Calcipotriol Monohydrate

Approved Indications:

• Plaque Psoriasis (Psoriasis Vulgaris):
  – Adults: Topical treatment of mild to moderate chronic plaque psoriasis of the scalp and body.
  – Children ≥6 years: For psoriasis vulgaris on the body.
  – Children ≥12 years: For scalp psoriasis.

Off-label/Clinically Accepted Uses:

• Psoriatic Nail Disease (limited evidence, topical use under specialist supervision).
• Vitiligo (adjunct therapy, particularly in combination with corticosteroids or UVB).
• Seborrheic Dermatitis (occasionally used as adjunct therapy).

Adults:

• Topical Ointment/Cream/Foam:
• Apply thinly to affected areas twice daily (morning and evening).
• Maximum weekly dose: Should not exceed 100 g of Calcipotriol Monohydrate.

Scalp Application (Scalp Solution):

• Apply twice daily, massaging gently into the scalp.
• Maximum safe dose is 60 mL/week.

Pediatric Use:

• 6–12 years: Up to 50 g/week on the body.
• 12–18 years: Up to 75 g/week on the body; up to 60 mL/week on the scalp.
• Safety in children under 6 years is not established.

Elderly:

• No specific dose adjustments required. Monitor for calcium disturbances.

Renal/Hepatic Impairment:

• No formal studies; use with caution, monitor serum calcium in severe impairment.

Administration Notes:

• Avoid contact with face, eyes, and mucous membranes.
• Do not apply to more than 30% of body surface area.
• Avoid occlusive dressings unless prescribed.

Calcipotriol Monohydrate is a synthetic derivative of vitamin D3. It binds to vitamin D receptors (VDRs) on keratinocytes, modulating gene transcription to inhibit keratinocyte proliferation and enhance differentiation, which are abnormally regulated in psoriasis. Additionally, it exhibits immunomodulatory effects by reducing pro-inflammatory cytokine release from T-cells and dendritic cells, thereby reducing psoriatic inflammation.

• Absorption: Minimal systemic absorption (<1%) with normal usage; increased if applied over large areas or under occlusion.
• Distribution: High affinity for VDRs in the skin; systemic distribution is negligible.
• Metabolism: Rapid hepatic metabolism to inactive metabolites via the liver.
• Excretion: Primarily excreted via bile; minor urinary excretion.
• Half-life: Approximately 2–4 hours (systemically).
• Onset of Action: Improvement seen in 1–2 weeks, maximal response in 4–8 weeks.

• Pregnancy:
  – FDA Category C.
  – Animal studies have shown fetal abnormalities at high doses; no well-controlled studies in humans. Use only if potential benefit justifies the potential risk to the fetus.
• Lactation:
  – Unknown whether Calcipotriol is excreted in human breast milk.
  – Avoid application to chest area to prevent infant ingestion. Use with caution during breastfeeding.

• Primary Class: Topical Vitamin D Analog
• Subclass: Synthetic Vitamin D3 Derivative (Non-steroidal antipsoriatic agent)

• Hypersensitivity to Calcipotriol or any excipients
• Hypercalcemia or evidence of calcium metabolism disorders
• Severe hepatic or renal impairment (relative contraindication)
• Erythrodermic, exfoliative, or pustular psoriasis
• Use on face, genital areas, or skin folds (unless prescribed)

• Hypercalcemia Risk: Excessive application may cause elevated serum calcium levels; monitor in high-dose or long-term use.
• UV Exposure: Avoid excessive sunlight or UV therapy; Calcipotriol may increase photosensitivity.
• Face & Sensitive Areas: Avoid use on face, mucous membranes, or flexural areas due to high absorption and irritation risk.
• Pediatric Use: Limit use to indicated age groups; monitor calcium if prolonged use.
• Elderly Patients: Monitor for calcium disturbances and local skin irritation.

Common Side Effects (≥1%):

• Dermatologic: Local skin irritation, erythema, itching, dryness, burning sensation
• Scalp Use: Irritation or folliculitis

Less Common / Rare:

• Hypercalcemia or hypercalciuria (usually reversible on dose reduction)
• Contact dermatitis
• Photosensitivity
• Exacerbation of psoriasis (rebound)

Serious Reactions:

• Generalized pustular psoriasis (rare)
• Facial dermatitis due to misapplication

• Vitamin D Supplements or Calcium Supplements: Risk of additive hypercalcemia
• Topical Steroids: Can be safely co-administered; often used in combination therapies
• Phototherapy (UVB/PUVA): May enhance effect but increase risk of irritation; caution advised
• CYP450 Enzyme Effects: No significant systemic interactions due to minimal absorption

• NICE and AAD guidelines continue to recommend Calcipotriol as first-line topical therapy for mild to moderate plaque psoriasis.
• Combination formulations with betamethasone dipropionate are increasingly favored for enhanced efficacy and better tolerability.
• Emphasis on limiting total weekly dosage and use under medical supervision in pediatric populations.

• Store at below 25°C (77°F); do not freeze.
• Protect from light and moisture.
• Do not refrigerate unless otherwise specified by manufacturer.
• Keep container tightly closed after use.
• Foam formulations: Pressurized containers – protect from heat and puncture.