Review of the Animal and Clinical Pharmacology of Diflunisal

doi:10.1002/phar.1983.3.2p2.9

Paper

Review of the Animal and Clinical Pharmacology of Diflunisal

Published Mar 1, 1983 · R. Davies

Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy

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17

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0

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Abstract

Diflunisal is a new salicylic acid derivative identified after a search for a compound with improved potency, enhanced gastrointestinal tolerance relative to its antiinflammatory activity, and a longer duration of action than that of aspirin. Animal and clinical studies have confirmed these properties. As an inhibitor of cyclooxygenase tested in vitro in a sheep seminal vesicle preparation, diflunisal was less potent than indomethacin but 10 to 20 times more active than aspirin. In addition, it was shown biochemically to act as a moderate free radical scavenger. Diflunisal is well absorbed from the gastrointestinal tract, is subject to dose‐dependent pharmacokinetics (like aspirin), and reaches steady‐state levels in a predictable fashion in most persons. The drug is excreted by the kidneys, and its apparent half‐life is lengthened in the presence of renal failure. A number of drug interactions have been described. Diflunisal produces reversible effects on platelet aggregation when given in high doses, whereas aspirin produces irreversible aggregation at low doses. Measurements of fecal blood loss and endoscopic examinations have confirmed the improved gastrointestinal tolerance of diflunisal compared to aspirin.

Literature Review

Study Snapshot

Diflunisal is a new salicylic acid derivative with improved potency, enhanced gastrointestinal tolerance, and longer duration of action compared to aspirin, offering potential for use in pain management.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Review of the Animal and Clinical Pharmacology of Diflunisal

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References

Diflunisal in the Treatment of the Pain of Osteoarthritis Summary of Clinical Studies

Diflunisal is a highly effective and well-tolerated nonsteroidal antiinflammatory drug for short- and long-term treatment of osteoarthritis pain, comparable to aspirin and better tolerated than ibuprofen.

A 12‐hour Evaluation of the Analgesic Efficacy of Diflunisal, Propoxyphene, A Propoxyphene‐Acetaminophen Combination, and Placebo in Postoperative Oral Surgery Pain

Diflunisal 500 and 1000 mg effectively relieve postoperative oral surgery pain for 12 hours, with diflunisal 1000 mg being significantly superior to the propoxyphene-acetaminophen combination.

Captopril: Clinical Pharmacology and Benefit‐to‐Risk Ratio in Hypertension and Congestive Heart Failure

Captopril is effective and safe for treating resistant hypertension and congestive heart failure, with a benefit-to-risk ratio favorable for its use in these conditions.

Effects of diflunisal on platelet function and fecal blood loss

Diflunisal inhibits platelet function less than aspirin, with doses in the same range as aspirin showing similar effects.

Influence of chronic renal failure and hemodialysis on diflunisal plasma protein binding

Chronic renal failure and hemodialysis decrease diflunisal plasma protein binding, with oleic acid potentially playing a competitive inhibitory role.

Decreased body clearance of diflunisal in renal insufficiency--an alternative explanation.

Renal insufficiency leads to decreased body clearance of diflunisal, providing an alternative explanation for its pharmacokinetics.

Comparison of the effects of diflunisal and other salicylates on the intragastric electropotential

Diflunisal and other salicylates significantly decrease the intragastric electropotential difference in anaesthetized cats, potentially causing gastric mucosal damage and gastrointestinal bleeding.

Citations