Usage
- Calcipotriol is prescribed for the topical treatment of mild to moderately severe plaque psoriasis (psoriasis vulgaris), which can manifest on the body or scalp. It can also be used for other skin conditions as determined by a physician.
- Pharmacological classification: Vitamin D analogue, antipsoriatic.
- Mechanism of action: Calcipotriol is a synthetic analog of vitamin D3. It binds to and activates the vitamin D receptor, which modulates keratinocyte proliferation and differentiation, thereby reducing the excessive skin cell growth seen in psoriasis.
Alternate Names
- Calcipotriene (International Nonproprietary Name)
- Brand names: Dovonex, Sorilux, Calcitrene.
How It Works
- Pharmacodynamics: Calcipotriol inhibits keratinocyte proliferation and promotes their differentiation, normalizing the epidermal cell cycle and reducing psoriatic plaques. It also has anti-inflammatory effects. It may also temporarily increase calcium levels in the blood (hypercalcemia).
- Pharmacokinetics: Topical application leads to minimal systemic absorption. When absorbed systemically, it is metabolized in the liver and excreted via renal and fecal routes.
- Mode of action: Binds to the vitamin D receptor (VDR), a nuclear transcription factor that regulates gene expression related to cell growth, differentiation, and immune function.
- Receptor binding: Vitamin D receptor.
- Elimination pathways: Primarily hepatic metabolism, followed by renal and fecal excretion.
Dosage
Standard Dosage
Adults:
- Ointment: Apply a thin layer to affected areas once or twice daily. Start with twice daily application (morning and evening). Maintenance: once daily. Maximum weekly dose: 100g.
- Scalp solution: Apply to affected areas twice daily. Maximum weekly dose: 60ml.
- Cream/Foam: Apply to affected area(s) twice daily.
- Gel: Once daily.
- If using multiple formulations (e.g., ointment and scalp solution), the total weekly dose of calcipotriol should not exceed 5mg. (e.g., 60ml scalp solution + 40g ointment, or 40ml solution + 60g ointment).
Children:
- Ointment:
- 6-11 years: 50g maximum weekly dose.
- 12-17 years: 75g maximum weekly dose.
- Use in children under 6 years old: Limited experience; consult specialist for guidance. Other formulations are not recommended for children under 18.
- Pediatric safety considerations: Monitor for hypercalcemia and local skin reactions.
Special Cases:
- Elderly Patients: No specific dosage adjustment is typically needed.
- Patients with Renal Impairment: Contraindicated in severe renal impairment. Caution advised in moderate impairment; monitor calcium levels.
- Patients with Hepatic Dysfunction: Contraindicated in severe hepatic impairment. Caution advised in moderate impairment; monitor calcium levels.
- Patients with Comorbid Conditions: Monitor calcium levels and watch for drug interactions.
Clinical Use Cases
Calcipotriol is not systemically administered and hence not typically used in scenarios like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its usage is limited to topical application for the management of plaque psoriasis.
Dosage Adjustments
Adjustments based on renal/hepatic function are necessary (see “Special Cases” above). Monitor calcium levels closely.
Side Effects
Common Side Effects
- Skin irritation (burning, stinging, itching, redness, dryness, peeling) at the application site.
- Worsening of psoriasis.
Rare but Serious Side Effects
- Hypercalcemia (high blood calcium), indicated by symptoms like nausea, vomiting, constipation, increased thirst, frequent urination, muscle weakness, confusion.
- Allergic contact dermatitis.
Long-Term Effects
- Potential for skin atrophy with prolonged use, especially when used in combination with corticosteroids.
Adverse Drug Reactions (ADR)
- Severe allergic reactions (rare).
- Erythrodermic psoriasis (exacerbation).
Contraindications
- Hypersensitivity to calcipotriol.
- Hypercalcemia or vitamin D toxicity.
- Severe renal or hepatic impairment.
- Disorders of calcium metabolism.
- Acute psoriatic eruption (scalp solution).
Drug Interactions
- Concomitant use of other vitamin D analogues or calcium supplements increases the risk of hypercalcemia.
- Some medications (e.g., thiazide diuretics) can also increase calcium levels.
- CYP450 interactions: No significant interactions are known.
- Photosensitizing medications may increase the risk of sunburn.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: C (US FDA). Data regarding safety is limited; use only if potential benefit outweighs risk.
- Breastfeeding: It is unknown if calcipotriol is excreted in breast milk. Exercise caution; wash hands thoroughly and avoid applying to the chest area to prevent neonatal exposure.
Drug Profile Summary
- Mechanism of Action: Vitamin D analogue; inhibits keratinocyte proliferation and promotes differentiation.
- Side Effects: Local skin irritation, hypercalcemia (rare).
- Contraindications: Hypersensitivity, hypercalcemia, severe renal/hepatic impairment.
- Drug Interactions: Vitamin D analogues, calcium supplements, photosensitizing medications.
- Pregnancy & Breastfeeding: Caution advised; potential risk to fetus/neonate.
- Dosage: Topical, once or twice daily; maximum doses as described above.
- Monitoring Parameters: Serum calcium levels (especially with higher doses or prolonged use).
Popular Combinations
- Calcipotriol is often combined with betamethasone dipropionate (a corticosteroid) in a single formulation for enhanced efficacy. This combination reduces inflammation and improves plaque clearance.
Precautions
- General Precautions: Avoid contact with face and eyes. Wash hands thoroughly after application. Monitor calcium levels.
- Specific Populations: As described above.
- Lifestyle Considerations: Protect treated skin from excessive sunlight.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Calcipotriol?
A: See the detailed Dosage section above.
Q2: Can Calcipotriol be used on the face?
A: Use with extreme caution on the face as it can cause irritation. Avoid contact with eyes.
Q3: How long does it take for Calcipotriol to work?
A: Improvement is usually seen within a few weeks, but it can take up to 8 weeks for optimal results.
Q4: What should I do if I miss a dose?
A: Apply the missed dose as soon as you remember. If it’s almost time for your next dose, skip the missed dose and continue with your regular schedule.
Q5: Can I use Calcipotriol with other psoriasis treatments?
A: Yes, but it’s crucial to consult with a physician. Combining with other topical treatments, phototherapy, or systemic medications may require dosage adjustments or monitoring.
Q6: What are the signs of hypercalcemia?
A: Nausea, vomiting, constipation, increased thirst/urination, muscle weakness, confusion, and fatigue. Contact a doctor immediately if these symptoms occur.
Q7: Is Calcipotriol safe during pregnancy?
A: Data are limited. Use only if potential benefit justifies the potential risk to the fetus. Discuss with a doctor to evaluate individual circumstances.
Q8: Can I use Calcipotriol while breastfeeding?
A: Exercise caution. It is unknown if calcipotriol passes into breast milk. Avoid applying to the chest area, and wash hands thoroughly to minimize infant exposure.
Q9: What are the long-term effects of Calcipotriol use?
A: Potential for skin atrophy with prolonged use, particularly when combined with a corticosteroid. Regular monitoring is recommended.