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Is Metformin A Biguanide?

Metformin: A New Oral Biguanide

Metformin: A New Oral Biguanide

Volume 18, Issue 3 , MayJune 1996, Pages 360-371 Get rights and content The biguanide metformin is an oral anti-hyperglycemic agent used in the treatment of patients with noninsulin-dependent diabetes mellitus (NIDDM). Metformin is an important addition to the drug therapy options available for these patients because it reduces blood glucose levels predominantly by decreasing hepatic glucose production and release and also by increasing peripheral tissue sensitivity to insulin; it does not stimulate insulin secretion from the beta cells in the pancreas. Metformin also has a potentially beneficial effect by reducing serum lipid levels. Its glycemic control is similar to that of the sulfonylureas and is effective as monotherapy or in combination with sulfonylureas or insulin. Unlike sulfonylureas and insulin, it does not cause a gain in body weight, and when used as monotherapy, it does not cause hypoglycemia. The most common side effects associated with metformin are mild, transient, gastrointestinal symptoms, which are usually self-limiting. These side effects can be minimized by initiating metformin therapy at a low dose and gradually titrating upward, and by taking metformin with meals. Lactic acidosis caused by metformin is rare, and the risk of this complication may be diminished by the observance of prescribing precautions and contraindications that avoid accumulation of metformin or lactate in the body. In patients who are not getting the desired effect with sulfonylureas, it is useful to combine sulfonylureas with metformin therapy. Metformin should be considered a first-line agent, particularly in obese and/or hyperlipidemic NIDDM patients. Continue reading >>

Biguanide | Definition Of Biguanide By Medical Dictionary

Biguanide | Definition Of Biguanide By Medical Dictionary

Biguanide | definition of biguanide by Medical dictionary A member of the class of oral antihyperglycemic agents that works by limiting glucose production and glucose absorption, and by increasing the body's sensitivity to insulin. Glucophage is one member of this drug class. Want to thank TFD for its existence? Tell a friend about us , add a link to this page, or visit the webmaster's page for free fun content . Biguanides also decrease hepatic metabolism of lactate and have a negative ionotropic effect on the heart, both of which elevate lactate levels (11). Continuous venovenous haemodiafiltration for metformin-induced lactic acidosis Metformin is a biguanide that is currently approved for treatment of type 2 diabetes. Metformin-associated lactic acidosis in a patient with vertebral artery dissection The two companies expect approval for combination therapy of FASTCI/STARSIS with biguanide agents. Ajinomoto, Astellas Pharma Jointly File Application Seeking Additional Approval for Combination Therapy of FASTIC/STARSIS Tablets, Fast-acting Postprandial Hypoglycemic Agent, with Biguanide What is our justification for instructing people managed with diet alone and/or biguanide (metformin) therapy, with adequate glycaemic control to keep testing regularly, and what is the evidence for this? Continue reading >>

Biguanides

Biguanides

As a class of medication used to treat type 2 diabetes, biguanides lower blood sugar in two ways. Their primary action is to reduce the amount of sugar produced by the liver. In addition, they can also increase the amount of sugar absorbed by muscle cells and decrease insulin resistance. According to the federal Agency for Healthcare Research and Quality (AHRQ), biguanides can lower A1c levels by one point and may also decrease levels of bad cholesterol more than other diabetes medications. Who should use biguanides? Individuals who are unable to control their blood glucose levels with diet or exercise alone may be prescribed a biguanide medication. Drugs in this class may be taken alone or combined with another medication such as a sulfonylurea. In addition, biguanides may be used to improve the effectiveness of insulin therapy. Biguanides have been shown to be effective in treating children and adolescents diagnosed with type 2 diabetes. In some cases, biguanides may be used to treat pre-diabetes. This class of medications is not recommended for those with very low insulin levels as well as those with serious medical conditions such as kidney, lung or liver disease. Those preparing for major surgery also should not take a biguanide. Medications in the biguanide class Metformin is the only biguanide medication currently available. As an individual medication, it sold under several brand names, including the following: Glucophage and Glucophage XR Riomet Fortamet There are also several combination medications available that include both metformin and another medicine. These include the following brand name drugs: Metaglip (glipizide and metformin) Glucovance (glyburide and metformin) Prandimet (repaglinide and metformin) Avandamet (rosiglitazone and metformin) Common bi Continue reading >>

Biguanides - Prices And Information - Goodrx

Biguanides - Prices And Information - Goodrx

Lifted Restrictions Mean More Diabetics Can Use Metformin! Metformin ( Glucophage ) is first line therapy for diabetes which carries the benefit of helping with weight loss. Its cheap, does not result in risky low blood sugars (hypoglycemia), has a cheap genericoh AND it may help you live longer. See More 8 Weeks on a Strict Diet May Get Rid of Diabetes When you arediagnosed with type 2 diabetes (also known as adult-onset diabetes), youre advised to accept it asa lifelong disease that may require oral medications andfor 50% of people with type 2 diabetesinsulin within 10 years. See More Diabetesspecifically type 2 or adult onset diabetesis a growing epidemic in the United States, in part to the increase inobesity over thepast 10 years. However, there are several medications that (with healthy diet and excercise) can help keep your blood sugar under control. See More Is Metformin the Key to Preventing Aging? Metformin is an inexpensive generic drug widely used for type 2 diabetes in the U.S. Although it onlycosts pennies, it is now featured on the World Health Organizations list of essential medications. Now, metformin (the brand is Glucophage ) is also being studied for cancer and aging prevention. See More Continue reading >>

What Are Biguanides For Diabetes? Metformin For Diabetes

What Are Biguanides For Diabetes? Metformin For Diabetes

They could come back if your doctor raises your dose. Taking metformin with food can help. While doctors used to avoid prescribing this drug to people who've had kidney trouble, it may be OK for someone with mild or moderate kidney disease . When you use metformin for a long time, it could lower the amount of vitamin B-12 in your body too much. Your doctor may want to check your B-12 level, especially if you have anemia or nerve damage in your feet or hands ( peripheral neuropathy ). One large study has linked long-term metformin use to higher chances of getting Alzheimer's dementia and Parkinson's disease . But we need more research to understand the connection better and what it means. Some people who take metformin can get a lactic acid buildup in their blood. It's rare and more likely to happen if you: Continue reading >>

Biguanides Class Drugs - Suitability, Benefits & Side Effects

Biguanides Class Drugs - Suitability, Benefits & Side Effects

Biguanides prevent the production of glucose in the liver The term biguanide refers to a group of oral type 2 diabetes drugs that work by preventing the production of glucose in the liver , improving the bodys sensitivity towards insulin and reducing the amount of sugar absorbed by the intestines. The only available biguanide medication is metformin, which is commonly used as a first-line treatment for type 2 diabetes (i.e. the first option for type 2 diabetics who are unable to control their blood sugars through diet and exercise alone). Metformin is usually prescribed as a single treatment (monotherpay), but it can also be combined with other medication in a single tablet - for example, metformin + pioglitazone (Competact), metformin + vildagliptin (Eucreas) and metformin + sitagliptin (Janumet). Its also sometimes prescribed in combination with insulin for people with type 1 diabetes. As already mentioned, metformin is the only biguanide available on the market. However, there are two different versions of the drug; Metformin IR (immediate release) - taken up to three times a day Metformin SR (slow release) - usually taken once per day Metformin IR is sold under the brand name Glucophage, while the trade name for metformin PR is Glucophage SR. Biguanides work by preventing the liver from converting fats and amino-acids into glucose. They also activate an enzyme (AMPK) which helps cells to respond more effectively to insulin and take in glucose from the blood. Metformin is generally suitable for most people with type 2 diabetes as a first line of medication if lifestyle changes have no sufficiently lowered blood glucose levels. Metformin can be taken on its own, as a monotherapy, or in addition to other oral or injectable diabetes medications. It may also be prescrib Continue reading >>

Is Metformin A Perfect Drug? Updates In Pharmacokinetics And Pharmacodynamics

Is Metformin A Perfect Drug? Updates In Pharmacokinetics And Pharmacodynamics

Is Metformin a Perfect Drug? Updates in Pharmacokinetics and Pharmacodynamics Author(s): Magdalena Markowicz-Piasecka* , Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul Muszyskiego 1, 90-151 Lodz, Poland Kristiina M. Huttunen , School Of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Yliopistonranta 1C, POB 1627, 70211 Kuopio, Finland Lukasz Mateusiak , Students Research Group, Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul Muszyskiego 1, 90-151 Lodz, Poland Elzbieta Mikiciuk-Olasik , Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul Muszyskiego 1, 90-151 Lodz, Poland Joanna Sikora . Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul Muszyskiego 1, 90-151 Lodz, Poland Journal Name: Current Pharmaceutical Design Metformin, a synthetic biguanide, is currently one of the most frequently recommended medicationsfor type 2 diabetes treatment around the world. This review presents the latest discoveries in the pharmacokineticsof metformin, especially the role of transporters (e.g. Organic Cation Transporters OCTs, Multidrug and ToxinExtrusion transporters MATE) in oral absorption, distribution, elimination and biochemical effects of metforminin humans. We also review the associations between genetic variations of metformin transporters, their pharmacokineticsand drug efficacy or drug responses. In the second part of this paper, we highlight the current knowledge on novel metformin actions including favourableeffects on lipid profile (e.g. decreasing plasma tr Continue reading >>

Metformin Hydrochloride Extended Release

Metformin Hydrochloride Extended Release

About this medication Metformin Hydrochloride Extended Release is the name of the medication. It comes in the form of a tablet, and should be taken by mouth. It belongs to a class of medications called Biguanide. Why is this medication prescribed This medication is used to treat type-2 diabetes and pre-diabetes conditions. Normally, when you eat food, the body breaks down all of the sugars and starches into a sugar called glucose. This is the basic fuel for the cells in the body. The body needs Insulin to be able to use this sugar for energy. Insulin takes the sugar from the blood into the cells. In type 2 diabetes, either the body does not produce enough insulin or the cells ignore the insulin. This causes glucose to build up in the blood instead of going into cells. It can lead to serious diabetes complications. How does it work Metformin Hydrochloride belongs to a group of medications called Biguanides. They work by decreasing the amount of sugar produced by the liver and increasing the amount of sugar absorbed by muscle cells. As a result you get more sugar in the cells and less is in the blood. How to use it This medication comes as a tablet. You should put it in your mouth and swallow it with a glass of water. Do not chew, break or crush it. Swallow it whole. What to do if you are pregnant Tell your physician if you become pregnant. There are not enough studies about this medication in pregnant women. Use the medication during pregnancy only if clearly needed. Continue reading >>

Re-evaluation Of A Biguanide, Metformin: Mechanism Of Action And Tolerability.

Re-evaluation Of A Biguanide, Metformin: Mechanism Of Action And Tolerability.

Re-evaluation of a biguanide, metformin: mechanism of action and tolerability. Centre E. Grossi Paoletti, University of Milano. Pharmacol Res. 1994 Oct-Nov;30(3):187-228. Metformin is a biguanide antidiabetic medication, that has been in use for over 30 years. Its mechanism of action, unknown until a few years ago, is now linked to an improved peripheral sensitivity to insulin, through a stimulated tissue glucose uptake by a transporter linked system. Interest in metformin has been revived by the recent observation of a specific activity of this agent on some of the major traits of the so called 'polymetabolic syndrome' (or 'syndrome X'), characterized by: insulin resistance, hypertriglyceridemia, hypertension and reduced fibrinolytic activity. Metformin, in studies examining one or more of these, has been shown, possibly through its peripheral insulin sensitizing mechanism, to correct most of the major symptoms characterizing this insulin resistance syndrome. Metformin, similarly to the other biguanide phenformin, has been rated as potentially dangerous, because of the possible induction of lactic acidosis, in some cases with a fatal outcome. Metformin is, however, associated with a very low incidence of lactic acidosis because, differently from phenformin, it does not undergo liver metabolism and, as a consequence, there are no high-risk groups, displaying an impaired metabolic handling. In this review, in addition to an overall evaluation of the more recent data on the mechanism of action and clinical use of metformin, a detailed clinical analysis of all published cases of lactic acidosis is provided. These data indicate that the risk in metformin use is negligible, provided that care is taken when prescribing the drug to patients with suspected clinical risks of la Continue reading >>

History Of The Biguanides

History Of The Biguanides

The medicinal properties of the French Lilac, Galega Officinalis, also known as Goat's Rue, were already known in medieval Europe, when it was observed to reduce the diuresis associated with diabetes. Research on derivatives of guanidine, its main active principle, began in the early part of the twentieth century, but the discovery of insulin and the gastro-intestinal side effects and hepatotoxicity of these agents delayed further development until the 1950s when the biguanides phenformin, buformin and metformin were introduced into clinical use. By 1978 increasing reports of lactic acidosis associated with the use of phenformin led to the withdrawal of phenformin and buformin from the market. Metformin did not become available in the USA until 1995, but was widely used elsewhere, and became increasingly popular when UKPDS showed it to reduce macrovascular morbidity and mortality. Since then many studies have demonstrated its excellent clinical utility which currently makes it the first-line drug of choice for the treatment of type 2 diabetes. The actions of metformin are still somewhat obscure, and its apparent benefits in cardiovascular disease and cancer have prompted further investigation of this fascinating drug. Galega officinalis (as the term "officinalis" implies) was recognised as a medicinal herb in the middle ages, and used to treat a variety of illnesses. It was claimed to alleviate the diuresis associated with diabetes, and is still listed as a treatment for this condition in modern herbal pharmacopoeias[1]. It contains large amounts of guanidine which has toxic side effects when eaten by cattle; the plant is classed as a noxious weed in 35 US states. Guanidine was shown to have glucose lowering effects in 1918, and two synthetic diguanides known as Synthal Continue reading >>

Mechanism Of Metformin: A Tale Of Two Sites

Mechanism Of Metformin: A Tale Of Two Sites

Metformin (dimethylbiguanide) features as a current first-line pharmacological treatment for type 2 diabetes (T2D) in almost all guidelines and recommendations worldwide. It has been known that the antihyperglycemic effect of metformin is mainly due to the inhibition of hepatic glucose output, and therefore, the liver is presumably the primary site of metformin function. However, in this issue of Diabetes Care, Fineman and colleagues (1) demonstrate surprising results from their clinical trials that suggest the primary effect of metformin resides in the human gut. Metformin is an orally administered drug used for lowering blood glucose concentrations in patients with T2D, particularly in those overweight and obese as well as those with normal renal function. Pharmacologically, metformin belongs to the biguanide class of antidiabetes drugs. The history of biguanides can be traced from the use of Galega officinalis (commonly known as galega) for treating diabetes in medieval Europe (2). Guanidine, the active component of galega, is the parent compound used to synthesize the biguanides. Among three main biguanides introduced for diabetes therapy in late 1950s, metformin (Fig. 1A) has a superior safety profile and is well tolerated. The other two biguanides, phenformin and buformin, were withdrawn in the early 1970s due to the risk of lactic acidosis and increased cardiac mortality. The incidence of lactic acidosis with metformin at therapeutic doses is rare (less than three cases per 100,000 patient-years) and is not greater than with nonmetformin therapies (3). Major clinical advantages of metformin include specific reduction of hepatic glucose output, with subsequent improvement of peripheral insulin sensitivity, and remarkable cardiovascular safety, but without increasi Continue reading >>

Biguanide - Wikipedia

Biguanide - Wikipedia

Except where otherwise noted, data are given for materials in their standard state (at 25C [77F], 100kPa). Biguanide ( /bawnad/ ) is the organic compound with the formula HN(C(NH)NH2)2. It is a colorless solid that dissolves in water to give highly basic solution. These solutions slowly hydrolyse to ammonia and urea. [1] The term "biguanidine" often refers specifically to a class of drugs that function as oral antihyperglycemic drugs used for diabetes mellitus or prediabetes treatment. [2] Metformin - widely used in treatment of diabetes mellitus type 2 Phenformin - withdrawn from the market in most countries due to toxic effects Buformin - withdrawn from the market due to toxic effects Buformin . A butyl derivative of biguanidine. Phenformin . A phenethylated biguanidine. Galega officinalis (French lilac) was used in diabetes treatment for centuries. [3] In the 1920s, guanidine compounds were discovered in Galega extracts. Animal studies showed that these compounds lowered blood glucose levels. Some less toxic derivatives, synthalin A and synthalin B, were used for diabetes treatment, but after the discovery of insulin , their use declined. Biguanides were reintroduced into Type 2 diabetes treatment in the late 1950s. Initially phenformin was widely used, but its potential for sometimes fatal lactic acidosis resulted in its withdrawal from most pharmacopeias (in the U.S. in 1978). [4] Metformin has a much better safety profile, and it is the principal biguanide drug used in pharmacotherapy worldwide. Biguanides do not affect the output of insulin, unlike other hypoglycemic agents such as sulfonylureas and meglitinides . Therefore, they are effective in Type 2 diabetics; and in Type 1 diabetes when used in conjunction with insulin therapy. The mechanism of action of bi Continue reading >>

Metformin: Historical Overview

Metformin: Historical Overview

, Volume 60, Issue9 , pp 15661576 | Cite as Metformin (dimethylbiguanide) has become the preferred first-line oral blood glucose-lowering agent to manage type 2 diabetes. Its history is linked to Galega officinalis (also known as goats rue), a traditional herbal medicine in Europe, found to be rich in guanidine, which, in 1918, was shown to lower blood glucose. Guanidine derivatives, including metformin, were synthesised and some (not metformin) were used to treat diabetes in the 1920s and 1930s but were discontinued due to toxicity and the increased availability of insulin. Metformin was rediscovered in the search for antimalarial agents in the 1940s and, during clinical tests, proved useful to treat influenza when it sometimes lowered blood glucose. This property was pursued by the French physician Jean Sterne, who first reported the use of metformin to treat diabetes in 1957. However, metformin received limited attention as it was less potent than other glucose-lowering biguanides (phenformin and buformin), which were generally discontinued in the late 1970s due to high risk of lactic acidosis. Metformins future was precarious, its reputation tarnished by association with other biguanides despite evident differences. The ability of metformin to counter insulin resistance and address adult-onset hyperglycaemia without weight gain or increased risk of hypoglycaemia gradually gathered credence in Europe, and after intensive scrutiny metformin was introduced into the USA in 1995. Long-term cardiovascular benefits of metformin were identified by the UK Prospective Diabetes Study (UKPDS) in 1998, providing a new rationale to adopt metformin as initial therapy to manage hyperglycaemia in type 2 diabetes. Sixty years after its introduction in diabetes treatment, metformin h Continue reading >>

The Origins Of Metformin

The Origins Of Metformin

Goat's rue, French lilac, Italian fitch, and professor weed are all names for the same plant: Galega officinalis. This perennial herb, 3 feet tall and with purple, blue, or white flowers, was used in folk medicine to treat diabetes starting in the Middle Ages, maybe earlier. Though it gave rise to metformin, one of the most popular diabetes medications in the world, G. officinalis is now widely considered poisonous. In the early 20th century, researchers isolated a compound from G. officinalis called guanidine, which could lower blood glucose levels in animals but was also toxic. Chemists found that they could make the compound more tolerable by bonding two guanidines together, forming a biguanide. Metformin is one such biguanide, first synthesized in 1929 and then clinically developed in the late 1950s by the French physician Jean Sterne, who gave it its first trade name, Glucophage ("glucose eater"). Two other biguanides—phenformin and buformin—were also produced around this time but later withdrawn because they became associated with lactic acidosis. This condition results from a buildup of lactic acid in the blood, lowering its pH to unhealthy levels. It can be particularly dangerous for people with diabetes. Metformin seemed guilty by association, and the damage done to its reputation meant that metformin took time to catch on, even though it was later shown to trigger lactic acidosis only in rare cases. Over the next few decades, studies about metformin's safety and efficacy trickled in, but it wasn't until the landmark United Kingdom Prospective Diabetes Study (1977 to 1997) that metformin gained the renown that it enjoys today. In the study, overweight and obese people with type 2 diabetes on metformin lived longer and had fewer heart attacks than those wit Continue reading >>

Biguanides - Type2diabetes.com

Biguanides - Type2diabetes.com

Join the conversation. register now or log in Biguanides is a class of prescription medication used for the treatment of type 2 diabetes. The pancreas produces insulin, a hormone, that transfers glucose (sugar) found in the bloodstream into cells in order to provide fuel. Glucose in the bloodstream comes from the food and drinks you consume. In people with type 2 diabetes, the body either does not produce sufficient quantity of insulin, or the insulin that is produced does not work as it should to transport glucose from the bloodstream to the cells. The only biguanide to treat type 2 diabetes is metformin which is sold under several brand names, namely: Glucophage, Glucophage XR, Fortamet, Glumetza and Riomet. Metformin , a type of biguanide, is an oral medication that is available in the form of an immediate release tablet, an extended release tablet and a solution. Metformin lowers blood glucose levels mainly by decreasing the amount of glucose produced by theliver. In addition, it increases the quantity of glucose absorbed by muscle cells and in doing so, decreases insulin resistance. According to the AACE guidelines, metformin is usually the first line therapy prescribed for people with type 2 diabetes, along with diet and exercise , to obtain blood glucose control. It is also used in combination therapy with other oral antidiabetic agents or insulin in those patients that need additional treatment to achieve blood glucose control. Metformin should be taken exactly as prescribed by your doctor. It should not be taken by patients whose kidneys dont work properly since its usage can increase the risk of developing a potentially deadly condition called lactic acidosis, where excessive lactic acid builds up in the bloodstream. Patients should get kidney function tests Continue reading >>

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