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ALERT: U.S. Boxed Warning
The FDA-approved labeling includes a boxed warning. See Warnings/Precautions section for a concise summary of this information. For verbatim wording of the boxed warning, consult the product labeling or www.fda.gov.
Medication Safety Issues
Sound-alike/look-alike issues:
Pimecrolimus may be confused with tacrolimus
Pronunciation
(pim e KROE li mus)
U.S. Brand Names
Generic Available
No
Canadian Brand Names
Pharmacologic Category
Use: Labeled Indications
Short-term and intermittent long-term treatment of mild-to-moderate atopic dermatitis in patients not responsive to conventional therapy or when conventional therapy is not appropriate
Pregnancy Risk Factor
C
Pregnancy Considerations
There are no adequate and well-controlled studies in pregnant women; use only if clearly needed.
Lactation
Excretion in breast milk unknown/not recommended
Breast-Feeding Considerations
Due to the potential for serious adverse reactions in the nursing infant, breast-feeding is not recommended.
Contraindications
Hypersensitivity to pimecrolimus or any component of the formulation
Warnings/Precautions
Boxed warnings:
• Malignancy: See “Concerns related to adverse effects” below.
Concerns related to adverse effects:
• Local symptoms: May cause local symptoms (eg, burning, soreness, stinging) during first few days of treatment; usually self-resolving.
• Lymphadenopathy: May be associated with development of lymphadenopathy; possible infectious causes should be investigated. Discontinue use in patients with unknown cause of lymphadenopathy or acute infectious mononucleosis.
• Malignancy: [U.S. Boxed Warning]: Topical calcineurin inhibitors have been associated with rare cases of lymphoma and skin malignancy; avoid use on malignant or premalignant skin conditions (eg, cutaneous T-cell lymphoma). Should be used for short-term and intermittent treatment using the minimum amount necessary for the control of symptoms; application should be limited to involved areas. Safety of intermittent use for >1 year has not been established. [U.S. Boxed Warning]: The use of Elidel® in children <2 years of age is not recommended, particularly since the effect on immune system development is unknown.
• Skin papilloma: Papilloma/warts have been observed with use; discontinue pimecrolimus until resolution if worsening or do not respond to conventional treatment.
Disease-related concerns:
• Atopic dermatitis: Diagnosis should be reconfirmed if sign/symptoms do not improve within 6 weeks of treatment. Patients with atopic dermatitis are predisposed to skin infections, and pimecrolimus therapy has been associated with risk of developing eczema herpeticum, varicella zoster, and herpes simplex.
• Erythroderma: Safety not established in patients with generalized erythroderma.
• Skin diseases which may increase systemic absorption: Not recommended for use in patients with Netherton's syndrome or skin conditions which may increase the potential for systemic absorption.
Special populations:
• Immunocompromised patients: Should not be used in immunocompromised patients.
• Pediatrics: Not for use in children <2 years of age.
Other warnings/precautions:
• Appropriate use: Topical calcineurin agents are considered second-line therapies in the treatment of atopic dermatitis/eczema, and should be limited to use in patients who have failed or cannot tolerate treatment with other therapies. Do not apply to areas of active bacterial or viral infection; infections at the treatment site should be cleared prior to therapy.
• Sun exposure: Avoid artificial or natural sunlight exposure, even when Elidel® is not on the skin.
Adverse Reactions
>10%:
Central nervous system: Headache (7% to 25%), fever (1% to 13%)
Local: Burning at application site (2% to 26%; tends to resolve/improve as lesions resolve)
Respiratory: Nasopharyngitis (8% to 27%), cough (2% to 16%), upper respiratory tract infection (4% to 19%), bronchitis (?11%)
Miscellaneous: Influenza (3% to 13%)
1% to 10%:
Dermatologic: Skin infection (2% to 6%), folliculitis (1% to 6%), impetigo (2% to 4%), skin papilloma (warts) (?3%), acne (?2%), herpes simplex dermatitis (? 2%), molluscum contagiosum (?2%), urticaria (?1%)
Endocrine & metabolic: Dysmenorrhea (1% to 2%)
Gastrointestinal: Diarrhea (1% to 8%), gastroenteritis (?7%), abdominal pain (?4%), constipation (?4%)
Local: Irritation at application site (?6%), pruritus at application site (1% to 6%), erythema at application site (?2%)
Ocular: Eye infection (?1%)
Otic: Ear infection (1% to 6%), otitis media (1% to 3%)
Respiratory: Pharyngitis (1% to 8%), asthma (1% to 4%), asthma aggravated (?4%), nasal congestion (1% to 3%), sinusitis (1% to 3%), epistaxis (?3%), dyspnea (?2%), pneumonia (?2%), rhinorrhea (?2%), wheezing (?1%)
Miscellaneous: Viral infection (?7%), tonsillitis (?6%), hypersensitivity (3% to 5%), herpes simplex infection (?4%), bacterial infection (1% to 2%)
<1%: Eczema herpeticum, lymphadenopathy
Postmarketing and/or case reports: Anaphylaxis, angioneurotic edema, facial edema, flushing (ethanol-associated), ocular irritation (following application near eyes), malignancy (basal cell carcinoma, squamous cell carcinoma, malignant melanoma, lymphoma), skin discoloration
Metabolism/Transport Effects
Substrate of CYP3A4 (minor)
Drug Interactions
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of Pimecrolimus. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of Pimecrolimus. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (topical pimecrolimus may increase the potential for experiencing facial flushing following the consumption of alcoholic beverages).
Storage
Store at 15°C to 30°C (59°F to 86°F); do not freeze.
Mechanism of Action
Penetrates inflamed epidermis to inhibit T cell activation by blocking transcription of proinflammatory cytokine genes such as interleukin-2, interferon gamma (Th1-type), interleukin-4, and interleukin-10 (Th2-type). Pimecrolimus binds to the intracellular protein FKBP-12, inhibiting calcineurin, which blocks cytokine transcription and inhibits T-cell activation. Prevents release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/IgE.
Pharmacodynamics/Kinetics
Absorption: Poor when applied to 13% to 62% body surface area in adults for up to a year; detectable blood levels were observed in a higher proportion of children, as compared to adults
Dosage
Children ?2 years and Adults: Topical: Apply thin layer to affected area twice daily; rub in gently and completely. Note: Limit application to involved areas. Continue as long as signs and symptoms persist; discontinue if resolution occurs; re-evaluate if symptoms persist >6 weeks.
Administration: Topical
Do not use with occlusive dressings. Burning at the application site is most common in first few days; improves as atopic dermatitis improves. Limit application to areas of involvement. Continue as long as signs and symptoms persist; discontinue if resolution occurs; re-evaluate if symptoms persist >6 weeks.
Patient Education
This medication is for external use only. Avoid alcohol use while using this medication. Do not use for any skin disorder except that for which it was prescribed. Avoid getting any medication in or close to eyes. Apply as often as directed by prescriber, in thin film to affected area. Do not cover with bandages or occlusive dressings. Wash and dry hands thoroughly before and after applying (if affected area is not on hands). Avoid artificial or natural sunlight even when drug not applied to skin. Discontinue therapy after signs and symptoms have disappeared; restart treatment at first sign of recurrence. You may experience burning at site of application, this will usually last less than 5 days, and go away as skin condition improves. You may experience headache, fever, cough, nasal or throat irritation, flu-like symptoms, diarrhea, or constipation; contact prescriber if these persist. Contact prescriber if skin condition worsens or if symptoms persist longer than 6 weeks. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
None reported
Mental Health: Effects on Psychiatric Treatment
None reported
Nursing: Physical Assessment/Monitoring
See Administration directions. Assess knowledge/teach patient appropriate use, interventions to reduce side effects, and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Cream, topical:
Elidel®: 1% (30 g, 60 g, 100 g)
Pricing: U.S. (www.drugstore.com)
Cream (Elidel)
1% (30): $92.30
1% (60): $168.14
1% (100): $261.54
International Brand Names
Lexi-Comp.com
Last full review/revision July 2009
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