Calcipotriol/ja: Difference between revisions

Calcipotriol is also available as [[Calcipotriol/betamethasone dipropionate]], a fixed-dose [[combination medication]] with the synthetic [[corticosteroid]] [[betamethasone dipropionate]] for the treatment of [[plaque psoriasis]].

==Medical uses==

Chronic plaque psoriasis is the chief medical use of calcipotriol. It has also been used successfully in the treatment of [[alopecia areata]].

==Contraindications==

Hypersensitivity, use on face, hypercalcaemia, or evidence of vitamin D toxicity are the only [[contraindications]] for calcipotriol use.

==Adverse effects==

Adverse effects by frequency:

;Very common (> 10% frequency):

* Burning

* Itchiness

* Skin irritation

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;Common (1–10% frequency):

* [[Dermatitis]]

* Dry skin

* [[Erythema]]

* Peeling

* Worsening of psoriasis including facial/scalp

* Rash

;Uncommon (0.1–1% frequency):

* Exacerbation of [[psoriasis]]

;Rare (< 0.1% frequency):

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* Allergic contact dermatitis

* [[Hypercalcaemia]]

* [[Photosensitivity]]

* Changes in pigmentation

* Skin atrophy

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== Interactions ==

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==Pharmacology==

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===Mechanism of action===

The precise mechanism of calcipotriol in remitting psoriasis is not well understood.  However, it has been shown to have comparable affinity with calcitriol for the [[vitamin D receptor]] (VDR), while being less than 1% as active as the calcitriol in regulating [[calcium metabolism]].  The vitamin D receptor belongs to the steroid/thyroid receptor superfamily, and is found on the cells of many different tissues including the thyroid, bone, kidney, and [[T cell]]s 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.

In mouse studies, topical calcipotriol administration to the ear and dorsal skin led to a dose-dependent increase in the production of the epithelial cell-derived cytokine [[Thymic stromal lymphopoietin|TSLP]] by [[keratinocyte]]s, and triggered [[atopic dermatitis]] at high concentrations. This upregulation of TSLP production due to calcipotriol application is thought to be mediated through the [[Coactivation (Transcription)|coactivation]] of [[Calcitriol receptor|vitamin D receptor]]/[[Retinoid X receptor alpha|RXRα]] and vitamin D receptor/[[Retinoid X receptor beta|RXRβ]] heterodimers. As psoriasis is typically thought to be partially driven by [[T helper cell|Th1]]/[[T helper 17 cell|Th17]] inflammatory cytokines, calcipotriol treatment at appropriate concentrations may alleviate psoriasis symptoms by repressing Th1/Th17 inflammation through TSLP production, which is linked to a [[T helper cell|Th2]] response. However, it is important to note that this has not yet been confirmed.

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===Pharmacokinetics===

After application and systemic uptake, calcipotriol undergoes rapid [[hepatic]] metabolism. Calcipotriol is metabolized to MC1046 (the α,β−unsaturated ketone analog), which is subsequently metabolized to its primary metabolite, the saturated ketone analog MC1080. MC1080 is then slowly metabolized to [[calcitroic acid]].

==Chemistry==

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== External links ==

{{Antipsoriatics}}

{{Vitamins}}

{{Vitamin D receptor modulators}}