Diclofenac-Potassium in Migraine

McNeely, Wendy; Goa, Karen L.

doi:10.2165/00003495-199957060-00016

Cited by 47 publications

(51 citation statements)

References 21 publications

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“…Diclofenac (DCF) is a nonsteroidal anti-inflammatory drug (NSAID) that is prescribed to alleviate symptoms associated with ankylosing spondylitis, osteoarthritis, rheumatoid arthritis, and migraine (McNeely and Goa, 1999;Depomed, 2009;Novartis, 2011). DCF is generally well tolerated, although long-term usage has been implicated with a variety of adverse events in a subset of patients.…”

Section: Introductionmentioning

confidence: 99%

Multidrug Resistance-Associated Protein 3 Plays an Important Role in Protection against Acute Toxicity of Diclofenac

et al. 2015

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Diclofenac (DCF) is a nonsteroidal anti-inflammatory drug commonly prescribed to reduce pain in acute and chronic inflammatory diseases. One of the main DCF metabolites is a reactive diclofenac acyl glucuronide (DCF-AG) that covalently binds to biologic targets and may contribute to adverse drug reactions arising from DCF use. Cellular efflux of DCF-AG is partially mediated by multidrug resistanceassociated proteins (Mrp). The importance of Mrp2 during DCFinduced toxicity has been established, yet the role of Mrp3 remains largely unexplored. In the present work, Mrp3-null (KO) mice were used to study the toxicokinetics and toxicodynamics of DCF and its metabolites. DCF-AG plasma concentrations were 90% lower in KO mice than in wild-type (WT) mice, indicating that Mrp3 mediates DCF-AG basolateral efflux. In contrast, there were no differences in DCF-AG biliary excretion between WT and KO, suggesting that only DCF-AG basolateral efflux is compromised by Mrp3 deletion. Susceptibility to toxicity was also evaluated after a single high DCF dose. No signs of injury were detected in livers and kidneys; however, ulcers were found in the small intestines. Furthermore, the observed intestinal injuries were consistently more severe in KO compared with WT. DCF covalent adducts were observed in liver and small intestines; however, staining intensity did not correlate with the severity of injuries, implying that tissues respond differently to covalent modification. Overall, the data provide strong evidence that (1) in vivo Mrp3 plays an important role in DCF-AG disposition and (2) compromised Mrp3 function can enhance injury in the gastrointestinal tract after DCF treatment.

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Section: Introductionmentioning

confidence: 99%

Multidrug Resistance-Associated Protein 3 Plays an Important Role in Protection against Acute Toxicity of Diclofenac

et al. 2015

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“…In a multicenter, double-blind, randomized trial, diclofenac potassium, known to be effective in the treatment of migraine headache at dosages of 50 or 100 mg [28], was shown to be more effective in the treatment of episodic tension-type headache than placebo at low dosages (12.5 and 25 mg) [26]. In addition, diclofenac potassium was found to be comparable with 400 mg of ibuprofen.…”

Section: Nonsteroidal Anti-inflammatory Drugsmentioning

confidence: 96%

Current and potential future drug therapies for tension-type headache

Ashina

2003

Current Science Inc

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Tension-type headache is a common primary headache with tremendous socioeconomic impact. Establishment of an accurate diagnosis is important before initiation of any pharmacologic therapy. Simple analgesics and nonsteroidal anti-inflammatory drugs are the mainstays of treatment of episodic tension-type headache. The tricyclic antidepressant amitriptyline is the drug of choice in the preventive treatment of chronic tension-type headache. Progress in basic neuroscience has emphasized the importance of nitric oxide inhibition and N-methyl-D-aspartate and alpha-amino-3-hydroxy-5-methylisoxasole-4-propionic acid receptor antagonism in the treatment of chronic pain. It has been demonstrated that inhibition of nitric oxide is effective in chronic tension-type headache. These interesting data indicate that more specific and effective treatment possibilities will emerge in the future.

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“…Согласно недавно полученным данным [12] калиевая соль диклофе-нака в форме таблеток с немедлен-ным высвобождением (50 и 100 мг) оказывает очень хорошее обезболи-вающее действие при лечении миг-рени, поскольку концентрация пре-парата в плазме крови достигала ма-ксимальной в среднем через 1 ч пос-ле приема (через 0,33-2 ч), а аналь-гезирующий эффект развивался че-рез 60-90 мин. Сравнивая скорость всасывания, можно заключить, что диклофенак калия в форме саше будет давать гораздо более быстрый обезбо-ливающий эффект.…”

Section: обсуждение и заключениеunclassified

Pharmacokinetics of diclofenac potassium after oral administration of sachets and tablets

Марцо¹,

Monti²,

Кривелли³

et al. 2008

Modern Rheumatology Journal

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Диклофенак (2(2,6 дихлоро-анилино)фенилацетиловая кислота, CAS 15307-86-5) -нестероидный противовоспа-лительный препарат, используемый для купирования боли и лечения воспалительных процессов различной локализации (рис. 1) [1].Существует множество фармацевтических форм дикло-фенака, благодаря чему его можно применять перорально, ректально, внутримышечно или местно. Препарат предста-влен в виде свободной кислоты, натриевой и калиевой соли, причем калиевая соль диклофенака гораздо лучше раство-ряется в воде [1,2].Цель исследования -сравнительный анализ фармако-кинетических показателей и изменений во времени сыворо-точной концентрации калиевой соли диклофенака, после перорального приема в дозе 50 мг в форме саше или табле-ток, покрытых сахарной оболочкой. Дизайн исследования: две формы препарата, перекрестное исследование с двумя периодами при однократном введении препарата.

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Diclofenac-Potassium in Migraine

Cited by 47 publications

References 21 publications

Multidrug Resistance-Associated Protein 3 Plays an Important Role in Protection against Acute Toxicity of Diclofenac

Multidrug Resistance-Associated Protein 3 Plays an Important Role in Protection against Acute Toxicity of Diclofenac

Current and potential future drug therapies for tension-type headache

Pharmacokinetics of diclofenac potassium after oral administration of sachets and tablets

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