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Tolbutamide information from DrugsUpdate  

See Available Brands of Tolbutamide in India

P - Caution when used during pregnancy
L - Caution when used during lactation
LI - Lab *

Tolbutamide is a first generation potassium channel blocker, sulfonylurea oral hypoglycemic drug sold under the brand name Orinase. This drug may be used in the management of type II diabetes if diet alone is not effective. Tolbutamide stimulates the secretion of insulin by the pancreas. Since the pancreas must synthesize insulin in order for this drug to work, it is not effective in the management of type I diabetes. It is not routinely used due to a higher incidence of adverse effects compared to newer second generation sulfonylureas, such as glyburide.

Pharmacodynamics

Pharmacokinetics

Tolbutamide acts mainly by enhancing insulin secretion and is only effective when some residual pancreatic β-cell activity is present. It may enhance peripheral sensitivity to insulin and reduce basal hepatic glucose production during long-term admin.

Duration
10 hours.

Absorption
Readily absorbed from the GI tract.

Distribution
Protein-binding: Extensive (95%). Half-life: 4-25 hours. Distributed into breastmilk.

Metabolism
Metabolised in the liver by cytochrome P450 isoenzyme CYP2C9.

Excretion

Excreted in the urine mainly as metabolites with little hypoglycaemic activity.

Tolbutamide Indications / Tolbutamide Uses

Information Not Available

Tolbutamide Adverse Reactions / Tolbutamide Side Effects

Hypoglycaemia, nausea, epigastric fullness, heartburn, headache, allergic skin reactions, jaundice, hyponatraemia, hepatic dysfunction, photosensitivity, syndrome of inappropriate secretion of antidiuretic hormone (SIADH) and blood dyscrasias.

Precautions

Overdosage
Symptoms: Hypoglycaemia. Management: In mild hypoglycemia without loss of consciousness or neurologic findings, treat with oral glucose, drug dosage and meal patterns adjustments. In severe hypoglycaemia with coma, seizure or other neurological impairment, immediate hospitalisation is needed. In hypoglycaemic coma, rapid IV injection of concentrated (50%) dextrose, followed by continuous infusion of a more dilute (10%) dextrose inj in order to maintain the blood glucose > 100 mg/dl. Monitor closely for a minimum of 24-48 hours as hypoglycaemia may recur.

Special Precautions

Renal, hepatic, adrenocortical or thyroid function impairment; stress due to surgery or trauma, history of hepatic porphyria. Pregnancy and lactation. Frequently monitor glucose and hepatic function during initial phase.

Other Drug Interactions

Hypoglycaemic symptoms masked by β-blockers. Hypoglycaemic effect reduced by corticosteroids, thiazide diuretics, β-blockers, niacin, oral contraceptives, sympathomimetics, thyroid preparations, estrogens, phenytoin, phenothiazines, calcium-channel blocking agents and isoniazid. Hypoglycaemic effect enhanced by dicoumarol, salicylates, phenylbutazone, fibrates (e.g. clofibrate, gemfibrozil), chloramphenicol, cyclophosphamide and azole antifungals. Disulfiram-like reaction with alcohol.

Other Interactions

Information Not Available

Dosage

Oral
Type 2 diabetes mellitus
Adult: Initially, 1-2 g daily, given either as a single dose with breakfast or, more commonly in divided doses. Maintenance dose: 0.25-2 g daily. Max: 3 g daily.
Elderly: Dose adjustments may be needed.

Renal impairment: Dose adjustments may be needed.
Hepatic impairment: Dose adjustments may be needed.

Intravenous
Diagnosis of insulinoma and other pancreatic disorders
Adult: 1 g IV as a 5% solution over 2-3 minutes.
Elderly: Dose adjustments may be needed.

Renal impairment: Dose adjustments may be needed.
Hepatic impairment: Dose adjustments may be needed.

Food(before/after)

Should be taken with food

List of Contraindications

Tolbutamide and Pregnancy

Caution when used during pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Tolbutamide and Lactation

Caution when used during lactation

Tolbutamide and Children

Safety and efficacy have not been established

Tolbutamide and Geriatic

Particularly susceptible to hypoglycemic action. Hypoglycemia may be difficult to recognize in elderly.

Tolbutamide and Other Contraindications

Diabetes complicated by ketosis, acidosis, diabetic coma; as sole therapy in IDDM; severe renal impairment.

Storage

Oral
Store at 15-30°C

Lab interference

Oral
Store at 15-30°C

Tolbutamide brands in India:

Rastinone

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