II. Background
- Listed for historical purposes only
- See Second Generation Sulfonylurea instead
III. Indications
-
Type II Diabetes Mellitus (historical)
- Replaced by Second Generation Sulfonylurea agents
IV. Mechanism
-
Sulfonylureas trigger Insulin release from pancreatic beta cells
- Sulfonylureas stimulate Potassium channel closure on pancreatic beta cell surface
- Secretagogues do NOT burn out the beta cells sooner
- Sulfonylureas may also increase tissue Insulin sensitivity
V. Medications
- Acetohexamide (Dymelor)
- Dose: 500 to 750 mg orally daily or divided twice daily
- Chlorpropamide (Diabinese)
- Dose: 100 to 250 mg up to 750 mg daily or divided twice daily
- Antidiuretic effect (used in Diabetes Insipidus)
- Tolazamide (Tolinase)
- Dose: 250-500 mg orally daily or divided twice daily
- Tolbutamide (Orinase)
- Dose: 1000 to 2000 mg orally daily or divided twice daily
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| Definition (NCI) | An intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. Acetohexamide is metabolized in the liver to its active metabolite hydroxyhexamide. |
| Definition (MSH) | A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D000092 |
| SnomedCT | 391708007, 391707002, 387210001, 39064002 |
| LNC | LP17249-1, MTHU012977 |
| English | Benzenesulfonamide, 4-acetyl-N-((cyclohexylamino)carbonyl)-, 3-Cyclohexyl-1-(p-acetylphenylsulfonyl)urea, Cyclamide, 4-Acetyl-N-((cyclohexylamino)carbonyl)benzenesulfonamide, 1-(p-Acetylbenzenesulfonyl)-3-Cyclohexylurea, N-(p-Acetylbenzenesulfonyl)-N'-cyclohexylurea, N-(p-Acetylphenylsulfonyl)-N'-cyclohexylurea, Acetohexamide, acetohexamide (medication), Acetohexamide [Chemical/Ingredient], acetoHEXAMIDE, acetohexamide, Acetylcholine chloride - chemical (substance), Acetohexamide - chemical (substance), Acetohexamide - chemical, Acetylcholine chloride - chemical, Acetohexamide (product), Acetohexamide (substance), ACETOHEXAMIDE, AcetoHEXAMIDE |
| Swedish | Acetohexamid |
| Czech | acetohexamid |
| Finnish | Asetoheksamidi |
| Russian | ATSETOGEKSAMID, АЦЕТОГЕКСАМИД |
| Japanese | アセトヘキサミド |
| Polish | Acetoheksamid, Dymelor |
| Spanish | acetohexamida (producto), acetohexamida (sustancia), acetohexamida, Acetohexamida |
| French | Acétohexamide |
| German | Acetohexamid |
| Italian | Acetoesamide |
| Portuguese | Acetoexamida |
Ontology: Chlorpropamide (C0008287)
| Definition (NCI) | A long-acting, first-generation sulfonylurea with hypoglycemic activity. Compared to other sulfonylureas, chlorpropamide has an increased risk of prolonged hypoglycemia because of its long half-life. |
| Definition (MSH) | A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277) |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D002747 |
| SnomedCT | 111154004, 386991003 |
| LNC | LP16075-1, MTHU003325 |
| English | Chlorpropamide, Clorpropamid, Benzenesulfonamide, 4-chloro-N-((propylamino)carbonyl)-, Urea, 1-((p-chlorophenyl)sulfonyl)-3-propyl-, CHLORPROPAMIDE, 4-Chloro-4-((propylamino)carbonyl)benzenesulfonamide, Chlorpropamide [Chemical/Ingredient], chlorproPAMIDE, chlorpropamide, Chlorpropamide (product), Chlorpropamide (substance), ChlorproPAMIDE |
| Swedish | Klorpropamid |
| Czech | chlorpropamid |
| Finnish | Klooripropamidi |
| Russian | KHLORPROPAMID, ХЛОРПРОПАМИД |
| Croatian | KLORPROPAMID |
| Polish | Chlorpropamid |
| Japanese | クロルプロパミド, クロルプロパマイド |
| Spanish | clorpropamida (producto), clorpropamida (sustancia), clorpropamida, Clorpropamida |
| French | Chlorpropamide |
| German | Chlorpropamid, Clorpropamid |
| Italian | Clorpropamide |
| Portuguese | Clorpropamida |
Ontology: Tolazamide (C0040372)
| Definition (NCI) | An intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. Tolazamide is converted into five major metabolites that are excreted into the urine. Tolazamide is more potent than tolbutamide and similar in potency to chlorpropamide on a milligram basis. This agent may cause cholestatic jaundice. |
| Definition (MSH) | A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D014042 |
| SnomedCT | 34393009, 387186009 |
| LNC | LP17254-1, MTHU010006 |
| English | Tolazamide, Benzenesulfonamide, N-(((hexahydro-1H-azepin-1-yl)amino)carbonyl)-4-methyl-, tolazamide, tolazamide (medication), TOLAZAMIDE, Tolazamide [Chemical/Ingredient], TOLAZamide, 4-(p-Tolylsulfonyl)-1,1-hexamethylenesemicarbazide, 1-(Hexahydro-1H-azepin-1-yl)-3-(p-tolylsulfonyl)urea, Tolazamide (product), Tolazamide (substance) |
| Swedish | Tolazamid |
| Czech | tolazamid |
| Finnish | Tolatsamidi |
| Russian | TOLAZAMID, ТОЛАЗАМИД |
| Japanese | トラザミド |
| Polish | Tolazamid |
| Spanish | tolazamida (producto), tolazamida (sustancia), tolazamida, Tolazamida |
| French | Tolazamide |
| German | Tolazamid |
| Italian | Tolazamide |
| Portuguese | Tolazamida |
Ontology: Tolbutamide (C0040374)
| Definition (NCI) | A short-acting, first-generation sulfonylurea with hypoglycemic activity. Compared to second-generation sulfonylureas, tolbutamide is more likely to cause adverse effects, such as jaundice. This agent is rapidly metabolized by CYPC29. |
| Definition (MSH) | A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290) |
| Definition (CSP) | sulfonylurea compound used as a hypoglycemic in the treatment of noninsulin dependent diabetes mellitus. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D014044 |
| SnomedCT | 33124007, 373481003 |
| LNC | LP32705-3, LP16296-3, MTHU010007 |
| English | Tolbutamide, Benzenesulfonamide, N-((butylamino)carbonyl)-4-methyl-, tolbutamide (medication), Tolbutamide [Chemical/Ingredient], TOLBUTamide, TOLBUTAMIDE, N-[(butylamino)carbonyl]-4-methylbenzenesulfonamide, tolbutamide, Tolbutamide (product), Tolbutamide (substance) |
| Swedish | Tolbutamid |
| Czech | tolbutamid |
| Finnish | Tolbutamidi |
| Russian | BUTAMID, TOLBUTAMID, БУТАМИД, ТОЛБУТАМИД |
| Japanese | トルブタミド, 1-ブチル-p-トリルスルホニル尿素 |
| Polish | Tolbutamid, Diabetol |
| Spanish | tolbutamida (producto), tolbutamida (sustancia), tolbutamida, Tolbutamida |
| French | Tolbutamide |
| German | Tolbutamid |
| Italian | Tolbutamide |
| Portuguese | Tolbutamida |
Ontology: First generation sulfonylurea (C1300197)
| Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| SnomedCT | 386049002 |
| English | First generation sulfonylurea (product), First generation sulfonylurea, First generation sulphonylurea |
| Spanish | sulfonilurea de primera generación (producto), sulfonilurea de primera generación |
