Oral Diabetes Medication Information

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Overview Sulfonylureas Biguanides Thiazolidendiones Alpha Glucosidase Inhibitors   Insulin Enhancers

Table of Available Drugs

Oral Hypoglycemic Agents

The last few years have been remarkable for the number and variety of new oral medications for the treatment of Type 2 diabetes. We have gone from only one class of drug to 5 classes in the last 3 years.

The decisions as to which drugs to use is now even more complex, and you will need to work closely with your diabetes team so they can determine the best strategy for treating your diabetes.

Oral hypoglycemic agents are pills which help to reduce your blood sugar levels. They are not oral insulin, but allow some diabetes patients to have normal glucose glucose levels when diet and exercise is not enough.

Proper diet and weight loss are the primary treatments for Type 2 diabetes. These pills are used after diet alone has failed, or if diet alone is extremely unlikely to work. If you do lose weight and follow a diet, sometimes the pills can be discontinued.

We generally do not use diabetes pills during pregnancy.

There are now studies supporting the use of certain oral diabetes medications in pregnant patients. We feel that more experience with oral medications during pregnancy is needed before they can be used in routine cases. There may be special circumstances that warrant the use of oral medications in pregnancy.  

There are 5 major categories:

Sulfonylurea drugs (SU), thiazolidendiones (T), biguanide (BG) , meglitinides (M), and alpha glucosidase inhibitors (AGI).

Click here to see the table of available drugs in the US.

Oral medications are only effective if your pancreas is still producing insulin. This is most likely to be the case if you are middle aged or elderly with mild Type 2 diabetes. These pills are not recommended for persons with Type 1 diabetes as they do not secrete enough insulin for the pill to work.

Again, these pills are not insulin. If diabetes pills are not successful, then your doctor may add insulin, or change to insulin alone.

Sulfonylurea drugs

These all work in a similar way, stimulating the pancreas to release more insulin and helping the body to become more sensitive to insulin. The major differences in them are cost and how long they work in your body. There are two generations of sulfonylureas... The first generation are Orinase, Dymelor, Tolinase, and Diabenese. Only Diabenese (chlorpropamide)  is used much in our group at this time.

Second generation drugs are glipizide (Glucotrol and Glucotrol XL), glyburide (Micronase, Diabeta, and Glynase), and Amaryl.

These drugs work best when diabetes has not been present for very long, and is mild. They may cause weight gain as a side effect.

Side effects are rare, and include hypoglycemia,stomach upset, loss of appetite, skin rash or itching, and liver function abnormalities.

Special note should be made of chlorpropamide. It is extremely long acting and may not be suitable for some people. In addition it can interact with alcohol in some persons to cause an "Antabuse effect" of beet red flushing and headache. This wears off on its own but is frightening.

Biguanides / Metformin / Glucophage

At this time, the only biguanide available is Glucophage (metformin). Developed by Lipha in France, metformin has been used for decades in Europe, but is a relative newcomer to the US. It is now the most widely prescribed agent for treatment of diabetes in the USA.

Metformin increases the sensitivity of liver and muscle to insulin. It does not increase insulin secretion from the pancreas to any extent. It can be used in combination with a sulfonylurea drug if the SU drug alone is not sufficient.

It has some unique advantages. It reduces triglycerides somewhat, and the average person loses about 5 pounds on the drug. It often works when other oral drugs fail. When used alone, we do not see any hypoglycemia like the SU drugs.

There may be an advantage to using drugs that reduce insulin levels, however this has not been proven by any clinical trials of SU drugs vs. metformin or troglitazone.

We caution everyone about the potential gastrointestinal complaints that commonly come up at the time the drug is started. We see complaints of abdominal cramping, loose stools, loss of appetite for the first few days. These usually last 1 - 5 days and then resolve even as the drug is continued. If they persist, please call us!

There is a serious concern about a potentially fatal condition known as lactic acidosis. This is accumulation of acid in your blood that can make you very sick and even die. Most, but not all, of these cases occur in persons with kidney disease.

For this reason, we avoid prescribing Glucophage when the serum creatinine level is above 1.5, or if you have significant heart failure or liver disease.

In addition, since tests involving contrast dye....like an IVP, CT Scan, arteriogram or heart cath.... can affect the kidneys we recommend stopping the Glucophage for 2 days until we can verify the kidneys are functioning well. Please call us if another doctor schedules any dye tests or surgery on you, and you are taking Glucophage.

Symptoms of lactic acidosis would be shortness of breath, severe weakness, muscle pains, abdominal pains, and generalized malaise. If these happen to you on Glucophage, please call your doctor!

There are more rare side effects such as B-12 deficiency. We can monitor for this if any signs develop of B12 deficiency.

Glucophage will be available generically late in 2001, which we hope will reduce the cost significantly. Glucophage XR and Glucovance will retain patent protection, thus will probably retain their current pricing after the introduction of generic equivalents to Glucophage.

Thiazolidinediones Avandia (rosiglitazone) ,Actos (piaglitazone)

We have expanded information available on glitazones, click here. 

Alpha Glucosidase Inhibitors (Precose / acarbose)

Precose is a novel agent for the US market. It does nothing relating to your liver, muscle, or pancreas. It works by slowing down absorption of starch from the intestinal tract. In doing so, it allows your own body to process carbohydrate more effectively.

Studies indicate a drop in glycohemoglobin of about 0.5 points. If you only monitor before meals, you may not see the effect of Precose as it helps prevent the sharp rise in glucose just after the meal. It has very little effect on the fasting glucose in the morning.

The limiting factor in Precose usage in our experience is patient side effects. This drug is a real gas producer. In order to minimize this side effect we start Precose very , very slowly. The usual schedule is as follows for a 50mg tablet:

If side effects develop, we move back one week. Even with this schedule, we see a lot of people discontinue the drug due to gas.

Insulin Enhancers

Starlix (nateglinide) &  Prandin  (repaglinide)

Prandin, was approved by the US FDA in December 1997. This agent is a very short acting stimulant of insulin release, and works by enhancing insulin secretion from the beta cells of the pancreas. The drug has minimal renal excretion thus may be useful in patients with impaired renal function.  The effect of this drug is very short. It is designed to be taken with each meal in order to stimulate insulin release and allow handling of the carbohydrate load from that meal. If a meal is skipped, so is the Prandin. If an extra meal is eaten, extra Prandin may be appropriate.

Recommended starting dose is 0.5 mg with each meal for patients previously on diet alone, or 1 - 2 mg with each meal for those on sulfonylurea drugs, and is titrated up to 4mg before each meal if necessary.

Starlix, (nateglinide) was released for use in the USA in early 2001. It appears to enhance insulin release more quickly than Prandin, and has a lower risk of hypoglycemia. Half life of the medication is short, and it can be used safely in people with kidney disease.  Starlix has been approved for use by itself, or in combination with Glucophage.

Table of Available Drugs

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This page last updated: 10/23/05