ENSTILAR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ENSTILAR (ENSTILAR).
ENSTILAR is a combination of calcipotriene (a vitamin D analog) and betamethasone dipropionate (a corticosteroid). Calcipotriene binds to vitamin D receptors, modulating cell proliferation and differentiation. Betamethasone suppresses inflammation by inhibiting phospholipase A2, reducing prostaglandin and leukotriene synthesis.
| Metabolism | Calcipotriene undergoes hepatic metabolism; betamethasone dipropionate is metabolized via CYP3A4. |
| Excretion | Calcipotriol is primarily excreted via bile/feces (approximately 70% of absorbed dose). Betamethasone dipropionate is mainly excreted renally (60-70% as metabolites) and up to 20-30% via feces. For the combination, renal excretion of betamethasone metabolites predominates, with fecal excretion of calcipotriol. |
| Half-life | Calcipotriol: terminal half-life ~12 hours. Betamethasone dipropionate: terminal half-life ~16-22 hours. Clinically, this supports once-daily application. |
| Protein binding | Calcipotriol: ~94% bound to plasma proteins, primarily albumin. Betamethasone dipropionate: ~64% bound, mainly to albumin and corticosteroid-binding globulin. |
| Volume of Distribution | Calcipotriol: Vd ~1.6 L/kg, indicating extensive tissue distribution. Betamethasone dipropionate: Vd ~1.4 L/kg, also widely distributed. |
| Bioavailability | Topical: systemic absorption minimal (<1% for calcipotriol, ~5-7% for betamethasone dipropionate with occlusive use; otherwise <1% each). Oral data not applicable. |
| Onset of Action | Topical: noticeable improvement in plaque psoriasis within 1-2 weeks of daily application. |
| Duration of Action | Clinical effect persists with continued use; rebound may occur upon discontinuation. Once-daily application maintains efficacy. |
Apply to affected area once daily for up to 4 weeks. Maximum 100 g/day or 30 g/week. Not for use on face, axillae, or groin.
| Dosage form | AEROSOL, FOAM |
| Renal impairment | No dosage adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment; use with caution. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh class C). Not studied in moderate impairment; avoid use. Caution in mild impairment. |
| Pediatric use | Safety and efficacy not established in patients under 18 years; not recommended. |
| Geriatric use | No specific adjustment; use caution due to higher risk of corticosteroids-related adverse effects (e.g., skin atrophy, HPA axis suppression) and potential for impaired renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ENSTILAR (ENSTILAR).
| Breastfeeding | Systemic absorption is minimal; however, trace amounts may appear in breast milk following topical application. M/P ratio: not established. Caution should be exercised, avoiding application to breast area to prevent infant ingestion. Short-term use on limited areas is unlikely to cause adverse effects in breastfed infants. |
| Teratogenic Risk | Enstilar (calcipotriene 0.005% and betamethasone dipropionate 0.064%) is classified as Pregnancy Category C. Topical corticosteroids have shown teratogenic effects in animal studies, but no adequate human studies exist. Calcipotriene is a vitamin D analogue; risks are theoretical due to low systemic absorption. First trimester: limited data, but avoid high doses. Second and third trimesters: minimal risk with topical use, but prolonged high-dose application may lead to fetal growth restriction or adrenal suppression. Systemic absorption is low (<1%) with recommended use. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to any component","Known or suspected disorders of calcium metabolism","Use on face, groin, or axillae","Viral, fungal, or bacterial skin infections at treatment site"]
| Precautions | ["Hypercalcemia and hypercalciuria due to calcipotriene","Hypothalamic-pituitary-adrenal (HPA) axis suppression from corticosteroid","Local adverse reactions including skin atrophy, striae, and telangiectasias","Photosensitivity reactions","Avoid use on face, groin, or axillae","Not recommended in patients with known or suspected disorders of calcium metabolism"] |
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| Fetal Monitoring | Monitor for maternal adrenal suppression if used over large areas, under occlusion, or for prolonged periods. Assess fetal growth if used extensively. Evaluate for signs of hypercalcemia (calcipotriene component) if applied to >30% body surface area. No routine fetal monitoring required for standard use. |
| Fertility Effects | No known effects on human fertility. Animal studies with calcipotriene and betamethasone at high doses have not shown impaired fertility. Topical use at recommended doses is unlikely to impact reproductive function. |