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Antidiabetic Agents, Sulfonylurea  (Systemic)

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Brand Names

Some commonly used brand names are:

In the U.S.—

  • Amaryl4
  • DiaBeta6
  • Diabinese2
  • Dymelor1
  • Glucotrol5
  • Glucotrol XL5
  • Glynase PresTab6
  • Micronase6
  • Orinase8
  • Tolinase7

In Canada—

  • Albert Glyburide6
  • Apo-Chlorpropamide2
  • Apo-Glyburide6
  • Apo-Tolbutamide8
  • DiaBeta6
  • Diabinese2
  • Diamicron3
  • Dimelor1
  • Euglucon6
  • Gen-Glybe6
  • Med Glybe6
  • Novo-Butamide8
  • Novo-Glyburide6
  • Novo-Propamide2
  • Nu-Glyburide6
  • Orinase8

Note:

For quick reference, the following sulfonylurea antidiabetic agents are numbered to match the corresponding brand names.

Another commonly used name for glyburide is glibenclamide.

This information applies to the following medicines:
1.  Acetohexamide (a-set-oh-HEX-a-mide)
2.  Chlorpropamide (klor-PROE-pa-mide)
3.  Gliclazide (GLIK-la-zide)*
4.  Glimepiride (GLYE-me-pye-ride)
5.  Glipizide (GLIP-i-zide)
6.  Glyburide (GLYE-byoo-ride)
7.  Tolazamide (tole-AZ-a-mide)
8.  Tolbutamide (tole-BYOO-ta-mide)
‡  Generic name product may be available in the U.S.
§  Generic name product may be available in Canada
*  Not commercially available in the U.S.
†  Not commercially available in Canada

Category


Description

Sulfonylurea antidiabetic agents (also known as sulfonylureas) are used to treat a certain type of diabetes mellitus (sugar diabetes) called type 2 diabetes. When you have type 2 diabetes, insulin is still being produced by your pancreas. Sometimes the amount of insulin you produce may not be enough or your body may not be using it properly and you may still need more. Sulfonylureas work by causing your pancreas to release more insulin into the blood stream. All of the cells in your body need insulin to help turn the food you eat into energy. This is done by using sugar (or glucose) in the blood as quick energy. Or the sugar may be stored in the form of fats, sugars, and proteins for use later, such as for energy between meals.

Sometimes insulin that is being produced by the body is not able to help sugar get inside the body's cells. Sulfonylureas help insulin get into the cells where it can work properly to lower blood sugar. In this way, sulfonylureas will help lower blood sugar and help restore the way you use food to make energy.

Many people with type 2 diabetes can control their blood sugar level with diet or diet and exercise alone. Following a diabetes diet plan and exercising will always be important with any type of diabetes. To work properly, the amount of sulfonylurea you use must be balanced against the amount and type of food you eat and the amount of exercise you do. If you change your diet, your exercise, or both, you will want to test your blood sugar level so that it does not drop too low (hypoglycemia) or rise too high (hyperglycemia). Your health care professional will teach you what to do if this happens.

Sometimes patients with type 2 diabetes might need to change to treatment with insulin for a short period of time during pregnancy or for a serious medical condition, such as diabetic coma; ketoacidosis; severe injury, burn, or infection; or major surgery. In these conditions, insulin and blood sugar can change fast and blood sugar can be best controlled with insulin instead of a sulfonylurea.

At some point, a sulfonylurea may stop working as well and your blood sugar level will go up. You will need to know if this happens and what to do. Instead of taking more of this medicine, your doctor may change you to another sulfonylurea. Or your doctor may have you inject small doses of insulin or take another oral antidiabetic medicine called metformin along with your sulfonylurea to help the insulin you make work better. If that does not bring down the amount of sugar in your blood, your doctor may have you stop taking the oral antidiabetic agents and begin receiving only insulin injections.

Chlorpropamide may also be used for other conditions as determined by your doctor.

Oral antidiabetic medicines do not help diabetic patients who have type 1 diabetes because these patients cannot produce or release insulin from their pancreas gland. Their blood sugar is best controlled by insulin injections.

Sulfonylureas are available only with your doctor's prescription, in the following dosage forms:



Before Using This Medicine

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For sulfonylurea medicines, the following should be considered:

Allergies—Tell your doctor if you have ever had any unusual or allergic reaction to sulfonylureas, or to sulfonamide-type (sulfa) medicines, including thiazide diuretics (a certain type of water pill). Also tell your health care professional if you are allergic to any other substances, such as foods, preservatives, or dyes.

Pregnancy—Sulfonylureas are rarely used during pregnancy. The amount of insulin you need changes during and after pregnancy. For this reason, it is easier to control your blood sugar using injections of insulin, rather than with the use of sulfonylureas. Close control of your blood sugar can reduce your chance of having high blood sugar during the pregnancy and of your baby gaining too much weight, or having birth defects. Be sure to tell your doctor if you plan to become pregnant or if you think you are pregnant. If insulin is not available or cannot be used and sulfonylureas are used during pregnancy, they should be stopped at least 2 weeks before the delivery date (one month before for chlorpropamide and glipizide). Lowering of blood sugar can occur as a rebound effect at delivery and for several days following birth and will be watched closely by your health care professionals.

Breast-feeding—Chlorpropamide and tolbutamide pass into human breast milk and glimepiride passes into the milk of rats. Chlorpropamide and glimepiride are not recommended in nursing mothers but, in some cases, tolbutamide has been used. It is not known if other sulfonylureas pass into breast milk. Check with your doctor if you are thinking about breast-feeding.

Children—There is little information about the use of sulfonylureas in children. Type 2 diabetes is unusual in this age group.

Older adults—Some elderly patients may be more sensitive than younger adults to the effects of sulfonylureas, especially when more than one antidiabetic medicine is being taken or if other medicines that affect blood sugar are also being taken. This may increase your chance of developing low blood sugar during treatment. Furthermore, the first signs of low or high blood sugar are not easily seen or do not occur at all in older patients. This may increase the chance of low blood sugar developing during treatment.

Also, elderly patients who take chlorpropamide are more likely to hold too much body water.

Other medicines—Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Do not take any other medicine, unless prescribed or approved by your doctor . When you are taking sulfonylurea antidiabetic drugs, it is especially important that your health care professional know if you are taking any of the following:

Other medical problems—The presence of other medical problems may affect the use of the sulfonylurea antidiabetic medicines. Make sure you tell your doctor if you have any other medical problems, especially:


Proper Use of This Medicine

Use this medicine only as directed even if you feel well and do not notice any signs of high blood sugar. Do not take more of this medicine and do not take it more often than your doctor ordered. To do so may increase the chance of serious side effects. Remember that this medicine will not cure your diabetes but it does help control it. Therefore, you must continue to take it as directed if you expect to lower your blood sugar and keep it low. You may have to take an antidiabetic medicine for the rest of your life. If high blood sugar is not treated, it can cause serious problems, such as heart failure, blood vessel disease, eye disease, or kidney disease.

Your doctor will give you instructions about diet, exercise, how to test your blood sugar levels, and how to adjust your dose when you are sick.

For patients taking glipizide extended-release tablets :

Dosing—

The dose of these medicines will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of these medicines. If your dose is different, do not change it unless your doctor tells you to do so.

The number of tablets that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the amount of sugar in your blood or urine.

Missed dose—

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage—

To store this medicine:


Precautions While Using This Medicine

Your doctor will want to check your progress at regular visits , especially during the first few weeks that you take this medicine.

It is very important to follow carefully any instructions from your health care team about:

In case of emergency—There may be a time when you need emergency help for a problem caused by your diabetes. You need to be prepared for these emergencies. It is a good idea to:

Too much of a sulfonylurea can cause low blood sugar (also called hypoglycemia). Symptoms of low blood sugar must be treated before they lead to unconsciousness (passing out). Different people may feel different symptoms of low blood sugar. It is important that you learn which symptoms of low blood sugar you usually have so that you can treat it quickly.

High blood sugar (hyperglycemia) is another problem related to uncontrolled diabetes. If you have any symptoms of high blood sugar, contact your health care team right away. If high blood sugar is not treated, severe hyperglycemia can occur, leading to ketoacidosis (diabetic coma) and death.


Side Effects of This Medicine

Side Effects of This Medicine

The use of sulfonylurea antidiabetic agents has been reported, but not proven in all studies, to increase the risk of death from heart and blood vessel disease. Patients with diabetes are already more likely to have these problems if they do not control their blood sugar. Some sulfonylureas, such as glyburide and gliclazide, can have a positive effect on heart and blood vessel disease. It is important to know that problems can occur, but it is also not known if other sulfonylureas, particularly tolbutamide, help to cause these problems. It is known that if blood sugar is not controlled, such problems can occur.

Along with their needed effects, sulfonylureas may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Also, check with your doctor as soon as possible if any of the following side effects occur:

Other side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. However, check with your doctor if any of the following side effects continue or are bothersome:

For patients taking chlorpropamide or tolbutamide:

Other side effects not listed above may also occur in some patients. If you notice any other effects, check with your doctor.


Additional Information

Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although this use is not included in product labeling, chlorpropamide is used in certain patients with the following medical condition:

If you are taking this medicine for water diabetes, the advice listed above that relates to diet for patients with sugar diabetes does not apply to you. However, the advice about hypoglycemia (low blood sugar) does apply to you. Call your doctor right away if you feel any of the symptoms described.

Other than the above information, there is no additional information relating to its proper use, precautions, or side effects for this use.

Revised: 12/29/1999

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