دورية أكاديمية
[Pharmacological action and clinical effects of falecalcitriol, a highly potent derivative of active vitamin D3].
| العنوان: | [Pharmacological action and clinical effects of falecalcitriol, a highly potent derivative of active vitamin D3]. |
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| المؤلفون: | Ohtsuka N; Business Strategy Division, Taisho Pharmaceutical Co., Ltd., 24-1, Takata 3-chome, Toshimaku, Tokyo 170-8633, Japan., Urayama K |
| المصدر: | Nihon yakurigaku zasshi. Folia pharmacologica Japonica [Nihon Yakurigaku Zasshi] 2002 Dec; Vol. 120 (6), pp. 427-36. |
| نوع المنشور: | Journal Article; Review |
| اللغة: | Japanese |
| بيانات الدورية: | Publisher: Nippon Yakuri Gakkai Country of Publication: Japan NLM ID: 0420550 Publication Model: Print Cited Medium: Print ISSN: 0015-5691 (Print) Linking ISSN: 00155691 NLM ISO Abbreviation: Nihon Yakurigaku Zasshi Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Tokyo, Nippon Yakuri Gakkai. |
| مواضيع طبية MeSH: | Calcitriol/*administration & dosage , Calcitriol/*analogs & derivatives , Calcitriol/*pharmacology, Animals ; Bone and Bones/metabolism ; Calcitriol/chemistry ; Cell Division/drug effects ; Clinical Trials as Topic ; Dose-Response Relationship, Drug ; Humans ; Hyperparathyroidism, Secondary/drug therapy ; Hyperparathyroidism, Secondary/etiology ; Hypoparathyroidism/drug therapy ; Keratinocytes/cytology ; Kidney Failure, Chronic/complications ; Osteomalacia/drug therapy ; Parathyroid Glands/cytology ; Parathyroid Hormone/metabolism ; Rickets/drug therapy ; Structure-Activity Relationship |
| مستخلص: | Much effort has been made to create highly potentiated active vitamin D for better clinical applications and falecalcitriol was successfully synthesized as one of such candidates with highly potent and long-lasting effects. Its chemical structure has a calcitriol side chain modification in which both methyls at positions C-26 and C-27 are substituted by tri-fluoromethyls. The mechanism for its strong and long-lasting effects is probably due to altered side chain metabolism and decreased inactivation. Although C-24 position hydroxylation catalyzed by Cyp24 inactivates calcitriol, falecarcitriol is metabolized to C-23S hydroxylated metabolite by the same enzyme Cyp24 and this metabolite still has strong activity. Stronger action of falecalcitriol has been shown in target organs or cells of active vitamin D such as bone, parathyroid cells, and keratinocytes, when compared with calcitriol, the endogenous active form of vitamin D. Daily oral administration of falecalcitriol at doses lower than those required for calcitriol has been shown to have clinical effects for the treatment of diseases such as hyperparathyroidism due to chronic renal failure (2 degrees HPT), rickets, osteomalacia and hypoparathyroidism. The comparative study with alfacalcidol showed its specific action on parathyroid hormone suppression and better improvement of bone metabolism markers in 2 degrees HPT patients. |
| Number of References: | 35 |
| المشرفين على المادة: | 0 (Parathyroid Hormone) FXC9231JVH (Calcitriol) G70A8514T8 (26,26,26,27,27,27-hexafluoro-1,25-dihydroxyvitamin D3) |
| تواريخ الأحداث: | Date Created: 20030117 Date Completed: 20030312 Latest Revision: 20190901 |
| رمز التحديث: | 20240627 |
| DOI: | 10.1254/fpj.120.427 |
| PMID: | 12528474 |
| قاعدة البيانات: | MEDLINE |
| تدمد: | 0015-5691 |
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| DOI: | 10.1254/fpj.120.427 |