tolbutamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihyperglycaemics | 2696 | 64-77-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.50 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.11 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 123.17 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 85 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.12 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.21 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.05 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 7 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 22, 1961 | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A10BB03 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Sulfonylureas |
| ATC | V04CA01 | VARIOUS DIAGNOSTIC AGENTS OTHER DIAGNOSTIC AGENTS Tests for diabetes |
| FDA CS | M0020795 | Sulfonylurea Compounds |
| FDA EPC | N0000175608 | Sulfonylurea |
| MeSH PA | D007004 | Hypoglycemic Agents |
| CHEBI has role | CHEBI:35526 | antidiabetic |
| CHEBI has role | CHEBI:77746 | Homo sapiens metabolite |
| CHEBI has role | CHEBI:90415 | insulin secretagogues |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diabetes mellitus type 2 | indication | 44054006 | DOID:9352 |
| Diagnostic Test for Pancreatic Islet Cell Adenoma | indication | ||
| Alcoholism | contraindication | 7200002 | |
| Asthenia | contraindication | 13791008 | |
| Hepatic porphyria | contraindication | 55056006 | DOID:3133 |
| Hypopituitarism | contraindication | 74728003 | DOID:9406 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Hypoglycemic disorder | contraindication | 237630007 | |
| Primary adrenocortical insufficiency | contraindication | 373662000 | |
| Surgical procedure | contraindication | 387713003 | |
| Traumatic injury | contraindication | 417746004 | |
| Fever greater than 100.4 Fahrenheit | contraindication | 426000000 | |
| Prolonged-Severe Nausea and Vomiting | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.23 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sulfonylurea receptor 1, Kir6.2 | Ion channel | BLOCKER | Kd | 5.05 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Solute carrier family 22 member 6 | Transporter | Ki | 4.26 | CHEMBL | |||||
| ATP-sensitive inward rectifier potassium channel 11 | Ion channel | BLOCKER | IC50 | 4.50 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4017888 | VUID |
| N0000146241 | NUI |
| D00380 | KEGG_DRUG |
| 4017888 | VANDF |
| 4017889 | VANDF |
| C0040374 | UMLSCUI |
| CHEBI:27999 | CHEBI |
| CHEMBL782 | ChEMBL_ID |
| DB01124 | DRUGBANK_ID |
| D014044 | MESH_DESCRIPTOR_UI |
| 5505 | PUBCHEM_CID |
| 6848 | IUPHAR_LIGAND_ID |
| 602 | INN_ID |
| 473-41-6 | SECONDARY_CAS_RN |
| 982XCM1FOI | UNII |
| 10635 | RXNORM |
| 4482 | MMSL |
| 5595 | MMSL |
| 5596 | MMSL |
| d00394 | MMSL |
| 000908 | NDDF |
| 000909 | NDDF |
| 109194005 | SNOMEDCT_US |
| 33124007 | SNOMEDCT_US |
| 373481003 | SNOMEDCT_US |
| CHEMBL1200874 | ChEMBL_ID |
Pharmaceutical products:
None