Apo-Tolbutamide - General Information
A sulphonylurea hypoglycemic agent with actions and uses similar to those of chlorpropamide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290)
Pharmacology of Apo-Tolbutamide
Apo-Tolbutamide, a second-generation sulfonylurea antidiabetic agent, is used with diet to lower blood glucose levels in patients with diabetes mellitus type II. Apo-Tolbutamide is twice as potent as the related second-generation agent glipizide. Apo-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.
Apo-Tolbutamide for patients
Treatment with tolbutamide may increase the risk of death from cardiovascular disease compared to treatment of diabetes with diet alone or diet plus insulin. Discuss with your doctor the risks and benefits of treatment with tolbutamide. Know the signs and symptoms of low blood sugar (hypoglycemia), which include headache, drowsiness, weakness, dizziness, fast heartbeat, sweating, tremor, and nausea. Carry a piece of hard candy or glucose tablets with you to treat episodes of low blood sugar. Follow your diet, medication, and exercise routines closely. Changing any of them can affect blood sugar levels. Do not change your dose of tolbutamide without first talking to your doctor. Avoid alcohol. It lowers blood sugar and may interfere with your diabetes treatment.
Sulphinpyrazone, a drug used as an antithrombotic agent and inhibitor of platelet aggregation has a potent side effect as a uricosuric agent. The uricosuric side effect increases the urinary excretion of uric acid effectively blocking hepatic conjugation. Tests show that Sulphinpyrazone’s effect on Tolbutamide is a reduction of liver function to 60% of normal without interfering with protein binding. Taking alpha-lipoic acid or chromium with tolbutamide may require a change in the drug's dosage. Use ephedra with caution when taking tolbutamide; ephedra can raise blood sugar levels.
You should not take tolbutamide if you have had an allergic reaction to it. Tolbutamide should not be taken if you are suffering from diabetic ketoacidosis (a life-threatening medical emergency caused by insufficient insulin and marked by excessive thirst, nausea, fatigue, pain below the breastbone, and fruity breath). In addition, Tolbutamide should not be used as the sole therapy in treating type 1 (insulin-dependent) diabetes.
Additional information about Apo-Tolbutamide
Apo-Tolbutamide Indication: Used as an oral hypoglycemic agent in non-insulin-dependent (type 2) Diabetes Miletus with adult onset.
Mechanism Of Action: Sulfonylureas lower blood glucose in patients with type 2 diabetes 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Tolbutamide
Synonyms: Not Available
Drug Category: Hypoglycemic Agents; Sulfonylureas
Drug Type: Small Molecule; Approved
Other Brand Names containing Tolbutamide: Aglicid; Apo-Tolbutamide; Arkozal; Artosin; Artozin; Butamid; Butamide; Diaben; Diabetamid; Diabetol; Diabuton; Diasulfon; Dirastan; Dolipol; Drabet; Glyconon; Ipoglicone; Mobenol; Novo-Butamide; Orabet; Oralin; Orezan; Orinase; Orinase Diagnostic; Orinaz; Oterben; Pramidex; Rastinon; Restinon; Sk-tolbutamide; Tol-Tab; Tolbusal; Tolbutamid; Toluina; Tolumid; Toluvan; Tolylsulfonylbutylurea; Willbutamide;
Absorption: Well absorbed. Absorption is unaltered if taken with food but is increased with high pH.
Toxicity (Overdose): Oral, mouse: LD50 = 2600 mg/kg
Protein Binding: 96%
Half Life: 4.5-6.5 hours in normal adults
Dosage Forms of Apo-Tolbutamide: Tablet Oral
Chemical IUPAC Name: 1-butyl-3-(4-methylphenyl)sulfonylurea
Chemical Formula: C12H18N2O3S
Tolbutamide on Wikipedia: http://en.wikipedia.org/wiki/Tolbutamide
Organisms Affected: Humans and other mammals