Generation | Generic name | Trade name (United States) | Time to peak, hours | Half-life, hours | Duration of action, hours | Metabolism and clearance | Active metabolites |
First | Chlorpropamide | Diabinase | 2-7 | 36* | 24-72 | Hepatically by CYP2C9; renally as active metabolite (55%) and unchanged drug (20%) | Yes |
First | Tolbutamide | Orinase | 3-4 | 4.5-6.5* (range 3-28) | 6-12 (up to 24 after repeated dosing) | Hepatically by CYP2C9; renally as active metabolite (30%)¶ | Yes |
First | Tolazamide | Tolinase | 3-4 | 4-8* | 12-24 | Hepatically; renally as active metabolite (35%) and unchanged drug (7%) | Yes |
Second | Gliclazide (not available in United States) | Diamicron (Canada and elsewhere) | 2-4 | 8-12 | 12-24 | Hepatically by CYP2C9 | No |
Second | Glipizide | Glucatrol | 1-3 | 2-5 | 16-24 | Hepatically by CYP2C9; renally as unchanged drug (<10%) | No |
Second | Glipizide | Glucatrol XL | 6-12 | 7 | 24 | Hepatically by CYP2C9; renally as unchanged drug (<10%) | No |
Second | Glyburide (glibenclamide) | Micronase DiaBeta Glynase | 2-6 | 10* | <24 | Hepatically by CYP2C9; renally as active metabolites (36%) | Yes |
Third | Glimepiride | Amaryl | 2-3 | 5-9* | 16-24 | Hepatically by CYP2C9; renally as active metabolite (63%)Δ | Yes |
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