Impact of concomitant antacid administration on gabapentin plasma exposure and oral bioavailability in healthy adult subjects.
Summary of "Impact of concomitant antacid administration on gabapentin plasma exposure and oral bioavailability in healthy adult subjects."
The aim of this open-label, randomized, and 3-period crossover study was to evaluate the influences of concomitant antacid administration on the plasma disposition, intestinal absorption, and urinary excretion of gabapentin in humans. Gabapentin (200 mg) was orally administered alone, with 1 g magnesium oxide (MgO), or with 20 mg omeprazole to 13 healthy adult subjects. Oral bioavailability (BA) of gabapentin was estimated by 24-hour urine collection. The C(max), T(max) and AUC(0-∞) of gabapentin + MgO were significantly lower than that of gabapentin alone (by 33%, 36% and 43%, respectively) and gabapentin + omeprazole (by 29%, 46% and 40%, respectively), respectively. In contrast, no significant differences were observed in the plasma disposition parameters of gabapentin between the alone and omeprazole treatments. The gabapentin BA in the MgO treatment was significantly lower, by 32% and 39%, compared to the alone and omeprazole treatments, respectively. There was no significant difference in the gabapentin BA between the alone and omeprazole treatments. Concomitant MgO and omeprazole did not affect the renal clearance of gabapentin. In conclusion, concomitant MgO decreased the gabapentin exposure through the reduction of intestinal absorption extent and rate. This reduction may be independent of the suppression of gastrointestinal acidification caused by antacids.
Department of Hospital Pharmacy, Hamamatsu University School of Medicine.
This article was published in the following journal.
Name: Drug metabolism and pharmacokinetics
Medical and Biotech [MESH] Definitions
The giving of drugs, chemicals, or other substances by mouth.
Hard or soft soluble containers used for the oral administration of medicine.
Therapy using oral or topical photosensitizing agents with subsequent exposure to light.
Disorders associated with acute or chronic exposure to compounds containing ARSENIC (ARSENICALS) which may be fatal. Acute oral ingestion is associated with gastrointestinal symptoms and an encephalopathy which may manifest as SEIZURES, mental status changes, and COMA. Chronic exposure is associated with mucosal irritation, desquamating rash, myalgias, peripheral neuropathy, and white transverse (Mees) lines in the fingernails. (Adams et al., Principles of Neurology, 6th ed, p1212)
Administration of a drug or chemical by the individual under the direction of a physician. It includes administration clinically or experimentally, by human or animal.
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