Tolbutamide
Tolbutamide Uses, Dosage, Side Effects, Food Interaction and all others data.
Tolbutamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It is structurally similar to acetohexamide, chlorpropamide and tolazamide and belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Tolbutamide appears to be metabolized in the liver. Tolbutamide and its metabolites are excreted in urine (75-85%) and feces.
Tolbutamide, a first-generation sulfonylurea antidiabetic agent, is used with diet to lower blood glucose levels in patients with diabetes mellitus type II. Tolbutamide is twice as potent as the related second-generation agent glipizide. Tolbutamide lowers blood sugar by stimulating the pancreas to secrete insulin and helping the body use insulin efficiently. The pancreas must be able to produce insulin for this drug to work.
| Trade Name | Tolbutamide |
| Availability | Discontinued |
| Generic | Tolbutamide |
| Tolbutamide Other Names | Tolbutamida, Tolbutamide, Tolbutamidum, Tolylsulfonylbutylurea |
| Related Drugs | Farxiga, metformin, Trulicity, Lantus, Victoza, Tresiba, Levemir |
| Weight | 500mg, |
| Type | Oral tablet |
| Formula | C12H18N2O3S |
| Weight | Average: 270.348 Monoisotopic: 270.103813142 |
| Protein binding | Approximately 95% bound to plasma proteins. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | Pharmachemie |
| Available Country | United States, Netherlands |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Tolbutamide is a sulfonylurea used to treat hyperglycemia in patients with type 2 diabetes mellitus.
For treatment of NIDDM (non-insulin-dependent diabetes mellitus) in conjunction with diet and exercise.
Tolbutamide is also used to associated treatment for these conditions: Type 2 Diabetes Mellitus
How Tolbutamide works
Sulfonylureas lower blood glucose in patients with NIDDM by directly stimulating the acute release of insulin from functioning beta cells of pancreatic islet tissue by an unknown process that involves a sulfonylurea receptor (receptor 1) on the beta cell. Sulfonylureas inhibit the ATP-potassium channels on the beta cell membrane and potassium efflux, which results in depolarization and calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis, an effect similar to that of glucose.
Toxicity
Oral, mouse: LD50 = 2600 mg/kg
Food Interaction
- Avoid alcohol. Ingesting alcohol may precipitate a disulfiram-like reaction (flushing, nausea), or hypoglycemia.
- Take with or without food.
[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.
Tolbutamide Drug Interaction
Moderate: epinephrine, sulfamethoxazole / trimethoprim, aspirin, insulin glargine, furosemideUnknown: amphetamine / dextroamphetamine, spironolactone, zolpidem, amoxicillin / clavulanate, docusate, losartan, ipratropium, atorvastatin, methotrexate, mexiletine, mometasone nasal, acetaminophen / hydrocodone, oxycodone, acetaminophen, tiotropium
Tolbutamide Disease Interaction
Major: cardiovascular risk, DKA, renal/liver diseaseModerate: hypoglycemia, G6PD deficiency, hyponatremia
Elimination Route
Readily absorbed following oral administration. Tolbutamide is detectable in plasma 30-60 minutes following oral administration of a single dose with peak plasma concentrations occurring within 3-5 hours.
Absorption is unaltered if taken with food but is increased with high pH.
Half Life
Approximately 7 hours with interindividual variations ranging from 4-25 hours. Tolbutamide has the shortest duration of action, 6-12 hours, of the antidiabetic sulfonylureas.
Elimination Route
Unchanged drug and metabolites are eliminated in the urine and feces. Approximately 75-85% of a single orally administered dose is excreted in the urine principally as the 1-butyl-3-p-carboxyphenylsulfonylurea within 24 hours.
Innovators Monograph
You find simplified version here Tolbutamide
