Metforminhydrochlorid

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

Metformin hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R22:Gesundheitsschädlich beim Verschlucken.
  R36/38:Reizt die Augen und die Haut.

• S-Sätze Betriebsanweisung:

  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
  S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.

• Beschreibung

  Metformin is a biguanide with diverse biological activities. Metformin (250 mg/kg, i.p.) increases hepatic AMPK activity and reduces blood glucose by more than 50% in a liver kinase B1-dependent manner in mice fed normal and high-fat diets, respectively, and reduces blood glucose by 40% in ob/ob mice. It reduces weight gain, hepatic lipid droplet content, and total cholesterol, LDL cholesterol, and triglyceride levels in the plasma of diet-induced obese mice when administered at doses of 10 or 50 mg/kg per day. It also reverses increased hepatic triglyceride and apolipoprotein A5 levels, as well as hepatic steatosis, in a dose-dependent manner in an ob/ob mouse model of non-alcoholic fatty liver disease (NAFLD). Metformin (250 mg/kg) reduces tumor growth in an HCT116 p53^-\- human colon cancer mouse xenograft model, but has no effect on HCT116 p53^-\- tumors overexpressing recombinant S. cerevisiae Ndi1 NADH dehydrogenase, a single-subunit ortholog of the multi-subunit mammalian mitochondrial complex I. Formulations containing metformin have been used in the treatment of type 2 diabetes.

• Chemische Eigenschaften

  Crystalline Solid

• Originator

  Diabetex ,Germania

• Verwenden

  Metformin hydrochloride may be used as a pharmaceutical primary standard for the determination of the analyte in pharmaceutical formulations and human plasma samples by analytical techniques.

• Verwenden

  1,1-Dimethylbiguanide hydrochloride is used as an antidiabetic agent, used in polycystic ovary syndrome, non-alcoholic fatty liver disease and diabetes mellitus type 2. It may also reduce weight gain in people taking atypical antipsychotics, used in a study to investigate its role in enhancing the secretions of plasma active glucagon-like peptide-1 (GLP-1) levels.

• Verwenden

  Anti-diabetic and anti-cancer activity

• Verwenden

  An oral hypoglycemic agent

• Definition

  ChEBI: A hydrochloride resulting from the reaction of metformin with one molar equivalent of hydrogen chloride.

• Manufacturing Process

  The boiling mixture of 1,000 L xylene, 450 kg dimethylamine and 840 kg dicyanamide was added 365 kg hydrogene chloride. Yield of biguanide, 1,1- dimethyl-, hydrochloride 1,588 kg (96%). Biguanide, 1,1-dimethyl-, hydrochloride may be recrystallysed from methanol.

• Trademarks

  Fortamet (Andrx); Glucophage (Bristol-Myers Squibb); Glumetza (Depomed); Riomet(Ranbaxy).

• Therapeutic Function

  Oral hypoglycemic

• Allgemeine Beschreibung

  1,1-Dimethylbiguanide hydrochloride (metformin) is a strong base. It forms well defined salts and possessing excellent coordination capacity with transition metals, forming highly colored bidentate chelate complexes. Metformin (MET) exists in various forms: diprotonated (H₂MET)²⁺ in strong acidic solution, monoprotonated (HMET)⁺ in weak acid, MET in neutral and deprotonated (MET)^- in strong alkali solution. It is an oral antidiabetic drug. Pharmacokinetics of metformin has been studied. Determination of metformin in human plasma has been described by simple HPLC-UV method. Metformin is reported to increase plasma active glucagon-like peptide-1 (GLP-1) in humans.

• Flammability and Explosibility

  Non flammable

• Biologische Aktivität

  Antidiabetic agent; lowers plasma glucose levels and improves insulin sensitivity. Inhibits hepatic gluconeogenesis via activation of the LKB1/AMPK pathway. Displays antiproliferative effects in cancer cell lines.

• Biochem/physiol Actions

  Metformin is an antidiabetic agent that reduces blood glucose levels and improves insulin sensitivity. Its metabolic effects, including the inhibition of hepatic gluconeogenesis, are mediated at least in part by activation of the LKB1-AMPK (AMP-activated protein kinase) pathway. Activation of this pathway also appears to be involved in the antiproliferative and proapoptotic actions of metformin in cancer cell lines.

• Clinical Use

  
  Non-insulin dependent diabetes mellitus
  Polycystic ovary syndrome

• Veterinary Drugs and Treatments

  Metformin may be useful in the adjunctive treatment of non-insulin dependent diabetes mellitus in cats. Only limited trials of the drug have been performed in cats, with only very limited success when the drug is used alone. Studies comparing its safety and efficacy with other oral antihyperglycemics (e.g., glipizide or insulin) were not located.

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Alcohol: increased risk of lactic acidosis.
  Cimetidine: inhibits renal excretion of metformin

• Stoffwechsel

  Metformin is not metabolised to any great extent, and is entirely excreted unchanged in the urine.

• Lager

  Room temperature

• Einzelnachweise

  [1] ZHOU G, MYERS R W, LI Y, et al. Role of AMP-activated protein kinase in mechanism of metformin action.[J]. The Journal of clinical investigation, 2001, 1 1: 0. DOI:10.1172/jci13505
  [2] REUBEN J. SHAW. The Kinase LKB1 Mediates Glucose Homeostasis in Liver and Therapeutic Effects of Metformin[J]. Science, 2005, 310 5754. DOI:10.1126/science.1120781
  [3] W-Y SHI. Therapeutic metformin/AMPK activation blocked lymphoma cell growth via inhibition of mTOR pathway and induction of autophagy[J]. Cell Death & Disease, 2012, 3 3: e275-e275. DOI:10.1038/cddis.2012.13
  [4] DANIELA FORTUNATO RÊGO. Anti-tumor effects of metformin on head and neck carcinoma cell lines: A systematic review.[J]. Oncology Letters, 2017, 13 2: 554-566. DOI:10.3892/ol.2016.5526
  [5] SO-YOUNG LEE. PGC1α Activators Mitigate Diabetic Tubulopathy by Improving Mitochondrial Dynamics and Quality Control.[J]. Journal of Diabetes Research, 2017: 6483572. DOI:10.1155/2017/6483572
  [6] ZHI ZHENG. Sirtuin 1-mediated cellular metabolic memory of high glucose via the LKB1/AMPK/ROS pathway and therapeutic effects of metformin.[J]. Diabetes, 2012, 61 1: 217-228. DOI:10.2337/db11-0416
  [7] NIKITA KATILA . Metformin lowers α-synuclein phosphorylation and upregulates neurotrophic factor in the MPTP mouse model of Parkinson’s disease[J]. Neuropharmacology, 2017, 125: Pages 396-407. DOI:10.1016/j.neuropharm.2017.08.015
  [8] ANTHONY P. COLL. GDF15 mediates the effects of metformin on body weight and energy balance[J]. Nature, 2019, 578 7795: 444-448. DOI:10.1038/s41586-019-1911-y

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