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No interaction between H2 blockers and isoniazid.

O Paulsen, P Höglund, L G Nilsson

European Journal of Respiratory Diseases

|April 1, 1986

Summary

H2 blockers like cimetidine and ranitidine do not affect isoniazid absorption or metabolism. This suggests that the uptake and elimination of isoniazid are independent of gastric pH changes induced by these drugs.

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Area of Science:

Pharmacokinetics
Drug Metabolism
Gastrointestinal Physiology

Background:

Antacids and anticholinergic drugs can alter drug absorption by affecting gastric emptying.
The impact of reduced gastric acidity on isoniazid absorption and metabolism remains unclear.
H2 blockers (cimetidine, ranitidine) reduce gastric acid production.

Purpose of the Study:

To investigate the influence of H2 blockers (cimetidine and ranitidine) on the uptake and elimination of isoniazid.
To determine if isoniazid absorption and metabolism are affected by reduced gastric acidity.

Main Methods:

Healthy volunteers (13 total) were administered isoniazid.
Cimetidine and ranitidine were administered to assess their impact on isoniazid pharmacokinetics.
Volunteers were categorized as rapid or slow acetylators to account for metabolic variability.

Main Results:

H2 blockers did not delay or reduce the uptake of isoniazid.
Isoniazid absorption was found to be independent of gastric pH.
Neither isoniazid acetylation nor the oxidative metabolism of acetylated isoniazid was affected by cimetidine or ranitidine.

Conclusions:

The absorption and elimination of isoniazid are not significantly influenced by H2 blockers.
Isoniazid's pharmacokinetic profile appears to be independent of gastric pH.
Concurrent use of H2 blockers with isoniazid is unlikely to alter its efficacy or safety due to altered metabolism.

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