Setnikar I
Rotta Research Laboratorium S.p.A., Monza, Italy.
Int J Tissue React. 1992;14(5):253-61.
The medicinal therapy of osteoarthritis is based on the use of analgesics, NSAIDs and corticosteroids to relieve pain and inflammation. In addition, "chondroprotective" agents (CPA) are used to stop the evolution of the disease. In this review the biochemical and pharmacological activities of some of the most widely used CPAs are described. All of these show more or less marked antiinflammatory activities, which for some of them are the result of an inhibition of cyclo-oxygenase and of prostaglandin biosynthesis, in which case they should be more properly classified as mild NSAIDs. Only two of the CPAs reviewed, diacerein and D-glucosamine sulfate, elicit antiinflammatory and antireactive effects without significant inhibition of the prostaglandin biosynthesis. These agents have also remarkable chondroprotective effects, and only these two agents should be classified as true CPAs. In particular glucosamine sulfate, which naturally occurs in the human body and is almost devoid of toxicity, is suitable for long-term therapeutic use. This, with its chondrometabolic, antireactive and antiarthritic properties, represents the pharmacological rationale for the use of glucosamine sulfate as a disease-modifying agent in osteoarthritis.
骨关节炎的药物治疗基于使用镇痛药、非甾体抗炎药和皮质类固醇来缓解疼痛和炎症。此外,“软骨保护剂”(CPA)被用于阻止疾病的发展。在这篇综述中,描述了一些最广泛使用的CPA的生化和药理活性。所有这些药物都或多或少表现出明显的抗炎活性,其中一些药物的抗炎活性是抑制环氧化酶和前列腺素生物合成的结果,在这种情况下,它们应更恰当地归类为轻度非甾体抗炎药。在综述的CPA中,只有双醋瑞因和硫酸D-葡萄糖胺这两种药物在不显著抑制前列腺素生物合成的情况下引发抗炎和抗反应作用。这些药物也具有显著的软骨保护作用,只有这两种药物应被归类为真正的CPA。特别是硫酸葡萄糖胺,它天然存在于人体中且几乎没有毒性,适合长期治疗使用。其软骨代谢、抗反应和抗关节炎特性,为硫酸葡萄糖胺作为骨关节炎疾病改善药物的使用提供了药理学依据。