Your activity: 66 p.v.
< Back
your limit has been reached. plz Donate us to allow your ip full access, Email: sshnevis@outlook.com

Pharmacokinetics of the sulfonylureas

Pharmacokinetics of the sulfonylureas
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
Time to peak and duration of effect are as reported in product labeling and small pharmacokinetic studies; these values may be increased in overdose.
* Half-life prolonged in older adults or renal impairment; duration of action may be prolonged.
¶ Active metabolite (hydroxytolbutamide) has less hypoglycemic effect than parent drug.
Δ Active metabolite (cyclohexylhydroxymethyl derivative) has less hypoglycemic effect than parent drug.
Graphic 72580 Version 2.0