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药品详细

Metformin (二甲双胍 )

化学结构式图
中文名
二甲双胍
英文名
Metformin
分子式
Not Available
化学名
1-carbamimidamido-N,N-dimethylmethanimidamide
分子量
Average: 129.1636
Monoisotopic: 129.101445377
CAS号
657-24-9
ATC分类
A10B Oral Blood Glucose Lowering Drugs, Excl. Insulins
药物类型
small molecule
阶段
商品名
Apo-Metformin;Fortamet;Gen-Metformin;Glucophage;Glucophage XR;Glycon;Novo-Metformin;Nu-Metformin;Riomet;
同义名
Metformin HCL;metformin hydrochloride;
基本介绍

A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289)

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  • Actavis elizabeth llc
  • Alphapharm party ltd
  • Alvogen inc
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  • Apotex inc etobicoke site
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  • Barr laboratories inc
  • Bristol myers squibb co
  • Bristol myers squibb co pharmaceutical research institute
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  • Glenmark generics ltd
  • Granules india ltd
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  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mutual pharmacal co
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Neurosci inc
  • Nostrum pharmaceuticals inc
  • Provident pharmaceutical inc
  • Ranbaxy laboratories ltd
  • Ranbaxy pharmaceuticals inc
  • Sandoz inc
  • Sun pharmaceutical industries ltd
  • Teva pharmaceuticals usa inc
  • Torrent pharma inc
  • Torrent pharmaceuticals ltd
  • Watson laboratories
  • Watson laboratories inc
  • Watson laboratories inc florida
  • Zydus pharmaceuticals usa inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Witters LA: The blooming of the French lilac. J Clin Invest. 2001 Oct;108(8):1105-7. Pubmed
  2. UNGAR G, FREEDMAN L, SHAPIRO SL: Pharmacological studies of a new oral hypoglycemic drug. Proc Soc Exp Biol Med. 1957 May;95(1):190-2. Pubmed
  3. Lord JM, Flight IH, Norman RJ: Metformin in polycystic ovary syndrome: systematic review and meta-analysis. BMJ. 2003 Oct 25;327(7421):951-3. Pubmed
  4. Marchesini G, Brizi M, Bianchi G, Tomassetti S, Zoli M, Melchionda N: Metformin in non-alcoholic steatohepatitis. Lancet. 2001 Sep 15;358(9285):893-4. Pubmed
  5. Nair S, Diehl AM, Wiseman M, Farr GH Jr, Perrillo RP: Metformin in the treatment of non-alcoholic steatohepatitis: a pilot open label trial. Aliment Pharmacol Ther. 2004 Jul 1;20(1):23-8. Pubmed
剂型
Form Route Strength
Tablet Oral
Tablet, extended release Oral
规格
Unit description Cost Unit
Fortamet er 1000 mg tablet 6.93 USD tablet
Fortamet 1000 mg 24 Hour tablet 6.01 USD tablet
Fortamet 500 mg 24 Hour tablet 2.55 USD tablet
Fortamet er 500 mg tablet 2.48 USD tablet
Glucophage 1000 mg tablet 2.33 USD tablet
Metformin hcl crystals 2.14 USD g
Glucophage 850 mg tablet 1.94 USD tablet
Glucophage XR 750 mg 24 Hour tablet 1.8 USD tablet
Glucophage xr 750 mg tablet 1.71 USD tablet
Metformin hcl 1000 mg tablet 1.48 USD tablet
MetFORMIN HCl 750 mg 24 Hour tablet 1.25 USD tablet
Metformin hcl 850 mg tablet 1.22 USD tablet
Glucophage XR 500 mg 24 Hour tablet 1.17 USD tablet
Glucophage 500 mg tablet 1.14 USD tablet
Glucophage xr 500 mg tablet 1.14 USD tablet
Glucophage xr 500 mg tablet sa 1.11 USD tablet
MetFORMIN HCl 500 mg 24 Hour tablet 0.75 USD tablet
Metformin hcl 500 mg tablet 0.72 USD tablet
Glucophage 850 mg Tablet 0.38 USD tablet
Glucophage 500 mg Tablet 0.3 USD tablet
Riomet 500 mg/5 ml solution 0.27 USD ml
Riomet 500 mg/5ml Solution 0.27 USD ml
Apo-Metformin 850 mg Tablet 0.21 USD tablet
Co Metformin 850 mg Tablet 0.21 USD tablet
Mylan-Metformin 850 mg Tablet 0.21 USD tablet
Novo-Metformin 850 mg Tablet 0.21 USD tablet
Nu-Metformin 850 mg Tablet 0.21 USD tablet
Pms-Metformin 850 mg Tablet 0.21 USD tablet
Ratio-Metformin Hydrochloride 850 mg Tablet 0.21 USD tablet
Sandoz Metformin Fc 850 mg Tablet 0.21 USD tablet
Pms-Metformin 500 mg Tablet 0.13 USD tablet
Ran-Metformin 500 mg Tablet 0.13 USD tablet
Ratio-Metformin Hydrochloride 500 mg Tablet 0.13 USD tablet
Sandoz Metformin Fc 500 mg Tablet 0.13 USD tablet
Zym-Metformin 500 mg Tablet 0.13 USD tablet
Apo-Metformin 500 mg Tablet 0.13 USD tablet
Co Metformin 500 mg Tablet 0.13 USD tablet
Mylan-Metformin 500 mg Tablet 0.13 USD tablet
Novo-Metformin 500 mg Tablet 0.13 USD tablet
Nu-Metformin 500 mg Tablet 0.13 USD tablet
化合物类型
Type small molecule
Classes
  • Biguanides
Substructures
  • Biguanides
  • Guanidines
  • Carboxamidines
适应症
Diabetes 糖尿病;
药理
Indication For use as an adjunct to diet and exercise to improve glycemic control in adult patients (18 years and older) with type 2 diabetes.
Pharmacodynamics Metformin is an antihyperglycemic agent, which improves glucose tolerance in patients with type 2 diabetes, lowering both basal and postprandial plasma glucose. Metformin is not chemically or pharmacologically related to any other classes of oral antihyperglycemic agents. Unlike sulfonylureas, metformin does not produce hypoglycemia in either patients with type 2 diabetes or normal subjects and does not cause hyperinsulinemia. With metformin therapy, insulin secretion remains unchanged while fasting insulin levels and daylong plasma insulin response may actually decrease.
Mechanism of action Metformin's pharmacologic mechanisms of action are different from other classes of oral antihyperglycemic agents. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. These effects are mediated by the initial activation by Metformin of AMP-activated protein kinase (AMPK), a liver enzyme that plays an important role in insulin signaling, whole body energy balance, and the metabolism of glucose and fats. Activation of AMPK is required for metformin's inhibitory effect on the production of glucose by liver cells. Increased peripheral utilization of glucose may be due to improved insulin binding to insulin receptors. AMPK probably also plays a role, as metformin administration increases AMPK activity in skeletal muscle. AMPK is known to cause GLUT4 deployment to the plasma membrane, resulting in insulin-independent glucose uptake.
Absorption Absorbed over 6 hours, bioavailability is 50 to 60% under fasting conditions. Food delays absorption.
Volume of distribution Not Available
Protein binding Metformin is negligibly bound to plasma proteins.
Metabolism

Metformin is not metabolized.
Route of elimination Intravenous single-dose studies in normal subjects demonstrate that metformin is excreted unchanged in the urine and does not undergo hepatic metabolism (no metabolites have been identified in humans) nor biliary excretion.
Half life 6.2 hours
Clearance Not Available
Toxicity Acute oral toxicity (LD50): 350 mg/kg [Rabbit]. It would be expected that adverse reactions of a more intense character including epigastric discomfort, nausea, and vomiting followed by diarrhea, drowsiness, weakness, dizziness, malaise and headache might be seen.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Melting point 223-226 oC
Experimental Properties
Property Value Source
water solubility Freely soluble as HCl salt PhysProp
logP -0.5 PhysProp
pKa 12.4 Various sources
Predicted Properties
Property Value Source
water solubility 1.38e+00 g/l ALOGPS
logP -1.83 ALOGPS
logP -0.92 ChemAxon Molconvert
logS -1.97 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 5 ChemAxon Molconvert
hydrogen donor count 4 ChemAxon Molconvert
polar surface area 88.99 ChemAxon Molconvert
rotatable bond count 0 ChemAxon Molconvert
refractivity 56.64 ChemAxon Molconvert
polarizability 13.43 ChemAxon Molconvert
药物相互作用
Drug Interaction
Cimetidine Cimetidine may increase the therapeutic and adverse effects of metformin by increasing its serum concentration. Consider alternate therapy.
Glucosamine Possible hyperglycemia
Somatropin recombinant Somatropin may antagonize the hypoglycemic effect of metformin. Monitor for changes in fasting and postprandial blood sugars.
食物相互作用
  • Avoid alcohol.
  • Take with food to reduce irritation.

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