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: |
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:
Local symptoms: see adverse drug reactions. |
Adverse Reactions |
Local: Burning at application site , Irritation at application site, pruritus at application site, erythema at application site |
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. |
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: 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 |
Pimecrolimus
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Pimecrolimus Containing Brands
Pimecrolimus is used in following diseases
Drug - Drug Interactions of Pimecrolimus
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