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:
![[Image]](http://www.myfamilydrugstore.com/img2/Glucophage_f.jpg)
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)
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Tags: Conditions & Treatments, Glucophage (Metformin), Medications, Type 2 Diabetes