Calcipotriol is only found in individuals that have used or taken this drug. It is a synthetic derivative of calcitriol or Vitamin D. The precise mechanism of calcipotriol in remitting psoriasis is not well-understood. However, it has been shown to have a comparable affinity with calcitriol 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, kidney, 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.
Calcipotriene is a synthetic vitamin D derivative usually formulated for topical dermatological use, antipsoriatic Calcipotriene (calcipotriol) competes equally with active 1,25-hydroxy-2D3 (the natural form of vitamin D) for 1,25-hydroxy-2D3 receptors in regulating cell proliferation and differentiation. It induces differentiation and suppresses the proliferation of keratinocytes, reversing abnormal keratinocyte changes in psoriasis, and leads to normalization of epidermal growth. (NCI04)
Mechanism of Action of Calcipotriol
The precise mechanism of calcipotriol in remitting psoriasis is not well-understood, however, it has been shown to have a comparable affinity with calcitriol for the Vitamin D receptor while being less than 1% the activity 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, kidney, and T cells of the immune system. T cells are known to play a role in psoriasis and are believed to undergo modulation of gene expression with the binding of calcipotriol to the VDR. This modulation is thought to affect gene products related to cell differentiation and proliferation.
Topically applied calcipotriol has low hypercalcaemic potential and, in contrast to topical corticosteroids, oral retinoids and orally administered calcitriol, methotrexate and cyclosporin, calcipotriol do not appear to be associated with a risk of serious adverse events. Thus, at this early stage in its clinical development, calcipotriol appears to be an effective and well-tolerated topical therapy for the management of psoriasis; if promising preliminary clinical findings are confirmed, calcipotriol will represent a major advance in this difficult area of therapeutics.
Drug Indications of Calcipotriol
- For the treatment of moderate plaque psoriasis in adults.
- Psoriasis Vulgaris
- Treatment of psoriasis
- Drugs used to treat or prevent skin disorders or for the routine care of the skin.
Side Effects of Calcipotriol
Common side effects (probably affect up to 1 in 10 people)
- Rash.
- Burning or stinging feeling.
- Dry skin.
- Itching skin.
- Redness.
- Itchy rash and skin inflammation in the area where the medicine is used.)
- Worsening of your psoriasis.
- Red, itchy, scaly rash. Blisters may form.
- These may weep or become crusty (eczema).
The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.
Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.
- burning, dry, irritated, peeling, or red skin
- face and scalp irritation (when the medication is transferred from another part of the body)
- itching, redness, and swelling of the skin
Stop taking the medication and seek immediate medical attention if any of the following occur:
- symptoms of a serious allergic reaction (e.g., rash, itching, swelling, difficulty breathing, dizziness)
- symptoms of high blood calcium levels (e.g., fatigue, mental confusion, loss of appetite, depression, nausea or vomiting, constipation)
For the cream—Systemic absorption of the cream has not been studied but is thought to be less than that of the ointment.
For the ointment—Approximately 6% (± 3%, SD) of the applied dose of radiolabeled calcipotriene ointment is absorbed systemically when the ointment is applied topically to psoriasis plaques; about 5% (± 2.6%, SD) is absorbed when applied to normal skin.
For the solution—Approximately 1% of the applied dose is systemically absorbed.
Drug Interactions of Calcipotriol
Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications that you are taking. Also, tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them. Depending on your specific circumstances, your doctor may want you to:
- stop taking one of the medications,
- change one of the medications to another,
- change how you are taking one or both of the medications, or
- leave everything as is.
What form(s) does this medication come in?
Cream
- Each gram of white cream contains calcipotriol 50 µg. Nonmedicinal ingredients:
- cetostearyl alcohol, chlorallylhexaminium chloride (domicile 200), disodium edetate, disodium phosphate dihydrate, glycerol 85%, liquid paraffin, macrogol cetostearyl ether, purified water, and white soft paraffin.
Ointment
- Each gram of faintly translucent white to yellowish ointment contains calcipotriol 50 µg.
- Nonmedicinal ingredients – disodium edetate, disodium phosphate dihydrate, DL-a-tocopherol, liquid paraffin, polyoxyethylene-(2)-stearyl ether, propylene glycol, purified water, and white soft paraffin.
Pregnancy Category of Calcipotriol
Pregnancy
This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.t is not known if calcipotriol passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.
Fertility
Studies in rats given calcipotriene in doses up to 54 mcg per kg of body weight (mcg/kg) per day (318 mcg per square meter of body surface area [mcg/m 2] per day) showed no impairment of fertility or of general reproductive performance.
Adequate and well-controlled studies have not been done in humans. There is evidence that calcitriol crosses the placenta; similar distribution is expected for calcipotriene.
Lactation
Maternal and fetal toxicity increased in pregnant rabbits given oral doses of 12 mcg/kg per day (132 mcg/m 2 per day). Incomplete ossification of the fetal pubic bones and forelimb phalanges occurred at doses of 36 mcg/kg per day (396 mcg/m 2 per day). Skeletal abnormalities, such as enlarged fontanelles and extra ribs, occurred in the fetuses of pregnant rats given oral doses of 54 mcg/kg per day (318 mcg/m 2 per day). The effect of skeletal enlargement is probably due to the alteration of calcium metabolism by the medication.
Pediatrics
Appropriate studies on the relationship of age to the effects of calcipotriene have not been performed in the pediatric population. Safety and efficacy have not been established. Because of a higher ratio of skin surface area to body mass, children are at greater risk than adults of systemic adverse effects when they are treated with topical medication.
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