Pimecrolimusum

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

Pimecrolimusum 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.

Pimecrolimusum 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. Pimecrolimusum prevents the activation of T-cells by blocking the effects of chemicals (cytokines) released by the body that stimulate T-cells. Pimecrolimusum also reduces the ability of mast cells to release chemicals that promote inflammation.

Pimecrolimusum
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Pimecrolimusum
Generic	Pimecrolimus
Pimecrolimus Other Names	Pimecrolimus, Pimecrolimusum
Type
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
Last Updated:	September 19, 2023 at 7:00 am

Uses

Pimecrolimusum 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.

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

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

How Pimecrolimusum works

Pimecrolimusum 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

Pimecrolimusum dosage

Apply a thin layer of Pimecrolimusum Cream, 1% to the affected skin twice daily. The patient should stop using Pimecrolimusum 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 Pimecrolimusum Cream, 1% should be avoided, and application should be limited to areas of involvement with atopic dermatitis

The safety of Pimecrolimusum Cream, 1% underocclusion, which may promote systemic exposure, has not been evaluated. Avoid use of Pimecrolimusum 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 Pimecrolimusum 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, C_max, 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 Pimecrolimusum Cream, 1% in pregnant women. Therefore, Pimecrolimusum 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.