Tolbutamide

Indications
 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.
Contraindications
 Diabetes complicated by ketosis, acidosis, diabetic coma; as sole therapy in IDDM; severe renal impairment.
Warnings / 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.
Adverse Reactions
 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.
Overdose Reactions
 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 inj 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 hr as hypoglycaemia may recur.
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.
See Below for More tolbutamide Drug Interactions
Lab Interactions
 May give false-positive result for urinary albumin with test using heat and acetic acid or sulfosalicylic acid. Tolbutamide may interfere with test results of radioactive iodine uptake by decreasing uptake of radioactive iodine.
Mechanism of Actions
 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 hr.
Absorption: Readily absorbed from the GI tract.
Distribution: Protein-binding: Extensive (95%). Half-life: 4-25 hr. 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.
Administration
 Should be taken with food.
Storage Conditions
 Oral: Store at 15-30°C.
ATC Classification
 A10BB03 - tolbutamide ; Belongs to the class of sulfonamides, urea derivatives. Used in the treatment of diabetes.
V04CA01 - tolbutamide ; Belongs to the class of diagnostic agents used to test for diabetes.
Storage
 Oral: Store at 15-30°C.
Available As
  • Tolbutamide 500 mg

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