Pharmacology: Sulphonylureas Flashcards Preview

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Flashcards in Pharmacology: Sulphonylureas Deck (16)
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1

what are the 2nd generation sulphonylureas that are used today

gliclazide, glipizide, glimepiride, glibenclamide

2

what cells do sulphonylureas act on

pancreatic beta cells

3

what part of the pancreatic beta cell do sulphonylureas bind to

SUR1 protein

4

what effect does sulphonylurea binding in pancreatic beta cells have to ATP sensitive K channels

closes them

5

describe how sulphonylurea binding acts to secrete insulin

closes Katp channels, depolarises membrane, triggers voltage gated Ca2+ channels, Ca2+ influx results in insulin exocytosis

6

describe the relation between sulphonylurea and glucose

glucose independent, insulin secreted when not needed(when glucose low or normal)

7

what result do sulphonylureas have on insulin

increase secretion

8

what type of drug are sulphonylureas

insulin secretagogues

9

what does sulphonylureas being glucose independent result in

hypoglycaemia

10

how potent are sulphonylureas

relatively potent, about same as metformin

11

what effect do sulphonylureas have on the weight of a patient

increase weight, by 1-2kg on average

12

what is the most commonly used sulphonylurea used in the UK, and at what dose

gliclazide, 40-80mg od, little benefit in going >80mg but max dose is 160

13

what are the possible side effects of sulphonylureas

hypoglycaemia, weight gain

14

what risk factors increase risk for hypoglycaemia

increased age, diabetes duration, creatinine, lower HbA1c(esp <50mmo/mol)

15

describe why sulphonylureas result in weight gain

insulin conc. increase, insulin is anabolic = increased carb storage.
insulin increases appetite

16

describe when in treatment pathway for diabetes sulphonylureas are used

second line(after metformin first line) in places where cost is a major issue(as its very cheap)