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Calcitriol
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Calcitriol
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| Systematic (IUPAC) name | |
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(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-ylidene]ethylidene]- 4-methylidene-cyclohexane-1,3-diol |
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| Identifiers | |
| CAS number | |
| ATC code | A11 D05AX03 |
| PubChem | |
| DrugBank | |
| 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. | |
| Legal status |
S4 (Au), POM (UK) |
| Routes | Oral, IV, topical |
Calcitriol (INN) (IPA: [kælsɪˈtraɪɒl, kælˈsɪtrɪɒl]) or 1,25-dihydroxycholecalciferol (abbreviated 1,25-(OH)2D3) is the active form of vitamin D found in the body (vitamin D3).
Calcitriol is marketed under various trade names including Rocaltrol (Roche), Calcijex (Abbott) and Decostriol (Mibe, Jesalis).
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, phosphate (PO43−) and parathyroid hormone (PTH) levels. It regulates 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 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
Additional images
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References
- ^ a b Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3
- ^ Calcitriol. In: Klasco RK, editor. Drugdex system. vol 128. Greenwood Village (CO): Thomson Micromedex; 2006.
| Antipsoriatics (D05) | |
|---|---|
| Topical: tars | Tar |
| Topical: antracens | Dithranol |
| Topical: psoralens | Trioxysalen - Methoxsalen |
| Topical: other | Fumaric acid - Calcipotriol - Calcitriol - Tacalcitol - Tazarotene |
| Systemic: psoralens | Trioxysalen - Methoxsalen - Bergapten |
| Systemic: retinoids | Etretinate - Acitretin |
Categories: Vitamins | Secosteroids
The content of this article is licensed under the GNU Free Documentation License (local copy). It uses material from the Wikipedia article "Calcitriol" modified August 9, 2007 with previous authors listed in its history.
