TACLONEX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TACLONEX (TACLONEX).
Combination of calcipotriene (a vitamin D analog) and betamethasone dipropionate (a corticosteroid). Calcipotriene binds to vitamin D receptors, modulating keratinocyte proliferation and differentiation, and suppressing immune responses. Betamethasone dipropionate binds to glucocorticoid receptors, inducing lipocortin synthesis, inhibiting phospholipase A2, and reducing prostaglandin and leukotriene production, thereby exerting anti-inflammatory, antipruritic, and vasoconstrictive effects.
| Metabolism | Calcipotriene undergoes hepatic metabolism primarily via CYP24A1; betamethasone dipropionate undergoes hepatic metabolism via CYP3A4 and CYP2C8. Both are excreted in feces and urine. |
| Excretion | Biliary/fecal: ~64% (calcipotriene) and ~98% (betamethasone dipropionate); renal: <1% (calcipotriene) and negligible (betamethasone dipropionate). |
| Half-life | Calcipotriene: ~4 hours; betamethasone dipropionate: ~5 hours (topical). Terminal half-life not clinically relevant due to local action. |
| Protein binding | Calcipotriene: ~94% bound to albumin; betamethasone dipropionate: ~64% bound to albumin. |
| Volume of Distribution | Not established for topical use; systemic absorption minimal. |
| Bioavailability | Topical: <1% of applied dose (calcipotriene) and <2% (betamethasone dipropionate) absorbed systemically. |
| Onset of Action | 1–2 weeks of daily topical application. |
| Duration of Action | Continuous application required; effect subsides within days to weeks after discontinuation. |
| Molecular Weight | Calcipotriene: 412.61 Da; Betamethasone dipropionate: 504.59 Da |
Apply topically to affected areas twice daily. Maximum weekly dose: 100 g. Not for use on face, groin, or axillae.
| Dosage form | OINTMENT |
| Renal impairment | No dosage adjustment required in renal impairment. Safety in severe renal impairment not established. |
| Liver impairment | No dosage adjustment required in hepatic impairment. Safety in severe hepatic impairment not established. |
| Pediatric use | Safety and efficacy in pediatric patients below 18 years have not been established. |
| Geriatric use | No specific dose adjustment recommended. Use caution due to increased risk of skin atrophy and systemic absorption. |
| 1st trimester | Topical calcipotriene/betamethasone dipropionate (Taclonex) is not recommended in the first trimester due to insufficient data. Use only if potential benefit justifies risk. |
| 2nd trimester | Use with caution in the second trimester; topical corticosteroids should be used at the lowest effective dose for the shortest duration. |
| 3rd trimester | Use with caution in the third trimester; prolonged use or high doses may cause fetal adrenal suppression. Avoid application to large areas or prolonged treatment. |
Clinical note
Comprehensive clinical and safety monograph for TACLONEX (TACLONEX).
| Placental transfer | Betamethasone dipropionate crosses the placenta, but calcipotriene has minimal placental transfer due to high molecular weight and rapid metabolism. The combined product has unknown placental transfer; based on components, transfer is likely minimal with topical use. |
| Breastfeeding | Topical application to small areas is likely compatible with breastfeeding; avoid application to the breast area. Limited systemic absorption reduces infant exposure, but betamethasone may be excreted in breast milk in small amounts. Monitor infant for potential adrenal suppression. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to calcipotriene, betamethasone dipropionate, or any component of the formulationUse on face, groin, or axillaeUse for treatment of erythrodermic, exfoliative, or pustular psoriasisKnown or suspected hypercalcemiaKnown or suspected Cushing's syndromeActive viral, fungal, or bacterial skin infections
| Precautions | May cause hypothalamic-pituitary-adrenal (HPA) axis suppression, especially with prolonged use or application to large surface areas; hypercalcemia; hypercalciuria; skin atrophy; striae; telangiectasias; purpura; and allergic contact dermatitis. Avoid use on face, axillae, or groin. Not for ophthalmic, oral, or intravaginal use. Discontinue if irritation occurs. |
| Food/Dietary | No significant food interactions. However, because calcipotriene can affect calcium metabolism, avoid high calcium intake (e.g., dairy, calcium supplements) if using large amounts or if renal impairment exists. Not necessarily restricted, but monitor calcium levels if hypercalcemia risk. |
Loading safety data…
| Lactation Rating | L3 - Limited Data |
| Teratogenic Risk | Pregnancy Category C. In animal reproduction studies, topical calcipotriene (0.003-0.3 mg/kg/day) caused skeletal abnormalities and increased fetal resorptions; betamethasone dipropionate (0.015-0.15 mg/kg/day) caused cleft palate and decreased fetal weight. No adequate human studies. Risk cannot be ruled out. Use only if potential benefit justifies risk. First trimester: avoid due to potential teratogenicity. Second/third trimester: limited data, use lowest effective dose for shortest duration. |
| Fetal Monitoring | Monitor maternal serum calcium and urine calcium if applied over large surface areas or prolonged use due to calcipotriene's effect on calcium metabolism. Monitor fetal growth by ultrasound due to potential corticosteroid effects. Monitor for maternal adrenal suppression if high doses used. No routine fetal monitoring specific to Taclonex. |
| Fertility Effects | No human data on fertility effects. Animal studies: calcipotriene (oral doses up to 0.6 mg/kg/day) did not impair fertility; betamethasone dipropionate (subcutaneous doses up to 0.05 mg/kg/day) prolonged estrous cycle and reduced fertility in rats. Use may theoretically affect fertility via systemic corticosteroid effects, but topical application limits systemic exposure. |
| Clinical Pearls | Taclonex (betamethasone dipropionate 0.064% and calcipotriene 0.005%) is a fixed-dose combination topical for plaque psoriasis. Apply once daily; no need for occlusion. Limit total weekly dose to <100 g to minimize adrenal suppression and hypercalcemia risk. Avoid face, groin, and axillae. Discontinue if skin atrophy or striae develop. |
| Patient Advice | Apply a thin layer to affected skin only once daily. · Do not cover the area with bandages or dressings unless directed. · Wash hands after application unless treating hands. · Avoid contact with eyes, mouth, and mucous membranes. · Do not use more than 100 grams per week. · Discontinue and contact doctor if severe irritation, skin thinning, or signs of infection occur. · Not for use on the face, groin, or underarms. · Avoid excessive sun exposure and tanning beds on treated areas. |