calcitriol topical

Action and Spectrum

Actions and spectrum: 

calcitriol topical is a form of Vitamin D3 that acts as an active form of the Vitamin D in the skin. It acts by binding to the specific receptors in the skin cells, promoting their normal growth and development.

calcitriol topical is used for the treatment of plaque psoriasis and mild to moderate chronic plaque psoriasis. Its spectrum of action is primarily focused on the skin, where it helps regulate cell growth and differentiation. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Psoriasis (4%) 

Skin discomfort (3%) 

Urine abnormality (4%) 

Hypercalciuria (3%) 

Pruritus (1%)  

>10% 

Hypercalcemia (24%)  

Post marketing Reports 

Erythema 

Acute blistering dermatitis 

Skin burning sensation 

Black Box Warning

Black Box Warning:  

There is no black box warning specifically associated with the use of calcitriol topical. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals who have a known hypersensitivity or allergy to calcitriol or any other components of the topical formulation should not use calcitriol topical. 
• Hypercalcemia: calcitriol topical should not be used in individuals with elevated levels of calcium in the blood, known as hypercalcemia. 
• Vitamin D toxicity: calcitriol topical is contraindicated in individuals with Vitamin D toxicity or excessive Vitamin D levels. 
• Skin infections: If there is an active skin infection at the application site, the use of calcitriol topical should be avoided until the infection is resolved. 
• Open wounds or ulcers: calcitriol topical should not be applied to damaged skin, open wounds, or skin with ulcers. 

Caution: 

• Hypercalcemia: calcitriol topical can increase calcium levels in the body, so caution is needed in individuals with conditions that may predispose them to hypercalcemia, such as primary hyperparathyroidism. 
• Renal impairment: Individuals with impaired kidney function may be at a higher risk of developing hypercalcemia when using calcitriol topical. Close monitoring of calcium levels is necessary in such cases. 
• Skin irritation: calcitriol topical may cause skin irritation or sensitization. If excessive irritation or allergic reactions occur, the use of the medication should be discontinued. 
• Use on the face: Caution should be exercised when applying calcitriol topical to the face, as the skin is more sensitive and prone to adverse reactions. 
• Avoid contact with eyes and mucous membranes: calcitriol topical should not come into contact with the eyes or mucous membranes. If accidental contact occurs, it should be rinsed thoroughly with water. 
• Pediatric use: The safety and efficacy of calcitriol topical in pediatric patients have not been established, so caution should be used when using this medication in children. 
• Pregnancy and lactation: The use of calcitriol topical during pregnancy or lactation should be discussed with a healthcare professional, as its safety in these situations has not been well studied. 

Comorbidities: 

• Kidney disease: calcitriol is the active form of Vitamin D and is metabolized in the kidneys. Individuals with impaired kidney function may have difficulty metabolizing calcitriol properly, leading to potential accumulation and increased risk of adverse effects. 
• Hypercalcemia: calcitriol topical can increase calcium levels in the body. Individuals with conditions such as primary hyperparathyroidism or other causes of hypercalcemia may require careful monitoring when using calcitriol topical. 
• History of kidney stones: Elevated calcium levels in the urine can increase the risk of developing kidney stones. patients with kidney stones may require caution and close monitoring when using calcitriol topical. 
• Calcium metabolism disorders: Conditions that affect calcium metabolism, such as hypercalcemia, hypocalcemia, or Vitamin D-related disorders, may require special consideration and monitoring when using calcitriol topical. 
• Hyperphosphatemia: calcitriol can affect phosphate levels in the body. Individuals with high levels of phosphate in their blood (hyperphosphatemia) may require close monitoring and management of phosphate levels when using calcitriol topical. 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: It is unknown whether drug gets excreted into human milk.  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

• Regulation of calcium and phosphorus metabolism: calcitriol binds to the VDR in the intestines, enhancing the absorption of calcium and phosphorus. This promotes normal calcium and phosphorus levels in the blood. 
• Modulation of cell growth and differentiation: calcitriol regulates the differentiation and growth of various cell types, including skin cells. It helps to normalize the production and differentiation of keratinocytes, the main cells in the epidermis. 
• Immune modulation: calcitriol has immune-modulating effects, including the suppression of pro-inflammatory cytokines and the promotion of anti-inflammatory responses. 

Pharmacodynamics: 

• Anti-inflammatory effects: calcitriol has anti-inflammatory properties and can inhibit the production of pro-inflammatory cytokines. It can reduce the inflammation associated with certain skin conditions, such as psoriasis. 
• Immunomodulatory effects: calcitriol can modulate the immune response by affecting immune cells, such as T lymphocytes. It helps to regulate immune function and reduce excessive immune activity seen in certain skin diseases. 
• Antiproliferative effects: calcitriol can inhibit the excessive proliferation of keratinocytes, which is a hallmark of conditions like psoriasis. By reducing the rate of cell division, calcitriol helps to normalize the turnover of skin cells.

Pharmacokinetics: 

Absorption 

calcitriol is readily absorbed through the skin when applied topically. The absorption rate may vary based on the formulation, skin integrity, and the presence of other factors that may enhance or hinder absorption. 

Distribution 

After absorption, calcitriol may undergo systemic distribution, reaching various tissues and target cells in the body. However, the distribution is primarily limited to the local skin area due to its topical application. 

Metabolism 

calcitriol undergoes metabolism in the liver and other tissues. The main metabolic pathway involves hydroxylation and oxidation, resulting in the formation of various metabolites. These metabolites are further metabolized to inactive compounds, such as calcitroic acid. 

Elimination and excretion 

The metabolites of calcitriol, along with any unmetabolized drug, are excreted primarily in the urine. The elimination half-life of calcitriol is short, with a duration of a few hours. 

Adminstartion

Administration: 

calcitriol topical is typically administered as a cream, ointment, or solution for external use. The specific administration instructions may vary depending on the formulation and the condition being treated. Here are some general guidelines for the administration of calcitriol topical: 

• Clean and dry affected area: Before applying calcitriol topical, ensure that the affected skin area is clean and dry. Gently clean the area with the soap and water. 
• Apply a thin layer: Take a small amount of the calcitriol topical formulation as directed by your healthcare provider. Spread a thin layer of medication over the affected skin area. Massage it gently until it is absorbed. 
• Avoid contact with eyes, mouth, and mucous membranes: Take care to avoid getting the medication into your eyes, mouth, or any mucous membranes. 
• Wash hands after application: After applying calcitriol topical, wash hands thoroughly with soap & water to remove any residue. This helps prevent unintentional contact with other areas of the body or transfer of the medication to others. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: calcitriol topical 

Pronounced: (cal-SI-tri-ol top-i-kal)  

Why do we use calcitriol topical? 

• Psoriasis: calcitriol topical is effective in treating plaque psoriasis. It helps to reduce the overgrowth of skin cells and inflammation associated with psoriasis. 
• Mild to moderate plaque psoriasis on the scalp: calcitriol topical can be used specifically for treating psoriasis on the scalp, helping to alleviate scaling, redness, and itching in this area. 
• Mild to moderate plaque psoriasis: calcitriol topical is also used for psoriasis affecting other areas of body, such as elbows, knees, and trunk. 
• Vitiligo: calcitriol topical may be prescribed for the treatment of vitiligo. It can help to repigment the affected areas and even out the skin tone.