Sources
Help build the largest human-edited directory on the web.
Submit a site - Become an editor
Wikipedia. Licensed under the GNU Free Documentation License.
Are you an expert in this subject? Join the discussion and share your knowledge at Wikipedia.org.
Calcipotriol
From Wikipedia, the free encyclopedia
 |
|
|
Calcipotriol
|
|
| Systematic (IUPAC) name | |
| (1R,3S)-5-[2-[(1R,3aR,7aS)-1-[(2S)-5- cyclopropyl-5-hydroxy-pent-3-en-2-yl]- 7a-methyl-2,3,3a,5,6,7-hexahydro-1H- inden-4-ylidene]ethylidene]-4-methylidene- cyclohexane-1,3-diol |
|
| Identifiers | |
| CAS number | |
| ATC code | D05 |
| PubChem | |
| Chemical data | |
| Formula | C27H40O3 |
| Mol. mass | 412.605 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 5 to 6% |
| Metabolism | Hepatic |
| Half life | ? |
| Excretion | Biliary |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Topical |
Calcipotriol (INN) or calcipotriene (USAN) is a sythetic derivative of calcitriol or Vitamin D. It is used in the treatment of psoriasis, marketed under the trade name Dovonex®.
Contents |
The efficacy of calcipotriol in the treatment of psoriasis was first noticed by the observation of patients receiving various forms of Vitamin D in an osteoporosis study. Unexpectedly, a patient's psoriasis lesions dramatically disappeared. [1]
The precise mechanism of calcipotriol in remitting psoriasis is not well-understood. However, it has been shown to have comparable affinity with calcitriol (Vit D) for the Vitamin D receptor, while being less than 1% as active as the calcitriol in regulating calcium metabolism. The Vitamin D receptor (VDR) belongs to the steroid/thyroid receptor superfamily, and is found on the cells of many different tissues including the thyroid, bone, kindney, and T cells of the immune system. T cells are known to play a role in psoriasis, and it is thought that the binding of calcipotriol to the VDR modulates the T cells gene transcription of cell differentiation and proliferation related genes.
Available as a cream, ointment or scalp solution (50mcg/mL), Calcipotriol is applied twice daily to plaque psoriasis on the body or scalp, but not the face. Improvement is usually detectable within 2 weeks. Most patients show some improvement, slightly more so than is seen with the use or corticosteroids alone. Tachyphalaxis does not occur, an improvement over glucocorticoid therapy.[2]
Calcipotriol has been shown in clinical trial to have an excellent safety profile. [3] Reports of hypercalicemia are rare.[4]
It is also available in combination with the synthetic glucocorticoid betamethasone under the trade name Dovobet®.
- ^ Morimoto, S., Kumahara, Y. A patient with psoriasis cured by 1-α-hydroxyvitamin D3. Med. J. Osaka Univ., 1985, 35:51-54
- ^ Kragbelle, K. Treatment of psoriasis with calicipotriol and other Vitamin D analogues. J. Am. Acad. Dermatol., 1992, 27:1001-1008.
- ^ Brunton, Laurence. Goodman and Gilman's The Pharmacological Basis of Therapeutics, 11th ed. McCraw-Hill, 2006. p. 1664. p. 1704-5.
- ^ Hardman et al. Hypercalicemia associated with calcipotriol (DOVONEX) treatment. Br Med J., 1993, 306:896.
- Leo Pharmaceuticals Product Monograph- Detailed information from the manufacturers, includes the blood testing recommendation (.pdf document).
- Calcipotriene information - U.S. NLM/NIH
 |
This pharmacology-related article is a stub. You can help Wikipedia by expanding it. |