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Metformin Gi Side Effects Mechanism

How To Prevent And Manage Metformin Side Effects

How To Prevent And Manage Metformin Side Effects

Metformin is the oral drug of choice for type 2 diabetics who do not respond well to diet and lifestyle changes alone unless contraindicated due to kidney problems. It has a long safety record. Scientific research has proven that metformin is just as good or even better at controlling blood sugar levels than other oral antidiabetic drugs and it causes less weight gain, less low blood sugar, and less cardiovascular events. Metformin is sold under the brand names Glucophage, Glucophage XR, Riomet, Fortamet and is also found in other combination diabetes medications. Metformin comes in the immediate release and extended release formulations. The immediate release formulation releases the medication all at once while the extended release formulations release medication over time. The extended release formulation has fewer gastrointestinal (GI) side effects, increases adherence to medications due to its once daily dosing, and has proven to be safer, more effective, and better tolerated than the Immediate release formulation. Some of the side effects to expect from metformin include: diarrhea nausea vomiting abdominal pain the passing of gas loss of appetite Some patients may experience other side effects such as: change in taste sensation weight loss indigestion heartburn stomach upset abnormal stool headache rhinitis infection discoloration of the nails hives (rash) itching plaques (scalp, elbows, and knees) low blood sugar (hypoglycemia) Serious side effects may occur in some patients under certain circumstances. These serious side effects are rare and include: chest pain lactic acidosis vitamin B12 deficiency hepatitis Continue Prevention and Treatment of Metformin Side Effects Gastrointestinal Discomfort Gastrointestinal discomfort includes abdominal pain, flatus (gas), Continue reading >>

Metformin

Metformin

Metformin, marketed under the trade name Glucophage among others, is the first-line medication for the treatment of type 2 diabetes,[4][5] particularly in people who are overweight.[6] It is also used in the treatment of polycystic ovary syndrome.[4] Limited evidence suggests metformin may prevent the cardiovascular disease and cancer complications of diabetes.[7][8] It is not associated with weight gain.[8] It is taken by mouth.[4] Metformin is generally well tolerated.[9] Common side effects include diarrhea, nausea and abdominal pain.[4] It has a low risk of causing low blood sugar.[4] High blood lactic acid level is a concern if the medication is prescribed inappropriately and in overly large doses.[10] It should not be used in those with significant liver disease or kidney problems.[4] While no clear harm comes from use during pregnancy, insulin is generally preferred for gestational diabetes.[4][11] Metformin is in the biguanide class.[4] It works by decreasing glucose production by the liver and increasing the insulin sensitivity of body tissues.[4] Metformin was discovered in 1922.[12] French physician Jean Sterne began study in humans in the 1950s.[12] It was introduced as a medication in France in 1957 and the United States in 1995.[4][13] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[14] Metformin is believed to be the most widely used medication for diabetes which is taken by mouth.[12] It is available as a generic medication.[4] The wholesale price in the developed world is between 0.21 and 5.55 USD per month as of 2014.[15] In the United States, it costs 5 to 25 USD per month.[4] Medical uses[edit] Metformin is primarily used for type 2 diabetes, but is increasingly be Continue reading >>

Does Anyone In The Rg Community Know The Mechanism Of Diarrhea Caused By Metformin?

Does Anyone In The Rg Community Know The Mechanism Of Diarrhea Caused By Metformin?

So, apparently Metformin induced diarrhea has a complex but at the same time simple mechanism. It resembles, on a small scale, what we gastroenterologists know as "after bypass surgery dumping syndrome", in which you have a simultaneous osmotic/hipermotility condition. Would it be too much to ask you to provide me w/a reference list in which I could read up on this topic as much as possible? It would be greatly appreciated. As a researcher and clinical gastroenterologist I work w/Metmorfin tolerability, especially diarhrea, that is present between 5-10% of the cases in patients beginning Metformin treatment or in those who are increasing their daily dose. There are also some susceptible ethnic populations such as the mestizo group, which are highly prevalent in most Latin American countries, (Mexico, CA and Pacific Andean Region) who are relatively intolerant to Metformin. As clinicians we usually deal w/this problem by progressively escalating the dose on a weekly basis and in more severe cases by adding on loperamide/psyllum as rescue medication. Now, in order to provide a better and tolerable metformin, first we need to understand what we are dealing with, and second, to work on a different improved delivery system such as NERF "novel extended release fotrmulations" and/or drug combinations. Continue reading >>

Gastritis Tied To Metformin-related Gastrointestinal Side Effects In Type 2 Diabetes

Gastritis Tied To Metformin-related Gastrointestinal Side Effects In Type 2 Diabetes

Gastritis tied to metformin-related gastrointestinal side effects in type 2 diabetes Gastritis tied to metformin-related gastrointestinal side effects in type 2 diabetes Gastritis tied to metformin-related gastrointestinal side effects in T2D HealthDay News For patients with type 2 diabetes , asymptomatic gastritis is associated with metformin-related gastrointestinal side effects, according to a study published in the Journal of Clinical Pharmacy and Therapeutics. Digestive disorders represent the most common metformin side effects for type 2 diabetes. The mechanism of these metformin side effects is unclear, noted Yuxin Huang, M.D., from the Shanghai Huadong Hospital affiliated to Fudan University, and colleagues. To examine whether asymptomatic chronic gastritis could influence metformin tolerance with patients with type 2 diabetes, the investigators culled data from 144 metformin-naive patients. All subjects started metformin at 500 mg/day and increased progressively to 1,500 mg/day over four weeks. Each week a score of gastrointestinal side effects was assessed, and metformin dose was adjusted as appropriate. Of the patients, 64 were categorized as non-gastritis subjects and 80 as chronic gastritis subjects based on endoscopy. No statistical difference was seen between the groups for gastrointestinal symptoms at baseline. With metformin, the mean scores for abdominal pain, nausea, vomiting, and bloating were 1.02 versus 2.18 (P=0.001), 0.20 versus 0.50 (P=0.022), 0 versus 0.06 (P=0.024), and 1.08 versus 1.71 (P=0.028), respectively, for non-gastritis versus gastritis subjects, over four weeks. The mean final metformin doses were 706.24 and 1,101.56 mg for gastritis and non-gastritis subjects, respectively (P=0.001). "Our data show for the first time that asymptoma Continue reading >>

Ondansetron And Metformin-induced Gastrointestinal Side Effects.

Ondansetron And Metformin-induced Gastrointestinal Side Effects.

Abstract Treatment with metformin is associated with a high incidence of gastrointestinal side effects of unknown mechanism. Metformin is a biguanide derivative, which resembles 5-HT3-receptor agonists in its structure. Activation of 5-HT3 receptors is known to induce nausea, vomiting, and diarrhea. In this study, we investigated if the gastrointestinal side effects produced by metformin were antagonized by ondansetron, a selective antagonist of 5-HT3 receptors. Patients experiencing gastrointestinal side effects were randomized to ondansetron (4 mg bid p.o.) or placebo while maintained on metformin (double-blind, parallel-group design). If side effects persisted or worsened, metformin was discontinued and the patient considered a therapeutic failure. Of the 98 subjects treated with metformin, 22 developed side effects to match the study entry criteria. Diarrhea was the most frequent side effect. Subjects were randomized to ondansetron (10/2 F/M, 42.8 +/- 2.3 years, 28.6 +/- 1.1 kg/m2, 2585 +/- 35 mg/d metformin) or placebo (9/1 F/M, 43 +/- 4.3 years, 29.7 +/- 1.8 kg/m2, 2715 +/- 71 mg/d metformin). Ondansetron showed no efficacy against metformin-induced side effects. A comparable number of therapeutic failures were observed in ondansetron (8/12; 66%) and placebo-treated subjects (5/10; 50%) (P<0.1). Mean nausea scores (numeric analog scale) before and during treatment with ondansetron were 6.3 +/- 1 and 6.9 +/- 1 cm, respectively. Nausea scores averaged 7.3 +/- 1.5 and 5.9 +/- 1.5 cm, before and during treatment with placebo (P>0.1). In conclusion, 5-HT3 receptors do not seem to play a role in metformin-induced gastrointestinal side effects. Continue reading >>

Metformin Side Effects

Metformin Side Effects

For the Consumer Applies to metformin: oral solution, oral tablet, oral tablet extended release Along with its needed effects, metformin may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention. Check with your doctor immediately if any of the following side effects occur while taking metformin: More common Abdominal or stomach discomfort cough or hoarseness decreased appetite diarrhea fast or shallow breathing fever or chills general feeling of discomfort lower back or side pain muscle pain or cramping painful or difficult urination sleepiness Less common Anxiety blurred vision chest discomfort cold sweats coma confusion cool, pale skin depression difficult or labored breathing dizziness fast, irregular, pounding, or racing heartbeat or pulse feeling of warmth headache increased hunger increased sweating nausea nervousness nightmares redness of the face, neck, arms, and occasionally, upper chest seizures shakiness shortness of breath slurred speech tightness in the chest unusual tiredness or weakness Rare Behavior change similar to being drunk difficulty with concentrating drowsiness lack or loss of strength restless sleep unusual sleepiness Some side effects of metformin may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them: More common Acid or sour stomach belching bloated excess air or gas in the stomach or intestines full feeling heartburn indiges Continue reading >>

How To Ease The Diarrhea Effects Of Metformin

How To Ease The Diarrhea Effects Of Metformin

Metformin is the most effective drug used to treat conditions such as polycystic ovarian syndrome and insulin resistance. It is also used to prevent and treat type 2 diabetes. Metformin works by regulating blood-sugar levels. Because of that, it promotes weight loss and can improve fertility. As with most prescription medications, metformin can have problematic side effects. But there is a marked decrease in side effects after the first month of taking metformin. The most common side effect of taking metformin is diarrhea. Instructions Reduce your dose, with the approval of a health-care professional. While diarrhea is most common in the initial weeks of taking metformin, reducing the dose may reduce the frequency, as it allows the body to adjust to the medication. The lowest dosage given is generally 500 mg. If you have started at a higher dose, the doctor may reduce the dosage to lessen side effects. Consider switching to the extended-release version of metformin. Talk to your health-care provider about doing so. As it is a slow-release medication, it may reduce diarrhea, because smaller amounts are absorbed over the day rather than hitting your system all at once. Keep in mind that the extended-release version is more expensive. Reduce consumption of carbohydrates and fat. People who follow a reduced–carbohydrate diet experience less diarrhea than those that do not. A diet that is rich in low-fat protein and low in carbohydrates, fats and sugar is optimal. Take metformin with a meal. It should never be taken on an empty stomach. When metformin is taken on an empty stomach, it reacts with stomach acid and can cause an increase in diarrhea and other gastrointestinal issues. Use over-the-counter medications to treat diarrhea. One such medication is Imodium. The relief Continue reading >>

New Findings About What Metformin Really Does

New Findings About What Metformin Really Does

As many of my readers know, there is no requirement that the companies that sell pharmaceutical drugs provide an accurate explanation of what it is that their drugs do or of how they do it. All that they have to prove is that the drug has an impact on some measurable phenomenon. The company may claim that a drug functions using a mechanism that is later proven to be untrue. This has been the case with the SSRI drugs which it turned out actually work by remodelling the nerves in the hippocampus, NOT by changing levels of serotonin. Metformin, which has been used for decades, is another drug whose effect is well understood--it lowers blood sugar and reduces the amount of insulin needed to lower blood sugar. This has been interpreted to mean that it lowers insulin resistance. But new findings are calling this into question, as we discover that metformin may actually be stimulating insulin release or blocking the liver's release of glucose rather than impacting insulin resistant cell receptors. The first finding is one I stumbled over recently, one which seems to have gone unnoticed by the medical press. It is that metformin appears to boost GLP-1 levels. GLP-1 is an incretin hormone secreted in the gut which stimulates the beta cell to secrete insulin in the presence of high blood sugars. GLP-1 may also lower glucagon production at the same time. While Byetta and Januvia are higly promoted as being incretin drugs, some little known research suggests that metformin may also raise the level of GLP-1 in the body. Enhanced secretion of glucagon-like peptide 1 by biguanide compounds. Yasuda N et al. Biochem Biophys Res Commun. 2002 Nov 15;298(5):779-84. This was old news, but it may partially explain some of the stomach symptoms people experience with metformin. GLP-1 stops or Continue reading >>

Metformin Side Effects And How To Deal With Them

Metformin Side Effects And How To Deal With Them

Metformin side effects include diabetic neuropathy, brain fog, and digestive issues. You can address them through diet, Vitamin B12, CoQ10, and exercise. Let us understand the drug Metformin in detail and study different forms of metformin, its uses and common metformin side effects along with how to deal with them. Metformin: What Is It Used For? Metformin is an old warhorse in the pharma battle against diabetes. It has been the mainstay in the treatment of Type 2 Diabetes for more than fifty years, often matching or outperforming newer drugs. In fact, many new combination drugs are often created with metformin as one of the main ingredients. Thanks to its long run in the pharmaceutical world, the side effects of Metformin are also well known. The Metformin-PCOS connection has been studied extensively since a majority of health complications associated with PCOS (polycystic ovarian syndrome) are due to hyperinsulinemia (high amounts of insulin in the blood stream). Metformin is known to reduce circulating insulin levels. The use of this drug in women with PCOS has shown highly encouraging results. RELATED: 10 Easy Breakfast Ideas For Diabetics Most Prescribed Names in Metformin Category Include: Fortamet: It is an extended-release formulation that contains metformin hydrochloride. The tablets are designed for once-a-day administration. They deliver either 500 mg or 1000 mg of metformin. The tablet is made using a patented technology called SCOTTM that delivers the active compound slowly and at a constant rate. Glucophage: Glucophage tablets contain metformin hydrochoride. They contain either 500 mg, 850 mg or 1000 mg of the active compound. Glucophage tablets do not contain any special covering and need to be taken multiple times a day until the prescribed dosage is me Continue reading >>

Metformin And Digestive Disorders

Metformin And Digestive Disorders

Digestive disorders (diarrhoea, vomiting) represent the most common metformin side-effects (around 30%) with this first-line drug treatment for type 2 diabetes. In healthy individuals, metformin affects glucose, vitamin B12 and the digestive uptake of bile salts. In the colon, it acts locally by modifying glucose cell metabolism. Different pathophysiological hypotheses have been proposed to explain the metformin-induced diarrhoea and vomiting, which can sometimes cause the patient to stop an effective treatment. These theories include stimulation of intestinal secretion of serotonin, changes in incretin and glucose metabolism, and bile-salt malabsorption. However, none of these hypotheses can be considered an adequate pathophysiological explanation of metformin digestive side-effects. In addition, there is a lack of experimental data to explain these highly patient-dependent adverse effects. The full text of this article is available in PDF format. Les troubles digestifs (diarrhée, vomissements) sous metformine représentent l’effet indésirable le plus fréquent (environ 30 %) pour le médicament de référence du diabète de type 2. Chez l’individu non diabétique, la metformine agit sur l’absorption digestive du glucose, de la vitamine B12 et des sels biliaires. Pour le côlon, elle agit localement en modifiant le métabolisme cellulaire. Différentes hypothèses physiopathologiques peuvent expliquer les diarrhées et vomissements qui peuvent obliger le patient à cesser un traitement efficace: stimulation de la sécrétion intestinale de sérotonine, modification des incrétines et du métabolisme du glucose ou malabsorption des sels biliaires. Aucune de ces hypothèses ne peut être considérée comme l’explication physiopathologique des effets secondaires Continue reading >>

Diabetes Drugs: Metformin

Diabetes Drugs: Metformin

Editor’s Note: This is the second post in our miniseries about diabetes drugs. Tune in on August 21 for the next installment. Metformin (brand names Glucophage, Glucophage XR, Riomet, Fortamet, Glumetza) is a member of a class of medicines known as biguanides. This type of medicine was first introduced into clinical practice in the 1950’s with a drug called phenformin. Unfortunately, phenformin was found to be associated with lactic acidosis, a serious and often fatal condition, and was removed from the U.S. market in 1977. This situation most likely slowed the approval of metformin, which was not used in the U.S. until 1995. (By comparison, metformin has been used in Europe since the 1960’s.) The U.S. Food and Drug Administration (FDA) required large safety studies of metformin, the results of which demonstrated that the development of lactic acidosis as a result of metformin therapy is very rare. (A finding that has been confirmed in many other clinical trials to date.) Of note, the FDA officer involved in removing phenformin from the market recently wrote an article highlighting the safety of metformin. Metformin works primarily by decreasing the amount of glucose made by the liver. It does this by activating a protein known as AMP-activated protein kinase, or AMPK. This protein acts much like an “energy sensor,” setting off cellular activities that result in glucose storage, enhanced entry of glucose into cells, and decreased creation of fatty acids and cholesterol. A secondary effect of the enhanced entry of glucose into cells is improved glucose uptake and increased storage of glycogen (a form of glucose) by the muscles. Additionally, the decrease in fatty acid levels brought about by metformin may indirectly improve insulin resistance and beta cell func Continue reading >>

Metformin - Oral, Glucophage

Metformin - Oral, Glucophage

are allergic to dapagliflozin or any of the ingredients in FARXIGA. Symptoms of a serious allergic reaction may include skin rash, raised red patches on your skin (hives), swelling of the face, lips, tongue, and throat that may cause difficulty in breathing or swallowing. If you have any of these symptoms, stop taking FARXIGA and contact your healthcare provider or go to the nearest hospital emergency room right away have severe kidney problems or are on dialysis. Your healthcare provider should do blood tests to check how well your kidneys are working before and during your treatment with FARXIGA Dehydration (the loss of body water and salt), which may cause you to feel dizzy, faint, lightheaded, or weak, especially when you stand up (orthostatic hypotension). You may be at a higher risk of dehydration if you have low blood pressure; take medicines to lower your blood pressure, including water pills (diuretics); are 65 years of age or older; are on a low salt diet, or have kidney problems Ketoacidosis occurred in people with type 1 and type 2 diabetes during treatment with FARXIGA. Ketoacidosis is a serious condition which may require hospitalization and may lead to death. Symptoms may include nausea, tiredness, vomiting, trouble breathing, and abdominal pain. If you get any of these symptoms, stop taking FARXIGA and call your healthcare provider right away. If possible, check for ketones in your urine or blood, even if your blood sugar is less than 250 mg/dL Kidney problems. Sudden kidney injury occurred in people taking FARXIGA. Talk to your doctor right away if you reduce the amount you eat or drink, or if you lose liquids; for example, from vomiting, diarrhea, or excessive heat exposure Serious urinary tract infections (UTI), some that lead to hospitalization, occu Continue reading >>

What Are The Possible Side Effects Of Metformin And Sitagliptin (janumet, Janumet Xr)?

What Are The Possible Side Effects Of Metformin And Sitagliptin (janumet, Janumet Xr)?

JANUMET® XR (sitagliptin and metformin HCl) Extended-Release Tablets JANUMET XR tablets contain two oral antidiabetic medications used in the management of type 2 diabetes: sitagliptin and metformin hydrochloride extended-release. Sitagliptin Sitagliptin is an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme. Sitagliptin phosphate monohydrate drug substance is used to manufacture JANUMET XR. Sitagliptin phosphate monohydrate is described chemically as 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-α]pyrazine phosphate (1:1) monohydrate with an empirical formula of C16H15F6N5O•H3PO4•H2O and a molecular weight of 523.32. The structural formula is: Sitagliptin phosphate monohydrate is a white to off-white, crystalline, non-hygroscopic powder. It is soluble in water and N,N-dimethyl formamide; slightly soluble in methanol; very slightly soluble in ethanol, acetone, and acetonitrile; and insoluble in isopropanol and isopropyl acetate. Metformin Hydrochloride Metformin hydrochloride (N,N-dimethylimidodicarbonimidic diamide hydrochloride) is a white to off-white crystalline compound with a molecular formula of C4H11N5•HCl and a molecular weight of 165.63. Metformin hydrochloride is freely soluble in water and is practically insoluble in acetone, ether, and chloroform. The pKa of metformin is 12.4. The pH of a 1% aqueous solution of metformin hydrochloride is 6.68. The structural formula is as shown: JANUMET XR consists of an extended-release metformin core tablet coated with an immediate-release layer of sitagliptin. The sitagliptin layer is coated with a soluble polymeric film. JANUMET XR is available for oral administration as tablets containing 64.25 mg sitagliptin phosphate monohyd 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 >>

Gastrointestinal Tolerability Of Extended-release Metformin Tablets Compared To Immediate-release Metformin Tablets: Results Of A Retrospective Cohort Study

Gastrointestinal Tolerability Of Extended-release Metformin Tablets Compared To Immediate-release Metformin Tablets: Results Of A Retrospective Cohort Study

Objective: Metformin, a biguanide antihyperglycemic medication, lowers blood glucose in patients with type 2 diabetes with minimal risk of hypoglycemia. Most common side effects include diarrhea, nausea and vomiting. Extended-release metformin (Glucophage XR)*, a once-daily tablet using the patented GelShield Diffusion System release mechanism, may be better tolerated than immediate-release metformin (Glucophage). This retrospective chart review examined the overall gastrointestinal (GI) tolerability of both formulations. Research Design and Methods: Patient charts were reviewed and data were collected from October 2001 to May 2002. Adult patients with type 2 diabetes started on extended-release metformin (metformin-XR) or switched from immediate-release metformin to metformin-XR within the previous 2 years were eligible for inclusion in the metformin-XR cohort. Patients started on immediate-release metformin within the previous 2 years were eligible for inclusion in the immediate-release metformin cohort. Previous experience of GI side effects while taking immediate-release metformin did not prevent inclusion in either cohort, though patients with significant underlying GI disease or moderate to severe hepatic or renal impairment were excluded. GI tolerability was assessed during the first year of treatment with immediate-release metformin or metformin-XR. Primary endpoints were overall GI tolerability and frequency of diarrhea during the first year of treatment. Results: A total of 471 patients' charts were reviewed and data were collected from four diabetes clinics; 310 (metformin-XR) and 158 (immediate-release metformin) eligible patients were included. Patients were, on average, 56 years old, and overweight (mean body mass index 33 kg/m2). The majority of patients Continue reading >>

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