Phenformin Chemische Eigenschaften,Einsatz,Produktion Methoden
R-S?tze Betriebsanweisung:
R22:Gesundheitssch?dlich beim Verschlucken.
S-S?tze Betriebsanweisung:
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Verwenden
N-Phenethylbiguanide is used in cancer treatment methods using thermotherapy and/or enhanced immunotherapy.
Definition
ChEBI: A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a 2-phenylethyl group. It was used as an anti-diabetic drug but was later withdrawn from the market due to potential risk of lactic acidos
s.
Weltgesundheitsorganisation (WHO)
Phenformin, a biguanide with oral hypoglycaemic activity, was
introduced in 1957 for the management of diabetes mellitus. By 1970 its use had
been associated with incidences of lactic acidosis and by 1976 clinical studies had
conclusively demonstrated that the hazards of phenformin treatment outweighed
the benefits. Preparations containing phenformin were withdrawn in several
countries and their use restricted in others. Elsewhere, however, proprietary
preparations containing this drug may remain available. The related biguanide,
buformin, has been also associated with lactic acidosis and has been subjected to
similar restrictions as phenformin, whereas there is some evidence that metformin
is less liable to induce lactic acidosis.
(Reference: (WHODI) WHO Drug Information, 2, 4, 1977)
Sicherheitsprofil
Poison by intraperitoneal, subcutaneous, and intravenous routes. Moderately toxic by ingestion. When heated to decomposition it emits toxic fumes of NOx.
Enzyminhibitor
This oral, biguanide-class antidiabetic (FWhydrochloride = 241.72 g/mol; M.P. = 175-178°C; typically supplied as the water-soluble hydrochloride salt), also known as phenethylbiguanide and phenylethylbiguanide, and named systematically as N’-b-phenethylformamidinyliminourea, was withdrawn from the U.S. market in 1977 due to high risk of inducing often fatal lactic acidosis. Target(s): cholesterol biosynthesis; 7-dehydrocholesterol reductase; diamine oxidase; glucose transport; insulysin; pyruvate kinase; and ubiquinol:cytochrome c reductase. Phenformin is an activator of AMP-stimulated protein kinase, and like ther AMPK activators also induce nucleoli re-organization, with attendanty changes in cell proliferation. Among the compounds tested, phenformin and resveratrol had the most pronounced impact on nucleolar organization. 1. McDonald & Dalidowicz Biochemistry
Phenformin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
