Pimecrolimus

Pimecrolimus Uses, Dosage, Side Effects, Food Interaction and all others data.

Pimecrolimus is a macrolactam and is a derivative of ascomycin. It is an immunosuppressant which inhibits the activation of T-cells and prevents the release of inflammatory mediators from mast cells. It is used for the short term or intermittent long term treatment for mild to moderate atopic eczema.

The mechanism of action of pimecrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12) and inhibits the calcium-dependent phosphatase, calcineurin. As a consequence, it inhibits T cell activation by blocking the transcription of early cytokines. In particular, pimecrolimus inhibits at nanomolar concentrations Interleukin-2 and interferon gamma (Th1-type) and Interleukin-4 and Interleukin-10 (Th2-type) cytokine synthesis in human T-cells. In addition, pimecrolimus prevents the release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/IgE.

Pimecrolimus is a chemical that is used to treat atopic dermatitis (eczema). Atopic dermatitis is a skin condition characterized by redness, itching, scaling and inflammation of the skin. The cause of atopic dermatitis is not known; however, scientists believe that it may be due to activation of the immune system by various environmental or emotional triggers. Scientists do not know exactly how pimecrolimus reduces the manifestations of atopic dermatitis, but pimecrolimus reduces the action of T-cells and mast cells which are part of the immune system and contribute to responses of the immune system. Pimecrolimus prevents the activation of T-cells by blocking the effects of chemicals (cytokines) released by the body that stimulate T-cells. Pimecrolimus also reduces the ability of mast cells to release chemicals that promote inflammation.

Trade Name Pimecrolimus
Generic Pimecrolimus
Pimecrolimus Other Names Pimecrolimus, Pimecrolimusum
Weight 1%
Type Topical cream
Formula C43H68ClNO11
Weight Average: 810.46
Monoisotopic: 809.4480897
Protein binding

74%-87% (in vitro, bound to plasma proteins)

Groups Approved, Investigational
Therapeutic Class Drugs affecting the immune response
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Pimecrolimus
Pimecrolimus

Uses

Pimecrolimus Cream is used for second-line therapy for the short-term and non-continuous chronic treatment of mild to moderate atopic dermatitis in non-immunocompromised adults and children 2 years of age and older, who have failed to respond adequately to other topical prescription treatments, or when those treatments are not advisable.

Pimecrolimus Cream is not used for use in children less than 2 years of age

Pimecrolimus is also used to associated treatment for these conditions: Vitiligo, Intertriginous psoriasis, Mild Atopic dermatitis, Moderate Atopic dermatitis, Refractory Atopic dermatitis

How Pimecrolimus works

Pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12) and inhibits the calcium-dependent phosphatase, calcineurin. As a consequence, it inhibits T cell activation by blocking the transcription of early cytokines. In particular, pimecrolimus inhibits at nanomolar concentrations Interleukin-2 and interferon gamma (Th1-type) and Interleukin-4 and Interleukin-10 (Th2-type) cytokine synthesis in human T cells. Also, pimecrolimus prevents the release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/lgE.

Dosage

Pimecrolimus dosage

Apply a thin layer of Pimecrolimus Cream, 1% to the affected skin twice daily. The patient should stop using Pimecrolimus Cream, 1% when signs and symptoms (e.g., itch, rash and redness) resolve and should be instructed on what actions to take if symptoms recur.

If signs and symptoms persist beyond 6 weeks, patients should be re-examined by their health care provider to confirm the diagnosis ofatopicdermatitis.

Continuous long-term use of Pimecrolimus Cream, 1% should be avoided, and application should be limited to areas of involvement with atopic dermatitis

The safety of Pimecrolimus Cream, 1% underocclusion, which may promote systemic exposure, has not been evaluated. Avoid use of Pimecrolimus Cream, 1% with occlusive dressings.

Side Effects

Common side effects include headache, common cold or stuffy nose, sore throat, cough flu (influenza), fever, viral infection. Some people may get viral skin infections (like cold sores, chicken pox, shingles, or warts) or swollen lymph nodes (glands).

Toxicity

Side effects include burning sensation, irritation, pruritus, erythema, and skin infections, at the application site.

Precaution

Avoid use in areas affected by active, cutaneous viral infections. Avoid contact with the eyes and mucous membranes. Immunosuppression may increase risk of lymphoma and other malignancies. Limit exposure to sunlight or other UV light. Mild to moderate sensation of warmth and/or burning may occur at the treatment site within 1-5 days of initiation. Safety of usage beyond 1 yr is not established. Renal or hepatic impairment. Monitor renal, hepatic, cardiac and visual functions, BP, serum glucose and electrolytes regularly. Pregnancy, lactation.

Interaction

Potential interactions between Pimecrolimus Cream, 1% and other drugs, including immunizations, have not been systematically evaluated. Due to low blood levels of pimecrolimus detected in some patients after topical application, systemic drug interactions are not expected, but cannot be ruled out. The concomitant administration of known CYP3A family of inhibitors in patients with widespread and/or erythrodermic disease should be done with caution. Some examples of such drugs are erythromycin, itraconazole, ketoconazole, fluconazole, calcium channel blockers and cimetidine.

Food Interaction

No interactions found.

Elimination Route

Because of the low systemic absorption of pimecrolimus following topical application the calculation of standard pharmacokinetic measures such as AUC, Cmax, half-life, etc. cannot be reliably done.

Elimination Route

80% of the drug is excreted in the feces.

Pregnancy & Breastfeeding use

Pregnancy Category C. There are no adequate and well-controlled studies with Pimecrolimus Cream, 1% in pregnant women. Therefore, Pimecrolimus Cream, 1% should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers: It is not known whether this drug is excreted in human milk. Because of the potential for serious adverse reactions in nursing infants from pimecrolimus, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Contraindication

Pimecrolimus Cream, 1% is contraindicated in individuals with a history of hypersensitivity to pimecrolimus or any of the components of the cream.

Special Warning

Renal Impairment: Dosage reduction is necessary.

Hepatic Impairment: Dosage reduction is necessary.

Storage Condition

Store Pimecrolimus Cream at room temperature between 20° to 25°C. Do not freeze

Innovators Monograph

You find simplified version here Pimecrolimus

Pimecrolimus contains Pimecrolimus see full prescribing information from innovator Pimecrolimus Monograph, Pimecrolimus MSDS, Pimecrolimus FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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