Exam 1 - Sulfanylureas 1st Gen

Question 1

What are the characteristics of 1st Generation Sulfanylureas?

Answer 1

● Potent  hypoglycemic agents
● MOA:  Close K+   ATP  channel →
depolarization of β­cell → open Ca+ 
channel →  insulin release
● Release of insulin in response to glucose is enhanced  
● Potentiate Insulin effects in tissue
● Reduction in serum glucagon
● S.E: hypoglycemia  
● dermatological (sulfa) allergies (rash,pruritis)
● nausea/vomitting
● Weight gain

Question 2

Which are the 1st Generation Sulfanylureas drugs?

Answer 2

Tolbutamide ( Orinase )
Chlorpropamide ( Diabinese )
Tolazamide ( Tolinase )
Acetohexamide ( Dymelor )

Question 3

What are the characteristics of Tolbutamide (Orinase)?

Answer 3

● Shortest acting
● TID dosing ­inconvenient
● Hepatic metabolized

Question 4

What are the characteristics of Chlorpropamide

( Diabinese )?

Answer 4

● 36h t 1/2 (bad in OD)
● Disulfuram ­like rxn to ethanol (nausea)
● SIADH increase sen. of kidney to ADH= Water retention

Question 5

What are the characteristics of Tolazamide ( Tolinase )?

Answer 5

● mildly active metabolite = dosing problems (seldom used)

● QD dosing

Question 6

What are the characteristics of Acetohexamide ( Dymelor )?

Answer 6

● potent active metabolite = complicates dosing (seldom used)
● Uricosuric action (↑’s uric acid elimination)
● QD dosing