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Pimecrolimus
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| Systematic (IUPAC) name | |
| (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS) -3-{(E)-2-[(1R,3R,4S)-4-Chloro-3 |
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| Identifiers | |
| CAS number | |
| ATC code | D11 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C43H68ClNO11 |
| Mol. mass | 810. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Chlorine (ˈklɔriːn from the Greek word 'χλωρóς' ( khlôros, meaning 'pale green' is the Chemical element with Atomic number 17 and Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 453 g/mol |
| Pharmacokinetic data | |
| Bioavailability | low systemic absorption |
| Protein binding | 74%–87% |
| Metabolism | Hepatic CYP3A |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | topical |
Pimecrolimus is an immunomodulating agent used in the treatment of atopic dermatitis (eczema). In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of A drug's efficiency may be affected by the degree to which it binds to the proteins within Blood plasma. Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems Cytochrome P450 family 3 subfamily A, also known as CYP3A, is a human Gene. The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction In Pharmacology and Toxicology, a route An immunomodulator is a drug used for its effect on the Immune system. Atopic dermatitis, also known as atopic eczema, is a disease characterized by Chronic inflammation of the skin which is atopic, hereditary and non-contagious 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. Novartis International AG is a multinational Pharmaceutical company based in Basel Switzerland that manufactures drugs such as Clozapine Galderma is an international pharmaceutical company specializing in the research development and marketing of therapeutic corrective and aesthetic solutions for Dermatology patients
Contents |
Pharmacology
Pimecrolimus is an ascomycin macrolactam derivative. Ascomycin, also called Immunomycin FR-900520 FK520 is an Ethyl analog of Tacrolimus (FK506 with strong immunosuppressant properties It has been shown in vitro that pimecrolimus binds to macrophilin-12 and inhibits calcineurin. Protein phosphatase 3 (formerly 2B catalytic subunit alpha isoform, also known as PPP3CA, is a human Gene. Thus pimecrolimus inhibits T-cell activation by inhibiting the synthesis and release of cytokines from T-cells. T cells belong to a group of White blood cells known as Lymphocytes, and play a central role in Cell-mediated immunity. Cytokines are a category of signalling Proteins and Glycoproteins that like Hormones and Neurotransmitters, are used extensively in cellular Pimecrolimus also prevents the release of inflammatory cytokines and mediators from mast cells. A mast cell (or mastocyte) is a resident cell of several types of tissues and contains many granules rich in Histamine and Heparin
Side effects
See also: Immunomodulators in the treatment of eczema
In January 2006, the United States Food and Drug Administration (FDA) announced that Elidel packaging would be required to carry a black box warning regarding the potential increased risk of lymph node or skin malignancy, as for the similar drug tacrolimus. Eczema (from Greek έκζεμα) is a form of Dermatitis, or Inflammation of the Epidermis. In the United States, a black box warning (also sometimes called a black label warning or boxed warning) is a type of warning that appears on the Package A Lymph node ( lɪmf noʊd is an organ consisting of many types of cells and is a part of the Lymphatic system. Skin cancer is a Malignant growth on the Skin which can have many causes Tacrolimus (also FK-506 or Fujimycin) is an immunosuppressive drug whose main use is after allogenic Organ transplant to reduce the Whereas current practice by UK dermatologists is not to consider this a significant real concern and they are increasingly recommending the use of such new drugs. The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom, the UK or Britain,is a Sovereign state located [1]
Dermatologists' and Allergists' professional societies, the American Academy of Dermatology[1], and the American Academy of Allergy, Asthma, and Immunology, have protested the inclusion of the black box warning. The American Academy of Dermatology ( AAD) is the largest organization of dermatologists in the world The American Academy of Allergy Asthma and Immunology (AAAAI is the largest medical specialty organization in the United States. The AAAAI states "None of the information provided for the cases of lymphoma associated with the use of topical pimecrolimus or tacrolimus in AD indicate or suggest a causal relationship. "[2]. In light of the known side effects of steroids which are used first line for many dermatological conditions, many doctors prefer to use this drug instead. In practice, other doctors use the drug as a second-line remedy only after conventional methods of treatment have failed.
Footnotes
- ^ N H Cox and Catherine H Smith (December 2002). Advice to dermatologists re topical tacrolimus (DOC). Therapy Guidelines Committee. British Association of Dermatologists.
External links
- Elidel official homepage
- FDA News
- NPS RADAR
- Offers more information on possible cancer risks of Elidel (Pimecrolimus)
- Article about American Academy of Dermatology speaking out against black box warning
- Report of the Calcineurin Task Force of the ACAAI and AAAAI
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