Tolbutamide

Overview

Tolbutamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It is structurally similar to acetohexamide, chlorpropamide and tolazamide and belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Tolbutamide appears to be metabolized in the liver. Tolbutamide and its metabolites are excreted in urine (75-85%) and feces.

Indication

For treatment of NIDDM (non-insulin-dependent diabetes mellitus) in conjunction with diet and exercise.

Associated Conditions

Type 2 Diabetes Mellitus

Clinical Trials

Title	Posted	Study ID	Phase	Status	Sponsor
Study to Evaluate the Effect of Multiple-Dose Ritlecitinib on the Pharmacokinetics (PK) of Tolbutamide	2021/10/28	NCT05097716	Phase 1	Completed	Pfizer
Licorice Botanical Dietary Supplements - Metabolism and Safety in Women	2019/05/13	NCT03948243	Phase 1	Completed	University of Illinois at Chicago
A Drug-Drug Interaction Study in Healthy Volunteers of the Effects of Tucatinib	2018/10/29	NCT03723395	Phase 1	Completed	Seagen Inc.
Drug Interaction Study of CT1812 in Healthy Volunteers	2018/10/23	NCT03716427	Phase 1	Completed	Cognition Therapeutics
Study in Healthy Subjects to Determine the Effect of Relacorilant on Exposure to Probe Substrates for Cytochrome P450s	2018/03/07	NCT03457597	Phase 1	Completed	Corcept Therapeutics
Effect of Pexidartinib on the Way the Body Processes CYP3A4 and CYP2C9 Substrates (Pharmacokinetics)	2017/09/25	NCT03291288	Phase 1	Completed	Daiichi Sankyo
A Study to Investigate the Potential Influence of Nitisinone on the Metabolism and the Transport of Other Drugs in Healthy Volunteers	2017/04/06	NCT03103568	Phase 1	Completed	Swedish Orphan Biovitrum
A PHASE 1, OPEN-LABEL, CROSS-OVER, FIXED SEQUENCE STUDY TO EVALUATE THE EFFECT OF MULTIPLE DOSES OF DS-1971A ON THE SINGLE DOSE PHARMACOKINETICS OF PROBE SUBSTRATES FOR CYP2B6, CYP2C8, CYP2C9, CYP2C19 AND CYP3A4 ENZYMES IN HEALTHY MALE AND FEMALE SUBJECTS	2015/06/16	NCT02473627	Phase 1	Completed	Daiichi Sankyo
A Study to Assess Effect of JNJ-54861911 on Pharmacokinetics of Cocktail Representatives for Cytochrome P450 (CYP) 3A4, CYP2B6, CYP2C9, and CYP1A2 Substrates	2014/08/07	NCT02211079	Phase 1	Completed	Janssen Research & Development, LLC
Multiple Doses of BI 207127 NA, BI 201335 NA Followed by the Combination of BI 207127 NA and BI 201335 NA in Healthy Male Volunteers	2014/07/08	NCT02182401	Phase 1	Terminated	Boehringer Ingelheim

FDA Drug Approvals

Approved Product	Manufacturer	NDC Code	Route	Strength	Effective Date
No FDA approvals found for this drug.

EMA Drug Approvals

Approved Product	Authorization Holder	Status	Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product	Manufacturer	Approval Number	Dosage Form	Strength	Approval Date
TOLMIDE TABLET 500 mg	BEACONS PHARMACEUTICALS PTE. LTD.	SIN04257P	TABLET	500 mg	4/20/1990
TOBUMIDE TABLET 500 mg	SUNWARD PHARMACEUTICAL PRIVATE LIMITED	SIN04045P	TABLET	500 mg	3/28/1990

NMPA Drug Approvals

Approved Product	Company	Approval Number	Drug Type	Dosage Form	Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product	Registration No.	Company	Licence No.	Strength	Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product	ARTG ID	Sponsor	Registration Type	Status	Registration Date
No TGA approvals found for this drug.

Health Canada Drug Approvals

Approved Product	Company	DIN	Dosage Form	Strength	Market Date
TOLBUTAMIDE TAB 500MG	Duchesnay Inc	00431168	Tablet - Oral	500 MG	12/31/1978
MOBENOL TABLETS 500MG	carter-horner corp.	00013889	Tablet - Oral	500 MG / TAB	12/31/1957
ORINASE 0.5GM	hoechst canada inc.	00012602	Tablet - Oral	500 MG / TAB	12/31/1957
TOLBUTAMIDE TAB 500MG	PRO DOC LIMITEE	00156663	Tablet - Oral	500 MG	12/31/1962
TOLBUTAMIDE	aa pharma inc	00312762	Tablet - Oral	500 MG	12/31/1975
ORINASE 1GM	hoechst canada inc.	00012610	Tablet - Oral	1 G / TAB	12/31/1966
NOVO-BUTAMIDE 500MG	novopharm limited	00021849	Tablet - Oral	500 MG	12/31/1968

CIMA AEMPS Drug Approvals

Approved Product	Company	Registration Number	Pharmaceutical Form	Prescription Type	Status
No CIMA AEMPS (Spain) approvals found for this drug.

Philippines FDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product	Company	Registration Number	Dosage Form	Strength	Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name	MA Holder	MA Number	Pharmaceutical Form	Active Ingredient	Authorization Date
No UK EMC drug information found for this drug.

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