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Flashcards in Diabetic Deck (17):
1

Examples of sensitisers

Biguanide (Metformin)
Thiazolidinediones

2

Examples of Sulfonylureas

Gliclazide
Glibenclamide (Glyburide)
Glipizide
Gliperimide
Tolbutamide

3

Mode of action of sulfonylureas

Binds to Beta cells sulfonyl urea receptors (SUR1). The binding then blocks ATP sensitive K+ channel. This depolarises the cells which results in calcium release and subsequent calmodulin activation. The end result is exocytosis of insulin containing secretory granules

4

Advantages of sulfonylureas

No effect on BP
No effect of LDL
Lower risk of gastrointestinal problems

5

Mode of action of Metformin

Activates AMP-activated protein kinase (Liver enzyme); inhibits gluconeogenesis in liver, decreases glucose absorption in the gut, stimulates GLUT4 deployment unto plasma membrane in skeletal muscles/

6

Contraindications for Metformin

Ketoacidosis
Use of general anaesthesia
Renal impairment (avoid if eGFR <30, adjust if eGFR <45)
Caution can provoke lactate acidosis

7

Common SE of metformin

Abdominal pain, anorexia, diarrhoea (transient), nausea, taste disturbance, vomiting
Increased risk of B12 deficiency

8

Examples of Thiazolidinediones

Pioglitazone
Rosiglitazone

9

Mode of action for thiazolidinediones

Acts as peroxisome proliferated activated receptor gamma (PPAR) in skeletal muscle, adipose tissue and liver cells. Results in transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In this way, pioglitazone both enhances tissue sensitivity to insulin and reduces hepatic gluconeogenesis

10

Examples of Dipeptidyl peptidase 4 inhibitor (Gliptins)

Sitagliptin
Vildagliptin
Saxagliptin
Alogliptin
Linagliptin

11

Mode of action of gliptins

Block DPP-4 which are enzymes which inactivate incretin hormones: Glucagon-like-peptide 1 (GLP-1), glucose dependent insulinotropic polypeptide (GIP). Incretin hormones increase insulin secretion. Therefore inhibiting DDP4 increases insulin levels.

12

Examples of Meglitinides

Repaglinide (Prandin)
Nateglinide

13

Mode of action of Meglitinide

Unlike sulfonylurea, meglitinides have no effect in the absence of glucose. Binds unto Sulfonylurea receptors with weaker affinity and faster dissociation. Results in depolarisation of the beta cell and secretion of insulin.

14

Side effects of meglitinides

Abdominal pain; constipation; diarrhoea; nausea; vomiting

15

Examples of fast acting insulin

Regular insulin (Humulin R, Novolin R)
Insulin lipro (Humalog)
Insulin aspart (Novolog)
Insulin glulisine (Apidra)

16

Examples of intermediate acting insulin

Isophane insulin
Neutral Protamine Hagedorn (NPH) (Humulin N, Novolin N)
Insulin zinc (Lente)

17

Examples of long acting insulin

Extended insulin zinc insulin (Ultralente)
Insulin glargine (Lantus)
Insulin detemir (Levemir)