Nabumetone:治疗使用和安全性管理的骨关节炎和类风湿性关节炎。

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Hedner T, Samulesson O Wahrborg P, Wadenvik H) KA,埃

Nabumetone:治疗使用和安全性管理的骨关节炎和类风湿性关节炎。

药。2004;64 (20):2315 - 43;讨论2344 - 5。

PubMed ID

15456329 (在PubMed

]

文摘

Nabumetone是一种非甾体类抗炎药物前体,发挥其药理作用通过代谢物6-methoxy-2-naphthylacetic酸(6-MNA)。Nabumetone本身非酸性的,以及吸收后,它经历了广泛的初步的代谢形成的主要循环活性代谢物(6-MNA)是一个更加优先的有效抑制剂cyclo-oxygenase (COX) 2。的三个主要代谢途径nabumetone O-demethylation,减少酮醇,和侧链的氧化裂解发生屈服醋酸衍生品。基本上没有nabumetone和< 1%不变的主要6-MNA代谢物会不变在尿液中排出,80%的剂量可以恢复,另外10%的粪便。Nabumetone在临床上主要用于骨关节炎(OA)患者或管理类风湿性关节炎(RA),以减少疼痛和炎症。的临床疗效nabumetone也被评估在强直性脊柱炎患者,软组织损伤和青少年类风湿性关节炎。最优的口服剂量nabumetone OA患者每天1克一次,这是良好的耐受性。治疗反应优于安慰剂,类似于非选择性COX抑制剂。在RA患者中,睡前nabumetone 1 g是最优的,但一个额外的0.5 - 1 g可以早上管理患者持续的症状。在RA, nabumetone表明阿司匹林(乙酰水杨酸)类似的临床疗效,双氯芬酸、吡罗昔康、布洛芬和萘普生。 Clinical trials and a decade of worldwide safety data and long-term postmarketing surveillance studies show that nabumetone is generally well tolerated. The most frequent adverse effects are those commonly seen with COX inhibitors, which include diarrhoea, dyspepsia, headache, abdominal pain and nausea. In common with other COX inhibitors, nabumetone may increase the risk of GI perforations, ulcerations and bleedings (PUBs). However, several studies show a low incidence of PUBs, and on a par with the numbers reported from studies with COX-2 selective inhibitors and considerably lower than for nonselective COX inhibitors. This has been attributed mainly to the non-acidic chemical properties of nabumetone but also to its COX-1/COX-2 inhibitor profile. Through its metabolite 6-MNA, nabumetone has a dose-related effect on platelet aggregation, but no effect on bleeding time in clinical studies. Furthermore, several short-term studies have shown little to no effect on renal function. Compared with COX-2 selective inhibitors, nabumetone exhibits similar anti-inflammatory and analgesic properties in patients with arthritis and there is no evidence of excess GI or other forms of complications to date.

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药物靶点

药物	目标	类	生物	药理作用	行动
Nabumetone	前列腺素合成酶2 G / H	蛋白质	人类	是的	抑制剂	细节