Gliclazid

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

Gliclazide Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R21:Gesundheitsschädlich bei Berührung mit der Haut.
  R36/38:Reizt die Augen und die Haut.
  R46:Kann vererbbare Schäden verursachen.
  R62:Kann möglicherweise die Fortpflanzungsfähigkeit beeinträchtigen.
  R63:Kann das Kind im Mutterleib möglicherweise schädigen.

• S-Sätze Betriebsanweisung:

  S25:Berührung mit den Augen vermeiden.
  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
  S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
  S53:Exposition vermeiden - vor Gebrauch besondere Anweisungen einholen.

• Chemische Eigenschaften

  White Cyrstalline Solid

• Originator

  Diamicron,Servier,France,1972

• Verwenden

  Gliclazide is an oral hypoglycemic agent used to treat non-insulin-dependent diabetes mellitus.Treatment of diabetes associated with obesity or vascular disease, for adults with type 2 diabetes.Diabetes is a chronic (long-lasting) health condition that affects how your body turns food into energy. Gliclazide reduces blood glucose levels by stimulating insulin secretion from the β-cells of the islets of Langerhans.

• Definition

  ChEBI: Gliclazide is a N-sulfonylurea. It has a role as a hypoglycemic agent, a radical scavenger and an insulin secretagogue.

• Manufacturing Process

  To a suspension containing 4.86 parts of 4-methylbenzenesulfonyl urethane (MP 80° to 82°C) and 36 parts of anhydrous toluene there are rapidly added 2.5 parts of N-amino-3-azabicyclo(3.3.0)octane (BP/18 mm = 86°C). The reaction mixture is heated under reflux for 1 hour. The resulting clear solution crystallizes on cooling. The crystals are filtered, washed with 2 parts of toluene, then recrystallized from anhydrous ethanol. There are obtained 3.8 parts of the desired product, MP 180° to 182°C.

• Therapeutic Function

  Oral hypoglycemic

• Allgemeine Beschreibung

  Chemically, gliclazide, 1-(3-azabicyclo[3.3.0]oct-3-yl)-3-p-tolylsulphonylurea (Diamicron), isvery similar to tolbutamide, with the exception of the bicyclicheterocyclic ring found in gliclazide. The pyrrolidineincreases its lipophilicity over that of tolbutamide,which increases its half-life. Even so, the p-methyl is susceptibleto the same oxidative metabolic fate as observedfor tolbutamide, namely, it will be metabolized to a carboxylicacid.

• Biochem/physiol Actions

  Oxidative modification of low-density lipoprotein (LDL) plays an important role in vascular dysfunction associated with diabetes mellitus. Gliclazide is a second-generation sulfonylurea with free-radical-scavenging activity. Incubation of human aortic smooth muscle cell (HASMC) with native human LDL (100 μg/mL) in the presence of increasing concentrations of gliclazide (1 to 10 μg/mL) resulted in a dose-dependent decrease in HASMC-mediated LDL oxidation. Exposure of HASMCs to gliclazide (1 to 10 μg/mL) and native LDL (100 μg/mL) also led to a dose-dependent decrease in oxidized LDL-induced human monocyte adhesion to HASMCs. In addition, incubation of HASMCs with gliclazide dramatically reduced the ability of oxidized LDL to stimulate the proliferation of these cells. Finally, treatment of HASMCs with gliclazide resulted in a marked decrease in oxidatively modified LDL-induced monocyte chemoattractant protein (MCP)-1 and human heat shock protein 70 (HSP 70) expression, both at the gene and protein levels. These results show that gliclazide, at concentrations in the therapeutic range (5 to 10 μg/mL), is effective in vitro in reducing vascular smooth muscle cell (VSMC) dysfunction induced by oxidatively modified LDL. Administration of gliclazide to type 2 diabetic patients could form part of the strategy for the prevention and management of diabetic cardiovascular diseases

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Analgesics: effects enhanced by NSAIDs.
  Antibacterials: effects enhanced by chloramphenicol, sulphonamides, tetracyclines and trimethoprim; effect reduced by rifamycins.
  Anticoagulants: effect possibly enhanced by coumarins; also possibly changes to INR.
  Antifungals: concentration increased by fluconazole and miconazole and possibly voriconazole - avoid with miconazole.
  Lipid-regulating drugs: possibly additive hypoglycaemic effect with fibrates.
  Sulfinpyrazone: enhanced effect of sulphonylureas.
  When gliclazide is used with nonsteroidal anti-inflammatory drug (especially salicylates), sulfa antibiotic, double coumarin anticoagulants, monoamine oxidase inhibitors, β-blockers, tetracycline, chloramphenicol, dicyclohexyl B piperidine, clofibrate, ethanol and other drugs, its dosage should be reduced to avoid hypoglycemia reaction.

• Stoffwechsel

  Gliclazide is extensively metabolised in the liver to metabolites that have no significant hypoglycaemic activity.
  Metabolites and a small amount of unchanged drug are excreted in the urine.

• Einzelnachweise

  [1] Patent: CN106588746, 2017, A. Location in patent: Paragraph 0105; 0106; 0107; 0108

Gliclazide Upstream-Materialien And Downstream Produkte

Gliclazid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(707)Suppliers

21187-98-4, Gliclazide Verwandte Suche: