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The First and Only
Immediate-Release Oral PPI

Executive Summary for ZEGERID® (omeprazole/sodium bicarbonate)




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What is ZEGERID® (omeprazole/sodium bicarbonate)?

ZEGERID (omeprazole/sodium bicarbonate) is a combination of omeprazole, a proton pump inhibitor (PPI), and sodium bicarbonate, an antacid, which raises intragastric pH and protects omeprazole from gastric acid degradation. ZEGERID is the first and only immediate-release oral PPI.

What differentiates ZEGERID from other drugs in its class?

ZEGERID (omeprazole/sodium bicarbonate) Capsules and Powder for Oral Suspension are unique among oral PPIs because they are immediate-release formulations, in contrast to all other oral PPIs, including capsules, tablets, orally disintegrating tablets, and suspensions, which are all delayed-release, enteric coated formulations. The sodium bicarbonate in ZEGERID raises intragastric pH and protects omeprazole from degradation by gastric acid, rather than an enteric coating as is used in other PPI formulations. Sodium bicarbonate in ZEGERID facilitates the rapid absorption of omeprazole and onset of initial acid suppression, with peak plasma concentrations of omeprazole being reached approximately 30 minutes after the first dose. Delayed-release omeprazole products or formulations are not therapeutically equivalent to ZEGERID, because ZEGERID has unique pharmacokinetic properties. Prilosec®, Prilosec OTC® or generic omeprazole are not interchangeable with ZEGERID, and there are no AB-rated generic equivalents to ZEGERID according to the FDA Orange Book.

Separate pharmacokinetic and pharmacodynamic studies of the antisecretory effects of repeated once-daily, prebreakfast dosing of ZEGERID Capsules and Powder for Oral Suspension were conducted. Median values for the time gastric pH > 4 for patients taking ZEGERID Oral Suspension and ZEGERID Capsules, 20 mg and 40 mg doses, ranged from 12.2 to 18.6 hours on day 7 (steady state). ZEGERID has a distinct pharmacokinetic profile, provides 24-hour acid control, and offers once-a-day dosing, bedtime or daytime, on an empty stomach at least one hour before a meal.

What data supports administration of ZEGERID at bedtime?

In reviewing the medical literature, many investigators recommend administering PPIs 15-30 minutes prior to meals to maximize acid suppression. There are published data that more than half (54%) of patients with poorly controlled gastroesophageal reflux disease (GERD) dose their PPIs sub-optimally. Almost a third (28%) of patients who dose sub-optimally take their PPIs at bedtime. The ability of a PPI formulation to be efficacious when administered at bedtime, without a subsequent meal would be a benefit to patients who are non-compliant with dosing prior to meals, as well as for patients who require nighttime control of gastric acidity. Two studies in which ZEGERID Powder for Oral Suspension was administered at bedtime, without a meal, and controlled intragastric acidity throughout the nighttime have recently been published. 1, 2

The most recent, published in 2007, was an open-label, randomized, cross-over study, completed by 49 patients with nocturnal symptoms of GERD, conducted to compare the effects of repeated bedtime administration of ZEGERID Oral Suspension 40 mg, delayed-release lansoprazole 30 mg, and delayed-release esomeprazole 40 mg on nocturnal gastric acidity. At steady state, a more rapid onset of control of nocturnal gastric acidity was observed with ZEGERID. After bedtime dosing at 10 PM, patients treated with ZEGERID first reached an intragastric pH > 4 at 10:15 PM, compared to 1:15 AM when treated with esomeprazole, and 3:15 AM when treated with lansoprazole.

Administration of ZEGERID at bedtime resulted in a substantial reduction in nocturnal acid breakthrough (NAB) compared to symmetric dosing of esomeprazole and lansoprazole. NAB is defined as nighttime periods with gastric pH < 4 for more than 1 continuous hour, during PPI therapy. The percentage of patients who experienced NAB was significantly less following treatment with ZEGERID, compared to treatment with either esomeprazole or lansoprazole (61% vs. 92% and 92%; P < 0.001, both comparisons).

Control of intragastric pH in the early part of the sleeping period may be important when managing patients who require nocturnal control of gastric acidity. Recent findings published by Hila et al. suggest that episodes of abnormal nocturnal acid reflux are significantly more frequent during the first half of the nighttime period, compared to the second half. During the first half of the night (10 PM to 2 AM), the percentage of time with gastric pH > 4 was significantly greater with ZEGERID, than after treatment with either esomeprazole or lansoprazole (51.9% versus 30.1% and 12.0%, respectively; P < 0.001, all comparisons). Median gastric pH was also significantly higher, during the first half of the night with bedtime administration of ZEGERID, compared to bedtime administration of esomeprazole or lansoprazole (4.34 versus 2.37 and 1.51, respectively; P < 0.001, all comparisons). 3, 4

Control of nocturnal gastric acidity was significantly better with ZEGERID over the entire 8-hour nighttime period 10 PM to 6 AM, compared to that associated with lansoprazole. The percentage of time with gastric pH > 4 for the 8-hour nighttime period was significantly greater following treatment with ZEGERID compared to that associated with lansoprazole therapy (53.4% versus 34.2%; P < 0.001). The median gastric pH for the same time interval was 4.04 for ZEGERID compared to 2.09 for lansoprazole (P < 0.001). Following bedtime administration of esomeprazole, the percent time gastric pH > 4 and median gastric pH were 54.9% and 4.85, respectively. While overall nighttime acid control associated with bedtime administration of esomeprazole was comparable to that observed with ZEGERID, control of early nighttime gastric acidity, from 10 PM to 2 AM, was significantly better with ZEGERID than with esomeprazole. No serious safety issues were associated with any of the drugs in this trial. 3

The first study involving administration of ZEGERID at bedtime, published in 2005, was a randomized, open-label, 2-period crossover trial in 36 patients with nocturnal symptoms of GERD, that compared the effects of ZEGERID Oral Suspension and pantoprazole on nocturnal gastric acidity. Pantoprazole is the only proton pump inhibitor with FDA-approved labeling for reduction in relapse rates of daytime and nighttime heartburn symptoms in patients with GERD. Repeated once-daily dosing of ZEGERID Oral Suspension 40 mg at bedtime produced significantly better nocturnal gastric acid control than repeated once daily predinner or twice daily (prebreakfast and bedtime) dosing with pantoprazole 40 mg delayed-release tablets (median gastric pH: 4.7 vs. 2.0 and 1.7; p<0.001 both comparisons; and percentage of time gastric pH > 4: 55% vs. 27% and 34%; p<0.001 both comparisons). Repeated once daily bedtime dosing with ZEGERID 40 mg and twice daily dosing with pantoprazole 40 mg gave similar 24-hour gastric pH control. No serious safety issues were associated with either drug in this trial. The overall conclusion of the study was that ZEGERID 40 mg dosed once daily at bedtime reduced nocturnal gastric acidity to a degree not observed with either once-daily or twice-daily dosing of delayed-release pantoprazole 40 mg. 5

For what indications is ZEGERID approved?

ZEGERID is indicated for heartburn and other symptoms associated with gastroesophageal reflux disease (GERD) (20 mg QD); for the short-term treatment (4-8 weeks) of erosive esophagitis diagnosed by endoscopy (20 mg QD); for maintenance of healing of erosive esophagitis (20 mg QD) (controlled studies do not extend beyond 12 months); for short-term treatment (4-8 weeks) of active duodenal ulcer (20 mg QD); for short-term treatment (4-8 weeks) of active benign gastric ulcer (40 mg QD); and for reduction of risk of upper gastrointestinal bleeding in critically ill patients (only powder for oral suspension 40 mg/1680 mg QD; use beyond 14 days has not been evaluated).

What important safety information do health care professionals need to know?

The most frequently reported adverse events with ZEGERID are headache, diarrhea, and abdominal pain. In critically ill patients treated with ZEGERID, adverse events generally reflected the serious, underlying medical condition of the patients, and were similar for patients treated with ZEGERID and with the comparator (acid-controlling) drug. Symptomatic response to therapy does not preclude the presence of gastric malignancy. Atrophic gastritis has been noted occasionally in gastric corpus biopsies from patients treated long term with omeprazole.

ZEGERID Capsules contain 303 mg of sodium per dose. ZEGERID Powder for Oral Suspension contains 460 mg of sodium per dose. This should be taken into consideration for patients on a sodium-restricted diet.

Sodium bicarbonate is contraindicated in patients with metabolic alkalosis and hypocalcemia. ZEGERID is contraindicated in patients with known hypersensitivity to any component of the formulation.

Since both 20 mg and 40 mg ZEGERID contain the same amount of sodium bicarbonate (1100 mg in capsules, 1680 mg in packets of powder for oral suspension), two 20 mg capsules are not equivalent to, and should not be substituted for, one 40 mg capsule, and two 20 mg packets are not equivalent to, and should not be substituted for, one 40 mg packet.

A complete set of references for this summary is available upon request. Contact Santarus Medical Affairs.


References

  1. Pezanoski JP, Gunaratnam NT, Gamarra R, Cowen MT. Correct and incorrect dosing of proton pump inhibitors and its impact on GERD symptoms. American College of Gastroenterology 69th Annual Meeting and Postgraduate Course; Orlando, Florida, USA: October 29-November 3, 2004:99 (10 Suppl):S11 (Abstract 32).

  2. Gunaratnam NT, Jessup TP, Inadomi J, Lascewskis DP. Sub-optimal proton pump inhibitor dosing is prevalent in patients with poorly controlled gastroesophageal reflux disease. Aliment Pharmacol Ther 2006;23: 1473-1477.

  3. Katz PO, Koch FK, Ballard ED, Bagin RG, Gautille TC, Checani GC, Hogan DL, Pratha VSV. Comparison of the effects of immediate-release omeprazole oral suspension, delayed-release lansoprazole capsules and delayed-release esomeprazole capsules on nocturnal gastric acidity after bedtime dosing in patients with night-time GERD symptoms, Aliment Pharmacol Ther 2007; 25: 197-205.

  4. Hila A, Castell DO. Nighttime reflux is primarily an early event. J Clin Gastroenterology 2005;39; 579-583.

  5. Castell D, Bagin R, Goldlust B, Major J, Hepburn B. Comparison of the effects of omeprazole immediate-release powder for oral suspension and pantoprazole delayed-release tablets on nocturnal acid breakthrough in patients with symptomatic gastoesophageal reflux disease. Aliment PHarmacol Ther 2005; 21:1467-74




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Physician Resources | Pharmacists Corner | Important Safety Information

Please see full prescribing information.

You can obtain additional information about ZEGERID by writing Santarus directly. To speak to a representative by phone or to report an adverse event, call Santarus' Medical Information Department at 1.888.778.0887, option 2 (M-F, 9:00 am to 7:00 pm, EST).

Product Description
ZEGERID contains omeprazole, a proton pump inhibitor (PPI), and sodium bicarbonate, an antacid, which raises the gastric pH and thus protects omeprazole from acid degradation.

Indications and Dosing for ZEGERID
ZEGERID is indicated for heartburn and other symptoms associated with gastroesophageal reflux disease (GERD)
(20 mg); for the short-term treatment (4-8 weeks) of erosive esophagitis diagnosed by endoscopy
(20 mg); for maintenance of healing of erosive esophagitis (20 mg) (controlled studies do not extend beyond 12 months); for short-term treatment (4-8 weeks) of active duodenal ulcer (20 mg); for short-term treatment (4-8 weeks) of active benign gastric ulcer (40 mg); and for reduction of risk of upper gastrointestinal bleeding in critically ill patients (only powder for oral suspension 40 mg; use beyond 14 days has not been evaluated).

Important Safety Information about ZEGERID
The most frequently reported adverse events with ZEGERID are headache, diarrhea, and abdominal pain. In 178 critically ill patients treated with ZEGERID Powder for Oral Suspension, adverse events generally reflected the serious, underlying medical condition of the patients, and were similar for patients treated with ZEGERID Powder for Oral Suspension than in those treated with the comparator (acid-controlling) drug. For more information about these and other events, please see Table 13 of the Full Prescribing Information. Symptomatic response to therapy does not preclude the presence of gastric malignancy. Atrophic gastritis has been noted occasionally in gastric corpus biopsies from patients treated long term with omeprazole.

ZEGERID Capsules contain 304 mg of sodium per dose. ZEGERID Powder for Oral Suspension contains 460 mg of sodium per dose. This should be taken into consideration for patients on a sodium-restricted diet.

Sodium bicarbonate is contraindicated in patients with metabolic alkalosis and hypocalcemia. ZEGERID is contraindicated in patients with known hypersensitivity to any component of the formulation.

Since both 20 mg and 40 mg ZEGERID contain the same amount of sodium bicarbonate (1100 mg in capsules,
1680 mg in packets of powder for oral suspension), two 20 mg capsules are not equivalent to, and should not be substituted for, one 40 mg capsule, and two 20 mg packets are not equivalent to, and should not be substituted for, one 40 mg packet.