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  • CLASSES

    Topical Antipsoriasis Products

    DEA CLASS

    Rx

    DESCRIPTION

    Topical vitamin D3 analog also named calcipotriol; used for topical symptomatic treatment of chronic plaque psoriasis; structurally similar to natural calcitriol.

    COMMON BRAND NAMES

    Calcitrene, Dovonex, Dovonex Scalp, Sorilux

    HOW SUPPLIED

    Calcipotriene/Calcitrene/Dovonex Topical Ointment: 0.005%
    Calcipotriene/Dovonex Scalp Topical Sol: 0.005%
    Calcipotriene/Dovonex Topical Cream: 0.005%
    Sorilux Topical Foam: 0.005%

    DOSAGE & INDICATIONS

    For the treatment of plaque psoriasis.
    NOTE: According to the American Academy of Dermatology (AAD), combining calcipotriene with a topical corticosteroid is more effective than either treatment alone. In addition, fewer adverse events were reported with combination therapy in most clinical studies.
    For the treatment of chronic, moderate scalp psoriasis.
    Topical dose (scalp solution)
    Adults

    Apply topically to the affected area(s) of scalp twice daily.

    Topical dosage (ointment)
    Adults

    Apply topically as a thin layer to affected area(s) once daily in the morning or twice daily in the morning and evening for up to 8 weeks. Do not exceed 100 g/week.

    Adolescents and Children >= 2 years†

    Limited data suggest twice daily application of calcipotriene for up to 8 weeks is effective and well tolerated at dosages up to 50 g/week. Clinical trials including children ages 2 to 14 years demonstrated marked improvement or clearing of psoriasis in more than 60% of patients after twice daily application for up to 8 weeks. The most commonly reported adverse effect was local skin irritation.

    Topical dosage (cream)
    Adults

    Apply topically as a thin layer to affected area(s) twice daily in the morning and evening for up to 8 weeks. Do not exceed 100 g/week.

    Topical dosage (foam)
    Adults

    Apply a thin layer twice daily to the affected areas; rub in gently and completely.

    MAXIMUM DOSAGE

    Adults

    100 g/week topically.

    Geriatric

    100 g/week topically.

    Adolescents

    Safety and efficacy have not been established.

    Children

    Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    No dosage adjustment required.

    Renal Impairment

    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    ADMINISTRATION

    Topical Administration

    Calcipotriene is for external use only. Do not apply to the face or eyes.
    Wash hands after use.

    Cream/Ointment/Lotion Formulations

    Cream or Ointment: Apply a thin film to the affected area and rub into the skin gently and completely.

    Other Topical Formulations

    Scalp Solution: Comb hair to remove scaly debris, and after suitably parting apply scalp solution. Rub in gently and completely, taking care to prevent the solution spreading onto the forehead. Avoid application of solution to eyes or unaffected scalp margins.
    Topical Foam: Shake well; dispense a small amount of foam into palm of the hand and gently rub into the affected area until foam disappears. If not treating the hands, wash after use. Avoid contact with eyes, mouth, and vagina. The propellant in the topical foam is flammable. Instruct the patient to avoid fire, flame, and/or smoking during and immediately following application.

    STORAGE

    Calcitrene :
    - Do not freeze
    - Store between 59 to 77 degrees F
    Dovonex:
    - Do not freeze
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F
    Dovonex Scalp:
    - Do not freeze
    - Flammable, keep away from heat and flame
    - Protect from direct sunlight
    - Store at controlled room temperature (between 68 and 77 degrees F)
    Sorilux:
    - Avoid exposure to heat
    - Do not freeze
    - Do not refrigerate
    - Do Not Store at Temperatures Above 120 degrees F (49 degrees C)
    - Flammable, keep away from heat and flame
    - Protect from direct sunlight
    - Store at 77 degrees F; excursions permitted to 59-86 degrees F
    - Store upright

    CONTRAINDICATIONS / PRECAUTIONS

    General Information

    Calcipotriene should not be used in patients with a history of hypersensitivity reactions to the drug or any components used in the preparation of the commercial product.

    Hypercalcemia, hypercalciuria, hypervitaminosis D, nephrolithiasis, occlusive dressing

    Calcipotriene is contraindicated when hypercalcemia or hypervitaminosis D are evident. Although systemic absorption of this agent is minimal, hypercalcemia, hypervitaminosis D, and/or hypercalciuria may occur. Hypercalcemia and/or hypercalciuria may increase renal calculi formation in patients with a history of nephrolithiasis. Topical application of more than 100 g/week should be avoided since hypercalcemia is more likely when this dose is exceeded. Do not cover with an occlusive dressing as this may enhance absorption of calcipotriene. Monitoring serum and urine calcium does not appear necessary during treatment at recommended dosages.

    Accidental exposure, ocular exposure

    Calcipotriene should not be applied to the face; avoid ocular exposure. Accidental exposure to unaffected areas of skin or scalp margins may lead to skin irritation and should be avoided. Calcipotriene should be discontinued if irritation develops. In some instances skin irritation has resolved with continued use.

    Children, infants, neonates

    Safety and efficacy of calcipotriene have not been established in neonates, infants, children, or adolescents. Age-related differences in treating psoriasis may result in increased sensitivity to calcipotriene. Children are at a greater risk of developing systemic adverse effects to topical medications because of a higher ratio of skin surface area to body mass.

    Sunlight (UV) exposure

    Excessive exposure to natural or artificial sunlight (UV) exposure with topical application of calcipotriene may increase the risk of skin tumor formation and should be avoided. It may also be prudent to limit or avoid the use of phototherapy or other photosensitizing agents.

    Pregnancy

    Calcipotriene is classified as FDA pregnancy risk category C. Adequate studies in pregnant women have not been conducted. According to the manufacturer, calcipotriene should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

    Breast-feeding

    According to the manufacturer, it is not known whether calcipotriene is excreted into human milk. After topical administration, only small amounts of the drug are absorbed into systemic circulation. Calcipotriene is a synthetic derivative of calcitriol, an active form of vitamin D. The American Academy of Pediatrics (AAP) considers vitamin D usually compatible with breast-feeding. Therefore, it is unlikely that topical administration of calcipotriene would pose significant risk to a nursing infant. Ensure that the infant does not come in contact in the areas where calcipotriene has been applied. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    ADVERSE REACTIONS

    Severe

    exfoliative dermatitis / Delayed / 1.0-10.0
    skin atrophy / Delayed / 0-1.0

    Moderate

    erythema / Early / 1.0-10.0
    contact dermatitis / Delayed / Incidence not known
    hypertension / Early / Incidence not known
    hypercalcemia / Delayed / Incidence not known
    constipation / Delayed / Incidence not known
    depression / Delayed / Incidence not known
    hypercalciuria / Delayed / Incidence not known

    Mild

    skin irritation / Early / 10.0-15.0
    rash (unspecified) / Early / 0-11.0
    pruritus / Rapid / 1.0-10.0
    xerosis / Delayed / 1.0-10.0
    folliculitis / Delayed / 0-1.0
    skin hyperpigmentation / Delayed / 0-1.0
    anorexia / Delayed / Incidence not known
    polydipsia / Early / Incidence not known
    weight loss / Delayed / Incidence not known
    weakness / Early / Incidence not known
    abdominal pain / Early / Incidence not known
    nausea / Early / Incidence not known
    vomiting / Early / Incidence not known
    fatigue / Early / Incidence not known

    DRUG INTERACTIONS

    Calcium Carbonate: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Calcium Carbonate; Magnesium Hydroxide: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Calcium Carbonate; Risedronate: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Calcium Salts: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Calcium: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Calcium; Vitamin D: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Chromium: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Collagenase: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Cyanocobalamin, Vitamin B12: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Hetastarch; Dextrose; Electrolytes: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Pantothenic Acid, Vitamin B5: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Polycarbophil: (Moderate) Use calcipotriene cautiously with other agents that can produce hypercalcemia, including calcium polycarbophil. Each 625 mg of calcium polycarbophil contains a substantial amount of calcium (approximately 125 mg). There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use.
    Pyridoxine, Vitamin B6: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).
    Zinc Salts: (Minor) There is evidence that calcipotriene can be absorbed in amounts that are sufficient to produce systemic effects, including elevated serum calcium; hypercalcemia has been observed in normal prescription use. Use calcipotriene cautiously with other agents that can produce hypercalcemia (e.g., calcium salts or supplements including calcium carbonate).

    PREGNANCY AND LACTATION

    Pregnancy

    Calcipotriene is classified as FDA pregnancy risk category C. Adequate studies in pregnant women have not been conducted. According to the manufacturer, calcipotriene should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

    According to the manufacturer, it is not known whether calcipotriene is excreted into human milk. After topical administration, only small amounts of the drug are absorbed into systemic circulation. Calcipotriene is a synthetic derivative of calcitriol, an active form of vitamin D. The American Academy of Pediatrics (AAP) considers vitamin D usually compatible with breast-feeding. Therefore, it is unlikely that topical administration of calcipotriene would pose significant risk to a nursing infant. Ensure that the infant does not come in contact in the areas where calcipotriene has been applied. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    MECHANISM OF ACTION

    The mechanism of action of calcipotriene, a synthetic analog of vitamin D3, is similar to naturally occurring 1,25-(OH)2-D3 (calcitriol). Calcitriol (i.e., active vitamin D3) is the metabolite of cholecalciferol (i.e., inactive vitamin D3). Calcipotriene binds to vitamin D receptors on epidermal cells and tissue cells. Activation of this ligand-receptor complex results in inhibition of cell proliferation and induction of cell differentiation in psoriatic skin. In addition, calcipotriene binds to vitamin D receptors on lymphocytes. Calcipotriene is also similar to calcitriol in its ability to suppress thymocyte proliferation, T-helper function, and lymphocyte proliferation. The exact role of these immunologic mechanisms in the reduction of psoriatic lesions is unknown.
     
    The binding affinity of calcipotriene to intestinal calcitriol receptors is similar to that of calcitriol, however animal studies demonstrated that calcipotriene is 100—200 times less potent than calcitriol on calcium metabolism when given systemically. It has been suggested that rapid liver metabolism or extensive metabolism of calcipotriene in epidermal keratinocytes is responsible for this difference.
     
    During short-term therapy of stable plaque psoriasis, calcium and bone metabolism in humans appear to be unaffected when calcipotriene is used at the recommended dosage (<100 grams/week). Calcipotriene administered for 4 weeks at the maximum weekly dosage (100 grams/week) resulted in significant increases in urine calcium.

    PHARMACOKINETICS

    Calcipotriene is administered topically. Although the distribution of absorbed calcipotriene and its metabolites have not been described, it is presumed to be similar to other vitamin D derivatives. It is unknown if calcipotriene and its metabolites cross the placenta or are distributed into breast milk. Absorbed calcipotriene is rapidly and extensively converted in the liver to a 24-ketone and a 22,23-hydrogenated derivative. In vitro data have shown that the parent compound is also metabolized by human keratinocytes. All metabolites identified thus far have negligible activity compared with the parent compound. Calcipotriene is minimally excreted in the urine and feces (< 1%).

    Topical Route

    Approximately 6% of a topical dose of calcipotriene is systemically absorbed when applied to psoriatic skin. Clinical improvement of psoriatic lesions occurs within 2 weeks, with maximal benefits observed in 4 to 8 weeks. The drug demonstrates a dose-dependent effect on erythema, thickness, and scaling of lesions.