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Pimecrolimus (Topical) (Monograph)

Brand name: Elidel
Drug class: Immunomodulatory Agents

Medically reviewed by Drugs.com on Mar 10, 2024. Written by ASHP.

Warning

  • Long-term safety of topical pimecrolimus not established.

  • Malignancies (e.g., skin cancers, lymphoma) reported rarely in patients treated with topical calcineurin inhibitors, including pimecrolimus; causal relationship not established.

  • Avoid continuous long-term use of topical pimecrolimus; limit application to areas affected by atopic dermatitis. (See Carcinogenicity under Cautions.)

  • Not indicated for use in children <2 years of age.

Introduction

Immunosuppressive agent; derivative of ascomycin (a macrolactam); structurally related to tacrolimus.

Uses for Pimecrolimus (Topical)

Atopic Dermatitis

Second-line therapy for short-term treatment and noncontinuous chronic treatment of mild to moderate atopic dermatitis (eczema) in immunocompetent adults and children ≥2 years of age who are unable to tolerate or have not responded to first-line therapies (e.g., corticosteroids) or for whom first-line therapies are inadvisable. (See Carcinogenicity under Cautions.)

Not indicated for use in children <2 years of age.

Pimecrolimus (Topical) Dosage and Administration

Administration

Topical Administration

Apply topically to the skin as a 1% cream. For external use only; do not use in the eyes or ingest.

Apply in thin layers to affected areas of skin.

Use minimum amount required to control symptoms; limit application to areas affected with atopic dermatitis. (See Carcinogenicity under Cautions.)

Do not use occlusive dressings or wrappings.

Dosage

Pediatric Patients

Atopic Dermatitis
Topical

Children ≥2 years of age: Apply to affected areas twice daily.

Treatment effects usually evident within 15 days; erythema and infiltration or papulation generally reduced within 8 days. Discontinue treatment following resolution of signs and symptoms (e.g., pruritus, rash, erythema). If manifestations persist beyond 6 weeks, reexamine patient and confirm diagnosis.

Adults

Atopic Dermatitis
Topical

Apply to affected areas twice daily.

Treatment effects usually evident within 15 days; erythema and infiltration or papulation generally reduced within 8 days. Discontinue treatment following resolution of signs and symptoms (e.g., pruritus, rash, erythema). If manifestations persist beyond 6 weeks, reexamine patient and confirm diagnosis.

Prescribing Limits

Pediatric Patients

Atopic Dermatitis
Topical

For short-term and intermittent use only; avoid continuous long-term use. Safety of noncontinuous use for >1 year not established. (See Carcinogenicity under Cautions.)

Adults

Atopic Dermatitis
Topical

For short-term and intermittent use only; avoid continuous long-term use. Safety of noncontinuous use for >1 year not established. (See Carcinogenicity under Cautions.)

Cautions for Pimecrolimus (Topical)

Contraindications

Warnings/Precautions

Warnings

Carcinogenicity

Possible increased risk of malignancies. (See Boxed Warning.)

Malignancies (including lymphoma and skin cancers) reported rarely in children and adults receiving topical pimecrolimus. Concerns also based on case reports of malignancies (including lymphoma and skin cancers) in patients (including transplant patients) receiving prolonged systemic treatment with calcineurin inhibitors (e.g., cyclosporine, tacrolimus); animal studies indicating dose-related increases in the risk of lymphoma and other malignancies with pimecrolimus and other calcineurin inhibitors; and known pharmacologic effects of these immunosuppressants.

Animal studies using topically or orally administered pimecrolimus in 3 species (mouse, rat, monkey) indicate increased risk of lymphoma and other malignancies (possibly due to immunosuppression ); risk appears to be related to dose and duration of exposure.

Risk associated with systemic therapy is related to intensity and duration of immunosuppression. The potential for systemic immunosuppression with topical pimecrolimus and the drug’s role in the development of malignancies in humans have not been established. Long-term studies in humans are needed to determine whether topical pimecrolimus is associated with an increased risk of malignancies. Until such data are available, FDA recommends limiting use to the labeled indication, reserving the drug for use as a second-line agent for short-term and intermittent treatment. (See Atopic Dermatitis under Uses, see Immunocompromised Patients under Cautions, and see Dosage and Administration.) Carefully evaluate potential risks and benefits of therapy.

Avoid use for malignant or premalignant skin conditions (e.g., cutaneous T-cell lymphoma [CTCL]), which may appear clinically similar to dermatitis.

General Precautions

Lymphadenopathy

Lymphadenopathy reported; usually related to infections and resolves following appropriate anti-infective therapy. Also reported in association with malignancy. Investigate etiology if lymphadenopathy develops. Discontinue pimecrolimus in the absence of a clear etiology or in the presence of acute infectious mononucleosis. Monitor patients with lymphadenopathy to ensure that it resolves.

Netherton’s Syndrome

Not recommended for use in patients with Netherton’s syndrome because of the potential for increased systemic absorption of pimecrolimus.

Generalized Erythroderma

Safety in patients with generalized erythroderma has not been established.

Dermatologic Reactions

Mild to moderate sensation of warmth and/or burning, stinging, soreness, and pruritus at the treatment site may occur within 1–5 days of initiating therapy. Reactions usually last no more than 5 days and improve as the lesions of atopic dermatitis resolve.

Infectious Complications

Clinical infections (e.g., bacterial, viral) at treatment sites should be resolved before initiating pimecrolimus therapy. Safety and efficacy not established for treatment of clinically infected atopic dermatitis.

Possible increased risk of varicella-zoster infections (chickenpox or shingles), herpes simplex virus infection, or eczema herpeticum.

Skin papilloma and/or warts may occur. If skin papilloma worsens or is unresponsive to conventional therapy, consider discontinuing pimecrolimus until complete resolution of the warts is achieved.

Septic arthritis reported in infants ≤1 year of age during clinical trials; however, causality not established.

Phototoxicity

Although phototoxicity not reported in humans, it may be prudent to minimize or avoid natural or artificial sunlight exposure during pimecrolimus therapy (including periods when no drug is on skin). Potential effects on skin response to ultraviolet (UV) damage are not known.

Animal photocarcinogenicity studies indicate shortened time to skin tumor formation following chronic topical pimecrolimus dosing with concurrent UV radiation exposure.

Immunocompromised Patients

Safety and efficacy not established and not recommended for use in immunocompromised adults or children.

Specific Populations

Pregnancy

Category C.

Lactation

Not known whether distributed into milk. Discontinue nursing or the drug.

Pediatric Use

Safety and efficacy not established and not recommended for use in children <2 years of age.

Increased incidence of upper respiratory tract infections in infants <24 months of age receiving pimecrolimus compared with those receiving placebo. Possible increased incidence of upper respiratory symptoms and/or infections in infants 3–23 months of age compared with older children; relationship to treatment not known.

Long-term effects on the developing immune system in infants and children are not known.

Not recommended for use in immunocompromised children.

Geriatric Use

Experience insufficient to determine whether patients ≥65 years of age respond differently than younger adults.

Common Adverse Effects

Upper respiratory tract infection, cough, nasopharyngitis, application site reactions (e.g., sensation of burning or warmth), headache.

Drug Interactions

No formal drug interaction studies have been performed.

Drugs Affecting Hepatic Microsomal Enzymes

Potential pharmacokinetic interaction with inhibitors of CYP3A4 in patients with widespread and/or erythrodermic disease.

Specific Drugs

Drug

Interaction

Comments

Antifungals, azoles

Potential interaction (inhibition of pimecrolimus metabolism) in patients with widespread and/or erythrodermic disease (which may increase systemic absorption)

Caution advised in patients with widespread and/or erythrodermic disease

Calcium-channel blocking agents

Potential interaction (inhibition of pimecrolimus metabolism) in patients with widespread and/or erythrodermic disease (which may increase systemic absorption)

Caution advised in patients with widespread and/or erythrodermic disease

Cimetidine

Potential interaction (inhibition of pimecrolimus metabolism) in patients with widespread and/or erythrodermic disease (which may increase systemic absorption)

Caution advised in patients with widespread and/or erythrodermic disease

Erythromycin

Potential interaction (inhibition of pimecrolimus metabolism) in patients with widespread and/or erythrodermic disease (which may increase systemic absorption)

Caution advised in patients with widespread and/or erythrodermic disease

Pimecrolimus (Topical) Pharmacokinetics

Absorption

Bioavailability

Not appreciably absorbed into systemic circulation following multiple topical applications in adults or children 2–14 years of age with atopic dermatitis. Increased systemic absorption occurs following topical application in infants 3–23 months of age with atopic dermatitis compared with older children, possibly because of the larger surface area to body mass ratio.

Occlusive dressings or wrappings may promote systemic exposure.

Distribution

Extent

Crosses placenta in rats and rabbits following oral administration.

Plasma Protein Binding

74–87% bound to plasma proteins in vitro.

Elimination

Metabolism

Studies using oral pimecrolimus indicate absorbed drug is metabolized in the liver principally via demethylation by CYP3A isoenzymes.

No evidence of skin-mediated metabolism.

Elimination Route

Studies using oral pimecrolimus indicated absorbed drug is eliminated principally in feces as metabolites.

Stability

Storage

Topical

Cream

25°C (may be exposed to 15–30°C). Do not freeze.

Actions

Advice to Patients

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Pimecrolimus

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Cream

1%

Elidel

Novartis

AHFS DI Essentials™. © Copyright 2024, Selected Revisions March 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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