Omeprazole: Effects on oxidative drug metabolism in the rat

D. A. Henry; J. F. Gerkens; P. J. Brent; P. J. Dosen

doi:10.1111/j.1440-1681.1986.tb00916.x

Omeprazole: Effects on oxidative drug metabolism in the rat

D. A. Henry^*, J. F. Gerkens, P. J. Brent, P. J. Dosen

^*Corresponding author for this work

Research output: Contribution to journal › Article › Research › peer-review

5 Citations (Scopus)

Abstract

SUMMARY

1. Omeprazole, a substituted benzimidazole and a potent gastric antisecretory drug has been tested for inhibition of microsomal drug oxidative function in the rat.

2. A single dose of 40 mg/kg prolonged pentobarbitone sleeping times from 118 (range 73–168) min to 195 (159–222) min (P < 0.01), pentobarbitone half‐lives from 89 (63–114) to 112 (54–146) min (P < 0.05) and aminopyrine breath ¹⁴CO₂ half‐lives from 43 (37–51) to 56 (49–79) min (P < 0.05). Omeprazole in doses of 20 mg/kg or less had no significant effect.

3. In prolonging pentobarbitone sleeping times omeprazole 40 mg/kg and an equimolar (30 mg/kg) dose of cimetidine were approximately equipotent.

4. These results contrast with studies in man in which much smaller doses of omeprazole have been shown to produce clinically significant inhibition of drug metabolism.

Original language	English
Pages (from-to)	377-381
Number of pages	5
Journal	Clinical and Experimental Pharmacology and Physiology
Volume	13
Issue number	5
DOIs	https://doi.org/10.1111/j.1440-1681.1986.tb00916.x
Publication status	Published - May 1986
Externally published	Yes

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title = "Omeprazole: Effects on oxidative drug metabolism in the rat",

abstract = "SUMMARY1. Omeprazole, a substituted benzimidazole and a potent gastric antisecretory drug has been tested for inhibition of microsomal drug oxidative function in the rat. 2. A single dose of 40 mg/kg prolonged pentobarbitone sleeping times from 118 (range 73–168) min to 195 (159–222) min (P < 0.01), pentobarbitone half‐lives from 89 (63–114) to 112 (54–146) min (P < 0.05) and aminopyrine breath 14CO2 half‐lives from 43 (37–51) to 56 (49–79) min (P < 0.05). Omeprazole in doses of 20 mg/kg or less had no significant effect. 3. In prolonging pentobarbitone sleeping times omeprazole 40 mg/kg and an equimolar (30 mg/kg) dose of cimetidine were approximately equipotent. 4. These results contrast with studies in man in which much smaller doses of omeprazole have been shown to produce clinically significant inhibition of drug metabolism.",

author = "Henry, {D. A.} and Gerkens, {J. F.} and Brent, {P. J.} and Dosen, {P. J.}",

year = "1986",

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AU - Henry, D. A.

AU - Gerkens, J. F.

AU - Brent, P. J.

AU - Dosen, P. J.

PY - 1986/5

Y1 - 1986/5

N2 - SUMMARY1. Omeprazole, a substituted benzimidazole and a potent gastric antisecretory drug has been tested for inhibition of microsomal drug oxidative function in the rat. 2. A single dose of 40 mg/kg prolonged pentobarbitone sleeping times from 118 (range 73–168) min to 195 (159–222) min (P < 0.01), pentobarbitone half‐lives from 89 (63–114) to 112 (54–146) min (P < 0.05) and aminopyrine breath 14CO2 half‐lives from 43 (37–51) to 56 (49–79) min (P < 0.05). Omeprazole in doses of 20 mg/kg or less had no significant effect. 3. In prolonging pentobarbitone sleeping times omeprazole 40 mg/kg and an equimolar (30 mg/kg) dose of cimetidine were approximately equipotent. 4. These results contrast with studies in man in which much smaller doses of omeprazole have been shown to produce clinically significant inhibition of drug metabolism.

AB - SUMMARY1. Omeprazole, a substituted benzimidazole and a potent gastric antisecretory drug has been tested for inhibition of microsomal drug oxidative function in the rat. 2. A single dose of 40 mg/kg prolonged pentobarbitone sleeping times from 118 (range 73–168) min to 195 (159–222) min (P < 0.01), pentobarbitone half‐lives from 89 (63–114) to 112 (54–146) min (P < 0.05) and aminopyrine breath 14CO2 half‐lives from 43 (37–51) to 56 (49–79) min (P < 0.05). Omeprazole in doses of 20 mg/kg or less had no significant effect. 3. In prolonging pentobarbitone sleeping times omeprazole 40 mg/kg and an equimolar (30 mg/kg) dose of cimetidine were approximately equipotent. 4. These results contrast with studies in man in which much smaller doses of omeprazole have been shown to produce clinically significant inhibition of drug metabolism.

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DO - 10.1111/j.1440-1681.1986.tb00916.x

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JO - Clinical and Experimental Pharmacology and Physiology

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IS - 5

ER -

Omeprazole: Effects on oxidative drug metabolism in the rat

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