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14-September-2008 18:02:45 - Calcitriol Calcitriol Systematic IUPAC name 1R,3S- 5-2-1R,3aR,7aS-1- 2R-6-hydroxy-6-methyl-heptan-2-yl- 7a-methyl-2,3,3a,5,6,7-hexahydro-1H- inden-4-ylideneethylidene- 4-methylidene-cyclohexane-1,3-diol Identifiers CAS number 32222-06-3 ATC code A11CC04 D05AX03 PubChem 134070 DrugBank APRD00246 Chemical data Formula C27H44O3 Mol. mass 416.64 g/mol Pharmacokinetic data Bioavailability ? Metabolism Renal Half life 5-8 hours Excretion Renal Therapeutic considerations Pregnancy cat. B3 Au, C U.S. Legal status S4 Au, POM UK Routes Oral, IV, topical Calcitriol INN pronounced /ËŒkælsɨˈtraɪɒl/, /ËŒkælˈsɨtriË?É’l/ or 1,25-dihydroxycholecalciferol abbreviated 1,25-OH2D3 also known as calitrol is the active form of vitamin D found in the body 1,25OH2D3. It increases the absorption of calcium and phosphate from the gastrointestinal tract and kidneys and inhibits release of calcitonin. Calcitriol is marketed under various trade names including Rocaltrol Roche, Calcijex Abbott and Decostriol Mibe, Jesalis. Contents 1 Production and function 2 Metabolism 3 Indications 4 Adverse effects 5 See also 6 Additional images 7 References Production and function It is produced in the kidneys via 25-Hydroxyvitamin D3 1-alpha-Hydroxylase by conversion from 25-hydroxycholecalciferol calcidiol. This is stimulated by a decrease in serum calcium and/or phosphate PO43-, and an increase in parathyroid hormone PTH and/or prolactin levels. It increases blood calcium levels by increasing the absorption of calcium and phosphate from the gastrointestinal tract, increasing calcium and phosphate reabsorption in the kidneys, and inhibiting the release of calcitonin. Calcitriol acts in concert with parathyroid hormone PTH. Calcitriol is also commonly used as a medication in the treatment of hypocalcemia and osteoporosis. Metabolism Calcitriol becomes calcitroic acid through the action of 24-hydroxylase. Calcitroic acid is excreted in the urine. Indications Calcitriol is indicated for:1 Treatment of hypocalcaemia - hypoparathyroidism, osteomalacia adults, rickets infants, children, renal osteodystrophy, chronic renal dialysis Treatment of osteoporosis Prevention of corticosteroid-induced osteoporosis Calcitriol is also sometimes used topically in the treatment of psoriasis, however the evidence to support its efficacy is inconclusive.2 The vitamin D analogue calcipotriol is more commonly used for psoriasis. Adverse effects The main adverse drug reaction associated with calcitriol therapy is hypercalcaemia - early symptoms include: nausea, vomiting, constipation, anorexia, apathy, headache, thirst, sweating, and/or polyuria. Compared to other vitamin D compounds in clinical use cholecalciferol, ergocalciferol, calcitriol has a higher risk of inducing hypercalcaemia. However, such episodes may be shorter and easier to treat due to its relatively short half-life.1 See also Vitamin D Additional images Calcitriol synthesis References ^ a b Rossi S, or. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3 ^ Calcitriol. In: Klasco RK, or. Drugdex system. vol 128. Greenwood Village CO: Thomson Micromedex; 2006. v d e Endocrine system: hormones/endocrine glands Peptide hormones, Steroid hormones Hypothalamic-pituitary Hypothalamus: TRH, CRH , GnRH, GHRH, somatostatin, dopamine - Posterior pituitary: vasopressin, oxytocin - Anterior pituitary: α FSH, LH, TSH, GH, prolactin, POMC ACTH, MSH, endorphins, lipotropin Adrenal axis Adrenal medulla: epinephrine, norepinephrine - Adrenal cortex: aldosterone, cortisol, DHEA Thyroid axis Thyroid: thyroid hormone T3 and T4 - calcitonin - Parathyroid: PTH Gonadal axis Testis: testosterone, AMH, inhibin - Ovary: estradiol, progesterone, inhibin/activin, relaxin pregnancy Other end. glands Pancreas: glucagon, insulin, somatostatin - Pineal gland: melatonin Non-end. glands Placenta: hCG, HPL, estrogen, progesterone - Kidney: renin, EPO, calcitriol, prostaglandin - Heart atrium: ANP - Stomach: gastrin, ghrelin - Duodenum: CCK, GIP, secretin, motilin, VIP - Ileum: enteroglucagon - Adipose tissue: leptin, adiponectin, resistin - Thymus: Thymosin - Thymopoietin - Thymulin - Skeleton: Osteocalcin - Liver/other: Insulin-like growth factor IGF-1, IGF-2 Target-derived NGF, BDNF, NT-3 v d e Vitamins A11 Fat soluble A: Retinol - Beta-carotene - Tretinoin - Alpha-carotene D3: 7-Dehydrocholesterol → Previtamin D3 → Cholecalciferol D3 → Calcidiol → Calcitriol active form → Calcitroic acid D2: Ergosterol → Ergocalciferol D2 D analogues: Dihydrotachysterol - Calcipotriol - Tacalcitol D4: Dihydroergocalciferol E: Tocopherol - Tocotrienol K: Naphthoquinone - Phylloquinone/K1 - Menatetrenone/K2 Water soluble: B vitamins B1 Thiamine - B2 Riboflavin - B3 Niacin, Nicotinamide - B5 Pantothenic acid, Dexpanthenol, Pantethine - B6 Pyridoxine, Pyridoxal phosphate, Pyridoxamine - B7 Biotin - B9 Folic acid, Folinic acid - B12 Cyanocobalamin, Hydroxocobalamin, Methylcobalamin, Cobamamide Water soluble: other C Ascorbic acid - Choline see also enzyme cofactors v d e Antipsoriatics D05 Topical: tars Tar Topical: antracens Dithranol Topical: psoralens Trioxysalen - Methoxsalen Topical: other Fumaric acid - vitamin D Calcipotriol, Calcitriol, Tacalcitol - Tazarotene Systemic: psoralens Trioxysalen - Methoxsalen - Bergapten Systemic: retinoids Etretinate - Acitretin Retrieved from http://en..org/wiki/Calcitriol Categories: Vitamins | Secosteroids Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch Þ‹Þ¨ÞˆÞ¬Þ€Þ¨Þ„Þ¦Þ?Þ° Español МакедонÑ?ки Polski Português This page was last modified on 9 September 2008, at 12:19
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