Kragballe K
Department of Dermatology, Marselisborg University Hospital, Arhus, Denmark.
Pharmacol Toxicol. 1995 Oct;77(4):241-6. doi: 10.1111/j.1600-0773.1995.tb01020.x.
Vitamin D is best known for its role in the regulation of calcium and bone metabolism. The effects of the biologically active form of vitamin D, 1,25-dihydroxyvitamin D3 (1,25 (OH)2D3), are mediated by binding to a specific intracellular vitamin D receptor, which is present in most tissues including the skin where it regulates the growth of epidermal cells. Calcipotriol is a synthetic analogue of 1,25(OH)2D3. In vitro the activity of calcipotriol is comparable to that of 1,25(OH)2D3. In vivo, however, the risk of calcipotriol changing calcium metabolism is greatly reduced. Animal studies have established that calcipotriol is 100-200 times less calcaemic than 1,25(OH)2-D3. This low calcaemic activity is mainly due to the rapid metabolism of calcipotriol. This pharmacological profile makes calcipotriol an ideal candidate for topical treatment of hyperproliferative skin disorders, such as psoriasis. This paper reviews the clinical experience with calcipotriol in psoriasis patients.
维生素D最为人熟知的作用是调节钙和骨代谢。维生素D的生物活性形式1,25 - 二羟基维生素D3（1,25(OH)2D3）的作用是通过与特定的细胞内维生素D受体结合来介导的，该受体存在于包括皮肤在内的大多数组织中，在皮肤中它调节表皮细胞的生长。卡泊三醇是1,25(OH)2D3的合成类似物。在体外，卡泊三醇的活性与1,25(OH)2D3相当。然而，在体内，卡泊三醇改变钙代谢的风险大大降低。动物研究表明，卡泊三醇的血钙升高作用比1,25(OH)2 - D3低100 - 200倍。这种低血钙活性主要归因于卡泊三醇的快速代谢。这种药理学特性使卡泊三醇成为局部治疗增殖性皮肤病（如银屑病）的理想候选药物。本文综述了卡泊三醇治疗银屑病患者的临床经验。
