Disclaimer:
Medidex is not a provider of medical services and all information is provided for the convenience of the user. No medical decisions should be made based on the information provided on this website without first consulting a licensed healthcare provider.This website is intended for persons 18 years or older. No person under 18 should consult this website without the permission of a parent or guardian.
tolbutamide
Overview
What is Tolbutamide?
Tolbutamide is an oral blood-glucose-lowering drug of the sulfonylurea class. Tolbutamide is a pure, white, crystalline compound which is practically insoluble in water. The chemical name is benzenesulfonamide, N-[(butylamino)-carbonyl]-4-methyl-. Its structure can be represented as follows:
Tolbutamide is supplied as compressed tablets containing 500 mg of tolbutamide, USP.
Each tablet for oral administration contains 500 mg of tolbutamide and the following inactive ingredients: colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose, sodium lauryl sulfate and sodium starch glycolate.
What does Tolbutamide look like?
What are the available doses of Tolbutamide?
Sorry No records found.
What should I talk to my health care provider before I take Tolbutamide?
Sorry No records found
How should I use Tolbutamide?
Tolbutamide tablets are indicated as an adjunct to diet to lower the blood glucose in patients with non-insulin-dependent diabetes mellitus (type II) whose hyperglycemia cannot be controlled by diet alone.
In initiating treatment for non-insulin-dependent diabetes, diet should be emphasized as the primary form of treatment. Caloric restriction and weight loss are essential in the obese diabetic patient. Proper dietary management alone may be effective in controlling the blood glucose and symptoms of hyperglycemia. The importance of regular physical activity should also be stressed, and cardiovascular risk factors should be identified and corrective measures taken where possible.
If this treatment program fails to reduce symptoms and/or blood glucose, the use of an oral sulfonylurea or insulin should be considered. Use of tolbutamide tablets must be viewed by both the physician and patient as a treatment in addition to diet, and not as a substitute for diet or as a convenient mechanism for avoiding dietary restraint. Furthermore, loss of blood glucose control on diet alone may be transient, thus requiring only short-term administration of tolbutamide tablets.
During maintenance programs, tolbutamide tablets should be discontinued if satisfactory lowering of blood glucose is no longer achieved. Judgments should be based on regular clinical and laboratory evaluations.
In considering the use of tolbutamide tablets in asymptomatic patients, it should be recognized that controlling the blood glucose in non-insulin dependent diabetes has not been definitely established to be effective in preventing the long-term cardiovascular or neural complications of diabetes.
There is no fixed dosage regimen for the management of diabetes mellitus with tolbutamide tablets or any other hypoglycemic agent. In addition to the usual monitoring of urinary glucose, the patient's blood glucose must also be monitored periodically to determine the minimum effective dose for the patient; to detect primary failure, i.e., inadequate lowering of blood glucose at the maximum recommended dose of medication; and to detect secondary failure, i.e., loss of an adequate blood glucose lowering response after an initial period of effectiveness. Glycosylated hemoglobin levels may also be of value in monitoring the patient's response to therapy.
Short-term administration of tolbutamide tablets may be sufficient during periods of transient loss of control in patients usually controlled well on diet.
What interacts with Tolbutamide?
- Tolbutamide tablets are contraindicated in patients with:
- 1.
- 2.
- 3.
What are the warnings of Tolbutamide?
SPECIAL WARNING ON INCREASED RISK OF CARDIOVASCULAR MORTALITY
The administration of oral hypoglycemic drugs has been reported to be associated with increased cardiovascular mortality as compared to treatment with diet alone or diet plus insulin. This warning is based on the study conducted by the University Group Diabetes Program (UGDP), a long-term prospective clinical trial designed to evaluate the effectiveness of glucose-lowering drugs in preventing or delaying vascular complications in patients with non-insulin-dependent diabetes. The study involved 823 patients who were randomly assigned to one of four treatment groups (Diabetes, 19 (supp.2):747-830, 1970).
UGDP reported that patients treated for 5 to 8 years with diet plus a fixed dose of tolbutamide (1.5 grams per day) had a rate of cardiovascular mortality approximately 2½ times that of patients treated with diet alone. A significant increase in total mortality was not observed, but the use of tolbutamide was discontinued based on the increase in cardiovascular mortality, thus limiting the opportunity for the study to show an increase in overall mortality. Despite controversy regarding the interpretation of these results, the findings of the UGDP study provide an adequate basis for this warning. The patient should be informed of the potential risks and advantages of tolbutamide and of alternative modes of therapy. Although only one drug in the sulfonylurea class (tolbutamide) was included in this study, it is prudent from a safety standpoint to consider that this warning may also apply to other oral hypoglycemic drugs in this class, in view of their close similarities in mode of action and chemical structure.
What are the precautions of Tolbutamide?
General
Array
All sulfonylurea drugs are capable of producing severe hypoglycemia. Proper patient selection, dosage, and instructions are important to avoid hypoglycemic episodes. Renal or hepatic insufficiency may cause elevated blood levels of tolbutamide and the latter may also diminish gluconeogenic capacity, both of which increase the risk of serious hypoglycemic reactions. Elderly, debilitated or malnourished patients, and those with adrenal or pituitary insufficiency are particularly susceptible to the hypoglycemic action of glucose-lowering drugs. Hypoglycemia may be difficult to recognize in the elderly, and in people who are taking beta-adrenergic blocking drugs. Hypoglycemia is more likely to occur when caloric intake is deficient, after severe or prolonged exercise, when alcohol is ingested, or when more than one glucose-lowering drug is used.
Array
Hemolytic Anemia
Treatment of patients with glucose 6-phosphate dehydrogenase (G6PD) deficiency with sulfonylurea agents can lead to hemolytic anemia. Because tolbutamide belongs to the class of sulfonylurea agents, caution should be used in patients with G6PD deficiency and a non-sulfonylurea alternative should be considered. In post-marketing reports, hemolytic anemia has also been reported in patients who did not have known G6PD deficiency.
Information for Patients
Patients should be informed of the potential risks and advantages of tolbutamide and of alternative modes of therapy. They should also be informed about the importance of adherence to dietary instructions, of a regular exercise program, and of regular testing of urine and/or blood glucose.
The risks of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development should be explained to patients and responsible family members. Primary and secondary failure should also be explained.
Laboratory Tests
Blood and urine glucose should be monitored periodically. Measurement of glycosylated hemoglobin may be useful.
A metabolite of tolbutamide in urine may give a false positive reaction for albumin if measured by the acidification-after-boiling test, which causes the metabolite to precipitate. There is no interference with the sulfosalicylic acid test.
Drug Interactions
The hypoglycemia action of sulfonylurea may be potentiated by certain drugs including non-steroidal anti-inflammatory agents and other drugs that are highly protein bound, salicylates, sulfonamides, chloramphenicol, probenecid, coumarins, monoamine oxidase inhibitors, and beta-adrenergic blocking agents. When such drugs are administered to a patient receiving tolbutamide, the patient should be observed closely for hypoglycemia. When such drugs are withdrawn from a patient receiving tolbutamide, the patient should be observed closely for loss of control.
Certain drugs tend to produce hyperglycemia and may lead to loss of control. These drugs include the thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs, and isoniazid. When such drugs are administered to a patient receiving tolbutamide, the patient should be closely observed for loss of control. When such drugs are withdrawn from a patient receiving tolbutamide, the patient should be observed closely for hypoglycemia.
A potential interaction between oral miconazole and oral hypoglycemic agents leading to severe hypoglycemia has been reported. Whether this interaction also occurs with the intravenous, topical or vaginal preparations of miconazole is not known.
Carcinogenicity and Mutagenicity
Bioassay for carcinogenicity was performed in both sexes of rats and mice following ingestion of tolbutamide for 78 weeks. No evidence of carcinogenicity was found.
Tolbutamide has also been demonstrated to be nonmutagenic in the Ames salmonella/mammalian microsome mutagenicity test.
Pregnancy
Array
Array
Prolonged severe hypoglycemia (4 to 10 days) has been reported in neonates born to mothers who were receiving a sulfonylurea drug at the time of delivery. This has been reported more frequently with the use of agents with prolonged half-lives. If tolbutamide is used during pregnancy, it should be discontinued at least 2 weeks before the expected delivery date.
Nursing Mothers
Although it is not known whether tolbutamide is excreted in human milk, some sulfonylurea drugs are known to be excreted in human milk. Because the potential for hypoglycemia in nursing infants may exist, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. If the drug is discontinued and if diet alone is inadequate for controlling blood glucose, insulin therapy should be considered.
Pediatric Use
Safety and effectiveness in children have not been established.
What are the side effects of Tolbutamide?
Hypoglycemia
See and .
Gastrointestinal Reactions
Cholestatic jaundice may occur rarely; tolbutamide should be discontinued if this occurs. Gastrointestinal disturbances, e.g., nausea, epigastric fullness, and heartburn, are the most common reactions and occur in 1.4% of patients treated during clinical trial. They tend to be dose related and may disappear when dosage is reduced.
Dermatologic Reactions
Allergic skin reactions, e.g., pruritus, erythema, urticaria, and morbilliform or maculopapular eruptions, occur in 1.1% of patients treated during clinical trials. These may be transient and may disappear despite continued use of tolbutamide; if skin reactions persist, the drug should be discontinued.
Porphyria cutanea tarda and photosensitivity reactions have been reported with sulfonylureas.
Hematologic Reactions
Leukopenia, agranulocytosis, thrombocytopenia, hemolytic anemia, aplastic anemia, and pancytopenia have been reported with sulfonylureas.
Metabolic Reactions
Hepatic porphyria and disulfiram-like reactions have been reported with sulfonylureas.
Endocrine Reactions
Cases of hyponatremia and the syndrome of inappropriate antidiuretic hormone (SIADH) secretion have been reported with this and other sulfonylureas.
Miscellaneous Reactions
Headache and taste alterations have occasionally been reported with tolbutamide administration.
What should I look out for while using Tolbutamide?
Tolbutamide tablets are contraindicated in patients with:
What might happen if I take too much Tolbutamide?
Overdosage of sulfonylureas including tolbutamide can produce hypoglycemia. Mild hypoglycemic symptoms without loss of consciousness or neurologic findings should be treated aggressively with oral glucose and adjustments in drug dosage and/or meal patterns. Close monitoring should continue until the physician is assured that the patient is out of danger. Severe hypoglycemic reactions with coma, seizure, or other neurological impairment occur infrequently, but constitute medical emergencies requiring immediate hospitalization. If hypoglycemic coma is diagnosed or suspected, the patient should be given a rapid intravenous injection of concentrated (50%) dextrose injection. This should be followed by a continuous infusion of a more dilute (10%) dextrose injection at a rate that will maintain the blood glucose at a level above 100 mg/dL. Patients should be closely monitored for a minimum of 24 to 48 hours since hypoglycemia may recur after apparent clinical recovery.
How should I store and handle Tolbutamide?
Protect from light and moisture. [see USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP.Store the unit-dose blister packages in the carton until contents have been used.Protect from light and moisture. [see USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP.Store the unit-dose blister packages in the carton until contents have been used.Protect from light and moisture. [see USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP.Store the unit-dose blister packages in the carton until contents have been used.Tolbutamide Tablets, USP are available containing 500 mg of tolbutamide, USP. The tablets are white to off-white round, scored tablets debossed with to the left of the score andto the right of the score on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-0215-01bottles of 100 tabletsNDC 0378-0215-05bottles of 500 tabletsStore at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Mylan Pharmaceuticals Inc.Morgantown, WV 26505REVISED FEBRUARY 2009TOLB:R14Tolbutamide Tablets, USP are available containing 500 mg of tolbutamide, USP. The tablets are white to off-white round, scored tablets debossed with to the left of the score andto the right of the score on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-0215-01bottles of 100 tabletsNDC 0378-0215-05bottles of 500 tabletsStore at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Mylan Pharmaceuticals Inc.Morgantown, WV 26505REVISED FEBRUARY 2009TOLB:R14Tolbutamide Tablets, USP are available containing 500 mg of tolbutamide, USP. The tablets are white to off-white round, scored tablets debossed with to the left of the score andto the right of the score on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-0215-01bottles of 100 tabletsNDC 0378-0215-05bottles of 500 tabletsStore at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Mylan Pharmaceuticals Inc.Morgantown, WV 26505REVISED FEBRUARY 2009TOLB:R14Tolbutamide Tablets, USP are available containing 500 mg of tolbutamide, USP. The tablets are white to off-white round, scored tablets debossed with to the left of the score andto the right of the score on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-0215-01bottles of 100 tabletsNDC 0378-0215-05bottles of 500 tabletsStore at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Mylan Pharmaceuticals Inc.Morgantown, WV 26505REVISED FEBRUARY 2009TOLB:R14Tolbutamide Tablets, USP are available containing 500 mg of tolbutamide, USP. The tablets are white to off-white round, scored tablets debossed with to the left of the score andto the right of the score on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-0215-01bottles of 100 tabletsNDC 0378-0215-05bottles of 500 tabletsStore at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Mylan Pharmaceuticals Inc.Morgantown, WV 26505REVISED FEBRUARY 2009TOLB:R14Tolbutamide Tablets, USP are available containing 500 mg of tolbutamide, USP. The tablets are white to off-white round, scored tablets debossed with to the left of the score andto the right of the score on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-0215-01bottles of 100 tabletsNDC 0378-0215-05bottles of 500 tabletsStore at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Mylan Pharmaceuticals Inc.Morgantown, WV 26505REVISED FEBRUARY 2009TOLB:R14Tolbutamide Tablets, USP are available containing 500 mg of tolbutamide, USP. The tablets are white to off-white round, scored tablets debossed with to the left of the score andto the right of the score on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-0215-01bottles of 100 tabletsNDC 0378-0215-05bottles of 500 tabletsStore at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Mylan Pharmaceuticals Inc.Morgantown, WV 26505REVISED FEBRUARY 2009TOLB:R14Tolbutamide Tablets, USP are available containing 500 mg of tolbutamide, USP. The tablets are white to off-white round, scored tablets debossed with to the left of the score andto the right of the score on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-0215-01bottles of 100 tabletsNDC 0378-0215-05bottles of 500 tabletsStore at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Mylan Pharmaceuticals Inc.Morgantown, WV 26505REVISED FEBRUARY 2009TOLB:R14
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Tolbutamide appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which tolbutamide lowers blood glucose during long-term administration has not been clearly established. With chronic administration in Type II diabetic patients, the blood-glucose-lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonylurea hypoglycemic drugs.
Some patients who are initially responsive to oral hypoglycemic drugs, including tolbutamide, may become unresponsive or poorly responsive over time. Alternatively, tolbutamide may be effective in some patients who have become unresponsive to one or more of the other sulfonylurea drugs.
Non-Clinical Toxicology
Tolbutamide tablets are contraindicated in patients with:The hypoglycemia action of sulfonylurea may be potentiated by certain drugs including non-steroidal anti-inflammatory agents and other drugs that are highly protein bound, salicylates, sulfonamides, chloramphenicol, probenecid, coumarins, monoamine oxidase inhibitors, and beta-adrenergic blocking agents. When such drugs are administered to a patient receiving tolbutamide, the patient should be observed closely for hypoglycemia. When such drugs are withdrawn from a patient receiving tolbutamide, the patient should be observed closely for loss of control.
Certain drugs tend to produce hyperglycemia and may lead to loss of control. These drugs include the thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs, and isoniazid. When such drugs are administered to a patient receiving tolbutamide, the patient should be closely observed for loss of control. When such drugs are withdrawn from a patient receiving tolbutamide, the patient should be observed closely for hypoglycemia.
A potential interaction between oral miconazole and oral hypoglycemic agents leading to severe hypoglycemia has been reported. Whether this interaction also occurs with the intravenous, topical or vaginal preparations of miconazole is not known.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
Review
Read user comments about the side effects, benefits, and effectiveness of losartan oral.
Overall User Ratings
514Total User Reviews
User Reviews
Learn about
User Reviews
Professional
Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72Tips
Tips
Interactions
Interactions
A total of 440 drugs (1549 brand and generic names) are known to interact with Imbruvica (ibrutinib). 228 major drug interactions (854 brand and generic names) 210 moderate drug interactions (691 brand and generic names) 2 minor drug interactions (4 brand and generic names) Show all medications in the database that may interact with Imbruvica (ibrutinib).