I am diabetic

Possible side effects
Stop taking metformin and seek emergency medical attention if you experience an allergic reaction (difficulty breathing; closing of the throat; swelling of the lips, tongue, or face; or hives).
A small number of people who have taken metformin have developed a serious condition called lactic acidosis that has been fatal in up to 50% of cases. Lactic acidosis has occurred most often in people whose kidneys were not working properly. Liver problems may also increase the risk of developing lactic acidosis. Stop taking metformin and call your doctor immediately if you experience a feeling of general discomfort or sickness; weakness; sore or aching muscles; trouble breathing, unusual drowsiness, dizziness or lightheadedness; unusual or unexplained stomach upset (after the initial stomach upset that may occur at the start of therapy with metformin); or the sudden development of a slow or irregular heartbeat. These may be signs of lactic acidosis.
Metformin does not usually cause hypoglycemia (low blood sugar). Nevertheless, hypoglycemia may occur in the treatment of diabetes, as a result of skipped meals, excessive exercise, or alcohol consumption. Know the signs and symptoms of low blood sugar, which include hunger, headache, drowsiness, weakness, dizziness, a fast heartbeat, sweating, tremor, and nausea. Carry a non-dietetic candy or glucose tablets to treat episodes of low blood sugar.
Other, less serious side effects may be more likely to occur. Continue to take metformin and talk to your doctor if you experience

• nausea, vomiting, abdominal pain, or diarrhea at the start of therapy;
• abdominal bloating or increased gas production; or
• decreased appetite or changes in taste (metallic taste in your mouth).

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.

 

What other drugs will affect Glucophage (Metformin)?

You may be more likely to have hyperglycemia (high blood sugar) if you are taking Glucophage with other drugs that raise blood sugar. Drugs that can raise blood sugar include:

• isoniazid;
• diuretics (water pills);
• steroids (prednisone and others);
• phenothiazines (Compazine and others);
• thyroid medicine (Synthroid and others);
• birth control pills and other hormones;
• seizure medicines (Dilantin and others); and
• diet pills, or medicines to treat asthma, colds or allergies.

You may be more likely to have hypoglycemia (low blood sugar) if you are taking Glucophage with other drugs that lower blood sugar. Drugs that can lower blood sugar include:

• some nonsteroidal anti-inflammatory drugs (NSAIDs);
• aspirin or other salicylates (including Pepto-Bismol);
• sulfa drugs (Bactrim and others);
• a monoamine oxidase inhibitor (MAOI);
• beta-blockers (Tenormin and others); or
• probenecid (Benemid).

Some medications may interact with Glucophage. Tell your doctor if you are using any of the following drugs:

• furosemide (Lasix);
• nifedipine (Adalat, Procardia);
• cimetidine (Tagamet) or ranitidine (Zantac);
• amiloride (Midamor) or triamterene (Dyrenium);
• digoxin (Lanoxin);
• morphine (MS Contin, Kadian, Oramorph);
• procainamide (Procan, Pronestyl, Procanbid);
• quinidine (Cardioquin, Quinidex, Quinaglute);
• trimethoprim (Proloprim, Primsol, Bactrim, Cotrim, Septra); or
• vancomycin (Vancocin, Lyphocin).

This list is not complete and there may be other drugs that can interact with Glucophage . Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor

 

What should I avoid while taking Glucophage (Metformin)?
Avoid excessive alcohol intake while taking metformin. Together, alcohol and metformin may increase the risk of lactic acidosis and hypoglycemia.
Follow diet, medication, and exercise routines closely. Changing any of these things can affect blood sugar levels.
Tell your doctor or other health care provider that you are taking this medication if you need to have surgery or x-ray procedures that require injection of contrast agents. Treatment with metformin may need to be stopped for a short period of time.
Do not take any over-the-counter cough, cold, allergy, pain, or weight-loss medications without first talking to your doctor.
Some conditions may increase the risk of developing lactic acidosis while taking metformin. Tell your doctor that you are taking metformin if you become ill; if you have a heart attack; have a stroke; develop congestive heart failure; experience diarrhea, vomiting, fever, or dehydration from any cause; decrease the amount of food or liquid in your normal diet, or develop other health conditions. You may need to stop treatment with metformin for a short amount of time until you are feeling better.

Contraindications
Metformin is contraindicated in patients with:
1. Renal disease or renal dysfunction (e.g., as suggested by serum creatinine levels ?1.5 mg/dL [males], ?1.4 mg/dL [females] or abnormal creatinine clearance) which may also result from conditions such as cardiovascular collapse (shock), acute myocardial infarction, and septicemia.
2. Known hypersensitivity to Metformin hydrochloride.
3. Acute or chronic metabolic acidosis, including diabetic ketoacidosis, with or without coma. Diabetic ketoacidosis should be treated with insulin.
Metformin should be temporarily discontinued in patients undergoing radiologic studies involving intravascular administration of iodinated contrast materials, because use of such products may result in acute alteration of renal function.

Warnings
Lactic Acidosis:
Lactic acidosis is a rare, but serious, metabolic complication that can occur due to Metformin accumulation during treatment with Metformin; when it occurs, it is fatal in approximately 50% of cases. Lactic acidosis may also occur in association with a number of pathophysiologic conditions, including diabetes mellitus, and whenever there is significant tissue hypoperfusion and hypoxemia. Lactic acidosis is characterized by elevated blood lactate levels (>5 mmol/L), decreased blood pH, electrolyte disturbances with an increased anion gap, and an increased lactate/pyruvate ratio. When Metformin is implicated as the cause of lactic acidosis, Metformin plasma levels >5 ?g/mL are generally found.
The reported incidence of lactic acidosis in patients receiving Metformin hydrochloride is very low (approximately 0.03 cases/1000 patient-years, with approximately 0.015 fatal cases/1000 patient-years). In more than 20,000 patient-years exposure to Metformin in clinical trials, there were no reports of lactic acidosis. Reported cases have occurred primarily in diabetic patients with significant renal insufficiency, including both intrinsic renal disease and renal hypoperfusion, often in the setting of multiple concomitant medical/surgical problems and multiple concomitant medications. Patients with congestive heart failure requiring pharmacologic management, in particular those with unstable or acute congestive heart failure who are at risk of hypoperfusion and hypoxemia, are at increased risk of lactic acidosis. The risk of lactic acidosis increases with the degree of renal dysfunction and the patient�s age. The risk of lactic acidosis may, therefore, be significantly decreased by regular monitoring of renal function in patients taking Metformin and by use of the minimum effective dose of Metformin. In particular, treatment of the elderly should be accompanied by careful monitoring of renal function. Metformin treatment should not be initiated in patients ? 80 years of age unless measurement of creatinine clearance demonstrates that renal function is not reduced, as these patients are more susceptible to developing lactic acidosis. In addition, Metformin should be promptly withheld in the presence of any condition associated with hypoxemia, dehydration, or sepsis. Because impaired hepatic function may significantly limit the ability to clear lactate, Metformin should generally be avoided in patients with clinical or laboratory evidence of hepatic disease. Patients should be cautioned against excessive alcohol intake, either acute or chronic, when taking Metformin, since alcohol potentiates the effects of Metformin hydrochloride on lactate metabolism. In addition, Metformin should be temporarily discontinued prior to any intravascular radiocontrast study and for any surgical procedure.
The onset of lactic acidosis often is subtle, and accompanied only by nonspecific symptoms such as malaise, myalgias, respiratory distress, increasing somnolence, and nonspecific abdominal distress. There may be associated hypothermia, hypotension, and resistant bradyarrhythmias with more marked acidosis. The patient and the patient�s physician must be aware of the possible importance of such symptoms and the patient should be instructed to notify the physician immediately if they occur. Metformin should be withdrawn until the situation is clarified. Serum electrolytes, ketones, blood glucose and, if indicated, blood pH, lactate levels, and even blood Metformin levels may be useful. Once a patient is stabilized on any dose level of Metformin, gastrointestinal symptoms, which are common during initiation of therapy, are unlikely to be drug related. Later occurrence of gastrointestinal symptoms could be due to lactic acidosis or other serious disease.
Levels of fasting venous plasma lactate above the upper limit of normal but less than 5 mmol/L in patients taking Metformin do not necessarily indicate impending lactic acidosis and may be explainable by other mechanisms, such as poorly controlled diabetes or obesity, vigorous physical activity, or technical problems in sample handling.
Lactic acidosis should be suspected in any diabetic patient with metabolic acidosis lacking evidence of ketoacidosis (ketonuria and ketonemia).
Lactic acidosis is a medical emergency that must be treated in a hospital setting. In a patient with lactic acidosis who is taking Metformin, the drug should be discontinued immediately and general supportive measures promptly instituted. Because Metformin hydrochloride is dialyzable (with a clearance of up to 170 mL/min under good hemodynamic conditions), prompt hemodialysis is recommended to correct the acidosis and remove the accumulated Metformin. Such management often results in prompt reversal of symptoms and recovery.

Precautions
Monitoring of renal function
Metformin is known to be substantially excreted by the kidney, and the risk of Metformin accumulation and lactic acidosis increases with the degree of impairment of renal function. Thus, patients with serum creatinine levels above the upper limit of normal for their age should not receive Metformin. In patients with advanced age, Metformin should be carefully titrated to establish the minimum dose for adequate glycemic effect, because aging is associated with reduced renal function. In elderly patients, particularly those > 80 years of age, renal function should be monitored regularly and, generally, Metformin should not be titrated to the maximum dose.
Before initiation of Metformin therapy and at least annually thereafter, renal function should be assessed and verified as normal. In patients in whom development of renal dysfunction is anticipated, renal function should be assessed more frequently and Metformin discontinued if evidence of renal impairment is present.

Use of concomitant medications that may affect renal function or Metformin dispostion
Concomitant medication(s) that may affect renal function or result in significant hemodynamic change or may interfere with the disposition of Metformin, such as cationic drugs that are eliminated by renal tubular secretion, should be used with caution.

Radiologic studies involving the use of intravascular iodinated contrast materials (for example, intravenous urogram, intravenous cholangiography, angiography, and computed tomography (CT) scans with intravascular contrast materials)
Intravascular contrast studies with iodinated materials can lead to acute alteration of renal function and have been associated with lactic acidosis in patients receiving Metformin. Therefore, in patients in whom any such study is planned, Metformin should be temporarily discontinued at the time of or prior to the procedure, and withheld for 48 hours subsequent to the procedure and reinstituted only after renal function has been re-evaluated and found to be normal.

Hypoxic states
Cardiovascular collapse (shock) from whatever cause, acute congestive heart failure, acute myocardial infarction and other conditions characterized by hypoxemia have been associated with lactic acidosis and may also cause prerenal azotemia. When such events occur in patients on Metformin therapy, the drug should be promptly discontinued.

Surgical procedures
Metformin therapy should be temporarily suspended for any surgical procedure (except minor procedures not associated with restricted intake of food and fluids) and should not be restarted until the patient�s oral intake has resumed and renal function has been evaluated as normal.

Alcohol intake
Alcohol is known to potentiate the effect of Metformin on lactate metabolism. Patients, therefore, should be warned against excessive alcohol intake, acute or chronic, while receiving Metformin.

Impaired hepatic function
Since impaired hepatic function has been associated with some cases of lactic acidosis, Metformin should generally be avoided in patients with clinical or laboratory evidence of hepatic disease.

Vitamin B12 levels
In controlled clinical trials of Metformin of 29 weeks duration, a decrease to subnormal levels of previously normal serum vitamin B12 levels, without clinical manifestations, was observed in approximately 7% of patients. Such decrease, possibly due to interference with B12 absorption from the B12-intrinsic factor complex, is, however, very rarely associated with anemia and appears to be rapidly reversible with discontinuation of Metformin or vitamin B12 supplementation. Measurement of hematologic parameters on an annual basis is advised in patients on Metformin and any apparent abnormalities should be appropriately investigated and managed.
Certain individuals (those with inadequate vitamin B12 or calcium intake or absorption) appear to be predisposed to developing subnormal vitamin B12 levels. In these patients, routine serum vitamin B12 measurements at two- to three-year intervals may be useful.

Change in clinical status of patients with previously controlled type 2 diabetes
A patient with type 2 diabetes previously well controlled on Metformin who develops laboratory abnormalities or clinical illness (especially vague and poorly defined illness) should be evaluated promptly for evidence of ketoacidosis or lactic acidosis. Evaluation should include serum electrolytes and ketones, blood glucose and, if indicated, blood pH, lactate, pyruvate, and Metformin levels.If acidosis of either form occurs, Metformin must be stopped immediately and other appropriate corrective measures initiated.

Hypoglycemia
Hypoglycemia does not occur in patients receiving Metformin alone under usual circumstances of use, but could occur when caloric intake is deficient, when strenuous exercise is not compensated by caloric supplementation,or during concomitant use with other glucose-lowering agents (such as sulfonylureas and insulin) or ethanol.
Elderly, debilitated, or malnourished patients, and those with adrenal or pituitary insufficiency or alcohol intoxication are particularly susceptible to hypoglycemic effects. Hypoglycemia may be difficult to recognize in the elderly, and in people who are taking beta-adrenergic blocking drugs.

Loss of control of blood glucose
When a patient stabilized on any diabetic regimen is exposed to stress such as fever, trauma, infection, or surgery, a temporary loss of glycemic control may occur. At such times, it may be necessary to withhold Metformin and temporarily administer insulin. Metformin may be reinstituted after the acute episode is resolved. The effectiveness of oral antidiabetic drugs in lowering blood glucose to a targeted level decreases in many patients over a period of time. This phenomenon, which may be due to progression of the underlying disease or to diminished responsiveness to the drug, is known as secondary failure, to distinguish it from primary failure in which the drug is ineffective during initial therapy. Should secondary failure occur with either Metformin or sulfonylurea monotherapy, combined therapy with Metformin and sulfonylurea may result in a response. Should secondary failure occur with combined Metformin/sulfonylurea therapy, it may be necessary to consider therapeutic alternatives including initiation of insulin therapy.

Information For Patients

Carcinogenesis/ Mutagenesis/ Impairment of Fertility
Long-term carcinogenicity studies have been performed in rats (dosing duration of 104 weeks) and mice (dosing duration of 91 weeks) at doses up to and including 900 mg/kg/day and 1500 mg/kg/day, respectively. These doses are both approximately four times the maximum recommended human daily dose of 2000 mg based on body surface area comparisons. No evidence of carcinogenicity with Metformin was found in either male or female mice. Similarly, there was no tumorigenic potential observed with Metformin in male rats. There was, however, an increased incidence of benign stromal uterine polyps in female rats treated with 900 mg/kg/day.
There was no evidence of mutagenic potential of Metformin in the following in vitro tests: Ames test (S. typhimurium), gene mutation test (mouse lymphoma cells), or chromosomal aberrations test (human lymphocytes). Results in the in vivo mouse micronucleus test were also negative.
Fertility of male or female rats was unaffected by Metformin when administered at doses as high as 600 mg/kg/day, which is approximately three times the maximum recommended human daily dose based on body surface area comparisons.

Pregnancy
Teratogenic Effects: Pregnancy Category B
Recent information strongly suggests that abnormal blood glucose levels during pregnancy are associated with a higher incidence of congenital abnormalities. Most experts recommend that insulin be used during pregnancy to maintain blood glucose levels as close to normal as possible. Because animal reproduction studies are not always predictive of human response, Metformin should not be used during pregnancy unless clearly needed.
There are no adequate and well-controlled studies in pregnant women with Metformin. Metformin was not teratogenic in rats and rabbits at doses up to 600 mg/kg/day. This represents an exposure of about two and six times the maximum recommended human daily dose of 2000 mg based on body surface area comparisons for rats and rabbits, respectively. Determination of fetal concentrations demonstrated a partial placental barrier to Metformin.

Nursing Mothers
Studies in lactating rats show that Metformin is excreted into milk and reaches levels comparable to those in plasma. Similar studies have not been conducted in nursing mothers. Because the potential for hypoglycemia in nursing infants may exist, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
If Metformin is discontinued, and if diet alone is inadequate for controlling blood glucose, insulin therapy should be considered.

Pediatric Use
The safety and effectiveness of Metformin for the treatment of type 2 diabetes have been established in pediatric patients ages 10 to 16 years (studies have not been conducted in pediatric patients below the age of 10 years).
Use of Metformin in this age group is supported by evidence from adequate and well-controlled studies of Metformin in adults with additional data from a controlled clinical study in pediatric patients ages 10 to 16 years with type 2 diabetes, which demonstrated a similar response in glycemic control to that seen in adults. In this study, adverse effects were similar to those described in adults.
A maximum daily dose of 2000 mg is recommended.

Geriatric Use
Controlled clinical studies of Metformin did not include sufficient numbers of elderly patients to determine whether they respond differently from younger patients, although other reported clinical experience has not identified differences in responses between the elderly and younger patients. Metformin is known to be substantially excreted by the kidney and because the risk of serious adverse reactions to the drug is greater in patients with impaired renal function, Metformin should only be used in patients with normal renal function. Because aging is associated with reduced renal function, Metformin should be used with caution as age increases. Care should be taken in dose selection and should be based on careful and regular monitoring of renal function. Generally, elderly patients should not be titrated to the maximum dose of Metformin.

Product description

Most Important Information about Glucophage (Metformin)

Pharmacokinetics

More information about Glucophage (Metformin):

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Absorption

The absolute bioavailability of a Metformin hydrochloride 500 mg tablet given under fasting conditions is approximately 50 to 60%. Studies using single oral doses of Metformin hydrochloride 500 mg to 1500 mg, and 850 mg to 2550 mg, indicate that there is a lack of dose proportionality with increasing doses, which is due to decreased absorption rather than an alteration in elimination. Food decreases the extent of and slightly delays the absorption of Metformin, as shown by approximately a 40% lower mean peak plasma concentration (Cmax), a 25% lower area under the plasma concentration versus time curve (AUC), and a 35 minute prolongation of time to peak plasma concentration (Tmax) following administration of a single 850 mg tablet of Metformin with food, compared to the same tablet strength administered fasting. The clinical relevance of these decreases is unknown.

Distribution

The apparent volume of distribution (V/F) of Metformin following single oral doses of Metformin hydrochloride 850 mg averaged 654 � 358 L. Metformin is negligibly bound to plasma proteins, in contrast to sulfonylureas, which are more than 90% protein bound. Metformin partitions into erythrocytes, most likely as a function of time. At usual clinical doses and dosing schedules of Metformin, steady state plasma concentrations of Metformin are reached within 24 to 48 hours and are generally <1 �g/mL. During controlled clinical trials of Metformin, maximum Metformin plasma levels did not exceed 5 �g/mL, even at maximum doses.

Metabolism

Intravenous single-dose studies in normal subjects demonstrate that Metformin is excreted unchanged in the urine and does not undergo hepatic metabolism (no metabolites have been identified in humans) nor biliary excretion.

Excretion

Renal clearance is approximately 3.5 times greater than creatinine clearance, which indicates that tubular secretion is the major route of Metformin elimination. Following oral administration, approximately 90% of the absorbed drug is eliminated via the renal route within the first 24 hours, with a plasma elimination half-life of approximately 6.2 hours. In blood, the elimination half-life is approximately 17.6 hours, suggesting that the erythrocyte mass may be a compartment of distribution.

Special Populations

Geriatric
Limited data from controlled pharmacokinetic studies of Metformin in healthy elderly subjects suggest that total plasma clearance of Metformin is decreased, the half-life is prolonged, and Cmax is increased, compared to healthy young subjects. From these data, it appears that the change in Metformin pharmacokinetics with aging is primarily accounted for by a change in renal function. Metformin treatment should not be initiated in patients ? 80 years of age unless measurement of creatinine clearance demonstrates that renal function is not reduced.

Pediatric
After administration of a single oral Metformin hydrochloride 500 mg tablet with food, geometric mean Metformin Cmax and AUC differed less than 5% between pediatric type 2 diabetic patients (12 to 16 years of age) and gender- and weight-matched healthy adults (20 to 45 years of age), all with normal renal function.

Gender
Metformin pharmacokinetic parameters did not differ significantly between normal subjects and patients with type 2 diabetes when analyzed according to gender (males = 19, females = 16). Similarly, in controlled clinical studies in patients with type 2 diabetes, the antihyperglycemic effect of Metformin hydrochloride tablets was comparable in males and females.

Race
No studies of Metformin pharmacokinetic parameters according to race have been performed. In controlled clinical studies of Metformin in patients with type 2 diabetes, the antihyperglycemic effect was comparable in whites (n=249), blacks (n=51), and Hispanics (n=24).

Renal Insufficiency
In patients with decreased renal function (based on measured creatinine clearance), the plasma and blood half-life of Metformin is prolonged and the renal clearance is decreased in proportion to the decrease in creatinine clearance.

Hepatic Impairment
No pharmacokinetic studies of Metformin have been conducted in patients with hepatic insufficiency.

Product description

Most Important Information about Glucophage (Metformin)

Possible Side Effects

More information about Glucophage (Metformin):

Cancer Benefit for Diabetes Drug Glucophage

Kidney Fund concerned about Glucophage fatality risk

FDA approves new indication for Glucovance oral antidiabetic

For more information look HERE: My Family Drugstore

What is the most important information I should know about Glucophage (Metformin)?

A small number of people who have taken metformin have developed a serious condition called lactic acidosis that has been fatal in up to 50% of cases. Lactic acidosis has occurred most often in people whose kidneys were not working properly. Liver problems may also increase the risk of developing lactic acidosis. Stop taking metformin and call your doctor immediately if you experience a feeling of general discomfort or sickness; weakness; sore or aching muscles; trouble breathing, unusual drowsiness, dizziness or lightheadedness; unusual or unexplained stomach upset (after the initial stomach upset that may occur at the start of therapy with metformin); or the sudden development of a slow or irregular heartbeat. These may be signs of lactic acidosis.
Avoid excessive alcohol intake while taking metformin. Together, alcohol and metformin may increase the risk of lactic acidosis and hypoglycemia.
Metformin does not usually cause hypoglycemia (low blood sugar). Nevertheless, hypoglycemia may occur in the treatment of diabetes, as a result of skipped meals, excessive exercise, or alcohol consumption. Know the signs and symptoms of low blood sugar, which include hunger, headache, drowsiness, weakness, dizziness, a fast heartbeat, sweating, tremor, and nausea. Carry non-dietetic candy or glucose tablets to treat episodes of low blood sugar.

What should I discuss with my doctor before taking Glucophage (Metformin)?

Do not take metformin without first talking to your doctor if you

• have kidney disease;
• have liver disease;
• have congestive heart failure;
• have acute or chronic metabolic acidosis, including diabetic ketoacidosis;
• have had a heart attack or a stroke;
• have a serious infection, illness, or injury;
• need to have surgery;
• need to have x-rays or other procedures using injectable contrast agents;
• are dehydrated (have lost water from your body) due to diarrhea, vomiting, fever, heat stroke, decreased fluid intake, or any other cause;
• drink alcohol; or
• are 80 years of age or older and have not had your kidney function tested.

You may not be able to take metformin, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above.
Contact your doctor if you develop a fever or an infection, require surgery, or if you experience a serious injury. Illness or injury may cause a loss of blood sugar control and insulin (or an adjustment of a current insulin dose) may be required for a period of time.
Metformin is in the FDA pregnancy category B. This means that it is unlikely to harm an unborn baby. Generally, insulin is the drug of choice for controlling diabetes during pregnancy. Do not take metformin without first talking to your doctor if you are pregnant or could become pregnant during treatment.
Metformin passes into breast milk and may affect a nursing baby. Do not take metformin without first talking to your doctor if you are breast-feeding a baby.
If you are over the age of 65 years, there may be an slight increase in the risk of developing lactic acidosis due to a natural decline in kidney function with advancing age. A lower dose or special monitoring may be necessary during your treatment.

Product description

Pharmacokinetics

Possible Side Effects

More information about Glucophage (Metformin):

Cancer Benefit for Diabetes Drug Glucophage

Kidney Fund concerned about Glucophage fatality risk

FDA approves new indication for Glucovance oral antidiabetic

For more information look HERE: My Family Drugstore

Drug Name

Glucophage (Metformin)

Generic Name

Metformin Tablets (met-FOR-min)

Manufacturer / Distributor

ALPHAPHARM PTY LTD

Looks like

Metformin is available with a prescription under the brand names Glucophage and Riomet. Other brand or generic formulations may also be available. Ask your pharmacist any questions you have about this medication, especially if it is new to you.

• Glucophage 500 mg–white, round, film-coated tablets
• Glucophage 850 mg–white, round, film-coated tablets
• Glucophage 1,000 mg–white, oval, film-coated tablets

Dosage Form

Tablets

Route Of Administration

ORAL

Alternatives

Diabecon, Karela, Actoplus Met

Drug Uses

Metformin is used for treating type II diabetes in adults and children. It may be used alone or in combination with other diabetic medications. Metformin also has been used to prevent the development of diabetes in people at risk for diabetes and to treat polycystic ovaries.

Drug class

Metformin is an oral medication that lowers blood glucose (sugar) and is used for treating type II diabetes. Insulin is a hormone, produced by the pancreas that lowers glucose levels in blood by reducing the amount of glucose, made by the liver and by increasing the removal of glucose from the blood by muscle and fat tissues. Diabetes results because of reduced production of insulin and reduced uptake (and effects) of insulin on the body’s tissues. Metformin acts by increasing the sensitivity of liver, muscle, fat, and other tissues to the uptake and effects of insulin. These actions lower the level of sugar in the blood. Unlike glucose-lowering drugs of the sulfonylurea class, e.g. glyburide (Micronase; Diabeta) or glipizide (Glucotrol), metformin does not increase the concentration of insulin in the blood and, therefore, does not cause excessively low blood glucose levels (hypoglycemia) when used alone. In scientific studies, metformin reduced the complications of diabetes such as heart disease, blindness and kidney disease. Metformin was approved by the FDA in December of 1994.

Contains

Metformin hydrochloride tablets USP contain 500 mg, 850 mg, or 1000 mg of Metformin hydrochloride. In addition, each tablet contains the following inactive ingredients:

• hypromellose,
• magnesium stearate,
• polyethylene glycol
• and povidone.

Chemical formula

Metformin hydrochloride is an oral antihyperglycemic drug used in the management of type 2 diabetes.
Metformin hydrochloride (N,N-dimethylimidodicarbonimidic diamide hydrochloride) is not chemically or pharmacologically related to any other classes of oral antihyperglycemic agents. The structural formula is as shown:

Metformin 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.

Mechanism of Action

Metformin is an antihyperglycemic agent which improves glucose tolerance in patients with type 2 diabetes, lowering both basal and postprandial plasma glucose. Its pharmacologic mechanisms of action are different from other classes of oral antihyperglycemic agents. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. Unlike sulfonylureas, Metformin does not produce hypoglycemia in either patients with type 2 diabetes or normal subjects and does not cause hyperinsulinemia. With Metformin therapy, insulin secretion remains unchanged while fasting insulin levels and day-long plasma insulin response may actually decrease.

How Taken

Take metformin exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain the instructions to you.
Take the tablets with a full glass of water.
Do not crush, chew, or break the Glucophage XR tablets. Swallow them whole. They are specially formulated to release the medication slowly in the body.
To ensure that you get a correct dose, measure the metformin solution with a dose-measuring spoon, dropper, or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist where you can get one.
Take metformin with a meal to reduce nausea, diarrhea, and upset stomach that may occur with metformin therapy. These symptoms may be more likely to occur during the first few weeks of therapy.
Occasionally, inactive ingredients in the metformin extended-release (Glucophage XR) tablets may pass through your body undissolved and appear in the stool as a soft mass. This is not harmful, and the medication has been absorbed by your body.
It is important to take metformin regularly to get the most benefit.
A decrease in vitamin B12 may also occur during metformin therapy. Your doctor may want to monitor your blood levels of vitamin B12 and you may need to take B12 supplements. A vitamin B12 deficiency may rarely cause anemia.
Your healthcare provider may recommend regular monitoring of blood sugar levels with blood or urine tests.

Dosage and Administration

There is no fixed dosage regimen for the management of hyperglycemia in patients with type 2 diabetes with Metformin or any other pharmacologic agent. Dosage of Metformin must be individualized on the basis of both effectiveness and tolerance, while not exceeding the maximum recommended daily dose. The maximum recommended daily dose of Metformin hydrochloride is 2550 mg in adults and 2000 mg in pediatric patients (10 to 16 years of age).
Metformin should be given in divided doses with meals. Metformin should be started at a low dose, with gradual dose escalation, both to reduce gastrointestinal side effects and to permit identification of the minimum dose required for adequate glycemic control of the patient.
During treatment initiation and dose titration, fasting plasma glucose should be used to determine the therapeutic response to Metformin and identify the minimum effective dose for the patient. Thereafter, glycosylated hemoglobin should be measured at intervals of approximately three months. The therapeutic goal should be to decrease both fasting plasma glucose and glycosylated hemoglobin levels to normal or near normal by using the lowest effective dose of Metformin, either when used as monotherapy or in combination with sulfonylurea or insulin.
Monitoring of blood glucose and glycosylated hemoglobin will also permit detection of primary failure, i.e., inadequate lowering of blood glucose at the maximum recommended dose of medication, and secondary failure, i.e., loss of an adequate blood glucose lowering response after an initial period of effectiveness.
Short-term administration of Metformin may be sufficient during periods of transient loss of control in patients usually well-controlled on diet alone.

Recommended Dosing Schedule

Adults
In general, clinically significant responses are not seen at doses below 1500 mg per day. However, a lower recommended starting dose and gradually increased dosage is advised to minimize gastrointestinal symptoms.
The usual starting dose of Metformin hydrochloride tablets USP is 500 mg twice a day or 850 mg once a day, given with meals. Dosage increases should be made in increments of 500 mg weekly or 850 mg every 2 weeks, up to a total of 2000 mg per day, given in divided doses. Patients can also be titrated from 500 mg twice a day to 850 mg twice a day after 2 weeks. For those patients requiring additional glycemic control, Metformin hydrochloride may be given to a maximum daily dose of 2550 mg per day. Doses above 2000 mg may be better tolerated given three times a day with meals.

Pediatrics
The usual starting dose of Metformin hydrochloride tablets USP is 500 mg twice a day, given with meals. Dosage increases should be made in increments of 500 mg weekly up to a maximum of 2000 mg per day, given in divided doses.

Transfer from Other Antidiabetic Therapy
When transferring patients from standard oral hypoglycemic agents other than chlorpropamide to Metformin, no transition period generally is necessary. When transferring patients from chlorpropamide, care should be exercised during the first two weeks because of the prolonged retention of chlorpropamide in the body, leading to overlapping drug effects and possible hypoglycemia.

Concomitant Metformin and Oral Sulfonylurea Therapy in Adult Patients
If patients have not responded to four weeks of the maximum dose of Metformin monotherapy, consideration should be given to gradual addition of an oral sulfonylurea while continuing Metformin at the maximum dose, even if prior primary or secondary failure to a sulfonylurea has occurred. Clinical and pharmacokinetic drug-drug interaction data are currently available only for Metformin plus glyburide (glibenclamide).
With concomitant Metformin and sulfonylurea therapy, the desired control of blood glucose may be obtained by adjusting the dose of each drug. In a clinical trial of patients with type 2 diabetes and prior failure on glyburide, patients started on Metformin hydrochloride 500 mg and glyburide 20 mg were titrated to 1000/20 mg, 1500/20 mg, 2000/20 mg or 2500/20 mg of Metformin hydrochloride and glyburide, respectively, to reach the goal of glycemic control as measured by FPG, HbA1c and plasma glucose response. However, attempts should be made to identify the minimum effective dose of each drug to achieve this goal. With concomitant Metformin and sulfonylurea therapy, the risk of hypoglycemia associated with sulfonylurea therapy continues and may be increased. Appropriate precautions should be taken.
If patients have not satisfactorily responded to one to three months of concomitant therapy with the maximum dose of Metformin and the maximum dose of an oral sulfonylurea, consider therapeutic alternatives including switching to insulin with or without Metformin.

Concomitant Metformin and Insulin Therapy in Adult Patients
The current insulin dose should be continued upon initiation of Metformin hydrochloride therapy. Metformin hydrochloride therapy should be initiated at 500 mg once daily in patients on insulin therapy. For patients not responding adequately, the dose of Metformin hydrochloride should be increased by 500 mg after approximately 1 week and by 500 mg every week thereafter until adequate glycemic control is achieved. The maximum recommended daily dose is 2500 mg for Metformin hydrochloride tablets. It is recommended that the insulin dose be decreased by 10% to 25% when fasting plasma glucose concentrations decrease to less than 120 mg/dL in patients receiving concomitant insulin and Metformin. Further adjustment should be individualised based on glucose-lowering response.

Missed Dose

Take the missed dose as soon as you remember (be sure to take the medicine with food). If it is almost time for your next dose, skip the missed dose and take the medicine at the next regularly scheduled time.
Do not take extra medicine to make up the missed dose.

Overdose

Seek emergency medical attention if you think you have used too much of this medicine. Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center ( http://www.aapcc.org/findyour.htm ), or emergency room immediately.
You may have signs of low blood sugar, such as

• hunger,
• headache,
• confusion,
• irritability,
• drowsiness,
• weakness,
• dizziness,
• tremors,
• sweating,
• fast heartbeat,
• seizure (convulsions),
• fainting, or coma.

An overdose of metformin may cause a life-threatening condition called lactic acidosis.
Get emergency medical help if you have any of these symptoms of lactic acidosis:

• weakness,
• increasing sleepiness,
• slow heart rate,
• cold feeling,
• muscle pain,
• shortness of breath,
• stomach pain,
• feeling light-headed,
• and fainting.

Storage

Store Glucophage at room temperature, between 68 and 77 degrees F (20 and 25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted.
Store away from heat, moisture, and light.
Do not store in the bathroom.
Keep Glucophage out of the reach of children and away from pets.

How Supplied

Metformin hydrochloride tablets USP are available as:

500 mg – each tablet contains 500 mg of Metformin hydrochloride.
Round, normal convex, film coated white tablet, unscored, debossed “MF / 1″ on one side and “G” on the other side.
Bottles of 100 – NDC 57315-047-01
Bottles of 500 – NDC 57315-047-04

850 mg – each tablet contains 850 mg of Metformin hydrochloride.
Round, normal convex, film coated white tablet, unscored, debossed “MF / 2″ on one side and “G” on the other side.
Bottles of 100 – NDC 57315-048-01
Bottles of 300 – NDC 57315-048-04
Bottles of 500 – NDC 57315-048-05

1000 mg – each tablet contains 1000 mg of Metformin hydrochloride.
Oblong, normal convex, film coated white tablet, scored, debossed “MF | 3″ on one side and “G” on the other side.
Bottles of 100 – NDC 57315-050-01
Bottles of 500 – NDC 57315-050-02

Most Important Information about Glucophage (Metformin)

Pharmacokinetics

Possible Side Effects

More information about Glucophage (Metformin):

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