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A diclofenac derivative without ulcerogenic properties

J L Wallace¹, B Reuter, C Cicala

¹Gastrointestinal Research Group, Faculty of Medicine, University of Calgary, Alberta, Canada.

European Journal of Pharmacology

|May 23, 1994

Summary

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Adding a nitroxybutyl group to diclofenac (nitrofenac) significantly reduced gastric ulceration in animal models. Nitrofenac maintained anti-inflammatory effects comparable to diclofenac without causing gastrointestinal damage.

Area of Science:

Pharmacology
Gastroenterology
Medicinal Chemistry

Background:

Nonsteroidal anti-inflammatory drugs (NSAIDs) like diclofenac are widely used but associated with significant gastrointestinal toxicity.
Developing safer NSAIDs with reduced ulcerogenic potential is a key challenge in drug development.

Purpose of the Study:

To evaluate the ulcerogenic properties of a novel diclofenac derivative, nitrofenac, which incorporates a nitroxybutyl moiety.
To compare the anti-inflammatory and prostaglandin synthesis inhibitory effects of nitrofenac and diclofenac.

Main Methods:

Gastric erosions and ulcers were induced in rats and rabbits, respectively, following administration of diclofenac or nitrofenac.
Prostaglandin E2 synthesis was measured in the stomach and in a peripheral inflammation model.

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Anti-inflammatory activity was assessed using a carrageenan-induced paw edema model.

Main Results:

Diclofenac caused dose-dependent gastric mucosal injury in rats and induced ulcers and intestinal damage in rabbits.
Nitrofenac administration did not result in gastric or intestinal damage in either species.
Both compounds exhibited similar inhibition of prostaglandin E2 synthesis and anti-inflammatory activity.

Conclusions:

The addition of a nitroxybutyl moiety to diclofenac significantly mitigates its ulcerogenic effects.
Nitrofenac retains the anti-inflammatory efficacy of diclofenac while demonstrating improved gastrointestinal safety.
This modification offers a promising strategy for developing safer NSAIDs.