EUCRISA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for EUCRISA (EUCRISA).
Phosphodiesterase 4 (PDE4) inhibitor, leading to increased intracellular cAMP levels and reduced proinflammatory cytokine production.
| Metabolism | Primarily metabolized via glucuronidation (UGT1A1, UGT1A3, UGT2B7, UGT2B17) and to a lesser extent via CYP1A2 and CYP2C9. |
| Excretion | Primarily hepatic metabolism via CYP3A4 and CYP2C19, with less than 1% of the dose excreted unchanged in urine and less than 1% in feces. |
| Half-life | At steady state, the elimination half-life is approximately 5.6 hours (range 2-10 hours), supporting twice-daily dosing. |
| Protein binding | Approximately 99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Apparent volume of distribution is approximately 2.3 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Topical administration: systemic bioavailability is low, approximately 7.7% (range 1-10%) of the applied dose, with minimal percutaneous absorption through intact skin. |
| Onset of Action | Topical application: clinical improvement in pruritus and dermatitis lesions observed within 1 week of initiating treatment. |
| Duration of Action | Symptom relief persists with continued twice-daily application; after discontinuation, effects typically wane over several days. |
Apply a thin layer to affected areas twice daily; maximum weekly dose 250 g.
| Dosage form | OINTMENT |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Approved for children aged 3 months and older: apply a thin layer to affected areas twice daily; maximum weekly dose 250 g. |
| Geriatric use | No specific dose adjustment; use same dosing as adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for EUCRISA (EUCRISA).
| Breastfeeding | No data on presence in human milk, effects on breastfed infant, or milk production. Systemic absorption is minimal (<1% bioavailability). The M/P ratio is unknown. Given negligible systemic exposure, risk to nursing infant is likely low. Caution: apply to smallest skin area and shortest duration possible. The American Academy of Pediatrics considers crisaborole compatible with breastfeeding when used appropriately. |
| Teratogenic Risk | EUCRISA (crisaborole) is a topical phosphodiesterase-4 inhibitor. Systemic absorption is minimal (bioavailability <1%). No adequate and well-controlled studies in pregnant women. Animal studies: In rats and rabbits, no evidence of fetal harm at topical doses up to 5 mg/kg/day (rat) and 10 mg/kg/day (rabbit). However, systemic exposure in animals was higher than at maximum recommended human dose (MRHD). Based on animal data, there is no risk of teratogenicity at clinically relevant exposures. Risk in first trimester is likely low; second and third trimesters: no known fetal risks. US FDA Pregnancy Category C (prior to 2015); current labeling uses Pregnancy and Lactation Rule. Overall, low risk due to minimal absorption. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to crisaborole or any component of the formulation"]
| Precautions | ["Application site reactions including pain, burning, and stinging","Risk of hypersensitivity reactions"] |
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| Fetal Monitoring | No specific maternal or fetal monitoring required for crisaborole use in pregnancy. Standard prenatal care. If applied to large body surface areas or compromised skin, monitor for adverse effects; but given low systemic absorption, routine monitoring is not indicated. |
| Fertility Effects | No human studies on fertility. Animal studies: No adverse effects on male or female fertility in rats at topical doses up to 5 mg/kg/day (systemic exposure ~10 times MRHD based on AUC). No evidence of impaired fertility attributable to crisaborole. No effect on sperm parameters or estrous cycle. |