Elidel
Elidel - General Information
Elidel is an immunomodulating agent used in the treatment of atopic dermatitis (eczema). It is currently available as a topical cream, once marketed by Novartis, (however Galderma will be promoting the molecule in Canada in early 2007) under the trade name Elidel. [Wikipedia]
Pharmacology of Elidel
Elidel 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. Elidel prevents the activation of T-cells by blocking the effects of chemicals (cytokines) released by the body that stimulate T-cells. Elidel also reduces the ability of mast cells to release chemicals that promote inflammation.
Elidel for patients
Patients using Elidel should receive the following information and instructions:
• Patients should use Elidel Cream as directed by the physician. Elidel Cream is for external use on the skin only. As with any topical medication, patients or caregivers should wash hands after application if hands are not an area for treatment.
• Patients should minimize or avoid exposure to natural or artificial sunlight (tanning beds or UVA/B treatment) while using Elidel Cream.
• Patients should not use this medication for any disorder other than that for which it was prescribed.
• Patients should report any signs or symptoms of adverse reactions to their physician.
• Therapy should be discontinued after signs and symptoms of atopic dermatitis have resolved. Treatment with Elidel should be resumed at the first signs or symptoms of recurrence.
• Use of Elidel may cause reactions at the site of application such as a mild to moderate feeling of warmth and/or sensation of burning. Patients should see a physician if an application site reaction is severe or persists for more than 1 week.
• The patient should contact the physician if no improvement in the atopic dermatitis is seen following 6 weeks of treatment, or if at any time the condition worsens.
Elidel Interactions
Potential interactions between Elidel and other drugs, including immunizations, have not been systematically evaluated. Due to the very 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.
Elidel Contraindications
Elidel (pimecrolimus) Cream 1% is contraindicated in individuals with a history of hypersensitivity to pimecrolimus or any of the components of the cream.
Additional information about Elidel
Elidel Indication: For treatment of mild to moderate atopic dermatitis.
Mechanism Of Action: Elidel 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Pimecrolimus
Synonyms: ASM 981; SDZ ASM 981
Drug Category: Anti-Inflammatory Agents, Non-Steroidal; Dermatologic Agents; Enzyme Inhibitors; Immunosuppressive Agents
Drug Type: Small Molecule; Approved; Investigational
Other Brand Names containing Pimecrolimus: Elidel;
Absorption: 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.
Toxicity (Overdose): Side effects include burning sensation, irritation, pruritus, erythema, and skin infections, at the application site.
Protein Binding: 74%-87% (in vitro, bound to plasma proteins)
Biotransformation: Metabolized by the CYP3A sub-family of metabolizing enzymes.
Half Life: Not Available
Dosage Forms of Elidel: Cream Topical
Chemical IUPAC Name: (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-3-{(E)-2-[(1R,3R,4S)-4-Chloro-3-methoxycyclohexyl]-1-methylvinyl}-8-ethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-14,16-dimethoxy-4,10,12,18-tetramethyl-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone
Chemical Formula: C43H68ClNO11
Pimecrolimus on Wikipedia: https://en.wikipedia.org/wiki/Pimecrolimus
Organisms Affected: Humans and other mammals
