DrugindexOnline^{2nd edition}

Pronouncation: (PIM-e-KROE-li-mus)
Class: Immunomodulator

Trade Names:
Elidel
- Cream 1%

Mechanism of Action

Pharmacology

Mechanism in atopic dermatitis is not known; however, pimecrolimus inhibits T-cell activation by blocking the transcription of early cytokines.

Pharmacokinetics

Absorption

After topical application, blood levels are routinely at or below the limit of quantification.

Distribution

In vitro studies indicate that plasma protein binding is 74% to 87%.

Metabolism

No evidence of skin-mediated drug metabolism.

Indications and Usage

Short-term and intermittent long-term treatment of mild to moderate atopic dermatitis in nonimmunocompromised patients 2 yr of age and older.

Contraindications

Standard considerations.

Dosage and Administration

Adults and children 2 yr of age and older

Topical Apply a thin layer to the affected skin bid. Reevaluate patient if symptoms persist beyond 6 wk of treatment.

General Advice

• For topical use only. Not for ophthalmic, oral, or intravaginal use.
• Avoid contact with eyes and areas of active cutaneous viral or bacterial infections.
• Stop using when signs and symptoms resolve.
• If signs and symptoms persist beyond 6 wk, reexamine patient to confirm atopic dermatitis diagnosis.
• Avoid long-term continuous application.
• Do not use with occlusive dressings because systemic exposure may be increased.

Storage/Stability

Store cream at controlled room temperature (59° to 86°F). Protect from freezing. Keep tube tightly capped.

Drug Interactions

CYP3A inhibitors (eg, calcium channel blockers, cimetidine, erythromycin, itraconazole, ketoconazole)

Use with caution in patients receiving pimecrolimus because possible interactions have not been ruled out.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (25%).

Dermatologic

Application site irritation, application site pruritus, skin infection (6%); impetigo (4%); skin papilloma (3%); acne, application site erythema, herpes simplex dermatitis, laceration (2%); urticaria (1%); facial edema, skin flushing (postmarketing).

EENT

Nasopharyngitis (20%); pharyngitis, sore throat (8%); ear infection, tonsillitis (6%); rhinitis (4%); acute tonsillitis, conjunctivitis, earache, epistaxis, streptococcal pharyngitis (3%); nasal congestion, otitis media, rhinorrhea (2%); eye infection (1%); ocular irritation (postmarketing).

GI

Diarrhea (8%); gastroenteritis, vomiting (7%); abdominal pain (4%); constipation, nausea (4%); upper abdominal pain (3%); loose stools (1%).

Genitourinary

Dysmenorrhea (2%).

Hematologic-Lymphatic

Lymphomas (postmarketing).

Local

Application site burning (26%).

Musculoskeletal

Arthralgia, back pain (2%).

Respiratory

Upper respiratory tract infection (19%); cough (16%); bronchitis (11%); aggravated asthma (4%); asthma, sinusitis (3%); acute bronchitis, dyspnea, pneumonia (2%); sinus congestion, wheezing (1%).

Miscellaneous

Influenza (13%); fever (12%); viral infection (7%); folliculitis (6%); hypersensitivity (5%); herpes simplex (4%); chickenpox (3%); bacterial infection, influenza-like symptoms, molluscum contagiosum, streptococcal infection (2%); accident (1%); anaphylactic reactions, angioneurotic edema, basal cell carcinoma, lymphomas, malignant melanoma, squamous cell carcinoma (postmarketing).

Precautions

Warnings Although a causal relationship has not been established, rare cases of malignancy (eg, skin, lymphoma) have been reported in patients treated with topical pimecrolimus. Avoid continuous long-term use of topical pimecrolimus and limit application to areas of atopic dermatitis.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 2 yr of age.

Immunocompromised patients

Do not use in immunocompromised adults and children.

Localized symptoms

Symptoms such as skin burning or pruritus may occur, most commonly during the first few days.

Lymphadenopathy

Investigate the etiology of lymphadenopathy occurring in patients receiving the topical ointment.

Malignant or premalignant skin conditions

Because malignant or premalignant skin conditions (eg, cutaneous T-cell lymphoma) can present as dermatitis, avoid use for malignant or premalignant skin conditions.

Netherton syndrome

Because of the risk for increased systemic exposure, do not use in patients with Netherton syndrome.

Sun exposure

Because the effects of pimecrolimus cream on skin response to ultraviolet damage are not known, patients should minimize or avoid natural or artificial sunlight exposure.

Viral infections

The topical ointment may be associated with increased risk of varicella zoster virus infection (chickenpox or shingles), herpes simplex virus infection, or eczema herpeticum.

Overdosage

Symptoms

There is no experience of overdose.

Patient Information

• Explain name, dose, action, and potential adverse reactions of drug.
• Obtain patient history, including drug history and any known allergies.
• Advise patient or caregiver to carefully read the Patient Information insert before using the first time and with each refill.
• Advise patient or caregiver that cream is applied topically only on areas that have eczema.
• Teach patient or caregiver proper technique for applying cream: Wash hands; apply a thin film of cream to cover skin areas with eczema; wash hands after applying cream unless hands are also being treated.
• Advise patient to not bathe, shower, or swim after applying cream because this could wash the cream off.
• Advise patient to use product exactly as prescribed.
• Advise patient that product is used for short periods, and, if needed, treatment may be repeated with breaks in between.
• Advise patient to stop using product when signs and symptoms of eczema resolve or as directed by health care provider.
• Advise patient to contact their health care provider if symptoms worsen, a skin infection occurs, or if symptoms do not improve after 6 wk of treatment.
• Advise patient using moisturizers to apply them after applying pimecrolimus cream.
• Caution patient not to cover treated areas with bandages, dressings, or wraps.
• Warn patient to avoid contact with the eyes.
• Advise patient to wash eyes with large amounts of cool water if cream comes in contact with the eyes and to contact health care provider if eye irritation persists.
• Advise patient that mild to moderate feelings of warmth and/or sensations of burning are the most common adverse reactions and to notify health care provider if these adverse reactions become severe or persist for more than 1 wk.
• Advise patient to talk to health care provider before using any other topical agents (eg, astringents, cosmetics, medicated soaps, other acne products) on treated skin.
• Warn patient to avoid unnecessary exposure to sun and sun lamps while using this medication. Advise patient to use sunscreens with minimum SPF of 15 and to wear protective clothing over treated areas when exposure cannot be avoided.
• Advise women to notify health care provider if pregnant, planning to become pregnant, or breast-feeding.
• Caution patient not to take any prescription or OTC medications, herbal preparations, or dietary supplements unless advised by health care provider.
• Advise patient that follow-up visits to examine the skin lesions may be necessary and to keep appointments.