Brand Names:

• Amaryl
• Diabeta
• Diabinese
• Glucotrol
• Glucotrol XL
• Glycron
• Glynase Pres-Tab
• Micronase
• Tolinase
• Tol-Tab
• Euglucon

Dosage Forms:

• Tablet
• Tablet, Extended Release
• Powder for Solution

Uses of This Medicine:

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.

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

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:

• Diabetes insipidus (water diabetes)

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.

Before Using This Medicine:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to medicines in this group or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children

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

Pregnancy

Sulfonylureas are rarely used during pregnancy. The amount of insulin needed changes during and after pregnancy. For this reason, it is easier to control blood sugar using injections of insulin, rather than with the use of sulfonylureas. Close control of blood sugar can reduce the chance of having high blood sugar during the pregnancy and of the 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). Glimepiride should not be used at all during pregnancy. 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 is not recommended in nursing mothers but, in some cases, tolbutamide has been used. Nursing mothers should not take glimepiride. It is not known if other sulfonylureas pass into breast milk. Check with your doctor if you are thinking about breast-feeding.

Other medicines

Using medicines in this class with any of the following medicines is not recommended. Your doctor may decide not to treat you with a medication in this class or change some of the other medicines you take.

• Bosentan

Using medicines in this class with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Acarbose
• Alatrofloxacin
• Balofloxacin
• Ciprofloxacin
• Clinafloxacin
• Enoxacin
• Fleroxacin
• Flumequine
• Gatifloxacin
• Gemifloxacin
• Grepafloxacin
• Levofloxacin
• Lomefloxacin
• Moxifloxacin
• Norfloxacin
• Ofloxacin
• Pefloxacin
• Prulifloxacin
• Rufloxacin
• Sparfloxacin
• Temafloxacin
• Tosufloxacin
• Trovafloxacin Mesylate

Other interactions

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using medicines in this class with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use your medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Ethanol

Other medical problems

The presence of other medical problems may affect the use of medicines in this class. Make sure you tell your doctor if you have any other medical problems, especially:

• Acid in the blood (acidosis) or
• Burns (severe) or
• Diabetic coma or
• Fever, high or
• Injury, severe or
• Ketones in the blood (diabetic ketoacidosis) or
• Surgery, major or
• Any other condition in which insulin needs change rapidly Insulin may be needed temporarily to control diabetes in patients with these conditions because changes in blood sugar may occur rapidly and without much warning. Also, your blood sugar may need to be tested more often.

• Diarrhea, continuing or
• Female hormone changes for some women (e.g., during puberty, pregnancy, or menstruation) or
• Infection, severe or
• Mental stress, severe or
• Overactive adrenal gland, not properly controlled or
• Problems with intestines, severe or
• Slow stomach emptying or
• Vomiting, continuing or
• Any other condition that causes severe blood sugar changes Insulin may be needed temporarily to control diabetes mellitus in patients with these conditions because changes in blood sugar may occur rapidly and without much warning. Also, your blood sugar may need to be tested more often

• Heart disease Chlorpropamide or tolbutamide causes some patients to retain (keep) more body water than usual. Heart disease may be worsened by this extra body water.

• Kidney disease or
• Liver disease Your blood sugar may be increased or decreased, partly because of slower removal of sulfonylurea from the body. This may change the amount of sulfonylurea you need.

• Underactive adrenal gland, not properly controlled or
• Underactive pituitary gland, not properly controlled or
• Undernourished condition or
• Weakened physical condition or
• Any other condition that causes low blood sugar Patients with these conditions may be more likely to develop low blood sugar while taking sulfonylureas.

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.

• Diet The daily number of calories in the meal plan should be adjusted by your doctor or a registered dietitian to help you reach and maintain a healthy body weight. In addition, regular meals and snacks are arranged to meet the energy needs of your body at different times of the day. It is very important that you follow your meal plan carefully.
• Exercise Ask your doctor what kind of exercise to do, the best time to do it, and how much you should do each day.
• Blood tests This is the best way to tell whether your diabetes is being controlled properly. Blood sugar testing helps you and your health care team adjust the dose of your medicine, meal plan, or exercise schedule.
• On sick days When you become sick with a cold, fever, or the flu, you need to take your usual dose of sulfonylurea, even if you feel too ill to eat. This is especially true if you have nausea, vomiting, or diarrhea. Infection usually increases your need to produce more insulin. Sometimes you may need to be switched from your sulfonylurea to insulin for a short period of time while you are sick to properly control blood sugar. Call your doctor for specific instructions. Continue taking your sulfonylurea and try to stay on your regular meal plan. If you have trouble eating solid food, drink fruit juices, nondiet soft drinks, or clear soups, or eat small amounts of bland foods. A dietitian or your health care professional can give you a list of foods and the amounts to use for sick days. Test your blood sugar level at least every 4 hours while you are awake and check your urine for ketones. If ketones are present, call your doctor at once. If you have severe or prolonged vomiting, check with your doctor. Even when you start feeling better, let your doctor know how you are doing.

For patients taking glipizide extended-release tablets:

• Swallow the tablet whole, without breaking, crushing, or chewing it.
• You may sometimes notice what looks like a tablet in your stool. Do not worry. After you swallow the tablet, the medicine in the tablet is absorbed inside your body. Then the tablet passes into your stool without changing its shape. The medicine has entered your body and will work properly.

Dosing

The dose medicines in this class 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 amount of medicine 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 medical problem for which you are using the medicine.

• For acetohexamide:
  • For treating type 2 diabetes:
    • For oral dosage form (tablets):
      • Adults At first, 250 milligrams (mg) once a day. Some elderly people may need a lower dose at first. Then, your doctor may change your dose a little at a time if needed. The dose is usually not more than 1.5 grams a day. If your dose is 1 gram or more, the dose is usually divided into two doses. These doses are taken before the morning and evening meals.
      • Children The type of diabetes treated with this medicine is rare in children. However, if a child needs this medicine, the dose would have to be determined by the doctor.

• For chlorpropamide:
  • For treating type 2 diabetes:
    • For oral dosage form (tablets):
      • Adults At first, 250 milligrams (mg) once a day. Some elderly people may need a lower dose of 100 to 125 mg a day at first. Then, your doctor may change your dose a little at a time if needed. The dose is usually not more than 750 mg a day.
      • Children The type of diabetes treated with this medicine is rare in children. However, if a child needs this medicine, the dose would have to be determined by the doctor.

• For gliclazide:
  • For treating type 2 diabetes:
    • For oral dosage form (tablets):
      • Adults 80 milligrams (mg) a day with a meal as a single dose or 160 to 320 mg divided into two doses taken with the morning and evening meals.
      • Children The type of diabetes treated with this medicine is rare in children. However, if a child needs this medicine, the dose would have to be determined by the doctor.

• For glimepiride:
  • For treating type 2 diabetes:
    • For oral dosage form (tablets):
      • Adults Glimepiride alone: At first, 1 to 2 milligrams (mg) once a day with breakfast or the first main meal. The dose then may be increased by your doctor based on your blood sugar level.
      • Adults Glimepiride with metformin: The usual dose is 8 mg once a day with breakfast or the first main meal.
      • Adults Glimepiride with insulin: The usual dose is 8 mg once a day with breakfast or the first main meal.
      • Children The type of diabetes treated with this medicine is rare in children. However, if a child needs this medicine, the dose would have to be determined by the doctor.

• For glipizide:
  • For treating type 2 diabetes:
    • For oral dosage form (tablets):
      • Adults At first, 5 milligrams (mg) once a day. Some elderly people may need a lower dose of 2.5 mg a day at first. Then, your doctor may change your dose a little at a time if needed. The dose is usually not more than 40 mg a day. If your dose is 15 mg or more, the dose is usually divided into two doses. These doses are taken thirty minutes before the morning and evening meals.
      • Children The type of diabetes treated with this medicine is rare in children. However, if a child needs this medicine, the dose would have to be determined by the doctor.
        • For oral dosage form (extended-release tablets):
          • Adults At first, 5 mg once a day with breakfast. Then, your doctor may change your dose a little at a time if needed. The dose is usually not more than 20 mg a day.
          • Children The type of diabetes treated with this medicine is rare in children. However, if a child needs this medicine, the dose would have to be determined by the doctor.

• For glyburide:
  • For treating type 2 diabetes:
    • For oral dosage form (nonmicronized tablets):
      • Adults At first, 2.5 to 5 milligrams (mg) once a day. Some elderly people may need a lower dose of 1.25 to 2.5 mg a day at first. Then, your doctor may change your dose a little at a time if needed. The dose is usually not more than 20 mg a day. If your dose is 10 mg or more, the dose usually is divided into two doses. These doses are taken with the morning and evening meals.
      • Children The type of diabetes treated with this medicine is rare in children. However, if a child needs this medicine, the dose would have to be determined by the doctor.
        • For oral dosage form (micronized tablets):
          • Adults At first, 1.5 to 3 mg a day. Some elderly people may need a low dose of 0.75 to 3 mg a day at first. Then, your doctor may change your dose a little at a time if needed. The dose is usually not more than 12 mg a day. If your dose is 6 mg or more, the dose is usually divided into two doses. These doses are taken with the morning and evening meals. A single dose is taken with breakfast or with the first meal.
          • Children The type of diabetes treated with this medicine is rare in children. However, if a child needs this medicine, the dose would have to be determined by the doctor.

• For tolazamide:
  • For treating type 2 diabetes:
    • For oral dosage form (tablets):
      • Adults At first, 100 to 250 milligrams (mg) once a day in the morning. Then, your doctor may change your dose a little at a time if needed. The dose is usually not more than 1 gram a day. If your dose is 500 mg or more, the dose is usually divided into two doses. These doses are taken with the morning and evening meals.
      • Children The type of diabetes treated with this medicine is rare in children. However, if a child needs this medicine, the dose would have to be determined by the doctor.

• For tolbutamide:
  • For treating type 2 diabetes:
    • For oral dosage form (tablets):
      • Adults At first, 1000 to 2000 milligrams (mg) a day. Some elderly people may need lower doses to start. The dose is usually divided into two doses. These doses are taken before the morning and evening meals. Your doctor may change your dose a little at a time if needed. The dose is usually not more than 3000 mg a day.
      • Children The type of diabetes treated with this medicine is rare in children. However, if a child needs this medicine, the dose would have to be determined by the doctor.

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

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

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:

• Alcohol Drinking alcohol may cause severe low blood sugar. Discuss this with your health care team.
• Tobacco If you have been smoking for a long time and suddenly stop, your dosage of sulfonylurea may need to be reduced. If you decide to quit, tell your doctor first.
• Other medicines Do not take other medicines unless they have been discussed with your doctor. This especially includes nonprescription medicines, such as aspirin, and medicines for appetite control, asthma, colds, cough, hay fever, or sinus problems.
• Counseling Other family members need to learn how to prevent side effects or help with side effects in the patient if they occur. Also, patients with diabetes, especially teenagers, may need special counseling about sulfonylurea or insulin dosing changes that might occur because of lifestyle changes, such as changes in exercise and diet. Furthermore, counseling on contraception and pregnancy may be needed because of the problems that can occur in women with diabetes who become pregnant.
• Travel Carry a recent prescription and your medical history. Be prepared for an emergency as you would normally. Make allowances for changing time zones, and keep your meal times as close as possible to your usual meal times.
• Protecting skin from sunlight Sulfonylureas can make you more sensitive to the sun. Use of sunblock products that have a skin protection factor (SPF) of at least 15 on your skin and lips can help to prevent sunburn. Do not use a sunlamp or tanning bed or booth.

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:

• Wear a medical identification (I.D.) bracelet or neck chain at all times. Also, carry an I.D. card in your wallet or purse that says that you have diabetes and a list of all of your medicines.
• Keep some kind of quick-acting sugar handy to treat low blood sugar.
• Have a glucagon kit and a syringe and needle available in case severe low blood sugar occurs. Check and replace any expired kits regularly.
• 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.
• Symptoms of low blood sugar can include: anxious feeling, behavior change similar to being drunk, blurred vision, cold sweats, confusion, cool pale skin, difficulty in concentrating, drowsiness, excessive hunger, fast heartbeat, headache, nausea, nervousness, nightmares, restless sleep, shakiness, slurred speech, and unusual tiredness or weakness.
• The symptoms of low blood sugar may develop quickly and may result from:
  • delaying or missing a scheduled meal or snack.
  • exercising more than usual.
  • drinking a significant amount of alcohol.
  • taking certain medicines.
  • taking too high a dose of sulfonylurea.
  • if using insulin, using too much insulin.
• Know what to do if symptoms of low blood sugar occur. Eating some form of quick-acting sugar when symptoms of low blood sugar first appear will usually prevent them from getting worse. Good sources of sugar include:
  • Glucose tablets or gel, fruit juice or nondiet soft drink (4 to 6 ounces [one-half cup]), corn syrup or honey (1 tablespoon), sugar cubes (6 one-half-inch sized), or table sugar (dissolved in water).
  • Do not use chocolate because its fat slows down the sugar entering the bloodstream.
  • If a snack is not scheduled for an hour or more you should also eat a light snack, such as crackers or a half sandwich, or drink an 8-ounce glass of milk.
  • Glucagon is used in emergency situations such as unconsciousness. Have a glucagon kit available, along with a syringe and needle, and know how to prepare and use it. Members of your household also should know how and when to use it.

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.

• Symptoms of high blood sugar appear more slowly than those of low blood sugar. Symptoms can include: blurred vision; drowsiness; dry mouth; flushed and dry skin; fruit-like breath odor; increased urination; loss of appetite; stomachache, nausea, or vomiting; tiredness; troubled breathing (rapid and deep); and unusual thirst.
• Symptoms of severe high blood sugar (called ketoacidosis or diabetic coma) that need immediate hospitalization include: flushed dry skin, fruit-like breath odor, ketones in urine, passing out, troubled breathing (rapid and deep).
• High blood sugar symptoms may occur if you:
  • have a fever, diarrhea, or an infection.
  • if using insulin, do not take enough insulin or skip a dose of insulin.
  • do not exercise as much as usual.
  • overeat or do not follow your meal plan.
  • Know what to do if high blood sugar occurs. Your doctor may recommend changes in your sulfonylurea dose or meal plan to avoid high blood sugar. Symptoms of high blood sugar must be corrected before they progress to more serious conditions. Check with your doctor often to make sure you are controlling your blood sugar, but do not change the dose of your medicine without checking with your doctor. Your doctor might discuss the following with you:
    • Decreasing your dose for a short time for special needs, such as when you cannot exercise as you normally do.
    • Increasing your dose when you plan to eat an unusually large dinner, such as on holidays. This type of increase is called an anticipatory dose.
    • Delaying a meal if your blood sugar is over 200 mg/dL to allow time for your blood sugar to go down. An extra dose or an injection of insulin may be needed if your blood sugar does not come down shortly.
    • Not exercising if your blood sugar is over 240 mg/dL and reporting this to your doctor immediately.
    • Being hospitalized if ketoacidosis or diabetic coma occurs with a possible change of treatment.

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 its needed effects, a medicine 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:

Less common

Convulsions (seizures)

unconsciousness

Check with your doctor as soon as possible if any of the following side effects occur:

More common

Low blood sugar

unusual weight gain

including anxious feeling

behavior change similar to being drunk

blurred vision

cold sweats

confusion

cool pale skin

difficulty in concentrating

drowsiness

excessive hunger

fast heartbeat

headache

nausea

nervousness

nightmares

restless sleep

shakiness

slurred speech

unusual tiredness or weakness

Less common

Peeling of skin

skin redness, itching, or rash

Rare

Chest pain

chills

coughing up blood

dark urine

fever

fluid-filled skin blisters

general feeling of illness

increased amounts of sputum (phlegm)

increased sweating

light-colored stools

pale skin

sensitivity to the sun

shortness of breath

sore throat

thinning of the skin

unusual bleeding or bruising

unusual tiredness or weakness

yellow eyes or skin

Rarely, for patients taking chlorpropamide or tolbutamide

Depression

retain (keep) more body water than usual, even less often with tolbutamide

swelling or puffiness of face, ankles, or hands

Some 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. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

Changes in sense of taste

constipation

diarrhea

dizziness

heartburn

increased amount of urine or more frequent urination

increased or decreased appetite

passing of gas

stomach pain, fullness, or discomfort

vomiting

Less common or rare

Difficulty in focusing the eyes

increased sensitivity of skin to sun

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