Tolazamide

Tolazamide is a prescription medication used to treat type 2 diabetes.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with tolazamide. See the “Tolazamide Precautions” section.

Common side effects of tolazamide include the following:

• nausea
• a feeling of fullness in the upper abdomen
• heartburn

This is not a complete list of tolazamide side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Tolazamide is usually taken once a day, with breakfast or the first main meal of the day. Follow your doctor's instructions.

Your blood sugar will need to be checked often, and you may need other blood tests at your doctor's office.

Low blood sugar (hypoglycemia) can happen to everyone who has diabetes. Symptoms include headache, hunger, sweating, confusion, irritability, dizziness, or feeling shaky. Always keep a source of sugar with you in case you have low blood sugar. Sugar sources include fruit juice, hard candy, crackers, raisins, and non-diet soda. Be sure your family and close friends know how to help you in an emergency.

If you have severe hypoglycemia and cannot eat or drink, use a glucagon injection. Your doctor can prescribe a glucagon emergency injection kit and tell you how to use it.

Also watch for signs of high blood sugar (hyperglycemia) such as increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, and weight loss.

Check your blood sugar carefully during times of stress, travel, illness, surgery or medical emergency, vigorous exercise, or if you drink alcohol or skip meals. These things can affect your glucose levels and your dose needs may also change. Do not change your medication dose or schedule without your doctor's advice.

Use tolazamide regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.

Tolazamide is only part of a treatment program that may also include diet, exercise, weight control, regular blood sugar testing, and special medical care. Follow your doctor's instructions very closely.

Store at room temperature away from moisture and heat.

Take the missed dose as soon as you remember (be sure to take the medicine with food). Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Get emergency medical help if you have signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

• severe skin rash, redness, or itching;

• easy bruising or bleeding,

• fever, chills, sore throat, mouth sores;

• pale or yellowed skin, dark colored urine;

• low blood sugar--headache, hunger, weakness, sweating, confusion, irritability, dizziness, fast heart rate, or feeling jittery; or

• low levels of sodium in the body--headache, confusion, slurred speech, severe weakness, vomiting, loss of coordination, feeling unsteady.

Common side effects may include:

• nausea;

• heartburn; or

• full feeling.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Usual Adult Dose for Diabetes Type 2:

Initial dose: 100 to 250 mg orally once a day
-Adjust dose based on blood glucose response
Maintenance dose: Average 250 to 500 mg/day; range: 100 to 1000 mg per day
-For doses greater than 500 mg, the dose maybe divided and given twice a day
Maximum dose: 1000 mg per day

Comments:
-For patients with a fasting blood glucose less than 200 mg/dL, the usual starting dose is 100 mg per day.
-Patients will generally have no further response to doses greater than 1000 mg/day
-Transferring patients from other antidiabetic regimens should be done conservatively: see dose adjustment section.

Use: As an adjunct to diet to lower blood glucose in patients with type 2 diabetes whose hyperglycemia cannot be controlled by diet alone.

Usual Geriatric Dose for Diabetes Type 2:

Initial dose: 100 mg orally once a day

Storage

Oral

Tight, light-resistant containers at 20–25°C.a b Protect from light.b

• Mechanism of long-term hypoglycemic action of sulfonylurea antidiabetic agents has not been clearly established.b Appears to lower blood glucose concentration principally by stimulating the secretion of endogenous insulin from the beta cells of the pancreas.a b

• Ineffective in the absence of functioning beta cells.a

• Lowers blood glucose concentration in diabetic and nondiabetic individuals.a b

• During prolonged administration, extrapancreatic effects (e.g., enhanced peripheral sensitivity to insulin, reduction of basal hepatic glucose production) may contribute to the hypoglycemic action.a b

• A gradual decline in the insulin secretory response to drug may occur; however, blood glucose lowering effect persists.b

• May produce a mild diuresis by enhancement of renal free water clearance.b

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 tolazamide, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to tolazamide 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.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of tolazamide in the pediatric population. Safety and efficacy have not been established .

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of tolazamide in the elderly. However, elderly patients are more likely to have age-related liver or kidney problems, which may require an adjustment of dosage in patients receiving tolazamide .

Pregnancy

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with 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. When you are taking tolazamide, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using tolazamide 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
• Aspirin
• Balofloxacin
• Besifloxacin
• Ciprofloxacin
• Disopyramide
• Dulaglutide
• Enoxacin
• Fleroxacin
• Flumequine
• Gatifloxacin
• Gemifloxacin
• Lanreotide
• Levofloxacin
• Lixisenatide
• Lomefloxacin
• Moxifloxacin
• Nadifloxacin
• Norfloxacin
• Octreotide
• Ofloxacin
• Pasireotide
• Pazufloxacin
• Pefloxacin
• Pioglitazone
• Prulifloxacin
• Rufloxacin
• Sparfloxacin
• Thioctic Acid
• Tosufloxacin

Using tolazamide with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Acebutolol
• Aminolevulinic Acid
• Atenolol
• Betaxolol
• Bisoprolol
• Bitter Melon
• Carteolol
• Carvedilol
• Celiprolol
• Clofibrate
• Esmolol
• Fenugreek
• Furazolidone
• Glucomannan
• Guar Gum
• Iproniazid
• Isocarboxazid
• Labetalol
• Levobunolol
• Linezolid
• Methylene Blue
• Metipranolol
• Metoprolol
• Moclobemide
• Nadolol
• Nebivolol
• Nialamide
• Oxprenolol
• Penbutolol
• Phenelzine
• Pindolol
• Practolol
• Procarbazine
• Propranolol
• Psyllium
• Rasagiline
• Safinamide
• Saxagliptin
• Selegiline
• Sotalol
• Timolol
• Tranylcypromine

Interactions with Food/Tobacco/Alcohol

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 tolazamide 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 tolazamide, 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 tolazamide. Make sure you tell your doctor if you have any other medical problems, especially:

• Alcohol intoxication or
• Underactive adrenal glands or
• Underactive pituitary gland 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 tolazamide .

• Diabetic ketoacidosis (ketones in the blood) or
• Type I diabetes—Should not be used in patients with these conditions .

• Fever or
• Infection or
• Surgery or
• Trauma—These conditions may cause temporary problems with blood sugar control and your doctor may want to treat you temporarily with insulin .

• Heart disease—Use with caution. May make this condition worse .

• Kidney disease or
• Liver disease—Higher blood levels of tolazamide may occur, which may cause serious problems .

Use tolazamide as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Take with meals.
• Take with the first meal of the day, if taking once a day.
• To gain the most benefit, do not miss doses.
• Keep taking this medicine as you have been told by your doctor or other health care provider, even if you feel well.

What do I do if I miss a dose?

• Take a missed dose as soon as you think about it, with a meal.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

Tolazamide is an oral blood-glucose-lowering drug of the sulfonylurea class. Tolazamide is a white or creamy-white powder very slightly soluble in water and slightly soluble in alcohol.

The chemical name is 1-(Hexahydro-1H-azepin-1-yl)-3-(p-tolylsulfonyl)urea. Tolazamide has the following structural formula:

C14H21N3O3S          M.W. 311.40

Each tablet for oral administration contains 250 mg or 500 mg of Tolazamide, USP and the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, microcrystalline cellulose, and sodium lauryl sulfate.

Tolazamide tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Tolazamide is contraindicated in patients with:

Tolazamide Tablets, USP are available containing either 250 mg or 500 mg of Tolazamide, USP.

The 250 mg tablets are white to off-white, round, scored tablets debossed with MYLAN above the score and 217 below the score on one side of the tablet and 250 on the other side. They are available as follows:

NDC 0378-0217-01
bottles of 100 tablets

The 500 mg tablets are white to off-white, round, scored tablets debossed with MYLAN above the score and 551 below the score on one side of the tablet and blank on the other side. They are available as follows:

NDC 0378-0551-01
bottles of 100 tablets

Store at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature].

Protect from light.

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

Mylan Pharmaceuticals Inc.
Morgantown, WV 26505

REVISED DECEMBER 2009
TLZ:R17

PRINCIPAL DISPLAY PANEL - 250 mg

NDC 0378-0217-01

Tolazamide
Tablets, USP
250 mg

Rx only      100 Tablets

Each tablet contains:
Tolazamide, USP           250 mg

Dispense in a tight, light-resistant
container as defined in the USP
using a child-resistant closure.

Keep container tightly closed.

Keep this and all medication
out of the reach of children.

Store at 20° to 25°C (68° to 77°F).
[See USP Controlled Room
Temperature.]

Protect from light.

Usual Adult Dosage: See
accompanying prescribing
information.

Mylan Pharmaceuticals Inc.
Morgantown, WV 26505 U.S.A.

Mylan.com

RM0217A12

PRINCIPAL DISPLAY PANEL - 500 mg

NDC 0378-0551-01

Tolazamide
Tablets, USP
500 mg

Rx only      100 Tablets

Each tablet contains:
Tolazamide, USP          500 mg

Dispense in a tight, light-resistant
container as defined in the USP
using a child-resistant closure.

Keep container tightly closed.

Keep this and all medication
out of the reach of children.

Store at 20° to 25°C (68° to 77°F).
[See USP Controlled Room
Temperature.]

Protect from light.

Usual Adult Dosage: See
accompanying prescribing
information.

Mylan Pharmaceuticals Inc.
Morgantown, WV 26505 U.S.A.

Mylan.com

RM0551A11

10-24 hours

Half-Life Elimination

7 hours

Protein Binding

94%

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience nausea, heartburn, or bloating. Have patient report immediately to prescriber severe dizziness, passing out, bruising, bleeding, severe loss of strength and energy, chills, pharyngitis, or signs of low blood sugar (dizziness, headache, fatigue, feeling weak, shaking, a fast heartbeat, confusion, hunger, or sweating) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Initial dose: 100 mg orally once a day

Substance Name

Tolazamide

CAS Registry Number

1156-19-0

Drug Class

Hypoglycemic Agents

Sulfonylurea Compounds