II. Indications

  1. Replaced by Second Generation Sulfonylurea agents for the management of Type II Diabetes Mellitus

III. Preparations

  1. Acetohexamide (Dymelor)
    1. Dose: 500-750 mg qd or divided ($14)
  2. Chlorpropamide (Diabinese)
    1. Dose: 100-250 up to 750 mg qd/bid
    2. Antidiuretic effect (used in Diabetes Insipidus)
  3. Tolazamide (Tolinase)
    1. Dose: 250-500 mg PO qd or divided ($2.81)
  4. Tolbutamide (Orinase)
    1. Dose: 1000-2000mg qd or divided bid ($2.75)

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Ontology: Acetohexamide (C0000992)

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