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Flashcards in Pharma 3 Diabetic Drugs Deck (25):
1

What is the action of insulin?

  • Activates GLUT4 to relocate to cell membrane and increase uptake of glucose into cells
  • inhibits glycogen breakdown and increases glucose uptake by liver and adipose
  • stimulates FA synthesis for transport as lipoproteins and inhibits lipolysis in adipocytes
  • Inhibitis proteolysis 

2

What are the normal values in which glucose are kept in plasma?

3.8 - 6.5 mmol.L

3

What is the effect of diabetes mellitus ie hyperglycaemia?

In the short term - not much

In long term - macrovascular (increases risk of IHD, stroke, and PVD) and microvascular damage (increases risk of retinopathies, neuropathies, and nephropathies)

4

What is type 1 and type 2 diabetes?

type 1 - autoimmune destruction of beta islet cells

type 2 - insulin resistance and decreased insulin output from beta cells

5

How are type 1 diabetics treated? What are the varieties of treatment offered and how are these utilised to mimic physiological functioning?

insulin subcutaneous injections

Can be short, intermediate or long acting

Basal bolus regimen - uses long acting insulin in background and then a fast acting insulin with meals - 5 injections per day

Pre-mixed insulin regime - mix of fast and slow acting insulin - 2 times per day

6

What are the 5 classes of drugs on offer for type 2 diabetics?

Biguanides, thiazolidinediones, sulphonylureas, meglitidine, incretin based therapies

7

What is the mechanism of action of biguanides and give an example drug. How much can it reduce HbA1c by?

e.g. metformin

Works by increasing cell sensitivity to insulin and inhibits hepatic gluconeogenesis.

2%

8

What are the pros and contraindications of metformin?

Pros - well tolerated, weight neutral, cheap, good at lowering glucose

Contraindications - compromised renal function or resp disease

9

What is the mechanism of action of thiazolidinediones (TZDs) and give an example drug. How much does it lower HbA1c by?

e.g. rosiglitazone or pioglitazone

Works by reducing gluconeogenesis  and increasing glucose uptake in muscles. This is done by binding to a nuclear hormone receptor site which activates the RXR receptor, upregulating genes that affect glucose and lipid metabolsim

1-1.5%

10

What are the pros and cons of TZDs? What are the contraindications?

pros - long half life, cannot cause hypoglycaemia

cons - may cause oedema, increase LDL and HDL, binds to albumin causing PK and PD consequences, weight gain

Contraindication - heart failure patients

11

What is the mechanism of action of sulphonylureas and give an example drug. How much do they reduce HbA1c by?

e.g. gliclazide

Act by binding to beta cells K+-ATP channel activity and increasing K+ conc within the cell and cause depolarisation. This results in increases of calcium ion entry into the cell and increases the insulin release from beta cells.

1-2%

12

What are the pros and cons of sulphonylureas? Contraindications?

pros - once a day

cons - can cause hypoglycaemia, bidns to albumin causing pk and pd consequences, weight gain and GI disturbances

13

Give an example meglitidine and mechanism of action. How much does it reduce HbA1c

e.g. repaglinide

Same as sulphonylureas - Act by binding to beta cells K+-ATP channel activity and increasing K+ conc within the cell and cause depolarisation. This results in increases of calcium ion entry into the cell and increases the insulin release from beta cells.

1%

14

pros of meglitidine?

pros - low risk of hypo, no weight gain

 

15

What is the order of therapy for type 2 diabetes?

lifestyle advice, metfomin, sulphonylureas, TZDs

If HbA1c levels not brough to 7% or below, move on to metformin and then sulphonylureas

if sulphonylureas doesnt bring down HbA1c to below 7.5% then go on to add a TZD, or start insulin therapy

16

Name 3 anti obesity drugs and how they work

orlistate - gastric and pancreatic lipase inhibitor

sibutramine - noradrenaline and serotonin reuptake inhibitor = appetite suppression

Rimonabant - cannabinoid antagonist

17

What are the 2 incretin based therapies?

DPP-4 inhibitors (gliptins),  and GLP-1 receptor agonists

18

Give an example drug of a DPP-4 inhibitor

Sitagliptin

19

Give an example GLP-1 receptor agonist

exenatide

20

What are the physiological effects of GLP-1?

  • Brain - decrease hunger
  • Stomach - decrease gastric emptying
  • pancreas - increased insulin secretion, decreased glucagon secretion
  • liver - decreased glucose production
  • muscle - increase glucose uptake

21

What is the mechanism of action of gliptins?

DPP-4 inhibitor inhibits breakdowns of incretins. Increatins stimulate increased insulin from beta cells and decreased glucagon from alpha cells.

22

What are the pros and cons of incretin related therapies?

pros - weight neutral, modest HbA1c reduction

cons - high cost, some GI symptoms

23

How do SGLT2 inhibitors work?

work by blocking SGLT2 in the proximal tubule which prevents glucose reabsorption

24

Give an example SGLT2 inhibitor and the major con to using them.

e.g. dapagliflozin

increased risk of lower UTIs

25

What is normal HbA1c levels?

6%