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RX BIN: 015558RX PCN: HTGroup ID: DDN6600Card Holder ID: DDN6600
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2019 Price of Orinase

$95.24200 tablets/500 mg
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Tolbutamide volume of distribution

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.

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2018 Statistics

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Discount Cards 16,000+


Clients Benefit 29%


Total savings $4,735,080

What is Tolbutamide

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 . 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 . 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 mechanism of action

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.

Dosage forms of Tolbutamide

Tabletoral1 g
Tabletoral500 mg/1
Tabletoral500 mg

Prescription Generics


International Brands

Mobenol Tablets 500mg


1-Butyl-3-(P-methylphenylsulfonyl)urea 1-Butyl-3-(P-tolylsulfonyl)urea


Carter Horner Corp.

CAS number






Affected organisms

Humans and other mammals

Indication of Tolbutamide

For treatment of NIDDM (non-insulin-dependent diabetes mellitus) in conjunction with diet and exercise.

Toxicity of Tolbutamide

Oral, mouse: LD sub50 /sub = 2600 mg/kg

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