Calcipotriol

ATC CodeD05AX02
CAS number112965-21-6
PUB number5288783
Drugbank IDDB02300
Empirical formulaC27H40O3
Molar mass (g·mol−1)412,6047
Physical statesolid
PKS value14,39
Solubility0,0135

Basics

Calcipotriol has an anti-inflammatory effect and is used to treat chronic plaque psoriasis (psoriasis vulgaris) on the scalp. Calcipotriol is produced synthetically and is a derivative of calcitriol (vitamin D). Calcipotriol therefore belongs to the group of vitamin D3 derivatives. Calcipotriol is applied to the skin as a cream (topical application), either alone or combined with the active ingredient betamethasone, which also has an anti-inflammatory effect.

Graphic structural formula of the active ingredient calcipotriol

Effect

Calcipotriol has growth-inhibiting (antiproliferative), anti-inflammatory (antiphlogistic) and immunomodulating effects. Calcipotriol binds to the vitamin D receptors. It inhibits the growth of keratinocytes, a group of skin cells that produce keratin. Calcipotriol also suppresses the production of inflammatory mediators, i.e. substances that drive the inflammatory process. Calcipotriol does this by binding to the vitamin D receptors located on the T-cells of the immune system. T cells are part of the body's own cellular immune defense and play a role in psoriasis.

Calcipotriol is broken down by the liver and excreted via the gallbladder. Studies show that around 6% have a systemic effect, i.e. they do not only act selectively (locally) on the scalp, but can also enter the body and possibly cause undesirable effects there.

Dosage

Always use calcipotriol exactly as described in the package leaflet or as advised by your doctor.

Calcipotriol is usually applied to the affected area twice a day, but can be reduced to once a day if necessary.

It is important to note that the affected area must not be larger than 30% of the total skin surface area (roughly equivalent to the surface area of an arm) and that no more than 5 mg of calcipotriol per week may be applied to the area, as in both cases the systemic absorption into the body may be too great. The topical application of calcipotriol should not last longer than 8 weeks.

Side effects

The following side effects may occur:

Very common:

  • Skin irritation

Frequent:

  • Worsening of psoriasis
  • Inflammatory skin reactions
  • Reddening of the skin
  • skin rash
  • Peeling of the skin
  • Burning on the skin
  • itching
  • Pain at the site of application

Occasionally:

  • Hypersensitivity reactions
  • Increased calcium content in the blood (hypercalcemia)
  • Sensitivity to light (photophobia)
  • swelling of the skin
  • scaly skin inflammation
  • dry skin
  • Increased calcium excretion in the urine (hypercalciuria)

Rarely:

Interactions

Interactions may occur if the following medicines are taken at the same time:

  • Salicylic acid inactivates calcipotriol and therefore the effect of the cream is weakened
  • systemic vitamin D products or products for calcium supplementation can increase the calcium concentration in the blood and thus trigger hypercalcemia

Contraindications

Calcipotriol must not be taken in the following cases

  • in case of allergy to calcipotriol
  • if liver or kidney function is severely impaired
  • with an increased concentration of calcium in the blood

Age restriction

As there is no experience with the use of calcipotriol in children and adolescents under the age of 18, it should not be used under the age of 18.

Pregnancy & breastfeeding

Calcipotriol should not be used during pregnancy as its safety has not been established.

Calcipotriol should not be used during breastfeeding , as it is not known whether the active substance passes into breast milk.

Thomas Hofko

Thomas Hofko

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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