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November 25, 2025
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Brand Name :
Orinase
Synonyms :
tolbutamide
Class :
Anti-diabetic, Sulphonyl ureas
Brand Name :
Orinase
Synonyms :
tolbutamide
Class :
Anti-diabetic, Sulphonyl ureas
Dosage Forms & StrengthsÂ
TabletÂ
500mgÂ
250mg to 2g orally daily or can be administered twice or thrice daily
Do not exceed 3g per day
Maintenance doses of more than two g/day are rarely necessary
Safety and Efficacy not establishedÂ
Dosage Forms & StrengthsÂ
TabletÂ
500mgÂ
250mg orally every day or twice or thrice a day
Do not exceed 3g per day
Maintenance doses of more than two g/day are rarely necessary
may increase the serum concentration of CYP2C9 Substrates
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of Sulfonylureas
may increase the hypoglycemic effect of Sulfonylureas
may increase the hypoglycemic effect of Sulfonylureas
may increase the hypoglycemic effect of Sulfonylureas
may increase the hypoglycemic effect of Sulfonylurea
may increase the hypoglycemic effect of Sulfonylureas
my increase the hypoglycemic effect of Sulfonylureas
my increase the hypoglycemic effect of Sulfonylureas
my increase the hypoglycemic effect of Sulfonylureas
may increase the Glucose-lowering effect of SGLT2 Inhibitors
may increase the therapeutic efficacy of each other when combined
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may increase the photosensitizing effect of Photosensitizing Agents
May increase the adverse effect of Sulfonylureas
relugolix/​estradiol/​norethindrone
may increase the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
relugolix/estradiol/norethindrone
may increase the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
may increase the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
may increase the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
may increase the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
may increase the hypoglycemic effect of Antidiabetic Agents
may diminish the serum concentration of Sulfonylureas
may diminish the serum concentration of Sulfonylureas
may increase the hypoglycemic effect of Antidiabetic Agents
may increase the hypoglycemic effect of Antidiabetic Agents
may increase the hypoglycemic effect of Antidiabetic Agents
may increase the hypoglycemic effect of Antidiabetic Agents
may increase the hypoglycemic effect of Antidiabetic Agents
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
bismuth subcitrate, metronidazole and tetracycline
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may increase the hypoglycemic effect of sulfonylureas
may decrease the therapeutic effect of Antidiabetic Agents
may decrease the therapeutic effect of Antidiabetic Agents
may decrease the therapeutic effect of Antidiabetic Agents
may decrease the therapeutic effect of Antidiabetic Agents
fibric acid derivatives increase the effect of hypoglycemia of sulfonylureas
fibric acid derivatives increase the effect of hypoglycemia of sulfonylureas
fibric acid derivatives increase the effect of hypoglycemia of sulfonylureas
fibric acid derivatives increase the effect of hypoglycemia of sulfonylureas
fibric acid derivatives increase the effect of hypoglycemia of sulfonylureas
When halometasone is used together with tolbutamide, this leads to elevated risk or seriousness of hyperglycemia
the excretion rate of tolbutamide, when decreased by pralidoxime, results in increased serum level
diatrizoate may lower the rate of excretion of tolbutamide, thereby raising the amount in the serum
tolbutamide may lower the excretion rate of ioxilan, potentially resulting in a higher serum level
methylprednisolone hemisuccinateÂ
When methylprednisolone hemisuccinate is aided with tolbutamide, this leads to elevated hyperglycemia risk
may enhance the serum concentration of tolbutamide by inducing CYP2C9 inhibitors
beta-blockers may increase the hypoglycemic effect of antidiabetic agents
beta-blockers may increase the hypoglycemic effect of antidiabetic agents
beta-blockers may increase the hypoglycemic effect of antidiabetic agents
beta-blockers may increase the hypoglycemic effect of antidiabetic agents
beta-blockers may increase the hypoglycemic effect of antidiabetic agents
may increase the hypoglycaemic effect
may increase the hypoglycaemic effect
may increase the hypoglycaemic effect
may increase the hypoglycaemic effect
may increase the hypoglycaemic effect
may increase the hypoglycemic effect of beta blockers
may enhance the effect of sulfonylureas
It may enhance the effect when combined with lixisenatide by pharmacodynamic synergism
may have an increased risk of hypoglycemia when combined with tolbutamide
probenecid could potentially lead to an elevation in the concentration serum of sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
when combined with bacitracin, the serum level of tolbutamide will increase, leading to decreased output of tolbutamide from the body
anticoagulant properties or actions of fluindione are increased with tolbutamide
the therapeutic effect of tolbutamide may be reduced
may have a decrease in excretion when combined with tolbutamide
the anti-diabetic efficacy of tolbutamide can be reduced with mometasone furoate
Actions and Spectrum:Â
Frequency not definedÂ
Dermatologic reactionsÂ
AgranulocytosisÂ
Aplastic anemiaÂ
HeartburnÂ
HypoglycemiaÂ
Disulfiram-like reactionsÂ
HyponatremiaÂ
ThrombocytopeniaÂ
Nausea/vomitingÂ
Contraindications/caution:Â
Contraindications:Â
Caution:Â
Pregnancy consideration: CÂ
Lactation:Â Â
Pregnancy category:Â
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.  Â
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.Â
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   Â
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   Â
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.   Â
Category N: There is no data available for the drug under this categoryÂ
Pharmacology:Â
Pharmacodynamics:Â
Pharmacokinetics:Â
AbsorptionÂ
tolbutamide is well-absorbed orally and reaches peak serum levels within 3-4 hours after administration. Â
DistributionÂ
The volume of distribution (Vd) of tolbutamide is 0.15 L/kg, indicating that it is primarily confined to the blood and extracellular fluid. Â
MetabolismÂ
tolbutamide is extensively metabolized in the liver by the hepatic P450 enzyme CYP2C9 to form inactive metabolites such as carboxytolbutamide and hydroxymethyltolbutamide. Â
Elimination and ExcretionÂ
tolbutamide is primarily eliminated in the urine, with approximately 70-80% of the drug and its metabolites excreted within 24 hours of administration. The half-life of tolbutamide is relatively short, ranging from 4.5 to 6.5 hours, indicating that it is rapidly eliminated from the body.Â
Administration:Â
tolbutamide is usually administered orally as a tablet, with dosages ranging from 500 to 2000 mg per day, depending on the patient’s condition and response to treatment. It is usually taken 1-2 times daily, with or after meals, to reduce the risk of hypoglycemia (low blood sugar)Â
Patient information leafletÂ
Generic Name: tolbutamideÂ
Pronunciation: [ tole-BYOO-ta-mide ]Â
Why do we use tolbutamide?Â
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