Diclofenac edema

CNS Dizziness (mefenamic acid, meloxicam, piroxicam, flurbiprofen, diciofenac, fenoprofen) headache (ketorolac, fenoprofen, indomethacin, diclofenac, flurbiprofen, meclofenamate, meloxicam, nabumetone, naproxen, tolmetin, ketoprofen, sulindac, celecoxib, mefenamic acid, piroxicam, ibuprofen) somnolence/drowsiness (fenoprofen, naproxen) asthenia (tolmetin, etodolac) malaise (etodolac) fatigue (indomethacin) insomnia (meloxicam). Dermatologic Rash/dermatitis, including maculopapular type (ibuprofen, sulindac, meclofenamate, oxaprozin, nabumetone, mefenamic acid, meloxicam) desquamation angioneurotic edema ecchymosis petechiae purpura alopecia pruritus (nabumetone, naproxen) eczema skin discoloration hyperpigmentation skin irritation peeling skin eruptions (naproxen). 

Ring-constrained analogues 37 of the anti-inflammatory drug, diclofenac, have been prepared by acid-catalyzed condensation of aldehydes (or ethylene ketals of ketones) with 36 (Equation 4) <1998MI201>. This reaction presumably proceeds via intramolecular nucleophilic attack by the carboxylic acid group on an iminium ion intermediate from condensation of the secondary amine. Interestingly, the compounds 37 showed comparable activities to diclofenac in the formalin-induced rat paw edema test. 

In a randomized comparison of celecoxib and diclofenac plus omeprazole, renal adverse events, including hypertension, peripheral edema, and renal insufficiency, were common and similar in the two groups (105). They occurred in the 24% of the patients who took celecoxib and in 31% of those who took diclofenac plus omeprazole. Among patients with renal impairment at baseline, 51% of those who took celecoxib and 41% of those who took diclofenac plus omeprazole had renal adverse events. Careful monitoring of renal function in patients taking COX-2 inhibitors or traditional NSAIDs is mandatory, especially in high-risk subjects (for example those with pre-existing renal disease, diabetes, or heart failure). 

Diclofenac is synthesized from N-phenyl-2,6-dichloroaniline (52). It is available in 120 different countries and, perhaps, is the most widely used NSAID in the world. It was introduced in the United States in 1989 but was first marketed in Japan in 1974. It ranks among the top prescription drugs in the United States. Diclofenac possesses structural characteristics of both arylalkanoic acid and the anthranilic acid classes of anti-inflammatory drugs, and it displays anti-inflammatory, analgetic, and antipyretic properties. In the carrageenan-induced rat paw edema assay, it is twice as potent as indomethacin and 450 times as potent as aspirin. As an analgetic, it is six times more potent than indomethacin and 40 times as potent as aspirin in the phenyl benzoquinone-induced writhing assay in mice. As an antipyretic, it is twice as potent as indomethacin and more than 350 times as potent as aspirin in the yeast-... 

The topical application of the EO of Myrica esculenta Buch. Ham. Ex D. Don. (Myricaceae) exhibited strong suppression of mouse ear edema, induced by xylene. The anti-in ammatory activ ity of the EO was found to be 85.3% at topical application. Diclofenac exposed 87.5% of inhibition, which is somewhat more than for the EO. Nevertheless M. esculenta EO showed potent anti in ammatory properties (Agnihotri et al., 2012). 

Another study was made on the anti-inflammatory effect in rodents of the EO of the Euphor-biaceae Croton cajucara Benth. (Sacaca, Euphorbiaceae) by Bighetti et al. (1999). At a dose of 100 mg/kg the EO exerted an anti-inflammatory effect in animal models of acute (canageenin-induced paw edema in mice) and chronic (cotton pellet granuloma) inflanunation. Compared with the negative control a dose-dependent reduction of carrageenin-induced edema was achieved. This EO also reduced chronic inflammation by 38%, whereas diclofenac only achieved an inhibition of 36%. The migration of neutrophils into the peritoneal cavity could not be inhibited by the EO. The anti-inflammatory effect seemed to be related to the inhibition of COX. 

Fluid retention and edema have been observed in some patients taking NSAIDs and therefore diclofenac should be used with caution in patients with a history of fluid retention or heart failure. 

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