Percutaneous Treatment of Acute Soft Tissue Lesions with Naproxen Gel and Ketoprofen Gel

Baixauli, Francisco Raga; Inglés, F.; Alcântara, Paulo Sérgio Martins de; Navarrete, Rocío; Puchol, E.; Vidal, Fernando; Castellá, Francisco Baixauli

doi:10.1177/030006059001800505

Cited by 17 publications

(13 citation statements)

References 4 publications

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“…1 Therefore, percutaneous administration of NSAIDs, like ketoprofen and naproxen, has been studied to minimize GI side-effects and other possible systemic side-effects due to high plasma peak levels after oral administration. [2][3][4] Recent studies have shown that GI sideeffects of NSAIDs are, at least partly, due to inhibition of the COX-1 enzyme, and thus it may not be possible to eliminate GI side-effects of NSAIDs by percutaneous administration. 5 However, a topically administered drug would be more suitable for treatment of local inflammatory and pain processes because of higher local drug concentration.…”

Section: Introductionmentioning

confidence: 99%

In vitro evaluation of acyloxyalkyl esters as dermal prodrugs of ketoprofen and naproxen

Rautio

Taipale

Gynther

et al. 1998

Journal of Pharmaceutical Sciences

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A series of acyloxyalkyl esters of ketoprofen and naproxen were synthesized and investigated as topical prodrugs with the aim of improving the dermal delivery of the drugs. In addition, some hydroxyalkyl esters of ketoprofen and naproxen were synthesized as possible intermediates of acyloxyalkyl prodrugs. All of the prodrugs were more lipophilic than their parent molecules, as evaluated by drug partitioning between 1-octanol and phosphate buffer at pH 7.4 (log Papp). However, their solubilities in aqueous solutions decreased markedly compared with the parent molecules. The prodrugs were stable toward chemical hydrolysis in aqueous solutions (pH 7.4), but were hydrolyzed to the parent drug both in 80% human serum and in human skin homogenate, with half-lives ranging from 4 to 137 min and from 13 to 403 min, respectively. The abilities of the selected naproxen acyloxyalkyl prodrugs to deliver naproxen through excised human skin were evaluated. Generally, the prodrugs showed similar dermal delivery as the parent drug through cadaver skin. In the present series of lipophilic prodrugs of naproxen, the prodrug with the highest aqueous solubility was the most effective prodrug to deliver naproxen through the skin.

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Section: Introductionmentioning

confidence: 99%

In vitro evaluation of acyloxyalkyl esters as dermal prodrugs of ketoprofen and naproxen

Rautio

Taipale

Gynther

et al. 1998

Journal of Pharmaceutical Sciences

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“…Detailed information can be found in the Supplemental Table (available online at http:// www.mayoclinicproceedings.org). The most commonly studied agents were NSAIDs (n¼26), [30][31][32]37,39,51,52,54,58,61,64,71,72,74,78,[80][81][82][84][85][86][87][88][89][90][91] followed by lidocaine (n¼9), 33,36,[40][41][42][43]55,65,83 capsaicin (n¼6), 29,35,38,53,73,75 and amitriptyline (n¼5). 45,47,59,67,68 Other agents studied included glyceryl trinitrate (n¼3), 44,48,69 opioids (n¼2), 50,60 menthol (n¼2), ...…”

Section: Study Characteristicsmentioning

confidence: 99%

“…45,47,59,67,68 Other agents studied included glyceryl trinitrate (n¼3), 44,48,69 opioids (n¼2), 50,60 menthol (n¼2), 62,92 pimecrolimus (n¼2), 28,49 and phenytoin (n¼2). 66,70 The most common indications were soft tissue injuries and related conditions (n¼17), 30,32,37,48,50,54,57,63,66,71,74,81,85,86,[89][90][91] followed by neuropathic pain (n¼17), 29,34,36,38,[40][41][42][43]47,59,65,67,72,73,78,82,87 experimental pain (n¼6), 45,53,56,64,…”

Section: Study Characteristicsmentioning

confidence: 99%

Topical Analgesics in the Management of Acute and Chronic Pain

Argoff

2013

Mayo Clinic Proceedings

107

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Oral analgesics are commonly prescribed for the treatment of acute and chronic pain, but these agents often produce adverse systemic effects, which sometimes are severe. Topical analgesics offer the potential to provide the same analgesic relief provided by oral analgesics but with minimal adverse systemic effects. This article describes the results of a systematic review of the efficacy of topical analgesics in the management of acute and chronic pain conditions. A literature search of MEDLINE/PubMed was conducted using the keywords topical analgesic AND chronic pain OR acute pain OR neuropathic pain and focused only on individual clinical trials published in English-language journals. The search identified 92 articles, of which 65 were eligible for inclusion in the review. The most commonly studied topical analgesics were nonsteroidal anti-inflammatory drugs (n=27), followed by lidocaine (n=9), capsaicin (n=6), amitriptyline (n=5), glyceryl trinitrate (n=3), opioids (n=2), menthol (n=2), pimecrolimus (n=2), and phenytoin (n=2). The most common indications were acute soft tissue injuries (n=18), followed by neuropathic pain (n=17), experimental pain (n=6), osteoarthritis and other chronic joint-related conditions (n=5), skin or leg ulcers (n=5), and chronic knee pain (n=2). Strong evidence was identified for the use of topical diclofenac and topical ibuprofen in the treatment of acute soft tissue injuries or chronic joint-related conditions, such as osteoarthritis. Evidence also supports the use of topical lidocaine in the treatment of postherpetic neuralgia and diabetic neuropathy. Currently, limited evidence is available to support the use of other topical analgesics in acute and chronic pain.

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“…Although the general acceptance of topical NSAIDs as a viable treatment option is relatively recent in the United States, they have been available in Europe for many years. 85,86 Worldwide, at least 15 topical NSAIDs have been available since 1999. 87 Factors that have likely limited their use in the United States include their availability only through compounding pharmacies and the general lack of coverage through traditional prescription medication plans.…”

Section: Topical Nsaidsmentioning

confidence: 99%