomeprazole (Nexium), lansoprazole (Prevacid), rabeprazole (Aciphex), and pantoprazole (Protonix). These drugs have different substitutions on their pyridine and/or benzimidazole groups but are remarkably similar in their pharmacological properties. Omeprazole is a racemic mixture of R- and S-isomers the S-isomer, esomeprazole (S-omeprazole), is eliminated less rapidly than R-omeprazole, which theoretically provides a therapeutic advantage because of the increased half-life. Despite claims to the contrary, all proton-pump inhibitors have equivalent efficacy at comparable doses. 

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