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Taclonex
Classes
Other Corticosteroid Combinations
Topical Antipsoriasis Agents
Administration
For external use only; do not apply to face, axillae, or groin. Avoid contact with eyes.
Instruct patients to wash their hands before and after use.
Avoid concurrent treatment with other topical medications at the site of application; calcipotriene can become chemically unstable and inactive when combined with other topical preparations.
Do not use with occlusive dressings. Instruct patients not to bandage, cover, or wrap the treated area.
If applied to exposed portions of the body, avoid excessive exposure to natural or artificial sunlight.
Topical ointment: Apply a thin film to the affected area(s) and rub it into the skin gently and completely.
Topical cream: Apply to the affected area(s) and rub gently to ensure the plaques are saturated. Do not apply if skin atrophy is present at the treatment site.
Topical suspension
For body application
Shake well before use.
Apply directly to the affected areas of the body. Rub in gently with fingertips.
Do not take a bath or shower immediately after use.
For scalp application
Shake well before use.
It is not necessary to wash hair prior to application.
Apply directly to the affected areas of the scalp. Rub in gently with fingertips.
Do not wash hair immediately after use.
Do not apply to the scalp in the 12 hours before or after any chemical treatments to the hair.
Topical foam
Shake well before use.
Apply a thin film to the affected area and rub it into the skin gently and completely.
The propellant is flammable. Avoid fire, flame, and smoking during and immediately following application.
Adverse Reactions
skin atrophy / Delayed / 0.1-1.9
hypervitaminosis D / Delayed / Incidence not known
ocular hypertension / Delayed / Incidence not known
visual impairment / Early / Incidence not known
erythema / Early / 0.4-2.1
contact dermatitis / Delayed / Incidence not known
hyperglycemia / Delayed / Incidence not known
hypercalcemia / Delayed / Incidence not known
hypercalciuria / Delayed / Incidence not known
glycosuria / Early / Incidence not known
Cushing's syndrome / Delayed / Incidence not known
physiological dependence / Delayed / Incidence not known
hypothalamic-pituitary-adrenal (HPA) suppression / Delayed / Incidence not known
adrenocortical insufficiency / Delayed / Incidence not known
impaired wound healing / Delayed / Incidence not known
skin ulcer / Delayed / Incidence not known
cataracts / Delayed / Incidence not known
pruritus / Rapid / 2.8-7.2
infection / Delayed / 0.8-7.0
pharyngitis / Delayed / 2.3-2.3
headache / Early / 2.0-2.0
skin hypopigmentation / Delayed / 0.1-1.4
folliculitis / Delayed / 0.1-1.4
skin irritation / Early / 0.4-1.4
paresthesias / Delayed / 0.2-1.4
rash / Early / 0.1-1.2
ecchymosis / Delayed / 1.0-1.0
skin hyperpigmentation / Delayed / 0.1-0.1
telangiectasia / Delayed / 0.1-0.1
striae / Delayed / Incidence not known
xerosis / Delayed / Incidence not known
miliaria / Delayed / Incidence not known
Common Brand Names
Enstilar, Taclonex, Taclonex Scalp, Wynzora
Dea Class
Rx
Description
Topical combination product containing a synthetic corticosteroid and vitamin D3 analog
Available as an ointment, foam, cream, and suspension
Ointment and foam approved for use up to 4 weeks; cream and suspension can be applied for up to 8 weeks
Dosage And Indications
Apply topically to the affected skin area(s) once daily for up to 8 weeks. Treatment may be discontinued earlier if control is achieved. Guidelines recommend use of combination treatments with vitamin D analogues and potent class 2 and 3 topical corticosteroids up to 52 weeks.
Apply a thin layer to the affected skin area(s) topically once daily for up to 4 weeks. Treatment may be discontinued earlier if control is achieved. Guidelines recommend use of combination treatments with vitamin D analogues and potent class 2 and 3 topical corticosteroids up to 52 weeks.
Apply a thin layer to the affected skin area(s) topically once daily for up to 4 weeks. Treatment may be discontinued earlier if control is achieved.[60239]
Apply a thin layer topically to the affected skin area(s) once daily for up to 4 weeks. Treatment may be discontinued earlier if control is achieved. Guidelines recommend use of combination treatments with vitamin D analogues and potent class 2 and 3 topical corticosteroids up to 52 weeks. The addition of calcipotriene/ betamethasone dipropionate ointment to low-dose cyclosporine can be used for the treatment of moderate to severe psoriasis.
Apply a thin layer topically to the affected skin area(s) once daily for up to 4 weeks. Treatment may be discontinued earlier if control is achieved.
Apply a thin layer topically to the affected skin area(s) once daily for up to 8 weeks. Treatment may be discontinued earlier if control is achieved. Guidelines recommend use of combination treatments with vitamin D analogues and potent class 2 and 3 topical corticosteroids up to 52 weeks.
Apply a thin layer topically to the affected skin area(s) once daily for up to 8 weeks. Treatment may be discontinued earlier if control is achieved.[43708]
Apply a thin layer topically to the psoriatic scalp area(s) once daily for up to 8 weeks. Treatment may be discontinued earlier if control is achieved. Guidelines recommend use of combination treatments with vitamin D analogues and potent class 2 and 3 topical corticosteroids up to 52 weeks.
Apply a thin layer topically to the psoriatic scalp area(s) once daily for up to 8 weeks. Treatment may be discontinued earlier if control is achieved.
Dosing Considerations
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
Drug Interactions
Calcium Acetate: (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: (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; Famotidine; 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; 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; Magnesium Hydroxide; Simethicone: (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; Simethicone: (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 Chloride: (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 Gluconate: (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).
Folic Acid, Vitamin B9: (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.
Porfimer: (Major) Avoid the concomitant use of porfimer with calcipotriene. Calcipotriene may enhance the ability of ultraviolet radiation to induce skin tumors. Coadministration of photosensitizing agents such as porfimer may increase this risk.
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).
Verteporfin: (Major) Use caution if coadministration of verteporfin with calcipotriene is necessary due to the risk of increased photosensitivity. Verteporfin is a light-activated drug used in photodynamic therapy; all patients treated with verteporfin will be photosensitive. Concomitant use of other photosensitizing agents like calcipotriene may increase the risk of a photosensitivity reaction.
How Supplied
Calcipotriene, Betamethasone/Calcipotriene, Betamethasone Dipropionate Topical Cream: 0.005-0.064%
Calcipotriene, Betamethasone/Calcipotriene, Betamethasone Dipropionate/Taclonex Topical Ointment: 0.005-0.064%
Calcipotriene, Betamethasone/Calcipotriene, Betamethasone Dipropionate/Taclonex/Taclonex Scalp Topical Susp: 0.005-0.064%
Enstilar Topical Foam: 0.005-0.064%
Maximum Dosage
100 g cream/ointment/suspension per week topically, or 60 g foam every 4 days topically; treatment of more than 30% body surface area is not recommended.
100 g cream/ointment/suspension per week topically, or 60 g foam every 4 days topically; treatment of more than 30% body surface area is not recommended.
60 g ointment/suspension per week topically, or 60 g foam every 4 days topically; treatment of more than 30% body surface area is not recommended; safety and efficacy of the cream have not been established.
12 years and older: 60 g ointment/suspension per week topically, or 60 g foam every 4 days topically; treatment of more than 30% body surface area is not recommended; safety and efficacy of the cream have not been established.
1 to 11 years: Safety and efficacy have not been established.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
Mechanism Of Action
Calcipotriene and betamethasone work in different ways to alleviate the signs and symptoms of psoriasis vulgaris (i.e., erythema, scaliness, and plaque elevation), although the mechanism for each is not completely understood. Calcipotriene and betamethasone each have major effects on markers of epidermal proliferation and keratinization. In the epidermis, keratin-10 is a marker of cell differentiation; calcipotriene has some effects on keratin-10 and betamethasone targets keratin-10 to normalize differentiation. Proliferating keratinocytes have Ki-67 positive nuclei, on which calcipotriene has significant effects. Betamethasone also reduces T-cell receptors, which decreases the production of cytokines. Overall, these actions exhibit a broad range of effects on inflammatory cells that cannot be achieved with the use of individual products.[31990] After the topical application of betamethasone; calcipotriene, clinical improvement of psoriatic lesions occurs within 1 to 2 weeks, with maximal benefits observed in 4 to 8 weeks.
Calcipotriene: The mechanism of action of calcipotriene, a synthetic analog of vitamin D3, is similar to that of naturally occurring calcitriol (i.e., active vitamin D3). Calcipotriene binds to vitamin D receptors on keratinocytes of both normal and psoriatic epidermal and tissue cells. Activation of this ligand-receptor complex results in inhibition of cell proliferation and induction of cell differentiation in psoriatic skin. These actions essentially reverse the abnormal cell changes occurring in psoriasis. 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. Nevertheless, the drug demonstrates a dose-dependent effect on erythema, thickness, and scaling of psoriatic lesions.[23819]
The binding affinity of calcipotriene to intestinal calcitriol receptors is similar to that of calcitriol (whose main function is to increase calcium absorption from the gut and promote normal bone formation and mineralization). However, animal studies demonstrated that calcipotriene is 100 to 200 times less potent than calcitriol on calcium metabolism when given systemically.[23816] It has been suggested that rapid liver metabolism or extensive metabolism of calcipotriene in epidermal keratinocytes is responsible for this difference.[23817] 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 (less than 100 grams per week). Calcipotriene administered for 4 weeks at the maximum weekly dosage (100 grams per week) resulted in significant increases in urine calcium.[23818] Additionally, systemic exposure of topical calcipotriene has been shown to induce alterations in intestinal calcium absorption leading to fluctuations in serum calcium, phosphate, and calcitriol levels.[31992]
Betamethasone: Corticosteroids exhibit anti-inflammatory, antipruritic, and vasoconstrictive properties. At the cellular level, corticosteroids induce peptides called lipocortins. Lipocortins antagonize phospholipase A2, an enzyme that causes the breakdown of leukocyte lysosomal membranes to release arachidonic acid. This action decreases the subsequent formation and release of endogenous inflammatory mediators including prostaglandins, kinins, histamines, liposomal enzymes, and the complement system. Early anti-inflammatory effects of topical corticosteroids include the inhibition of macrophage and leukocyte movement and activity in the inflamed area by reversing vascular dilation and permeability. Later inflammatory processes such as capillary production, collagen deposition, and keloid (scar) formation are also inhibited by corticosteroids. Clinically, these actions correspond to decreased edema, erythema, pruritus, plaque formation, and scaling in affected skin (i.e., psoriasis plaques).
Pharmacokinetics
Calcipotriene; betamethasone is applied topically to the skin. It is unknown if calcipotriene; betamethasone and its metabolites cross the placenta or are distributed into breast milk.
Calcipotriene: The distribution of absorbed calcipotriene and its metabolites have not been described, it is presumed to be similar to other vitamin D derivatives. 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.
Betamethasone: Betamethasone binds weakly to plasma proteins, and only the unbound portion of a circulating dose is active. Once absorbed, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. In addition, some corticosteroids and their metabolites are also excreted in the bile. The biological half-life of betamethasone is 35 to 54 hours.
The amount of calcipotriene; betamethasone absorbed following topical application is dependent on several factors including the integrity of the epidermal barrier (i.e., the presence of skin damage or inflammation), presence or absence of occlusive dressings, and the site of application (i.e., increased where the stratum corneum is thin such as the eyelids, genitalia, and face).
Calcipotriene: Approximately 6% of a topical dose of calcipotriene is systemically absorbed when applied to psoriatic skin.
Betamethasone: Topical corticosteroids can be absorbed from normal intact skin, and there may be a small extent of systemic absorption. After topical application to intact skin, up to 14% can be absorbed systemically; the extent is increased in areas of compromised skin integrity or occlusion. Repeated application results in a cumulative depot effect in the skin, which may lead to a prolonged duration of action, increased side effects, and increased systemic absorption.
Pregnancy And Lactation
Data are insufficient to determine if the use of calcipotriene; betamethasone during human pregnancy poses a risk for major birth defects, miscarriages, or adverse maternal or fetal outcomes. However, observational studies suggest an association between maternal exposure to potent or very potent topical corticosteroids (dose exceeding 300 grams) and low infant birth weight. In animal studies, an increased incidence of minor skeletal abnormalities was observed in the offspring of rats administered oral calcipotriene during organogenesis. Also, subcutaneous administration of betamethasone dipropionate to pregnant rats and rabbits during organogenesis resulted in fetal deaths, reduced fetal weight, and fetal malformations (cleft palate, abnormal tails). Calcipotriene; betamethasone should be used during pregnancy only if the potential benefit to the patient justifies the potential risk to the fetus. If treatment during pregnancy is required, apply the drug to the smallest area of skin and for the short duration possible.[31986] [43708]
It is not known if topically administered calcipotriene; betamethasone is excreted into breast milk. According to the manufacturer, because many drugs are excreted in human milk, caution should be exercised when it is administered to a breast-feeding mother. If treatment of a lactating mother is required, apply the drug to the smallest area of skin and for the short duration possible. Also, instruct the mother to avoid application to the breast while breast-feeding. 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 administered drug, health care providers are encouraged to report the adverse effect to the FDA.[31986]