Glucophage (Metformin)

Glucophage with the active ingredient metformin is a medication, used by diabetes patients of the 2nd type to control the levels of sugar in blood. Sometimes the drug is prescribed to be taken in complex with other medications, treating diabetes, or combined with insulin. It's not a recommended medicine for the treatment of the diabetes type 1 though.

The treatments for diabetes always aim to decrease sugar content in blood, to lower its level to the normal mark. Patients, diagnosed with the diabetes type 2, have a trouble with insulin management in their bodies: they either can't produce enough of it or aren't able to react properly to the insulin, produced by the organism. If insulin isn't controlled, a patient may develop serious health problems, like blindness, severe kidney disorders, amputations or heart diseases.

There are a few ways to lower the level of sugar in blood. They include diet and exercises, medications, taken by mouth and insulin shots.

If you have high blood sugar, you should resort to over-the-counter remedies only after you've tried to control blood sugar levels with non-medicinal methods - exercising, weight loss and diet. If your doctor advises you Glucophage, you will achieve the best results of the blood sugar control when you combine the medication with regular workouts and diet, recommended for your diabetes type.

Each tablet of Glucophage contains Metformin hydrochloride, as the active agent, Povidone, magnesium stearate, as the inactive ingredients and Hypromellose or hypromellose and polyethylene glycol, as the coating components.

Glucophage available dtrengths: 500 mg, 850 mg and 1000 mg tablets. The brand-name Glucophage, Glucophage XR and their generics currently have the license for sale. Other generics - Fortamet, Glumetza, and Riomet aren't yet lisenced for sale.


Uses

Glucophage and Glucophage XR (long-acting form) are prescribed for the treatment of the type 2 diabetes, as one of the component in the complex blood sugar control therapy for diabetes, that includes also diet and exercising.

Type 2 diabetes
Type 2 diabetes

Usage of Glucophage for the diabetes type 2 treatment


Type 2 diabetes is often referred to as "noninsulin-dependent diabetes", or "adult-onset diabetes". That is one of the most frequently diagnosed diabetes types, involving insulin resistance. What does that mean? Actually, it's a condition, associated with the improper response of the organism cells to insulin. This improper response suggests that the cells are unable to withdraw sugar from the blood. That leads toward sugar accumulation in blood - high sugar levels.

The causes of type 2 diabetes in every patient aren't completely understood by the doctors, however, they claim that obesity and hereditary predisposition towards the disease are, definitely, crucial factors in this case. The diabetes of the 2nd type is a very serious condition, as it's fraught with the development of such accompanying diseases in future as diabetic neuropathy, kidney failure, heart disease and erectile dysfunction in men.

Luckily, there are many methods of how to control blood sugar in patients with type 2 diabetes. When it comes to pharmacological remedies, there's a group of medications, influencing the activity of the pancreas. Under their action, the pancreas produces more insulin. Thus, the necessary therapeutic effect is achieved, however, these medicines may cause hypoglycemia, a condition when blood sugar levels reach their critically low mark.

Unlike these drugs, Glucophage produces different effects on the patient's organism. First of all, it decreases the sugar content, produced by the liver. Secondly, the medication causes the organism to absorb less sugar from the consumed food. And finally, it increases the sensitivity of the insulin receptors, promoting the organism's ability to respond to insulin. Glucophage doesn't impact the pancreas activity, causing it to increase insulin production. That's why, people, taking the medication, don't risk to get their sugar levels dangerously low.

Metformin and children
Metformin and children
 

How to treat diabetes? Role of Glucophage in diabetes treatment


The treatment of diabetes should start from the introduction of the necessary changes into the patient's lifestyle. These changes suggest providing all the necessary conditions for the organism so it can control blood sugar levels. The conditions include weight loss, a diet, prescribed for the patient's diabetes type, and regular physical activity. These measures help to lower your sugar levels in blood and prevent the development of serious diabetes-related conditions. Sometimes these lifestyle changes need to be supported by an anti-diabetic medicaion to obtain optimal results of the treatment. In these cases medicines like Glucophage are prescribed.

Can Glucophage be used in children?


Though Glucophage is approved for the treatment of diabetes type 2 in children as well, a child, who is going to take the medicine, must not be younger than 10 y.o., while Glucophage XR is prescribed only to the patients older than 17 y.o. Even if your child meets the age requirements for the Glucophage usage, it won't be unnecessary to discuss with your healthcare provider pros and cons of the medication usage for the diabetes treatment in children.
Off-label Metformin uses
Off-label Metformin uses
 

What are off-label uses of Glucophage?


The direct indication for the Glucophage usage is the diabetes 2 type treatment. However, the medication may be also recommended for the treatment of the following conditions:
  • Polycystic ovarian syndrome (PCOS)
  • Diabetes during pregnancy
  • HIV lipodystrophy (for HIV or AIDS patients)

Your healthcare provider may prescrive Glucophage for the mentioned off-label uses.


Dosage

Glucophage dosage
Glucophage dosage
 
Depending on the course of your disease, taking into account your age, accompanying medical conditions, if available, and other medicines you may be presently taking, your healthcare provider will decide on the prescribed dose of Glucophage or Glucophage XR for you. You are not supposed to change it without instructions of a medical professional. As you are proceeding with your therapy, your healthcare provider may increase your dosage, however, that has to be done gradually in order to avoid possible side effects: +500 mg a week or +850 mg once in 2 weeks.

Glucophage dosages for the type 2 diabetes


Children 10-16 y.o.: Glucophage 500 mg twice a day, as the starting dose and Glucophage 2000 mg per day, split between 2-3 intakes during the day, as the maximum dose.

Adults (from 17 y.o. and over) Glucophage 500 mg twice a day or 850 mg once a day, as the starting dose, and Glucophage 2550 mg per day, split between 2-3 intakes during the day, as the maximum dose.

Glucophage XR (the Long-Acting Form) dosages for the type 2 diabetes


The long-acting form of the medication is prescribed to the patients, who have reached the age of 17 and older people. Glucophage XR 500 mg once a day is the starting dose, while Glucophage XR 2000 mg once a day (Glucophage XR 1000 mg twice a day) is the maximum dose for this medication.
Insulin
Insulin

Glucophage dosage, when taken with insulin


If you combine the mediation with insulin, you must stick to the same dosage of insulin and the following medication dosages:
  • Glucophage and Glucophage XR 500 mg once a day is the starting dose
  • Glucophage 2500 mg and Glucophage XR 2000 mg is the maximum daily dosage in total

Glucophage dosing, when combined with insulin


The starting dose of both Glucophage and Glucophage XR for the people, taking insulin, is 500 mg once daily. The maximum total daily dose for the people, taking insulin, is 2500 mg for Glucophage and 2000 mg for Glucophage XR. Usually, when adding Glucophage to the insulin intake, you should continue with your normal insulin dose.

Important recommendations on how to take Glucophage


Glucophage should be taken as prescribed. In case of any uncertainties as to the medication and the way it makes you feel, clear them up with your healthcare provider or a pharmasist. Don't stop taking the medication without your doctor's instructions.

Take the medication at the same time every day with meals. Glucophage XR is taken with the evening meal.

When taking a tablet, don't split or chew it. Swallow it whole.

When a patient doesn't succeed to get his blood sugar levels under control after a month of therapy with the maximum Glucophage dose, he/she is prescribed an additional diabetes medication.

If you are currently taking Chlorpropamide (Diabinese) and plan to substitute it with Glucophage, be aware that you may encounter hypoglycemia (too low blood sugar), as Chlorpropamide can stay in your organism for a while even after you've stopped a therapy with this medication.

If you've forgotten to take your current Glucophage dose, don't take the double dose. If it's time for your next dose, skip the missed tablet and continue taking the medication as prescribed. If it's not the time for your next dose yet, you may take it as soon as you remember to cover for the missed one, i.e. earlier then you intended.


Warnings and Precautions

Glucophage contraindications
Glucophage contraindications
 
Possible contraindications for the Glucophage usage include:
  • Scheduled surgeries or radiological procedures
  • Serious liver conditions, like liver failure or cirrhosis
  • Poor kidney function, like renal failure
  • Pernicious anemia
  • Congestive heart failure
  • Allergies to the active or inactive ingredients of the medication
  • A heart attack or stroke history

Before you start taking Glucophage, pay attention to the following precautions to avoid undesired complications:

In rare cases Glucophage triggers the development of a very serious disease - lactic acidosis. Such conditions as kidney or liver failure, liver cirrhosis and congestive heart failure increase the risks of the lactic acidosis development in patients, who are taking Glucophage.

The medication is not recommended for the patients, who experience serious problems with liver functioning. The reason is an increased risk of lactic acidosis. The same is true for the people with poor kidney function. That's why it's important to check your kidneys before you start taking the medication. If blood test shows that your kidneys are not functioning properly, you should avoid taking the medicine.

You should avoid drinking alcohol when you are taking the medication, since it can also serve as a trigger of lactic acidosis.

If you are planning to have any surgeries, keep in mind that your therapy with Glucophage should be suspended for that period.

If you are planning to undergo some radiology tests, like, CT scans, x-rays or heart catheterizations, which are performed with the usage of contrast dye, be aware that Glucophage in combination with contrast dye may cause damage to your kidneys.

If you are not taking insulin along with the medication, during the period, when your organism is weakened by such conditions as injuries and surgeries, fever and infection, your level of sugar may get out of the control, even if generally your diabetes is well-controlled. Insulin shots are recommended in this case. It's advisable to check your level of vitamin B12, while you are taking the medication, since it can cause the vitamin B12 deficiency.

Glucophage therapy isn't compatible with severe dehydration. That's why, if you are having any conditions which may cause considerable loss of water in your organism, like fever, vomiting or diarrhea, let your healthcare provider know about it.

Inform your healthcare provider about any other medications, including food supplements, herbal remedies and vitamins, you are currently taking to eliminate the risks of their interaction with the drug.

Taking the medication during pregnancy should be discussed with your healthcare provider as it's not proved that Glucophage is absolutely safe for pregnant women. Besides, it's proved that the medication passes to a baby through breast milk. So, the option of taking the medication during the period of breastfeeding should be considered and discussed with a medical professional.

Normally Glucophage doesn't cause hypoglycemia, but being combined with other medicines, treating diabetes, it can, quite rarely though. Such factors as an old age, liver or kidney conditions, adrenal, pituitary and fasting before surgery may cause low blood sugar (hypoglycemia).

Diabetes patients, who should avoid Glucophage


  • Elderly people, 80 y.o. and over, especially if their kidney work hasn't been checked
  • People with the impaired kidney function
  • People with the severe course of the congestive heart failure
  • People, allergic to any active or inactive component in the medication composition
  • People, suffering from metabolic or diabetic ketoacidosis
  • People, suffering from other serious diseases, like a heart attack or stroke, a severe infection, etc.
  • People, expecting a surgery or radiology procedures with contrast agents involved
  • People, experiencing considerable dehydration


Side Effects

Two life-threatening side effects, the usage of Glucophage may cause, include an allergic reaction and lactic acidosis (critical accumulation of lactic acid in the organism). Both these conditions need to be medically attended immediately.

Glucophage side effects
Glucophage side effects
 
A severe allergic reaction may reveal itself through:
  • Face, lips, tongue, or throat edema
  • Breathing with difficulty
  • Hives

Lactic acidosis alarming symptoms include:
Other serious side effects include:
  • Flu symptoms: pain in the body, chills, fever
  • Swelling
  • Sudden rapid gain of weight
  • Difficulty breathing

Mild side effects may be expressed through:
  • Weakness
  • Mild nausea and digestive disorders
  • Headache
  • Pain in the muscles

Inform your physician about these or other side effects you are experiencing to get qualified instructions on whether to continue or stop your therapy with the medication.


Mechanism of action

Metformin activates the AMP-activated protein kinase enzyme, which leads towards lowering of the blood glucose and serum lipid concentrations. The medication's work is efficient only in the presence of insulin.

Being absorbed into the blood stream, Glucophage performs the following functions in the organism:
  • Improvement of the glycemic control
  • Lowering the hepatic glucose output (the main effect Glucophage produces in the organism)
  • Being absorbed into the blood stream, the medication also helps to utilize insulin-mediated glucose after meals
  • Decreasing concentrations of serum free fatty acid
  • Increasing glucose utilization in the bowels through nonoxidative metabolism. This process contributes to the production of the lactate that is metabolized in the liver, which can prevent hypoglycemia


History

Metformin formula
Metformin formula
 
Metformin, FDA approved in the USA in 1994 for the diabetes of the 2nd type, has been known for almost a hundred years. Its sugar-lowering properties were first tested on rabbits in 1929 and showed impressive results, which were later taken over by other guanidine analogs and insulin.

Metformin belongs to the anti-diabetic class of drugs, called biguanides, which originate from the plant Galega officinalis (French lilac or goat's rue).

In the 1970s, when other biguanides were withdrawn, metformin gained broad popularity as an anti-diabetic medication, whereas today it's the most frequently prescribed anti-diabetic medication in the world.

The medication was approved in Canada in 1972. Since 1995 the medicine is marketed in the USA. The 1st producer of the brand-name Glucophage was Bristol-Myers Squibb.


Generic Glucophage

Glucophage generic
Glucophage generic
 
Brand-name metformin versions presently include: Fortamet, Glumetza, and Riomet. They aren't manufactured in the generic versions. Fortamet, Glumetza, and Riomet aren't equivalent to Glucophage, Glucophage XR, or metformin ER.

Glucophage and Glucophage XR are produced by the company Bristol-Myers Squibb. Today the medications are available in their generic versions, manufactured by 10 pharmaceutic companies, including Goldline Pharmaceuticals, Teva Pharmaceuticals and Mylan Laboratories.

Generic Glucophage is presented in the strengths of Metformin 500 mg, 850 mg, and 1000 mg. Generic Glucophage XR is available in 2 strengths: Metformin ER 500 mg and 750 mg.

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