A List of Oral Medications for Diabetes 2 Treatment: Biguanides

Nov 2, 2010 by

Dabetes 2 treatment

Part 1 – Part 2

In Part 2 of our series Oral medications for diabetes 2 treatment we review biguanides, a second type of medication to treat type 2 diabetes. At the present time, the only biguanide available in the United States is Glucophage, also known by its generic name, metformin.

A short history of metformin

In the 1960s, a precursor of metformin, DBI-TD (also known as phenformin), was introduced as a twice-a-day medication for the control of glucose levels. It was a very effective medication, but it was removed from the market because of a rare but fatal complication called lactic acidosis.

Lactic acidosis is a condition in which lactic acids build up in the blood-stream; it is fatal in 50 percent of the people who develop it. This horrible side effect prompted researchers to develop metformin, a safer version of DBI-TD. It was introduced in Europe about 40 years ago but was not available in the United States until 1995.

How Glucophage works

Glucophage works by making the liver to produce less glucose. Since it does not directly affect insulin levels and probably does not affect the uptake of glucose by your muscles, it is not very effective for controlling the level of glucose after meals. Its greatest benefit seems to be in decreasing release of glucose by your liver during periods when you are fasting (such as between meals or at night).

It acts, basically, by disrupting a normal reaction of your liver. Here is how it works:

In a person without diabetes, both insulin and glucose levels are generally low when it is been more than four hours since the last meal. As a result, the liver normally increases its own production of glucose in order to keep the brain fed during this period of fasting. Once a meal is eaten, the levels of glucose and insulin in the blood rise, and the liver, sensing there is more insulin in the blood stops its own production of glucose.

In a person who is insulin resistant, however, the liver doesn’t seem to see insulin, even when there is plenty in the blood (such after a meal), so it doesn’t slow its own production; it mistakenly acts as if your blood glucose is low all the time. It continues to make glucose and releasing into your blood, even though, as a person with diabetes, your blood glucose levels are already too high. Glucophage stops this excess glucose production by the liver.

Liver

Since the most extended period of fasting for many people occurs overnight, the liver tends to be very busy during that time producing glucose; as a result, the morning glucose levels tend to be the highest of the day.

Glucophage works well to prevent these early morning highs by decreasing glucose production while you sleep. As an added benefit, it appears to cause less weight gain than most of the other diabetic medications and does not cause hypoglycemia.

Side effects of Glucophage

About 30 percent of the people who take Glucophage develop stomach upset of diarrhea; about 3 percent of those individuals find these side effects so intolerable that they cannot continue the medication. However, if you start out on a low dose that it is slowly increased over time and if you take the medicine with or immediately after a meal, those side effects can be minimized or eliminated.

A new version of Glucophage, Glucophage XR, is now available and has fewer gastrointestinal side effects.  Another side effect of Glucophage can be an increase in your level of triglycerides. Make sure your levels of triglycerides are monitored if you take this medication.

Glucophage can also cause lactic acidosis, but it is very rare. Only 30 of every 1 million people who take the drug experience eat each year. The signs of lactic acidosis are unusual muscle pain, fast and shallow breathing, slow or unsteady heartbeat, vomiting or a serious infection with dehydration and fever. To avoid these potentially dangerous effect do not take this medication if:

1.       You drink heavily

2.       You have liver disease, such as hepatitis

3.       You have liver disease

4.       You are 80 years or older

5.       You have poor circulation such as congestive heart failure or a condition that results in a low level of oxygen such as asthma

Caution should be taken if you are taken a test that involves contrast dye. During these types of tests, the kidneys excrete less lactic acid which can result in a buildup of the acid in the blood. Talk to your doctor if you are taking this type of test.

WARNING: Never stop taking any prescribed medication without your doctor directing you to do it.

How Glucophage is taken

Glucophage is generally taken twice a day, once in the morning and once at night. Occasionally, to minimize the effects, it is taken just once a day, in the evening, or in smaller doses before each meal three times a day. The initial dose is usually 500 mg with the evening meal. It is then increased to a maximum dose of 2,000 mg a day, twice a day. Above 2,000 mg per day, doesn’t seem to add any benefit while side effects could happen.

To your health!

Do not miss next article of the series where I’ll be talking about Thiazolidinediones (glitazones)

You may also want to read
Part 1 – Sulfonylureas

Emilia Klapp, R.D.,B.S.
www.TheDiabetesClub.com

 

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