Clinical experience with pantoprazole in gastroesophageal reflux disease.
BACKGROUND
Pantoprazole is a new proton pump inhibitor indicated for the treatment of erosive esophagitis associated with gastroesophageal reflux disease (GERD) and is available in both oral and intravenous (IV) formulations.


OBJECTIVE
This paper reviews the pharmacologic properties of pantoprazole and summarizes the findings from clinical studies of this drug.


METHODS
This review was compiled from the published literature, abstracts from clinical trials, and data on file with the manufacturer of pantoprazole.


RESULTS
Pantoprazole selectively accumulates in the acidic environment of gastric parietal cells and acts at the final step of acid secretion by binding 2 key cysteine residues of the proton pump involved in gastric acid production. The bioavailability of pantoprazole is not altered by concomitant administration of food or antacids or with repeated dosing. Both oral and IV formulations of pantoprazole exhibit linear pharmacokinetics. Several clinical trials have proved pantoprazole superior to histamine-2-receptor antagonists (H2RAs) in reducing acid secretion and elevating gastric pH levels. Pantoprazole has been shown to be more effective than ranitidine (P < 0.05), famotidine (P < 0.001), and nizatidine (P < 0.05), and at least as effective as omeprazole, in healing erosive esophagitis and relieving associated symptoms of GERD, including regurgitation. Pantoprazole is also more effective than the H2RA nizatidine for the treatment of nighttime heartburn (P < 0.05). Studies have shown pantoprazole to be well tolerated; adverse events, including headache, diarrhea, flatulence, abdominal pain, eructation, nausea, and rash, occurred in < or = 6% of patients. The oral and IV formulations of pantoprazole are equally potent in inhibiting gastric acid secretion; thus, switching between formulations requires no dosage adjustments. Special patient populations, including the elderly and patients with renal or mild to moderate hepatic impairment, can take pantoprazole without an adjustment in dosage.


CONCLUSIONS
Because of its unique pharmacokinetic properties, mechanism of action, and reduced potential for producing cytochrome P-450-based drug interactions, pantoprazole in both oral and IV formulations is effective over a full 24 hours and is well tolerated in a variety of patient types.
Avner
D L
DL
Gastroenterology, St. Mark's Hospital, Salt Lake City, Utah 84124, USA. davner1@pol.net
D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D000284:Administration, Oral; D000328:Adult; D000368:Aged; D000897:Anti-Ulcer Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D001562:Benzimidazoles / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D001682:Biological Availability; D002986:Clinical Trials as Topic; D003577:Cytochrome P-450 Enzyme System / Q000187:drug effects; D004347:Drug Interactions; D005764:Gastroesophageal Reflux / Q000188:drug therapy*; D006801:Humans; D007275:Injections, Intravenous; D009853:Omeprazole / Q000031:analogs & derivatives; D000077402:Pantoprazole; D054328:Proton Pump Inhibitors; D013454:Sulfoxides / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use
D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D000897:Anti-Ulcer Agents; D001562:Benzimidazoles; D054328:Proton Pump Inhibitors; D013454:Sulfoxides; D003577:Cytochrome P-450 Enzyme System; D000077402:Pantoprazole; D009853:Omeprazole