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.

  • 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.

  • 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.

  • 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 .
  • 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.
  • 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.

  • 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.