July 27, 2016
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"The US Food and Drug Administration (FDA) has approved a once-daily oral combination of linagliptin and metformin hydrochloride (Jentadueto XR, Boehringer Ingelheim and Eli Lilly & Co) for treating adults with type 2 diabetes.



How Supplied


TOLINASE (tolazamide) Tablets are indicated as an adjunct to diet to lower the blood glucose in patients with non-insulin dependent diabetes mellitus (Type II) whose hyperglycemia cannot be satisfactorily controlled by diet alone.

In initiating treatment for noninsulin-dependent diabetes, diet should be emphasized as the primary form of treatment. Caloric restriction and weight loss are essential in the obese diabetic patient. Proper dietary management alone may be effective in controlling the blood glucose and symptoms of hyperglycemia. The importance of regular physical activity should also be stressed and cardiovascular risk factors should be identified and corrective measures taken where possible.

If this treatment program fails to reduce symptoms and/or blood glucose, the use of an oral sul-fonylurea or insulin should be considered. Use of TOLINASE (tolazamide) must be viewed by both the physician and patient as a treatment in addition to diet and not as a substitute for diet or as a convenient mechanism for avoiding dietary restraint. Furthermore, loss of blood glucose control on diet alone may be transient thus requiring only short-term administration of TOLINASE (tolazamide) .

During maintenance programs, TOLINASE (tolazamide) should be discontinued if satisfactory lowering of blood glucose is no longer achieved. Judgments should be based on regular clinical and laboratory evaluations.

In considering the use of TOLINASE (tolazamide) in asymp-tomatic patients, it should be recognized that controlling the blood glucose in noninsulin-dependent diabetes has not been definitely established to be effective in preventing the long-term cardiovascular or neural complications of diabetes.


There is no fixed dosage regimen for the management of diabetes mellitus with TOLINASE (tolazamide) Tablets or any other hypoglycemic agent. In addition to the usual monitoring of urinary glucose, the patientㆆs blood glucose must also be monitored periodically to determine the minimum effective dose for the patient; to detect primary failure, ie, inadequate lowering of blood glucose at the maximum recommended dose of medication; and to detect secondary failure, ie, loss of adequate blood glucose response after an initial period of effectiveness. Glycosylated hemoglobin levels may also be of value in monitoring the patientㆆs response to therapy.

Short-term administration of TOLINASE (tolazamide) may be sufficient during periods of transient loss of control in patients usually controlled well on diet.

Usual Starting Dose

The usual starting dose of TOLINASE (tolazamide) Tablets for the mild to moderately severe Type II diabetic patient is 100-250 mg daily administered with breakfast or the first main meal. Generally, if the fasting blood glucose is less than 200 mg/dl, the starting dose is 100 mg/day as a single daily dose. If the fasting blood glucose value is greater than 200 mg/dl, the starting dose is 250 mg/day as a single dose. If the patient is malnourished, underweight, elderly, or not eating properly, the initial therapy should be 100 mg once a day. Failure to follow an appropriate dosage regimen may precipitate hypoglycemia. Patients who do not adhere to their prescribed dietary regimen are more prone to exhibit unsatisfactory response to drug therapy.

Transfer From Other Hypoglycemic Therapy Patients Receiving Other Oral Antidiabetic TherapyㆆTransfer of patients from other oral antidiabetes regimens to TOLINASE (tolazamide) should be done conservatively. When transferring patients from oral hypoglycemic agents other than chlor-propamide to TOLINASE (tolazamide) , no transition period or initial or priming dose is necessary. When transferring from chlorpropamide, particular care should be exercised to avoid hypoglycemia.

Tolbutamide: If receiving less than 1 gm/day, begin at 100 mg of tolazamide per day. If receiving 1 gm or more per day, initiate at 250 mg of tolaza-mide per day as a single dose.

Chlorpropamide: 250 mg of chlorpropamide may be considered to provide approximately the same degree of blood glucose control as 250 mg of tolazamide. The patient should be observed carefully for hypoglycemia during the transition period from chlorpropamide to TOLINASE (tolazamide) (one to two weeks) due to the prolonged retention of chlor-propamide in the body and the possibility of a subsequent overlapping drug effect.

Acetohexamide: 100 mg of tolazamide may be considered to provide approximately the same degree of blood glucose control as 250 mg of ace-tohexamide.

Patients Receiving InsulinㆆSome Type II diabetic patients who have been treated only with insulin may respond satisfactorily to therapy with TOLINASE (tolazamide) . If the patientㆆs previous insulin dosage has been less than 20 units, substitution of 100 mg of tolazamide per day as a single daily dose may be tried. If the previous insulin dosage was less than 40 units, but more than 20 units, the patient should be placed directly on 250 mg of tolazamide per day as a single dose. If the previous insulin dosage was greater than 40 units, the insulin dosage should be decreased by 50% and 250 mg of tolazamide per day started. The dosage of TOLINASE (tolazamide) should be adjusted weekly (or more often in the group previously requiring more than 40 units of insulin).

During this conversion period when both insulin and TOLINASE (tolazamide) are being used, hypoglycemia may rarely occur. During insulin withdrawal, patients should test their urine for glucose and acetone at least three times daily and report results to their physician. The appearance of persistent acetonuria with glycosuria indicates that the patient is a Type I diabetic who requires insulin therapy.

Maximum Dose

Daily doses of greater than 1000 mg are not recommended. Patients will generally have no further response to doses larger than this.

Usual Maintenance Dose

The usual maintenance dose is in the range of 100-1000 mg/day with the average maintenance dose being 250-500 mg/day. Following initiation of therapy, dosage adjustment is made in increments of 100 mg to 250 mg at weekly intervals based on the patientㆆs blood glucose response.

Dosage Interval

Once a day therapy is usually satisfactory. Doses up to 500 mg/day should be given as a single dose in the morning. 500 mg once daily is as effective as 250 mg twice daily. When a dose of more than 500 mg/day is required, the dose may be divided and given twice daily.

In elderly patients, debilitated or malnourished patients, and patients with impaired renal or hep-atic function, the initial and maintenance dosing should be conservative to avoid hypoglycemic reactions (see PRECAUTIONS section).


TOLINASE (tolazamide) Tablets are available in the following strengths and package sizes:

100 mg (white, round, scored, imprinted TOLINASE (tolazamide) 100)

Unit-of-Use Bottles of 100

NDC 0009-0070-02

250 mg (white, round, scored, imprinted TOLINASE (tolazamide) 250)

Bottles of 200

NDC 0009-0114-04

Bottles of 1000

NDC 0009-0114-02

Unit-of-Use Bottles of 100

NDC 0009-0114-05

500 mg (white, round, scored, imprinted TOLINASE (tolazamide) 500)

Unit-of-Use Bottles of 100

NDC 0009-0477-06

Store at controlled room temperature 20° to 25°C (68° to 77°F) [see USP].

Pharmacia & Upjohn Company, Kalamazoo, Michigan 49001, USA, Revised January 2000

This monograph has been modified to include the generic and brand name in many instances.

Last reviewed on RxList: 12/8/2004

How Supplied

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