Pimecrolimus

Therapeutic Class
Immunosuppressant Agent; Topical Skin Product
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.

Adult Doses

Mild-to-moderate atopic dermatitis:
Topical: Continue as long as signs and symptoms persist; discontinue if resolution occurs; re-evaluate if symptoms persist >6 weeks.

Contraindications

Hypersensitivity to pimecrolimus or any component of the formulation.

Boxed Warning

Topical calcineurin inhibitors have been associated with rare cases of lymphoma and skin malignancy.

Use in children <2 years of age is not recommended.

Warnings / Precautions

Point to take care before prescribing: 

  1. 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.
  2. Not for use in children <2 years of age.
  3. Do not apply to areas of active bacterial or viral infection; infections at the treatment site should be cleared prior to therapy.
  4. Should not be used in immunocompromised patients.
  5. Avoid use on malignant or premalignant skin conditions (e.g., cutaneous T-cell lymphoma). 
    Not recommended for use in patients with Netherton's syndrome or skin conditions which may increase the potential for systemic absorption.

Local symptoms: see adverse drug reactions.
Lymphadenopathy: May be associated with development of lymphadenopathy; possible infectious causes should be investigated.
Skin : Papilloma/warts.Pimecrolimus therapy has been associated with risk of developing eczema herpeticum, varicella zoster, and herpes simplex.
Sun exposure: Avoid artificial or natural sunlight exposure. 

Adverse Reactions

Local: Burning at application site , Irritation at application site, pruritus at application site, erythema at application site 
Central nervous system: Headache, fever 
Respiratory: Nasopharyngitis, cough, upper respiratory tract infection, bronchitis, Pharyngitis, asthma, asthma aggravated, nasal congestion, sinusitis, epistaxis, dyspnea, pneumonia, rhinorrhea, wheezing 
Endocrine & metabolic: Dysmenorrhea 
Dermatologic: Skin infection, folliculitis, impetigo, skin papilloma, acne, herpes simplex dermatitis, molluscum contagiosum, urticaria 
Gastrointestinal: Diarrhea, gastroenteritis, abdominal pain, constipation 
Ocular: Eye infection 
Otic: Ear infection, otitis media 
Miscellaneous: Influenza, Viral infection, tonsillitis, hypersensitivity, herpes simplex infection, bacterial infection, Anaphylaxis, angioneurotic edema, eczema herpeticum, facial edema, flushing, lymphadenopathy, ocular irritation, malignancy, skin discoloration

Food Interactions

Ethanol: Avoid ethanol (topical pimecrolimus may increase the potential for experiencing facial flushing following the consumption of alcoholic beverages).

Mechanism of Actions

Pimecrolimus, like tacrolimus, belongs to the ascomycin class of macrolactam immunosuppressives, 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, thereby preventing the cascade of immune and inflammatory signals. Pimecrolimus has a similar mode of action to that of tacrolimus but is more selective, with no effect on dendritic (Langerhans) cells. It has lower permeation through the skin than topical steroids or topical tacrolimus although they have not been compared with each other for their permeation ability through mucosa. In addition, in contrast with topical steroids, pimecrolimus does not produce skin atrophy.
Tacrolimus and pimecrolimus are both calcineurin inhibitors and function as immunosuppressants.

Metabolism

Substrate of CYP3A4 (minor)

Pharmacodynamics

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

Administration

Apply thin layer to affected area twice daily; rub in gently and completely;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.

Pregnancy Category

C: Drug Pregnancy Category Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Lactation

Excretion in breast milk unknown/not recommended.

ATC Classification
D11AH02
GenericPedia Classification
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    Pimecrolimus Containing Brands

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    Pimecrolimus is used in following diseases

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    Drug - Drug Interactions of Pimecrolimus
    Interaction
    Major, Avoid combination Dasatinib vs Pimecrolimus
    Minor, Monitor Therapy Darunavir vs Pimecrolimus
    Major, Avoid combination Altretamine vs Pimecrolimus
    Major, Avoid combination Carboplatin vs Pimecrolimus
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    Major, Avoid combination Eculizumab vs Pimecrolimus
    Major, Avoid combination Temozolomide vs Pimecrolimus
    Major, Avoid combination Thiotepa vs Pimecrolimus
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