http://www.fpnotebook.com/
First Generation SulfonylureaAka: Tolbutamide, Tolazamide, Chlorpropamide, Acetohexamide
- See Also
- Second Generation Sulfonylurea
- Oral Hypoglycemic Agents
- Background
- Discovered in 1940's when investigating antibiotics
- Preparations
- Acetohexamide (Dymelor)
- Dose: 500-750 mg qd or divided ($14)
- Chlorpropamide (Diabinese)
- Dose: 100-250 up to 750 mg qd/bid
- Antidiuretic effect (used in Diabetes Insipidus)
- Tolazamide (Tolinase)
- Dose: 250-500 mg PO qd or divided ($2.81)
- Tolbutamide (Orinase)
- Dose: 1000-2000mg qd or divided bid ($2.75)
|
|---|
| 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)
|
| English | Acetohexamide, ACETOHEXAMIDE PREPARATION, Cyclamide |
| Spanish | acetohexamida |
| Credits | 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)
|
| English | Chlorpropamide, CHLORPROPAMIDE PREPARATION, Clorpropamid |
| Spanish | clorpropamida |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
|
|
|---|
| 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)
|
| English | Tolazamide, TOLAZAMIDE PREPARATION |
| Spanish | tolazamida |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
|
|
|---|
| 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)
|
| English | Tolbutamide, TOLBUTAMIDE PREPARATION |
| Spanish | tolbutamida |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
|
First generation sulfonylurea (C1300197)
|
|---|
| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
|
| English | First generation sulfonylurea, First generation sulphonylurea |
| Spanish | sulfonilurea de primera generación, sulfonilurea de primera generacion |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
|
Navigation Tree
