SULFONYLUREAS
Initially introduced in 1955, the sulfonylureas are the oldest class of oral antidiabetic drugs and act on pancreatic beta-cells to increase insulin secretion. Most of the drugs in this class are no longer protected by patents and are available in generic forms.
Drugs in this class include chlorpropamide, gliclazide, glimepiride, glipizide, glyburide and tolazamide.
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CHLORPROPAMIDE
Tradename(s) Diabinese® Company(ies) Pfizer, Sandoz, Watson Lab and others Available doses 100 mg and 250 mg Dose per day once daily Side-effects hypoglycemia Eliminatino half-life 36 hours Metabolism excreted unchanged US patent status generic US FDA status approved October 1958 EMEA status Indication Chlorpropamide is indicated as an adjunct to diet to lower the blood glucose in patients with type 2 diabetes whose hyperglycemia cannot be controlled by diet alone.
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GLICLAZIDE
Tradename (s) Diamicron® Company(ies) Sandoz, Servier, Novopharm, Apotex Available doses 30 mg and 80 mg Dose per day once daily Side-effects hypoglycemia Elimination half-life 16 hours Metabolism essentially eliminated via the urine US patent status generic US FDA status not available in the US EMEA status approved Indication Gliclazide is indicated for the control of hyperglycemia in gliclazide responsive diabetes mellitus of stable, mild, non-ketosis prone, maturity onset or adult type which cannot be controlled by proper dietary management and exercise, or when isulin therapy is not appropriate.
N.B. the 30 mg pill is a slow-release formulation.
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GLIMEPIRIDE
Tradename(s) Amaryl®, Amarel® Company(ies) Sanofi-Aventis, Ranbaxy Laboratories , Mylan, Teva and others Available doses 1 mg, 2 mg and 4 mg Dose per day once daily Side-effects hypoglycemia Elimination half-life 5.3 hours Metabolism metabolized by oxidative biotransformation US patent status generic US FDA status approved November 1995 EMEA status approved December 1996 Indication Glimepiride is indicated as adjunct to diet and exercise, to lower the blood glucose in patients with noninsulin-dependent (type II) diabetes mellitus (NIDDIM) whose hyperglycemia cannot be controlled by diet and exercise alone. Comments Sanofi-Aventis reported sales of 451 million in 2006 and 392 million in 2007 .
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GLIPIZIDE
Tradename(s) Glucotorol®, Glucotorol XL®, Glibenese® Company(ies) Pfizer, Sandoz, Watson and others Available doses 2.5 mg, 5 mg and 10 mg Dose per day once daily Side-effects hypoglycemia Elimination half-life 2-5 hours Metabolism eliminated by hepatic biotransformation US patent status generic US FDA status approved May 1984 EMEA status Indication Glipizide is indicated as an adjunct to diet for the control of hyperglycemia and its associated symptomatology in patients with non-insulin-dependent diabetes mellitus (NIDDM; type II), after an adequate trial of dietary therapy has proved unsatisfactory.
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GLYBURIDE (or GLIBENCLAMIDE)
Tradename(s) Micronase®, Diabeta®, Glynase®, Euglucan®, Daonil®, Semi-Daonil® Company(ies) Roche, Sanofi-Aventis, Pfizer, Mylan, Teva, Sandoz and others Available doses 1.25 mg, 1.5 mg, 2.5 mg, 3 mg, 4.5 mg, 5 mg and 6 mg Dose per day once daily (with breakfast or first meal) Side-effects hypoglycemia Elimination half-life 10 hours Metabolism excreted as metabolites in the bile and urine US patent status generic US FDA status approved EMEA status Indication Glyburide is indicated as an adjunct to diet to lower the blood glucose in patients with non-insulin-dependent diabetes mellitus (Type II) whose hyperglycemia cannot be satisfactorily controlled by diet alone.
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TOLAZAMIDE
Tradename(s) Tolinase® Company(ies) Sandoz, Pfizer and others Available doses 100 mg, 250 mg and 500 mg Dose per day once per day with breakfast or first meal Side-effects hypoglycemia Elimination half-life 7 hours Metabolism metabolized to five major metabolites which are excreted principally in the urine US patent status generic US FDA status approved but no longer available EMEA status Indication Tolazamide is indicated as an adjunct to diet to lower the blood glucose in patients with non-insulin-dependent diabetes mellitus (Type II) whose hyperglycemia cannot be satisfactorily controlled by diet alone.
