ELIDEL
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 316.45 Da |
| 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 | Insufficient human data; animal studies show no teratogenicity at topical doses; avoid use unless clearly needed. |
| 2nd trimester | Insufficient human data; animal studies show no teratogenicity; avoid use unless clearly needed. |
| 3rd trimester | Insufficient human data; animal studies show no teratogenicity; avoid use unless clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for ELIDEL (ELIDEL).
| Placental transfer | Minimal systemic absorption after topical application; however, systemic exposure can occur. No studies on placental transfer; expected to be low based on molecular weight. |
| Breastfeeding | Not recommended during breastfeeding due to potential for serious adverse events in infants, including immune suppression and risk of infections. |
| Lactation Rating | L4 - Possibly Hazardous |
| 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 | 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. |
■ 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 formulationHistory of serious allergic reactionsNetherton syndromeGeneralized erythrodermaSkin conditions with impaired barrier function
| 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. |
| Food/Dietary | No known food interactions. Avoid grapefruit juice as it may increase drug levels (CYP3A4 inhibition). |
| Clinical Pearls | Topical calcineurin inhibitor for atopic dermatitis, reserved as second-line therapy for mild-to-moderate eczema due to boxed warning for rare malignancy risk. Apply thin layer only; avoid occlusive dressings. Do not use in immunocompromised patients. Intermittent use is recommended; continuous long-term use safety not established. |
| Patient Advice | Apply only to affected skin areas; avoid eyes, mouth, and open wounds. · Use for short durations; do not use continuously for extended periods. · Avoid sun exposure and tanning beds; use sunscreen on treated areas. · Do not cover treated skin with bandages or wraps unless instructed. · Report any signs of infection, skin burning, or new skin growths to your doctor. · This drug is for external use only; wash hands after application unless treating hands. · Do not use if you have a weakened immune system or active skin infection. |
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