Endocrinology Book

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First Generation Sulfonylurea

Aka: First Generation Sulfonylurea, Tolbutamide, Tolazamide, Chlorpropamide, Acetohexamide
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  1. See Also
    1. Second Generation Sulfonylurea
    2. Oral Hypoglycemic Agents
  2. Indications
    1. Replaced by Second Generation Sulfonylurea agents for the management of Type II Diabetes Mellitus
  3. 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)
Medication Costs
CHLORPROPAMIDE (on 2/10/2012 at Target.com)
CHLORPROPAMIDE 100 MG* Tablet #30 for $4.00 ($0.13/unit)
TOLBUTamide (on 2/9/2012 at DrugStore.com)
TOLBUTamide 500mg Tablets #60 for $37.39 ($0.62/unit)
TOLAZamide (on 2/9/2012 at DrugStore.com)
TOLAZamide 250mg Tablets #60 for $39.77 ($0.66/unit)
TOLAZamide 500mg Tablets #30 for $50.83 ($1.69/unit)
ChlorproPAMIDE (on 2/9/2012 at DrugStore.com)
ChlorproPAMIDE 100mg Tablets #60 for $30.99 ($0.52/unit)
ChlorproPAMIDE 250mg Tablets #60 for $55.99 ($0.93/unit)
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Acetohexamide (C0000992)

Definition (MSH) A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide.
Definition (NCI) A sulfonylurea with oral hypoglycemic properties that is used in the treatment of Type II diabetes mellitus. Acetohexamide lowers blood sugar by stimulating insulin release from the pancreas and increases the sensitivity of beta cells to glucose stimulus. This drug also increases the sensitivity of insulin receptors in muscle, liver, and adipose tissue thereby promoting glucose transport across cell membranes. This results in better controlled blood glucose levels. (NCI05)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D000092
SnomedCT 391708007, 391707002, 387210001, 39064002
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), Acetylcholine chloride - chemical (substance), Acetohexamide - chemical (substance), acetohexamide, Acetohexamide [Chemical/Ingredient], acetoHEXAMIDE, Acetohexamide (product), Acetohexamide (substance), Acetohexamide - chemical, Acetylcholine chloride - chemical, ACETOHEXAMIDE, AcetoHEXAMIDE
Swedish Acetohexamid
Czech acetohexamid
Spanish Acetylcholine chloride - chemical, Acetohexamide - chemical, acetohexamida (producto), acetohexamida (sustancia), acetohexamida, Acetohexamida
Finnish Asetoheksamidi
Russian ATSETOGEKSAMID, АЦЕТОГЕКСАМИД
Japanese アセトヘキサミド
Polish Acetoheksamid, Dymelor
French Acétohexamide
German Acetohexamid
Italian Acetoesamide
Portuguese Acetoexamida
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Chlorpropamide (C0008287)

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)
Definition (NCI) A sulfonylurea with oral hypoglycemic properties that is used in the treatment of Type II diabetes mellitus. Chlorpropamide stimulates pancreatic secretion of insulin and improves insulin release by increasing sensitivity of beta cells to glucose stimuli. This drug also increases the sensitivity of insulin receptors in muscle, liver, and adipose tissue thereby promoting glucose transport across cell membranes. This results in better controlled blood glucose levels. Chlorpropamide has the longest duration of action of the sulfonylurea class but could cause more severe and frequent side effects, including hypoglycemia and hyponatremia.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D002747
SnomedCT 111154004, 386991003
English Chlorpropamide, Clorpropamid, chlorpropamide, 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 (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
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Tolazamide (C0040372)

Definition (MSH) A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.
Definition (NCI) A sulfonylurea derivative and an antidiabetic agent with hypoglycemic property. Tolazamide binds to the ATP-dependent potassium channels on the plasma membrane of pancreatic beta-cells, which results in an inhibition of potassium efflux and membrane depolarization. Membrane depolarization stimulates calcium influx through voltage-gated calcium channels and subsequently induces the release of insulin from viable beta-cells thereby leading to a decrease in blood glucose levels. In addition, this agent potentiates the anti-diuretic effect of antidiuretic hormone (ADH).
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D014042
SnomedCT 34393009, 387186009
English Tolazamide, Benzenesulfonamide, N-(((hexahydro-1H-azepin-1-yl)amino)carbonyl)-4-methyl-, tolazamide, tolazamide (medication), TOLAZAMIDE, Tolazamide [Chemical/Ingredient], TOLAZamide, 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
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Tolbutamide (C0040374)

Definition (NCI) A first-generation sulfonylurea with hypoglycemic activity. Tolbutamide binds to and blocks adenosine triphosphate (ATP)-sensitive potassium channels on the beta cell membrane of the pancreatic islet tissues. This leads to potassium efflux, which results in depolarization, calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis. In addition, tolbutamide may increase the number and affinity of cell surface insulin receptors, thereby enhancing the peripheral response to insulin. Tolbutamide is a CYP2C9 substrate.
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 Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D014044
SnomedCT 33124007, 373481003
English Tolbutamide, tolbutamide, Benzenesulfonamide, N-((butylamino)carbonyl)-4-methyl-, tolbutamide (medication), Tolbutamide [Chemical/Ingredient], TOLBUTamide, 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
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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