Metformin Tablets

Overview of Metformin Tablets

Dosage Strength

Immediate Release: 500 mg, 1,000 mg
Extended Release: 500 mg, 750 mg

General Information

Similar to phenformin, an oral biguanide antidiabetic medicine that was taken off the market in the US in 1977 due to the onset of lactic acidosis, metformin is a biguanide antidiabetic agent. But with metformin, the chance for this adverse effect is significantly reduced. 1 While metformin’s effects are distinct from those of sulfonylureas and other anti-diabetic medications, they nonetheless work well together. In type 2 diabetes, metformin was discovered to produce comparable glycemic control to glyburide. even if it increased the likelihood of stomach issues. 2 In the treatment of polycystic ovarian syndrome (PCOS), metformin has been demonstrated to be effective; it reduces blood androgen levels, restores regular menstrual periods and ovulation, and may increase the likelihood of conception. 3 Additionally, based on the little data available, it may postpone the development of menarche in females who have precocious puberty and the onset of puberty in females who have an early-normal onset. 45 Both metformin and rigorous lifestyle change are effective in reducing the occurrence of diabetes, but lifestyle intervention has a stronger impact in patients with impaired glucose tolerance. 6 Even while lifestyle intervention is quite successful, the majority of patients who try lifestyle changes on their own during the first year after diagnosis fail. Therefore, it is advised that metformin and lifestyle interventions be started as soon as type 2 diabetes mellitus is diagnosed, according to a joint consensus algorithm for the treatment of the condition created by the American Diabetes Association (ADA) and the European Association for the Study of Diabetes. The effectiveness, safety, and affordability of metformin led to its selection as the first pharmacological therapy. 789 In addition, in a follow-up study to the UKPDS, researchers discovered that patients initially randomized to metformin therapy had a 33 percent relative reduction in risk of myocardial infarction and a 27 percent relative reduction in risk of death from any cause as compared to patients initially randomized to conventional therapy after 10 years of resuming typical care (RR 0.67, 95 percent CI 0.51—0.89; p=0.005). 10 The FDA did not approve metformin until December 1994, despite the fact that it had been available in Europe since the 1950s. It can be used alone or in conjunction with sulfonylureas, alpha-glucosidase inhibitors, or insulin to treat type 2 diabetes. In January 2001, the regular-release pills received approval for usage in children older than 10 years. In September 2003, Riomet, an oral treatment, received approval. Glucophage XR in October 2000, Fortamet in April 2004, and Glumetza in June 2005, each with a different medication delivery method, are three extended-release formulations that have been approved (see Pharmacokinetics section). When compared to regular-release metformin, the extended-release versions offer comparable glucose control, but have the benefit of once-daily treatment. Another benefit is the promise of less side effects, particularly gastrointestinal side effects (such as flatulence and diarrhea); however, larger trials contrasting regular-release and extended-release metformin are required to support these claims as the present trial results are inconsistent. 111213

References

1.Lalau JD, Lacroix C, Compagnon P, et al. Role of metformin accumulation in metformin-associated lactic acidosis. Diabetes Care 1995;18:779-84.
2.Hermann LS, Scherstein B, Bitzen PO, et al. Therapeutic comparison of metformin and sulfonylurea, alone, and in various combinations. A double-blind controlled study. Diabetes Care 1994;17:1100-9.
3.Kosasa TS. Making a Case for Metformin. OB/GYN 2003;48:69-80.
4.Ibanez L, Ong K, Valls C, et al. Metformin treatment to prevent early puberty in girls with precocious puberty. J Clin Endocrinol Metab 2006;91:2888-91.
5.Ibanez L, Valls C, Ong K, et al. Metformin therapy during puberty delays menarche, prolongs puberal growth, and augments adult height: a randomized study in low-birth-weight girls with early-normal onset of puberty. J Clin Endocrinol Metab 2006;0:2068-73.
6.Doggrell SA. Metformin & lifestyle intervention prevent Type 2 diabetes: lifestyle intervention has the greater effect. Expert Opin Pharmacother 2002;3:1011-3.
7.Inzucchi SE, Bergenstal RM, Buse JB, et al. Management of hyperglycemia in type 2 diabetes: a patient-centered approach. Position Statement of the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD). Diabetes
8.American Diabetes Association. Standards of medical care in diabetes-2012. Diabetes Care 2012;35(suppl1):S11-S63.
9.American Diabetes Association. Standards of medical care in diabetes-2014. Diabetes Care 2014;37(suppl1):S14-S80.
10.Holman RR, Paul SK, Bethel MA, et al. 10-year follow-up of intensive glucose control in type 2 diabetes. N Engl J Med 2008;359:1577-89.
11.Blonde L, Dailey GE, Jabbour SA, et al. Gastrointestinal tolerability of extended-release metformin tablets compared to immediate-release metformin tablets: results of a retrospective cohort study. Curr Med Res Opin 2004; 20(4):565-72.
12.31285
13.Wagstaff AJ, Figgit DP. Extended-release metformin hydrochloride. Single composition osmotic tablet formulation. Treat Endocrinol 2004;3:327-32.
14.Bailey CJ, Turner RC. Metformin. N Engl J Med 1996;334:574-9.
15.Glucophage®/Glucophage® XR (metformin) package insert. Princeton, NJ: Bristol-Myers Squibb Company; 2009 Jan.
16.Robert F, Fendri S, Hary L,et al. Kinetics of plasma and erythrocyte metformin after acute administration in healthy subjects. Diabetes Metab 2003;Gerich JE. Oral hypoglycemic agents. N Engl J Med 1989;321:1231—45.:279–83.
17.Bodmer M, Meier C, Krahenbuhl S, et al. Metformin, sulfonylureas, or other antidiabetes drugs and the risk of lactic acidosis or hypoglycemia. Diabetes Care 2008;31:2086-91.
18.Inzucchi SE, Bergenstal RM, Buse JB, et al. Management of hyperglycemia in type 2 diabetes: a patient-centered approach. Position statement of the ADA and EASD. Diabetes Care 2012. Epub ahead of print, doi: 10.2337/dc12-0413
19.Lipska KJ, Bailey CJ, Inzucchi SE. Use of metformin in the setting of mild-to-moderate renal insufficiency. Diabetes Care 2011;34:1432-1437.
20.Eurich DT, McAlister FA, Blackburn DF, et al. Benefits and harms of antidiabetic agents in patients with diabetes and heart failure: systematic review. BMJ 2007;335(7618):497 Epub 2007 Aug 30
21.Ting RZ, Szeto CC, Chan MH, et al. Risk factors of vitamin B12 deficiency in patients receiving metformin. Arch Intern Med 2006;166:1975-9.
22.Vanky E, Zahlsen K, Spigset O, et al. Placental passage of metformin in women with polycystic ovary syndrome. Fertil Steril 2005;83:1575-8.
23.Glueck CJ, Goldenberg N, Pranikoff J, et al. Height, weight, and motor-social development during the first 18 months of life in 126 infants born to 109 mothers with polycystic ovary syndrome who conceived on and continued metformin through pregnancy. Hum
24.Coetzee EJ, Jackson WPU. Metformin in management of pregnant insulin-dependent diabetics. Diabetologia 1979;16:421-425.
25.American College of Obstetricians and Gynecologists. ACOG Practice Bulletin Number 60: Pregestational diabetes mellitus. Obstet Gynecol 2005;105:675-85.
26.American College of Obstetricians and Gynecologists. ACOG Practice Bulletin Number 30: Gestational diabetes. Obstet Gynecol 2001;98:525-38.
27.Dhulkotia JS, Ola B, Fraser R, et al. Oral hypoglycemic agents vs insulin in management of gestational diabetes: a systematic review and metaanalysis. Am J Obstet Gynecol 2010;203:457.
28.Balani J, Hyer SL, Rodin DA, et al. Pregnancy outcomes in women with gestational diabetes treated with metformin or insulin: a case-control study. Diabet Med 2009;26:798-802.
29.Hale TW, Kristensen JH, Hackett LP, et al. Transfer of metformin into human milk. Diabetologia 2002;45:1509-14.
30.Gardiner SJ, Kirkpatrick CMJ, Begg EJ, et al. Transfer of metformin into human milk. Clin Pharmacol Ther 2003;73:71-7.
31.Briggs GG, Ambrose PJ, Nageotte MP, et al. Excretion of metformin into breast milk and the effect on nursing infants. Obstet Gynecol 2005;105:1437-41.
32.Glueck CJ, Salehi M, Sieve L, et al. Growth, motor, and social development in breast- and formula- fed infants of metformin-treated women with polycystic ovary syndrome. J Pediatr 2006;148:628-32.
33.Everett J. Use of oral antidiabetic agents during breastfeeding. J Hum Lact 1997;13:319-21.
34.American Academy of Pediatrics (AAP) Committee on Drugs. Transfer of drugs and other chemicals into human milk. Pediatrics 2001;108:776-89.
35.Spencer JP, Gonzalez LS, Barnhart DJ. Medications in the breast-feeding mother. Am Fam Physician; 64:119-26.
36.Spencer JP, Gonzalez LS, Barnhart DJ. Medications in the breastfeeding mother. Am Fam Physician; 64:119-26.
37.Glucophage®/Glucophage® XR (metformin) package insert. Princeton, NJ: Bristol-Myers Squibb Company; 2003 Apr.
38.Lasix® (furosemide) package insert. Bridgewater, NJ: Aventis Pharmaceuticals; 2004 Jan.
39.Bumex® (bumetanide) package insert. Nutley, NJ: Roche Laboratories, Inc.; 2003 Mar.
40.Demadex® (torsemide) package insert. Nutley, NJ: Roche Laboratories; 2003 Apr.
41.Chelliah A, Burge MR. Hypoglycemia in elderly patients with diabetes mellitus: causes and strategies for prevention. Drugs Aging 2001;21:511—30.
42.Burkhart KK, Metcalf S, Shurnas E, et al. Exchange transfusion and multidose activated charcoal following vancomycin overdose. Clin Toxicol 1992;30:285-Gerich JE. Oral hypoglycemic agents. N Engl J Med 1989;321:1231—45.4.
43.Humatrope™ (somatropin);package insert. Indianapolis, IN: Eli Lilly and Company; 2003 Jul.
44.GlucaGen® (glucagon) package insert. Princeton, NJ: Novo Nordisk Pharmaceuticals, Inc.; 2003 Aug.
45.Tsiodras S, Mantzoros C, Hammer S, et al. Effects of protease inhibitors on hyperglycemia, hyperlipidemia, and lipodystrophy: a 5-year cohort study. Arch Intern Med 2000;160(13):2050-2056.
46.Seamans KB, Gloor P, Dobell RA, et al. Penicillin-induced seizures during cardiopulmonary bypass: a clinical and electroencephalographic study. N Engl J Med 1968;278(16):861-868.
47.Lovallo W, Wilson MF, Vincent AS, et al: Blood pressure response to caffeine shows incomplete tolerance after short-term regular consumption. Hypertension 2004;43:760-765.
48.Lee AJ, Maddix DS. Trimethoprim/sulfamethoxazole-induced hypoglycemia in a patient with acute renal failure. Ann Pharmacother 1997;31:727—32.
49.Pandit MK, Burke J, Gustafson AB, et al. Drug-induced disorders of glucose tolerance. Ann Intern Med 1993;118:5Gerich JE. Oral hypoglycemic agents. N Engl J Med 1989;321:1231—45.—39.
50.Gerich JE. Oral hypoglycemic agents. N Engl J Med 1989;321:1231—45.
51.Hepsera® (adefovir dipivoxil) package insert. Foster City, CA: Gilead Sciences, Inc.; 2006 Sep.
52.Zantac® tablets and syrup (ranitidine hydrochloride) package insert. Research Triangle Park, NC: GlaxoSmithKline; 2007 Jun.
53.Proloprim® (trimethoprim) package insert. Bristol, TN: Monarch Pharmaceuticals, Inc.; 2000 Jan.
54.Bendayan R. Renal drug transport: A review. Pharmacotherapy 1996;16:971—85.
55.Procanbid® (procainamide) package insert. Bristol, TN: Monarch Pharmaceuticals; 2002 Jan.
56.Quinidex Extentabs® (quinidine sulfate extended-release tablets) package insert. Richmond, VA: A.H. Robbins Company; 2000 Sept.
57.Bonate PL, Reith K, Weir S. Drug interactions at the renal level: Implications for drug development. Clin Pharmacokinet 1998;34:375—404.
58.ProAmatine® (midodrine) package insert. Austria, GmbH: Nycomed; 2003 Oct.
59.Namenda (memantine) package insert. St. Louis, MO: Forest Pharmaceuticals; 2014 Aug.
60.Epivir® (lamivudine) package insert. Research Triangle Park, NJ: GlaxoSmithKline; 2006 Oct.
61.Baraclude™ (entecavir) package insert. Princeton, NJ: Bristol-Myers Squibb Company; 2007 Jul.
62.Somogyi A, Stockley C, Keal J, Rolan P et al. Reduction of metformin renal tubular secretion by cimetidine in man. Br J Clin Pharmacol 1987;23:545—51.
63.Lanoxin (digoxin) package insert. Research Triangle Park, NC: GlaxoSmithKline; 2013 Oct.
64.Tikosyn (dofetilide) package insert. New York, NY: Pfizer Labs; 2011 Feb
65.Manske CL. Hyperglycemia and intensive glycemic control in diabetic patients with chronic renal disease. Am J Kidney Dis 1998;32 (Suppl 3):S157—S171.
66.Cryer PE, Davis SN, Shamoon H. Hypoglycemia in diabetes. Diabetes Care 2003;26:1902—12.
67.Anderson V, Cannon CP, Stone PH, et al, for the TIMI IIIB Investigators. One-year results of the Thrombolysis In Myocardial Infarction (TIMI) IIIB clinical trial: a randomized comparison of tissue-type plasminogen activator versus placebo and early invasi
68.Scheen AJ, Lefebrve PJ. Antihyperglycaemic agents. Drug interactions of clinical importance. Drug Safety 1995;12:32—45.
69.Luna B, Feinglos MN. Drug-induced hyperglycemia. JAMA 2001;286:1945—8.
70.Menzies D, Dorsainvil P, Cunha B, et al. Severe and persistent hypoglycemia due to gatifloxacin interaction with oral hypoglycemic agents. Am J Med 2002;113:232—4.
71.Roberge R, Kaplan R, Frank R, et al. Glyburide-ciprofloxacin interaction with resistant hypoglycemia. Ann Emerg Med 2000;36:160—3.
72.Tequin® (gatifloxacin) package insert. Princeton, NJ: Bristol-Myers Squibb Company; 2006 Jan.
73.Carter BL, Small RE, Mandel MD, et al. Phenytoin-induced hyperglycemia. Am J Hosp Pharm 1981;38:1508-12.
74.Propulsid® (cisapride) package insert. Titusville, NJ; Janssen Pharmaceutica; 2000 Jan. NOTE: As of May 2000; Propulsid® has only been available in the United States via an investigational limited access program to ensure proper patient screening and pres
75.Reglan® (metoclopramide) package insert. Milwaukee, WI: Schwarz Pharma; 2004 Feb.
76.Zelnorm® (tegaserod maleate) package insert. East Hanover, NJ: Novartis Pharmaceuticals Corporation; 2004 April.
77.Lindenmayer JP, Czobor P, Volavka J, et al. Changes in glucose and cholesterol levels in patients with schizophrenia treated with typical or atypical antipsychotics. Am J Psych 2003;160:290—96.
78.Apidra™ (Insulin glulisine) package insert. Kansas City, MO: Aventis Pharmaceuticals, Inc.; 2004 Apr.
79.Hansen JB, Arkhammar PO, Bodvarsdottir TB, et al. Inhibition of insulin secretion as a new drug target in the treatment of metabolic disorders. Curr Med Chem 2004;11:1595—615.
80.Boyanov MA, Boneva Z, Christov VG. Testosterone supplementation in men with type 2 diabetes, visceral obesity, and partial androgen deficiency. Aging Male 2003;6:1—7.
81.Kapoor D, Goodwin E, Channer KS, et al. Testosterone replacement therapy improves insulin resistance, glycaemic control, visceral adiposity, and hypercholesterolaemia in hypogonadal men with type 2 diabetes. Eur J Clin Endocrinol 2006; 154:899—906.
82.Hobbs CJ, Jones RE, Plymate SR. Nandrolone, a 19-nortestosterone, enhances insulin-independent glucose uptake in normal men. J Clin Endocrinol Metab 1996; 81:1582—5.
83.Corrales JJ, Burgo RM, Garcia-Berrocal B, et al. Partial androgen deficiency in aging type 2 diabetic men and its relationship to glycemic control. Metabolism 2004;53:666—72.
84.Lee CH, Kuo SW, Hung YJ, et al. The effect of testosterone supplement on insulin sensitivity, glucose effectiveness, and acute insulin response after glucose load in male type 2 diabetics. Endocrine Res 2005;31:139—148.
85.Cohen JC, Hickman R. Insulin resistance and diminished glucose tolerance in powerlifters ingesting anabolic steroids. J Clin Endocrinol Metab 1987;64:960—3.
86.Chan JC, Cockram CS, Critchley JA. Drug-induced disorders of glucose metabolism. Mechanisms and management. Drug Saf 1996;15:135—57.
87.Greco AV, Mingrone G, Capristo E, et al. Effects of dexfenfluramine on free-fatty acid turnover and oxidation in obese patients with type 2 diabetes mellitus. Metabolism 1995;44(2-suppl 2):57-61.
88.Turtle, J.R. and Burgess, J.A. Hypoglycemic effect of fenfluramine in diabetes mellitus. Diabetes 1973; 22:858.
89.Sheela CG, Kumud K, Augusti KT. Anti-diabetic effects of onion and garlic sulfoxide amino acids in rats. Planta Med 1995;61:356—7.
90.Ryan EA, Pick ME, Marceau C. Use of alternative medicines in diabetes mellitus. Diabet Med 2001;18:242—5.
91.Bordia A, Verma SK, Srivastava KC. Effect of garlic (Allium sativum) on blood lipids, blood sugar, fibrinogen and fibrinolytic activity in patients with coronary artery disease. Prostaglandins Leukot Essent Fatty Acids 1998;58:257—63.
92.Castell D. Nephrogenic diabetes insipidus due to demethychlortetracycline hydrochloride. JAMA 1965;193(3):237-239.
93.Myers M: Effects of caffeine on blood pressure. Arch Intern Med 1988;148:1189.
94.Levothroid (levothyroxine sodium tablet) package insert. Shenandoah, IA: Lloyd Pharmaceutical; 2011 June.
95.Norpace (disopyramide) package insert. Chicago, IL: GD Searle LLC; 2006 Sept.
96.Wood JD, Peesker SJ. The effect on GABA metabolism in brain of isonicotinic acid hydrazide and pyridoxine as a function of time after administration. J Neurochem 1972;19(6):527-537.
97.Somavert® (pegvisomant) package insert. Kalamazoo, MI: Pharmacia and Upjohn Company; 2003 Jun.
98.Kazano (alogliptin;metformin) package insert. Deerfield, IL: Takeda Pharmaceuticals America, Inc.; 2013 Jan.
99.Acetazolamide package insert. Danbury, CT: Danbury Pharmaceutical; 1998 April.
100.Anderson RA, Cheng N, Bryden NA, et al. Elevated intakes of supplemental chromium improve glucose and insulin variables in individuals with type 2 diabetes. Diabetes 1997;46:1786—91.
101.Ravina A, Slezak L, Mirsky N, et al. Reversal of corticosteroid induced diabetes mellitus with supplemental chromium. Diabet Med 1999;16:164—7.
102.Baclofen package insert. Corona, CA: Watson Laboratories, Inc.; 2004 Jan.
103.Pentam 300 (pentamidine isethionate) injection package insert. Schaumburg, IL: APP Pharmaceuticals, LLC; 2008 Mar.
104.Sandostatin® (octreotide) package insert. East Hanover, NJ: Novartis Pharmaceuticals Corporation; 2005 Dec.
105.Hollander PA, Elbein SC, Hirsch IB, et al. Role of orlistat in the treatment of obese patients with type 2 diabetes. A 1-year randomized double-blind study. Diabetes Care 1998;21:1288—94.
106.Marathe PH, Wen Y, Norton J, et al. Effect of altered gastric emptying and gastrointestinal motility on metformin absorption. Br J Clin Pharmacol 2000;50:325—32.
107.Velcade® (bortezomib) package insert. Cambridge, MA: Millennium Pharmaceuticals, Inc.; 2008 Jun.Velcade® (bortezomib) package insert. Cambridge, MA: Millennium Pharmaceuticals, Inc.; 2008 Jun.
108.Yoshikawa M, Murakami T, Matsuda H, et al. Bioactive saponins and glycosides. III. Horse chestnut. (1): The structures, inhibitory effects on ethanol absorption, and hypoglycemic activity of escins Ia, Ib, IIa, IIb, and IIIa from the seeds of Aesculus hip
109.Keflex® (cephalexin) package insert. Indianapolis, IN: Dista Products Company; 2004 Jan.
110.Jayasagar G, Krishna Kumar M, Chandrasekhar K, et al. Effect of cephalexin on the pharmacokinetics of metformin in healthy human volunteers. Drug Metabol Drug Interact 2002;19:41—8.
111.Shimizu M, Kobayashi Y, Suzuki M, et al. Regulation of intestinal glucose transport by tea catechins. Biofactors 2000;13:61—5.
112.Sabu MC, Smitha K, Ramadassan K. Anti-diabetic activity of green tea polyphenols and their role in reducing oxidative stress in experimental diabetes. J Ethnopharmacol 2002;83:109—16.
113.Madsbad S, McNair P, Christensen MS, et al. Influence of smoking on insulin requirement and metbolic status in diabetes mellitus. Diabetes Care 1980;3:41—3.
114.IPLEX™ (mecasermin rinfabate) package insert. Glen Allen, VA: Insmed Incorporated; 2005 Dec.
115.Ranke MB. Insulin-like growth factor-1 treatment of growth disorders, diabetes mellitus, and insulin resistance. Trends Endocrinol Metab 2005;16:190—7.
116.Mohamed-Ali V, Pickney J. Therapeutic potential of insulin-like growth factor-1 in patients with diabetes mellitus. Treat Endocrinol 2002;1:399—410.
117.Deplin (L-methylfolate) package insert. Merck KGaA: Covington, LA; 09 Apr.
118.Trokendi XR (topiramate extended-release capsules) package insert. Rockville, MD: Supernus Pharmaceuticals; 2013 Aug.
119.Topamax® (topiramate) package insert. Raritan, NJ: Ortho-McNeil Pharmaceutical, Inc.; 2005 June.
120.Ranexa (ranolazine extended-release tablets) package insert. Foster City, CA: Gilead Sciences, Inc. 2013 Dec.
121.Bolen S, Feldman L, Vassy J, et al. Systematic review: comparative effectiveness and safety of oral medications for type 2 diabetes mellitus. Ann Intern Med 2007;147:386–99.

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