Tolazamid

Tolazamid Uses, Dosage, Side Effects, Food Interaction and all others data.

A sulphonylurea hypoglycemic agent with actions and uses similar to those of chlorpropamide.

Tolazamid is an oral blood glucose lowering drug of the sulfonylurea class. Tolazamid appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which tolazamide lowers blood glucose during long-term administration has not been clearly established. With chronic administration in Type II diabetic patients, the blood glucose lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonylurea hypoglycemic drugs. Some patients who are initially responsive to oral hypoglycemic drugs, including tolazamide, may become unresponsive or poorly responsive over time. Alternatively, tolazamide may be effective in some patients who have become unresponsive to one or more other sulfonylurea drugs. In addition to its blood glucose lowering actions, tolazamide produces a mild diuresis by enhancement of renal free water clearance.

Trade Name Tolazamid
Availability Discontinued
Generic Tolazamide
Tolazamide Other Names Tolazamid, Tolazamida, Tolazamide, Tolazamidum
Related Drugs Farxiga, metformin, Trulicity, Lantus, Victoza, Tresiba, Levemir
Type
Formula C14H21N3O3S
Weight Average: 311.4
Monoisotopic: 311.130362243
Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Tolazamid
Tolazamid

Uses

Tolazamid is a sulfonylurea used in the treatment of non insulin dependent diabetes mellitus.

For use 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.

Tolazamid is also used to associated treatment for these conditions: Type 2 Diabetes Mellitus

How Tolazamid works

Sulfonylureas likely bind to ATP-sensitive potassium-channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin.

Toxicity

Overdosage of sulfonylureas can produce hypoglycemia. Severe hypoglycemic reactions with coma, seizure, or other neurological impairment occur infrequently, but constitute medical emergencies requiring immediate hospitalization.

Food Interaction

  • Avoid excessive or chronic alcohol consumption. Ingesting alcohol may increase the risk of hypoglycemia.
  • Take with food. Taking tolazamide with breakfast may help reduce the risk of hypoglycemia.

[Moderate] GENERALLY AVOID: Alcohol may cause hypoglycemia or hyperglycemia in patients with diabetes.

Hypoglycemia most frequently occurs during acute consumption of alcohol.

Even modest amounts can lower blood sugar significantly, especially when the alcohol is ingested on an empty stomach or following exercise.

The mechanism involves inhibition of both gluconeogenesis as well as the counter-regulatory response to hypoglycemia.

Episodes of hypoglycemia may last for 8 to 12 hours after ethanol ingestion.

By contrast, chronic alcohol abuse can cause impaired glucose tolerance and hyperglycemia.

Moderate alcohol consumption generally does not affect blood glucose levels in patients with well controlled diabetes.

A disulfiram-like reaction (e.g., flushing, headache, and nausea) to alcohol has been reported frequently with the use of chlorpropamide and very rarely with other sulfonylureas.

MANAGEMENT: Patients with diabetes should avoid consuming alcohol if their blood glucose is not well controlled, or if they have hypertriglyceridemia, neuropathy, or pancreatitis.

Patients with well controlled diabetes should limit their alcohol intake to one drink daily for women and two drinks daily for men (1 drink = 5 oz wine, 12 oz beer, or 1.5 oz distilled spirits) in conjunction with their normal meal plan.

Alcohol should not be consumed on an empty stomach or following exercise.

Elimination Route

Rapidly and well absorbed from the gastrointestinal tract.

Half Life

The average biological half-life of the drug is 7 hours.

Elimination Route

Tolazamid is metabolized to five major metabolites ranging in hypoglycemic activity from 0% to 70%. They are excreted principally in the urine.

Innovators Monograph

You find simplified version here Tolazamid

*** Taking medicines without doctor's advice can cause long-term problems.
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