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Pimecrolimus

Pronunciation

(pim e KROE li mus)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Cream, External:

Elidel: 1% (30 g, 60 g, 100 g) [contains benzyl alcohol, cetyl alcohol, propylene glycol]

Brand Names: U.S.

  • Elidel

Pharmacologic Category

  • Calcineurin Inhibitor
  • Immunosuppressant Agent
  • Topical Skin Product

Pharmacology

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.

Absorption

Poor when applied to 13% to 62% body surface area in adults treated for atopic dermatitis for up to a year; detectable blood levels were observed in a higher proportion of children, as compared to adults. Does not penetrate psoriatic plaque (Menter, 2009)

Use: Labeled Indications

Atopic dermatitis: Second-line therapy for short-term and noncontinuous long-term treatment of mild to moderate atopic dermatitis in nonimmunocompromised patients 2 years and older who have failed to respond adequately to other topical prescription treatments, or when those treatments are not advisable.

Use: Unlabeled

Second-line treatment of oral lichen planus; treatment of intertriginous and facial psoriasis

Contraindications

Hypersensitivity to pimecrolimus or any component of the formulation

Dosage

Atopic dermatitis (mild-to-moderate): Children ≥2 years, Adolescents, and Adults: Topical: Apply thin layer to affected area twice daily. Note: Limit application to involved areas. Discontinue use when symptoms have resolved; re-evaluate if symptoms persist >6 weeks.

Oral lichen planus (off-label use): Adults: Topical: Apply twice daily for 1 month (Passeron, 2007; Volz, 2008)

Psoriasis (off-label use): Adults: Topical: Apply twice daily (Gribetz, 2004; Menter, 2009)

Administration

Apply a thin layer to affected skin. Limit application to areas of involvement. Do not use with occlusive dressings. Burning at the application site is most common in first few days; improves as atopic dermatitis improves. Discontinue use when symptoms have resolved; re-evaluate if symptoms persist >6 weeks. Moisturizers may be applied after use of pimecrolimus cream. Wash hands after use.

Oral lichen planus (off-label use): Apply to affected oral mucosa, cover with a thin layer of gauze to delay dilution with saliva (Volz, 2008). Eating, drinking or chewing gum was not allowed for 30 minutes after application (Passeron, 2007).

Hazardous agent; use appropriate precautions for handling and disposal (meets NIOSH 2014 criteria).

Storage

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F); do not freeze.

Drug Interactions

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of Pimecrolimus. Monitor therapy

CYP3A4 Inhibitors (Strong): May decrease the metabolism of Pimecrolimus. Monitor therapy

Immunosuppressants: Pimecrolimus may enhance the adverse/toxic effect of Immunosuppressants. Exceptions: Cytarabine (Liposomal). Avoid combination

Adverse Reactions

>10%:

Central nervous system: Headache (children and adolescents 11% to 25%; adults 7%), fever (children and adolescents 13%; adults 1%)

Infection: Influenza (3% to 13%)

Local: Local burning (adults 26%; children and adolescents 2% to 8%; tends to resolve/improve as lesions resolve), application site reaction (adults 15%; children and adolescents 2%)

Respiratory: Nasopharyngitis (infants, children, and adolescents 10% to 27%; adults 8%), upper respiratory tract infection (children and adolescents 14% to 19%; adults 4%), cough (children and adolescents 9% to 16%; adults 2%), bronchitis (children and adolescents ≤11%; adults ≤2%)

1% to 10%:

Dermatologic: Folliculitis (adults 6%; children and adolescents 1%), skin infection (5% to 6%), impetigo (4%), warts (children and adolescents ≤3%), acne vulgaris (≤2%), herpes simplex dermatitis (≤2%), molluscum contagiosum (children and adolescents ≤2%), urticaria (≤1%)

Gastrointestinal: Diarrhea (children and adolescents 1% to 8%; adults ≤2%), gastroenteritis (children and adolescents ≤7%; adults 2%), vomiting (1% to 4%), constipation (children and adolescents ≤4%), abdominal pain (≤3%), toothache (≤3%), nausea (1% to 2%)

Genitourinary: Dysmenorrhea (1% to 2%)

Hypersensitivity: Hypersensitivity (3% to 5%)

Infection: Viral infection (children and adolescents ≤7%), herpes simplex infection (≤4%), bacterial infection (1% to 2%), staphylococcal infection (1% to 2%), varicella (≤1%)

Local: Local irritation (adults ≤6%; children and adolescents ≤1%), local pruritus (1% to 6%), localized erythema (≤2%)

Neuromuscular & skeletal: Arthralgia (≤2%), back pain (≤2%)

Ocular: Conjunctivitis (≤2% to 3%), eye infection (≤1%)

Otic: Otic infection (1% to 6%), otitis media (1% to 3%)

Respiratory: Sore throat (4% to 8%), pharyngitis (children and adolescents 1% to 8%; adults 1%), tonsillitis (children and adolescents ≤6%; adults <1%), asthma (3% to 4%), asthma aggravated (children and adolescents ≤4%), streptococcal pharyngitis (children and adolescents 3%), nasal congestion (1% to 3%), sinusitis (1% to 3%), epistaxis (≤3%), dyspnea (≤2%), flu-like symptoms (≤2%), pneumonia (≤2%), rhinitis (≤2%), rhinorrhea (children and adolescents ≤2%), viral upper respiratory tract infection (≤2%), wheezing (children and adolescents ≤1%)

Miscellaneous: Laceration (children and adolescents ≤2%)

<1% (Limited to important or life-threatening): Anaphylaxis, angioedema, eczema (herpeticum), lymphadenopathy, malignant neoplasm (basal cell carcinoma, squamous cell carcinoma, malignant melanoma, malignant lymphoma), skin discoloration

ALERT: U.S. Boxed Warning

Appropriate use:

Long-term safety of topical calcineurin inhibitors has not been established. Avoid continuous, long-term use of topical calcineurin inhibitors, including pimecrolimus, in any age group, and limit application to areas of involvement with atopic dermatitis.

Malignancy:

Although a causal relationship has not been established, rare cases of malignancy (eg, skin malignancy, lymphoma) have been reported in patients treated with topical calcineurin inhibitors including pimecrolimus.

Pediatrics:

Pimecrolimus is not indicated for use in children younger than 2 years.

Warnings/Precautions

Concerns related to adverse effects:

• Infection: Patients with atopic dermatitis are predisposed to skin infections; therapy has been associated with an increased risk of developing eczema herpeticum, varicella zoster, and herpes simplex. Do not apply to areas of active bacterial or viral infection; local infections at the treatment site should be resolved prior to therapy.

• Local symptoms: May cause local symptoms (eg, burning, pruritus, soreness, stinging) during first few days of treatment; usually self-resolving as atopic dermatitis lesions heal.

• 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: [US Boxed Warning]: Topical calcineurin inhibitors (including pimecrolimus) have been associated with rare cases of lymphoma and skin malignancy; avoid use on malignant or premalignant skin conditions (eg, cutaneous T-cell lymphoma).

• Skin papilloma: Skin papilloma (warts) have been observed with use; discontinue use if there is worsening of skin papillomas or they 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.

• 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, including patients on concomitant systemic immunosuppressive therapy.

• Pediatric: [US Boxed Warning]: Use of pimecrolimus in children <2 years of age is not recommended, particularly since the effect on immune system development is unknown.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC, 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors, 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer’s labeling.

Special handling:

• Hazardous agent: Use appropriate precautions for handling and disposal (meets NIOSH 2014 criteria).

Other warnings/precautions:

• Appropriate use: [US Boxed Warning]: Continuous long-term use of calcineurin inhibitors (including pimecrolimus) should be avoided and application of cream should be limited to areas of involvement with atopic dermatitis. Safety of intermittent use for >1 year has not been established.

• Sun exposure: Avoid artificial or natural sunlight exposure, even when pimecrolimus is not on the skin.

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies following topical application.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience flu-like symptoms, sensation of warmth, headache, rhinorrhea, rhinitis, or pharyngitis. Have patient report immediately to prescriber enlarged lymph nodes, warts, cold sores, paresthesia, severe skin irritation, skin infection, skin ulcers, skin growths, or mole changes (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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