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تعداد آیتم قابل مشاهده باقیمانده : -74 مورد

Pharmacokinetics of select sulfonylureas

Pharmacokinetics of select sulfonylureas
Generation Generic name Brand name
(United States)
Time to peak
(hours)
Half-life
(hours)
Duration of action
(hours)
Metabolism and clearance Active metabolites
First* Chlorpropamide Diabinese 2 to 7 36 24 to 72 Hepatically by CYP2C9; renally as active metabolite (55%) and unchanged drug (20%) Yes
First* Tolbutamide Orinase 3 to 4 4.5 to 6.5
(range 3 to 28)
6 to 12
(up to 24 after repeated dosing)
Hepatically by CYP2C9; renally as active metabolite (30%)Δ Yes
Second* Gliclazide Diamicron
(Canada and elsewhere)
2 to 4 8 to 12 12 to 24 Hepatically by CYP2C9 No
Second* Gliclazide modified-release Diamicron MR
(Canada and elsewhere)
6 12 to 20 24 Hepatically by CYP2C9 No
Second Glipizide Glucotrol 1 to 3 2 to 5 16 to 24 Hepatically by CYP2C9; renally as unchanged drug (<10%) No
Second Glipizide extended-release Glucotrol XL 6 to 12 7 24 Hepatically by CYP2C9; renally as unchanged drug (<10%) No
Second Glyburide
(glibenclamide)

Micronase

DiaBeta

Glynase
2 to 6 10 <24 Hepatically by CYP2C9; renally as active metabolites (36%) Yes
Third Glimepiride Amaryl 2 to 3 5 to 9 16 to 24 Hepatically by CYP2C9; renally as active metabolite (63%) 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.

CYP: cytochrome P450.

* Not available in the United States but may be available elsewhere. Refer to local product availability.

¶ Half-life prolonged in older adults or renal impairment; duration of action may be prolonged.

Δ Active metabolite (hydroxytolbutamide) has less hypoglycemic effect than parent drug.

◊ Active metabolite (cyclohexylhydroxymethyl derivative) has less hypoglycemic effect than parent drug.
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