Metformin, Sulfonylureas, Or Other Antidiabetes Drugs And The Risk Of Lactic Acidosis Or Hypoglycemia
Metformin, Sulfonylureas, or Other Antidiabetes Drugs and the Risk of Lactic Acidosis or Hypoglycemia 3Boston Collaborative Drug Surveillance Program, Boston University School of Medicine, Lexington, Massachusetts 4Department of Epidemiology, School of Public Health, Boston University, Massachusetts 3Boston Collaborative Drug Surveillance Program, Boston University School of Medicine, Lexington, Massachusetts 4Department of Epidemiology, School of Public Health, Boston University, Massachusetts 5Basel Pharmacoepidemiology Unit, Division of Clinical Pharmacology and Toxicology, University Hospital Basel, Basel, Switzerland 1Division of Clinical Pharmacology and Toxicology, University Hospital Basel, Basel, Switzerland 2Division of Endocrinology, Diabetes, and Clinical Nutrition, University Hospital Basel, Basel, Switzerland 3Boston Collaborative Drug Surveillance Program, Boston University School of Medicine, Lexington, Massachusetts 4Department of Epidemiology, School of Public Health, Boston University, Massachusetts 5Basel Pharmacoepidemiology Unit, Division of Clinical Pharmacology and Toxicology, University Hospital Basel, Basel, Switzerland Corresponding author: Christoph R. Meier, [email protected] Received 2008 Jun 27; Accepted 2008 Aug 10. Copyright 2008, American Diabetes Association Readers may use this article as long as the work is properly cited, the use is educational and not for profit, and the work is not altered. See for details. This article has been cited by other articles in PMC. OBJECTIVELactic acidosis has been associated with use of metformin. Hypoglycemia is a major concern using sulfonylureas. The aim of this study was to compare the risk of lactic acidosis and hypoglycemia among patients with type 2 diabetes using oral antidiabetes drugs. RESEAR Continue reading >>
How Does Metformin Work?
Metformin is a type of oral medication used to treat type 2 diabetes — and according to Gary Scheiner, CDE, in his book, “Until There is a Cure,” metformin is the most prescribed medication for type 2 diabetes, and one of those most widely used drugs in the world. But type 1 diabetics can take metformin, too, explains Scheiner, if they’re struggling with insulin resistance and persistent high blood sugars. The brand names for metformin are Glucophage, Glucophage XR, Glumetza, Fortamet, and Riomet. Metformin has also been combined with other medications, giving you two diabetes treatment methods in one medication. Those combo-medications are: glyburide (Glucovance), glipizide (Metaglip), rosiglitazone (Avandamet), pioglitazone (Actoplus Met), sitagliptin (Janumet) and repaglinide (PrandiMet). [Download our free Guide to Type 2 Diabetes Medications] Metformin is taken in pill-form. It is generally taken twice per day, at breakfast and at dinner. For those with higher levels of insulin resistance, your doctor may prescribe metformin to be taken at all three meals: breakfast, lunch, and dinner. Benefits of Metformin: While there are a variety of oral medications to help people with type 2 diabetes reduce their blood sugar levels, they all work very differently in the body. Scheiner explains exactly how metformin works in the body: Metformin does not increase insulin levels and does not cause hypoglycemia. Instead, it decreases the amount of sugar produced by the liver and tends to suppress appetite. – “Until There is a Cure,” page 81 In every human body, the liver releases small amounts of glucose throughout the day. The primary effect of taking metformin is that this release of glucose from the liver is lessened, resulting in lower blood sugars. Metformin als Continue reading >>
Oral Diabetes Medications Summary Chart
What Oral Medications Are Available for Type 2 Diabetes? Type 2 diabetes results when the body is unable to produce the amount of insulin it needs to convert food into energy or when it is unable to use insulin appropriately. Sometimes the body is actually producing more insulin than is needed by a person to keep blood glucose in a normal range. Yet blood glucose remains high, because the body's cells are resistant to the effects of insulin. Physicians and scientists believe that type 2 diabetes is caused by many factors, including insufficient insulin and insulin resistance. They increasingly believe that the relative contribution each factor makes toward causing diabetes varies from person to person. It is important to know the name of your diabetes medicine (or medicines), how it is taken, the reasons for taking it and possible side-effects. Diabetes Pills How to Take How They Work Side Effects Of Note Biguanides Metformin (Glucophage) Metformin liquid ( Riomet) Metformin extended release (Glucophage XR, Fortamet, Glumetza) Metformin: usually taken twice a day with breakfast and evening meal. Metformin extended release: usually taken once a day in the morning. Decreases amount of glucose released from liver. Bloating, gas, diarrhea, upset stomach, loss of appetite (usually within the first few weeks of starting). Take with food to minimize symptoms. Metformin is not likely to cause low blood glucose. In rare cases, lactic acidosis may occur in people with abnormal kidney or liver function. Always tell healthcare providers that it may need to be stopped when you are having a dye study or surgical procedure. Sulfonylureas Glimepiride (Amaryl) Glyburide (Diabeta, Micronase) Glipizide (Glucotrol, Glucotrol XL) Micronized glyburide (Glynase) Take with a meal once or twice Continue reading >>
Anti-diabetic Medication
Instructions for use Oral hypoglycemic agents are successful in people only for noninsulin-dependent diabetes. There has been only limited use in animals. Because response to oral hypoglycemic agents in cats is unpredictable, it is recommended to use a trial first of at least 4 weeks. If the cat responds, the drug can be continued; otherwise, insulin may be indicated. Feed cats a high-fiber diet when using oral hypoglycemic agents. Transdermal glipizide (5-mg dose) in a PLO gel was evaluated in cats. Although the transdermal formulation produced a modest change in glucose concentrations, systemic absorption was only 20%. Oral Hypoglycemic Therapy Oral hypoglycemic agents are used in cats only to attenuate the physiologic abnormalities of type 2 diabetes by decreasing hepatic glucose output and glucose absorption from the intestine, increasing peripheral insulin sensitivity, and increasing insulin secretion from the pancreas. In cats, the clinician must rely on the response to oral hypoglycemic agents as a guide to whether the cat has sufficient β-cell function to be managed with oral hypoglycemic agents. Oral hypoglycemic agents used in cats include the sulfonylureas (glipizide) and α-glucosidase inhibitors (acarbose).16,18 Indications for oral hypoglycemic therapy in cats include normal or increased body weight, lack of ketones, probable type 2 diabetes with no underlying disease (pancreatitis, pancreatic tumor), history of diabetogenic medications, and owners' willingness to administer oral medication rather than an injection. Diet should consist of low-carbohydrate/high-protein foods only. The mechanism of action of the sulfonylureas is to increase insulin secretion and improve insulin resistance. Sulfonylureas, because of provocation of insulin release, may promot Continue reading >>
Anti-diabetic Medication
The non-sulfonylurea secretagogues are a newer class and include two currently available products: nateglinide (a phenylalanine derivative) and repaglinide, a benzoic acid derivative. J. Wright, in Encyclopedia of Food Sciences and Nutrition (Second Edition) , 2003 Oral hypoglycemic agents may be used either alone or in combination with other agents. The combination of sulfonylurea and metformin was shown to be effective in the UK Prospective Diabetes Study. Metformin and insulin are frequently used in combination in overweight patients with type 2 diabetes. Thiazolidenediones may also be used in combination with either a sulfonylurea or metformin; they have also been used successfully in combination with insulin but this practice is not yet universal. Sulfonylureas have also been used in combination with insulin (for example with isophane insulin used overnight) but this has not gained widespread acceptance. Uazman Alam1*, ... Rayaz A. Malik12, in Handbook of Clinical Neurology , 2014 Oral hypoglycemic agents and insulin in type 2 diabetes mellitus Oral hypoglycemic agents work on the premise that a reasonably adequate amount of endogenous insulin is produced and thus oral therapies are aimed at modulating either insulin release or sensitivity. However, insulin therapy alone in type 2DM does not modulate the underlying pathophysiology of insulin resistance. This pathologic process results in progressive cell decline through a reduction of cell mass, cell dysfunction, and pancreatic islet amyloid deposition (Porte and Kahn, 2001). Combinations of oral and insulin agents may improve efficacy with less deleterious effects on weight gain. A previous review of combination therapies in type 2DM suggested that there is benefit in attenuating weight gain, reducing insulin dos Continue reading >>
Type 2 Oral Diabetes Medications Side Effects, Differences, And Effectiveness
What are the types of oral diabetes medications? Currently, there are nine drug classes of oral diabetes medications approved for the treatment of type 2 diabetes. α-glucosidase inhibitors Biguanides Sulfonylureas Meglitinides Thiazolidinediones DPP-4 inhibitors Sodium-glucose cotransporter (SGLT)-2 inhibitors These medications differ in the way they function in the body to reduce blood glucose. Metformin (Glucophage) is the only biguanide available in the United States and is generally the first choice for oral treatment of type 2 diabetes mellitus. Metformin improves Sulfonylureas are the oldest classes of oral diabetes medications. Sulfonylureas work primarily by stimulating the release of insulin. Insulin is the hormone responsible for regulating blood glucose by increasing the uptake of blood glucose by tissues and increasing storage of glucose in the liver. Meglitinides and sulfonylureas have a similar mechanism of action. Meglitinides are short acting glucose lowering medications. They stimulate the secretion of insulin from the pancreas. Thiazolidinediones enhance insulin sensitivity meaning that the effect of a given amount of insulin is greater. Thiazolidinediones also are referred to as peroxisome proliferator-activated receptor ? or PPAR-? agonists. α-glucosidase inhibitors delay the digestion and absorption of starch or carbohydrates by inhibiting enzymes in the small intestine which help breakdown these molecules. The starches and carbohydrates are broken down into glucose, which then is absorbed from the intestine and increases the level in the blood. DPP-4 inhibitors help lower blood glucose by increasing the production of insulin from the pancreas and reducing the release of glucose from the liver. SGLT2 inhibitors or sodium-glucose cotransporter 2 in Continue reading >>
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Diabetes And Oral Hypoglycemics - Dosage, Side Effects, Conflicts With Other Drugs
Oral hypoglycemics are anti-diabetic drugs designed to help people with type 2 diabetes manage their condition. This section includes information about oral hypoglycaemic drugs and dosage, side effects, conflicts with other drugs and more. The major oral hypoglycemics drug types are: What is the recommended dosage for oral hypoglycemics? The dosage for all oral hypoglycemics varies depending on the individual patient. Your healthcare professional or GP should inform you of the correct dosage, as should the pharmacist who fills out your prescription. Never vary from your recommended dose of oral hypoglycemics. Should I go back and see my healthcare professional? See your healthcare professional regularly whilst you start taking an oral hypoglycaemic drug. This is to ensure that your new medicine is working and there are no side effects. Physicians may also wish to adjust your dosage or even chance to a different hypoglycemic if yours is not proving effective. Can I stop doing exercise and eating well? Anti-diabetic drugs such as oral hypoglycemics need to be balanced with meals and daily exercise. You should not stop eating a healthy diet and doing regular exercise , and your healthcare professional should be able to teach you how to get the balance right. Testing blood sugar regularly, eating well and exercising daily are all important aspects of diabetes management. Will my oral hypoglycemic drugs cure my diabetes? No, oral hypoglycemic drugs do not cure diabetes. However, they do lessen the risk of diabetes complications and help you to manage your diabetes. Will other drugs mix badly with my oral hypoglycemic drugs? You should consult with your healthcare professional on all of the medication you are taking and medical conditions you suffer from before being prescri Continue reading >>
Hypoglycemic Drugs
RARELY PRESCRIBED (lower potency, greater toxicity) Keywords 2nd Generation Sulfonylureas: Glimepiride, Glipizide & Glyburide Fewer drug interactions, & side effects, more commonly prescribed Repaglinide Continue reading >>
Management Of Blood Glucose With Noninsulin Therapies In Type 2 Diabetes
A comprehensive, collaborative approach is necessary for optimal treatment of patients with type 2 diabetes mellitus. Treatment guidelines focus on nutrition, exercise, and pharmacologic therapies to prevent and manage complications. Patients with prediabetes or new-onset diabetes should receive individualized medical nutrition therapy, preferably from a registered dietitian, as needed to achieve treatment goals. Patients should be treated initially with metformin because it is the only medication shown in randomized controlled trials to reduce mortality and complications. Additional medications such as sulfonylureas, dipeptidyl-peptidase-4 inhibitors, thiazolidinediones, and glucagon-like peptide-1 receptor agonists should be added as needed in a patient-centered fashion. However, there is no evidence that any of these medications reduce the risk of diabetes-related complications, cardiovascular mortality, or all-cause mortality. There is insufficient evidence on which combination of hypoglycemic agents best improves health outcomes before escalating to insulin therapy. The American Diabetes Association recommends an A1C goal of less than 7% for many nonpregnant adults, with the option of a less stringent goal of less than 8% for patients with short life expectancy, cardiovascular risk factors, or long-standing diabetes. Randomized trials in middle-aged patients with cardiovascular risk factors have shown no mortality benefit and in some cases increased mortality with more stringent A1C targets. Clinical recommendation Evidence rating References Metformin should be used as first-line therapy to reduce microvascular complications, assist in weight management, reduce the risk of cardiovascular events, and reduce the risk of mortality in patients with type 2 diabetes mell Continue reading >>
Metformin (oral Route)
Precautions Drug information provided by: Micromedex It is very important that your doctor check your progress at regular visits, especially during the first few weeks that you take this medicine. Blood and urine tests may be needed to check for unwanted effects. This medicine may interact with the dye used for an X-ray or CT scan. Your doctor should advise you to stop taking it before you have any medical exams or diagnostic tests that might cause less urine output than usual. You may be advised to start taking the medicine again 48 hours after the exams or tests if your kidney function is tested and found to be normal. Make sure any doctor or dentist who treats you knows that you are using this medicine. You may need to stop using this medicine several days before having surgery or medical tests. It is very important to carefully follow any instructions from your health care team about: Alcohol—Drinking alcohol may cause severe low blood sugar. Discuss this with your health care team. Other medicines—Do not take other medicines unless they have been discussed with your doctor. This especially includes nonprescription medicines such as aspirin, and medicines for appetite control, asthma, colds, cough, hay fever, or sinus problems. Counseling—Other family members need to learn how to prevent side effects or help with side effects if they occur. Also, patients with diabetes may need special counseling about diabetes medicine dosing changes that might occur with lifestyle changes, such as changes in exercise or diet. Counseling on birth control and pregnancy may be needed because of the problems that can occur in pregnancy for patients with diabetes. Travel—Keep a recent prescription and your medical history with you. Be prepared for an emergency as you would norm Continue reading >>
Understanding Oral Diabetes Medications
by Gail Brashers-Krug Today, almost 21 million Americans have diabetes, and more than 90 percent of those have type 2, or insulin resistant diabetes. Doctors often prescribe oral medications to treat type 2 diabetes, either alone or combination with insulin therapy. This article provides a guide to those oral medications. Which Diabetics Use Pills? With a few exceptions, diabetes comes in two types. Type 1 diabetes occurs when the body does not produce enough insulin on its own. To treat type 1, you must restore the proper amount of insulin—either by taking insulin (through injection or inhalation), or by receiving a transplant, either of an entire pancreas or of specialized pancreas cells, called islet cells. Type 1 cannot be treated with oral medications. Type 2 diabetes occurs when the body produces enough insulin, but gradually becomes insulin resistant—that is, loses the ability to process insulin. Type 2 is usually controlled first through diet and exercise, which improve your body’s ability to process its insulin. For most type 2 diabetics, however, diet and exercise changes are not enough. The next step is oral diabetes medication. Moreover, most type 2 diabetics eventually stop producing enough insulin, and often cease insulin production altogether. As a result, many type 2 diabetics will ultimately need insulin therapy in combination with their pills. How Do the Different Pills Work? Oral diabetes medications attack the problem in three ways. More insulin: Some pills stimulate your pancreas to produce more insulin. The first successful “diabetes pills” were the sulfonylureas (glyburide, glipizide, glimepiride, tolazamide, chlorpropamide, and tolbutamide). These are insulin secretagogues, that is, chemicals that cause your pancreas to produce more ins Continue reading >>
Combination Therapy For Patients With Type 2 Diabetes: Repaglinide In Combination With Metformin
Overview of Oral Antidiabetic Medications Currently, six classes of oral antidiabetic drugs (OADs) are available: biguanides (e.g., metformin), sulfonylureas (e.g., glimepiride), meglitinides (e.g., repaglinide), thiazolidinediones (e.g., pioglitazone), dipeptidyl peptidase IV inhibitors (e.g., sitagliptin), and -glucosidase inhibitors (e.g., acarbose).[ 20 ] Sulfonylureas (SUs) are the oldest and most widely used medications for the treatment of T2DM. Although SU therapy effectively lowers blood glucose concentrations (average decrease in FPG of 24 mmol/l, accompanied by a decrease in HbA1c of 12%) by stimulating insulin secretion from -cells, treatment with SUs is associated with a progressive linear decline in -cell function.[ 13 , 21 ] Eventual inability to maintain glycemic control reflects an advanced stage of -cell failure. Hypoglycemia is the most common and most serious adverse event associated with SU therapy, mainly because of insulin release being initiated even when glucose concentrations are below the normal threshold for normal physiologic glucose-stimulated insulin release. Weight gain, regarded as a class effect of SUs, is thought to result from an anabolic effect of increased insulin concentration.[ 22 ] Owing to decreased effectiveness of SUs over time and an associated decline in the insulin secretory reserve, combination therapy has focused mainly on adding insulin-sensitizing medications, including metformin and thiazolidinediones. -glucose inhibitors, including acarbose, are competitive inhibitors of membrane-bound intestinal -glucosidases that hydrolyze oligosaccharides, trisaccharides and disaccharides to glucose and other monosaccharides in the small intestine and thereby delay postprandial glucose absorption.[ 23 ] These agents are available Continue reading >>
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- A New Perspective On Metformin Therapy In Type 1 Diabetes
Metformin
A popular oral drug for treating Type 2 diabetes. Metformin (brand name Glucophage, Glucophage XR, Glumetza, Riomet) is a member of a class of drugs called biguanides that helps lower blood glucose levels by improving the way the body handles insulin — namely, by preventing the liver from making excess glucose and by making muscle and fat cells more sensitive to available insulin. Metformin not only lowers blood glucose levels, which in the long term reduces the risk of diabetic complications, but it also lowers blood cholesterol and triglyceride levels and does not cause weight gain the way insulin and some other oral blood-glucose-lowering drugs do. Overweight, high cholesterol, and high triglyceride levels all increase the risk of developing heart disease, the leading cause of death in people with Type 2 diabetes. Another advantage of metformin is that it does not cause hypoglycemia (low blood glucose) when it is the only diabetes medicine taken. Metformin is typically taken two to three times a day, with meals. The extended-release formula (Glucophage XR) is taken once a day, with the evening meal. The most common side effects of metformin are nausea and diarrhea, which usually go away over time. A more serious side effect is a rare but potentially fatal condition called lactic acidosis, in which dangerously high levels of lactic acid build up in the bloodstream. Lactic acidosis is most likely to occur in people with kidney disease, liver disease, or congestive heart failure, or in those who drink alcohol regularly. (If you have more than four alcoholic drinks a week, metformin may not be the best medicine for you.) Unfortunately, many doctors ignore these contraindications (conditions that make a particular treatment inadvisable) and prescribe metformin to people Continue reading >>
Oral Hypoglycemic Agents
Uha Reddy, MS 3 Oral hypoglycemic agents Mechanism of action Molecules Involved Hypoglycemia Sulfonylureas First generation ·Acetohexamide ·Chloropropamide (Diabinese) ·Tolbutamide (Orinase) Second generation ·Glipizide (Glucotrol) ·Glyburide (Diabeta, Micronase, Glynase) ·Glimepiride (Amaryl) Stimulate the release of insulin from pancreatic B-cells (can only be used in patients with some B-cell function) Second generation sulfonylureas can be given in much lower doses than first generation because of their structure. ATP-dependent potassium channels (on B-cells) contain the sulfonylurea receptor – binding inhibits these channels and alters the resting potential of the cell – this leads to calcium moving into the cell and insulin being secreted Most common side effect; occurs more often in long-acting sulfs (chloropropamide glyburide and glimepiride) Meglitinides Repaglinide (Prandin) Nateglinide (Starlix) Also, stimulate the release of insulin from pancreatic B-cells Also acts by regulating ATP-dependent K+ channels, but appears to have a different receptor Most common side effect Biguanide Metformin (Glucophage) Decreases hepatic glucose output and increases insulin sensitivity (muscle, liver); Also, anti-lipolytic effect which decreases amount of free fatty acids. Unknown ? Activation of AMP-activated protein kinase Less likely to cause hypoglycemia Thiazolidinediones Rosiglitazone (Avandia) Pioglitazone (Actos) Increase insulin sensitivity (muscle and liver) and decrease glucose production Bind and activate peroxisome proliferator-activated receptors (PPARs), which regulates gene expression; Two types: gamma and alpha expressed in different tissues Less likely to cause hypoglycemia Alpha-glucosidase inhibitors Acarbose (Precose) Miglitol (Glyset) Inhibit G Continue reading >>
Anti-diabetic Medication
Drugs used in diabetes treat diabetes mellitus by lowering glucose levels in the blood. With the exceptions of Insulin, exenatide, liraglutide and pramlintide, all are administered orally and are thus also called oral hypoglycemic agents or oral antihyperglycemic agents. There are different classes of anti-diabetic drugs, and their selection depends on the nature of the diabetes, age and situation of the person, as well as other factors. Diabetes mellitus type 1 is a disease caused by the lack of insulin. Insulin must be used in Type I, which must be injected. Diabetes mellitus type 2 is a disease of insulin resistance by cells. Type 2 diabetes mellitus is the most common type of diabetes. Treatments include (1) agents that increase the amount of insulin secreted by the pancreas, (2) agents that increase the sensitivity of target organs to insulin, and (3) agents that decrease the rate at which glucose is absorbed from the gastrointestinal tract. Several groups of drugs, mostly given by mouth, are effective in Type II, often in combination. The therapeutic combination in Type II may include insulin, not necessarily because oral agents have failed completely, but in search of a desired combination of effects. The great advantage of injected insulin in Type II is that a well-educated patient can adjust the dose, or even take additional doses, when blood glucose levels measured by the patient, usually with a simple meter, as needed by the measured amount of sugar in the blood. Insulin[edit] Main article: insulin (medication) Insulin is usually given subcutaneously, either by injections or by an insulin pump. Research of other routes of administration is underway. In acute-care settings, insulin may also be given intravenously. In general, there are three types of insulin, Continue reading >>
