Intravenous esomeprazole (40 mg and 20 mg) inhibits gastric acid secretion as effectively as oral esomeprazole: results of two randomized clinical studies.
OBJECTIVE
Two studies compared the effects of intravenous (i.v.) and oral esomeprazole (40 mg and 20 mg) on gastric acid suppression and pharmacokinetics after both single (day 1) and repeated (day 5) dosing.


METHODS
Two randomized, two-way, cross-over, comparative studies of similar design were performed in healthy male and female volunteers. In both studies, subjects received esomeprazole as a 30-min i.v. infusion or orally once-daily for 5 days, separated by a wash-out period of at least 13 days. In one study, which was double-blind (double dummy), subjects received 40 mg esomeprazole. In the other open study, subjects were given 20 mg esomeprazole.


RESULTS
In total, 40 and 24 subjects were randomized for treatment with 40 mg and 20 mg esomeprazole, respectively. No significant differences were found between i.v or oral administration of esomeprazole with respect to the amount of time with mean intragastric pH>4 throughout day 1 or day 5 of treatment in the 40 mg study (day 1, 10.1 h and 8.8 h versus day 5, 15.9 h and 15.3 h, respectively) and the 20 mg study (day 1, 7.3 h and 6.6 h versus day 5, 11.9 h and 12.3 h, respectively). The area under the plasma concentration-time curve values were higher following i.v. relative to oral administration on day 1 of dosing, with less pronounced differences after repeated (day 5) dosing. Both administration routes were similarly well tolerated.


CONCLUSIONS
Esomeprazole, 40 mg and 20 mg i.v., provides similar levels of intragastric acid control on both day 1 and day 5 of treatment compared with oral administration.
Wilder-Smith
Clive H
CH
GI Physiology Laboratory, Bern, Switzerland. cws@ggp.ch
Bondarov
Patrik
P
Lundgren
Marie
M
Niazi
Mohammad
M
Röhss
Kerstin
K
Ahlbom
Henrik
H
Nyman
Lars
L
D000284:Administration, Oral; D000328:Adult; D000897:Anti-Ulcer Agents / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D004334:Drug Administration Schedule; D064098:Esomeprazole / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D005260:Female; D005744:Gastric Acid / Q000378:metabolism*; D005745:Gastric Acidity Determination; D006801:Humans; D006863:Hydrogen-Ion Concentration / Q000187:drug effects; D007262:Infusions, Intravenous; D008297:Male; D008875:Middle Aged; D054328:Proton Pump Inhibitors
D000897:Anti-Ulcer Agents; D054328:Proton Pump Inhibitors; D064098:Esomeprazole