ELIDEL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ELIDEL (ELIDEL).
Inhibits T-cell activation by binding to macrophilin-12 (FKBP-12) and inhibiting calcineurin, thereby blocking cytokine transcription.
| Metabolism | Metabolized primarily by CYP3A4; major metabolite O-demethylated pimecrolimus. |
| Excretion | Renal (negligible, <1% unchanged) and biliary/fecal (approximately 97% as metabolites); less than 1% of the dose is excreted renally as unchanged drug. |
| Half-life | Terminal elimination half-life: 30–45 hours (mean 35 hours) following topical application; clinically, twice-daily dosing ensures therapeutic concentrations. |
| Protein binding | 99% bound to plasma proteins (primarily albumin and alpha-1-acid glycoprotein). |
| Volume of Distribution | Vd ~ 10 L/kg (extensive tissue distribution); suggests significant extravascular binding and penetration into tissues. |
| Bioavailability | Topical: Systemic bioavailability is approximately 4% (range 1–7%) of applied dose; absorption increases with extent of skin lesion and thickness of application. |
| Onset of Action | Topical: Clinical improvement may be observed within 1 week; significant reduction in pruritus and inflammation often noted after 3–5 days of twice-daily application. |
| Duration of Action | Duration of action is maintained with continuous twice-daily application; after discontinuation, therapeutic effect wanes over several days to weeks. |
| Action Class | Immunosuppressant- Calcineurin inhibitors |
| Brand Substitutes | Pacroma Cream, Picon Cream |
Apply a thin layer of 1% cream to affected areas twice daily.
| Dosage form | CREAM |
| Renal impairment | No dose adjustment required for any degree of renal impairment. |
| Liver impairment | No formal studies in hepatic impairment; use caution in severe impairment. |
| Pediatric use | Apply a thin layer of 1% cream twice daily for children aged 2 years and older; not indicated for children under 2 years. |
| Geriatric use | No specific dose adjustment recommended; apply a thin layer of 1% cream twice daily as for adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ELIDEL (ELIDEL).
| Breastfeeding | Not recommended. Pimecrolimus is excreted in milk in animal studies; unknown in humans. M/P ratio not available. Potential for serious adverse reactions in nursing infants. |
| Teratogenic Risk | FDA Pregnancy Category C. Systemic exposure is minimal after topical application, but animal studies have shown developmental toxicity. No adequate human studies; risk cannot be excluded. Avoid in pregnancy unless clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
Long-term safety of topical calcineurin inhibitors has not been established; rare cases of malignancy (e.g., lymphoma, skin cancer) have been reported; use should be limited to short-term and intermittent treatment.
| Serious Effects |
Hypersensitivity to pimecrolimus or any component of the formulation; history of malignancy; application to areas of active infection; Netherton syndrome; immunocompromised patients.
| Precautions | Increased risk of infections (e.g., eczema herpeticum, varicella zoster); avoid use on malignant or premalignant skin conditions; lymphadenopathy; photosensitivity; not recommended in patients with Netherton syndrome; potential for systemic immunosuppression; monitor for local irritation. |
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| No specific fetal monitoring required due to minimal systemic absorption. Monitor maternal application site for signs of infection or systemic effects. |
| Fertility Effects | No human data on fertility. Animal studies show no impairment of fertility at subcutaneously doses up to 10 mg/kg/day. |