Diclofenac: an update on its mechanism of action and safety profile

  title={Diclofenac: an update on its mechanism of action and safety profile},
  author={Tong J. Gan},
  journal={Current Medical Research and Opinion},
  pages={1715 - 1731}
  • T. Gan
  • Published 15 June 2010
  • Medicine
  • Current Medical Research and Opinion
BACKGROUND Diclofenac is a proven, commonly prescribed nonsteroidal anti-inflammatory drug (NSAID) that has analgesic, anti-inflammatory, and antipyretic properties, and has been shown to be effective in treating a variety of acute and chronic pain and inflammatory conditions. [] Key Method Reference citations resulting from publications identified in the literature search were reviewed when appropriate. METHODS This article reviews the established, putative, and emerging MOAs of diclofenac; compares the…
Advances in NSAID Development: Evolution of Diclofenac Products Using Pharmaceutical Technology
How pharmaceutical technology has been used to modify the pharmacokinetic properties of diclofenac, leading to the creation of novel drug products with improved clinical utility is illustrated.
A comparison of the therapeutic efficacy of diclofenac in osteoarthritis: a systematic review of randomised controlled trials
  • K. Pavelka
  • Medicine
    Current medical research and opinion
  • 2012
The efficacy of diclofenac is largely unchallenged in that it remains as effective as newer pain relief medications employed in OA.
Topical Nonsteroidal Anti-Inflammatory Drugs: The Importance of Drug, Delivery, and Therapeutic Outcome
  • R. Barkin
  • Medicine, Biology
    American journal of therapeutics
  • 2015
It is important to recognize that pharmacokinetic absorption from topical formulations can vary markedly, even between different formulations of the same drug, depending on the agent, the underlying disorder, and the site of application, and it is essential to consider the patient, the drug, andThe drug delivery mechanism when selecting a topical NSAID preparation.
Repurposing Drugs in Oncology (ReDO)—diclofenac as an anti-cancer agent
The case is made for further clinical investigation of the anticancer effects of DCF, particularly in combination with other agents - with a range of possible multi-drug and multi-modality combinations outlined in the supplementary materials accompanying the main paper.
Efficacy and Safety Profile of Diclofenac/Cyclodextrin and Progesterone/Cyclodextrin Formulations: A Review of the Literature Data
The newly approved lower dose of diclofenac associated with cyclodextrins is consistent with the European Medicines Agency recommendations reported in the revision of the Assessment Report for Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) and Cardiovascular Risk.
Topical Diclofenac, an Efficacious Treatment for Osteoarthritis: A Narrative Review
Topical NSAIDs such as diclofenac should be considered as a guideline-supported, generally well-tolerated, and effective first-line treatment option for knee and hand OA, especially for older patients and those who have comorbid conditions and/or risk factors for various systemic adverse events associated with oral NSAIDs.
Severe anaphylactic reaction to diclofenac.
Hepatoprotective and Nephroprotective Activity of Artemisia absinthium L. on Diclofenac-induced Toxicity in Rats
Non-steroidal anti-inflammatory drugs (NSAIDs), such as diclofenac, can lead to adverse effects on the gastrointestinal tract and the kidney, where the latter is partly due to reduced renal blood flow causing ischemia and subsequent necrosis.
Enhanced analgesic activity by cyclodextrins – a systematic review and meta-analysis
A systematic review to evaluate the analgesic activity of compounds complexed in cyclodextrins, analyzing whether these complexes improved analgesic efficacy found that the complexed drug had a significantly (p < 0.01) greater effect than the non-complexed drug.


An Evidence-Based Update on Nonsteroidal Anti-Inflammatory Drugs
This review will provide an educational update on the current evidence of the efficacy and adverse effects of NSAIDs, and an algorithm is proposed which delineates a general decision-making tree to select the most appropriate analgesic for an individual patient based on the evidence reviewed.
Diclofenac sodium. A reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy.
Diclofenac is one of the few NSAIDs of 'first choice' in the treatment of acute and chronic painful and inflammatory conditions and rarely produces gastrointestinal ulceration or other serious side effects.
Review of the pharmaceutical properties and clinical effects of the topical NSAID formulation, diclofenac epolamine.
DI-EP patches control pain and signs of joint or physical injury compared with placebo controls by 3-5 days with almost complete pain relief at 14 days, and was shown to have equivalent therapeutic effect to another DI diethylammonium gel formulation (Voltaren Emulgel).
Nonsteroidal anti-inflammatory drugs and hepatic toxicity: a systematic review of randomized controlled trials in arthritis patients.
  • A. Rostom, L. Goldkind, L. Laine
  • Medicine
    Clinical gastroenterology and hepatology : the official clinical practice journal of the American Gastroenterological Association
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Cox-2-specific inhibitors: definition of a new therapeutic concept.
The criteria that must be met to characterize a compound as COX-2-specific are outlined and clinical evidence of clear improvement in gastrointestinal tolerability and safety must be demonstrated in addition to complementary evidence of COx-2 selectivity obtained from enzyme, biochemical, and clinical pharmacology evaluations.
Gastrointestinal safety of cyclooxygenase-2 inhibitors: a Cochrane Collaboration systematic review.
  • A. Rostom, Katherine E Muir, G. Wells
  • Medicine
    Clinical gastroenterology and hepatology : the official clinical practice journal of the American Gastroenterological Association
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Mechanism of action of anti-inflammatory drugs.
  • J. Vane, R. Botting
  • Biology, Medicine
    Advances in experimental medicine and biology
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The activity of a number of NSAIDs has been investigated in several test systems, showing that most of those marketed have higher activities against COX-1 or are equipotent against both isoform, and there are several new non-steroidal COx-2 inhibitors in development.
Topical diclofenac and its role in pain and inflammation: an evidence-based review
Topical diclofenac is well tolerated, resulting mostly in mild, easily resolved local skin irritation, and is associated with fewer side-effects than other topical NSAIDs and a lower rate of gastrointestinal complications than oral NSAIDs.
Dissociation Between the Antinociceptive and Anti-Inflammatory Effects of the Nonsteroidal Anti-Inflammatory Drugs
SummaryThe authors challenge the general view that the analgesic effect of the nonsteroidal anti-inflammatory drugs (NSAIDs) can be universally attributed to their inhibitory effects on the synthesis
Effect of diclofenac sodium on the arachidonic acid cascade.