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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TACLONEX (TACLONEX).
| Breastfeeding | Excretion of topical calcipotriene or betamethasone dipropionate into human milk is unknown. Systemic absorption after topical application is minimal, but caution advised. No M/P ratio available. Use only if clearly needed, and avoid application to breast area to prevent infant ingestion. |
| 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. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to any component; use on skin with known or suspected viral, fungal, or bacterial infections; use on lesions with tuberculosis, syphilis, or perioral dermatitis; use on skin with acne vulgaris; use on skin with rosacea; use on skin with ulcerations or wounds.
| 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. |
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| 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. |