I am diabetic

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

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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):

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