Cyclosporin A Chemische Eigenschaften,Einsatz,Produktion Methoden
R-S?tze Betriebsanweisung:
R45:Kann Krebs erzeugen.
R60:Kann die Fortpflanzungsf?higkeit beeintr?chtigen.
R22:Gesundheitssch?dlich beim Verschlucken.
R40:Verdacht auf krebserzeugende Wirkung.
S-S?tze Betriebsanweisung:
S53:Exposition vermeiden - vor Gebrauch besondere Anweisungen einholen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn m?glich, dieses Etikett vorzeigen).
S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
S22:Staub nicht einatmen.
Beschreibung
Cyclosporine A is a powerful immunosuppressive drug intended for preventing rejection
of kidney, heart, and lung transplants.
A new era in the development of immunopharmacology began with the discovery of
cyclosporines.
Cyclosporines are produced by mycelial mushrooms Tolypocladium inflatum,
Tricoderma polysporum, and Cylindrocarpon lucidum, which are found in the ground.
Cyclosporine A is the first drug to affect a specific line of protecting cells of the body.
Unlike usual cytotoxics, it suppresses T-cells and acts on all cell lines simultaneously.
Cyclosporine A significantly eases the ‘reception’ of transplants, and increases the possibility of treating autoimmune system diseases.
Chemische Eigenschaften
White or almost white powder
Verwenden
Cyclosporin A is a hydrophobic cyclic peptide isolated from several fungal species including Cylindrocarpon, Fusarium, Trichoderma and Tolypocladium. Cyclosporin A inhibits T-cell activation and has been marketed since 1983 as an immunosuppressant in post-allogeneic organ transplant. Cyclosporin A acts by binding to the protein, cyclophilin (immunophilin), in T-lymphocytes causing inhibition of calcineurin (protein phosphatase 2B). Cyclosporin A reduces transcription of interleukin 2, and inhibits lymphokine production, interleukin release and NO synthesis induced by interleukin 1α, lipopolysaccharides and TNFα.
Definition
ChEBI: A cyclic nonribosomal peptide of eleven amino acids; an immunosuppressant drug widely used in post-allogeneic organ transplant to reduce the activity of the patient's immune system, and therefore the risk of organ rejection. Also causes reversible inhibiti
n of immunocompetent lymphocytes in the G0- and G1-phase of the cell cycle.
Indications
Allgemeine Beschreibung
White prismatic needles (from acetone) or white powder.
Air & Water Reaktionen
Slightly water soluble .
Reaktivit?t anzeigen
Cyclosporin A is an amide. Amides/imides react with azo and diazo compounds to generate toxic gases. Flammable gases are formed by the reaction of organic amides/imides with strong reducing agents. Amides are very weak bases (weaker than water). Imides are less basic yet and in fact react with strong bases to form salts. That is, they can react as acids. Mixing amides with dehydrating agents such as P2O5 or SOCl2 generates the corresponding nitrile. The combustion of these compounds generates mixed oxides of nitrogen (NOx).
Health Hazard
SYMPTOMS: Symptoms of exposure to Cyclosporin A include hepatotoxicity, nephrotoxicity, hyperkalemia, hyperuricemia, convulsions, renal dysfunction, tremor, hirsutism, hypertension, gum hyperplasia, cramps, acne, headache, diarrhea, nausea, vomiting, abdominal discomfort, paresthesia, flushing, leukopenia, lymphoma, sinusitis and gynecomastia. In 2% or less of persons exposed, it has caused allergic reactions, anemia, anorexia, confusion, conjunctivitis, edema, fever, brittle fingernails, gastritis, hearing loss, hiccups, hyperglycemia, muscle pain, peptic ulcer, thrombocytopenia and tinnitus. Rare reactions include anxiety, chest pain, constipation, depression, hair breaking hematuria, joint pain, lethargy, mouth sores, myocardial infarction, night sweats, pancreatitis, pruritus, swallowing difficulty, tingling, upper gastrointestinal bleeding, visual disturbance, weakness and weight loss. It has caused kidney and liver damage. An increased susceptibility to infection may occur. Other symptoms include gastrointestinal disturbance, rashes and angioedema.
Brandgefahr
Flash point data for Cyclosporin A are not available; however, Cyclosporin A is probably combustible.
Pharmakologie
Cyclosporine has no direct effect on keratinocytes and is not a mitotic inhibitor. Cyclosporine inhibits cytokine release, which results in a decreased recruitment of APCs into the epidermis and decreases immunoreactivity of lesions. Potential long-term side effects preclude cyclosporine’s use in all but very severe and recalcitrant psoriasis. Cyclosporine can be combined with lowdose methotrexate.
Nebenwirkungen
Cyclosporine’s main side effects, even at low doses, are hypertension and nephrotoxicity. Age, baseline blood pressure, and baseline creatinine levels are predictors of higher risks of side effects. Glomerular filtration rate (GFR) is a more sensitive test than creatinine for evaluating renal function, and a baseline is recommended in any high-risk patient. Longterm treatment with CSA may induce interstitial fibrosis and glomerular sclerosis, with more pronounced changes directly associated with duration of therapy. It should be administered only by dermatologists experienced in its use.
Sicherheitsprofil
Confirmed carcinogen
producing Hodghn's dlsease. Experimental
reproductive effects. Poison by
intraperitoneal and intravenous routes.
Moderately toxic by ingestion. Human
systemic effects by ingestion: increased body
temperature, cyanosis. Mutation data
reported. When heated to decomposition it
emits toxic fumes of NOx.
m?gliche Exposition
Cyclosporin A is a fungal metabolite;
an amide immunosuppressant drug used in various
surgeries.
Carcinogenicity
Cyclosporin A is known to be a human carcinogen based on sufficient evidence of carcinogenicity from studies in humans.
Versand/Shipping
UN3249 Medicine, solid, toxic, n.o.s., Hazard
Class: 6.1; Labels: 6.1-Poisonous materials.
Inkompatibilit?ten
Amides/imides react with azo and diazo
compounds to generate toxic gases. Flammable gases are
formed by the reaction of organic amides/imides with
strong reducing agents such as hydrideds and active metals.
Amides are very weak bases (weaker than water). Imides
are less basic yet and in fact react with strong bases to
form salts. That is, they can react as acids. Mixing amides
with dehydrating agents such as such as phosphorus pent-
oxide or thionyl chloride generates the corresponding
nitrile. The combustion of these compounds generates
mixed oxides of nitrogen (NOx).
Waste disposal
t is inappropriate and possibly
dangerous to the environment to dispose of expired or waste
drugs and pharmaceuticals by flushing them down the toilet
or discarding them to the trash. Household quantities of
expired or waste pharmaceuticals may be mixed with wet
cat litter or coffee grounds, double-bagged in plastic, discard
in trash. Larger quantities shall carefully take into consider-
ation applicable DEA, EPA, and FDA regulations. If possi-
ble return the pharmaceutical to the manufacturer for proper
disposal being careful to properly label and securely package
the material. Alternatively, the waste pharmaceutical shall be
labeled, securely packaged, and transported by a state
licensed medical waste contractor to dispose by burial in a
licensed hazardous or toxic waste landfill or incinerator.
Cyclosporin A Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
