Therapies for Diabetes (4.1) Flashcards
What is the first choice pharmacological treatment for Diabetes?
Biguanides
What is the mode of action of Metformin?
Decreases hepatic gluconeogenesis
Increases cell receptor sensitivity to glucose
Decreases glucose absorption from the gut
Increases glucose uptake into skeletal muscle and adipose tissue
What are the main ADRs of Metformin?
Dyspepsia
Diarrhoea
Risk of lactic acidosis in patients with renal failure as the drug is excreted renally
What is the mode of action of Gliclazide?
(Sulphonylurea) Stimulates pancreate B cells to secrete insulin;
1) Binds to and antagonises B cell K+ ATP channels
2) Increases K+ concentration which depolarises the cell
3) Opens calcium channels = Ca2+ influx
4) Insulin vesicles fuse with cell membrane
5) Insulin released via exocytosis = Increased insulin concentration
What are the main ADRs of Glizlazide?
Weight gain (Due to insulin being anabolic and increasing appetite) High risk of hypoglycaemia if the patient hasn't eaten - especially as the metabolites of Sulphonyureas are active
Why do NSAIDs increase the risk of hypoglycaemia in patients on Sulphonylureas?
Sulphonylureas are highly bound to albumin so NSAIDs displace them increasing their concentration and causing more ADRs
What is the mode of action of SGLT2 inhibitors?
Inhibit the SGLT2 transporter in the PCT causing less glucose to be reabsorbed so more is excreted in the urine
What are the ADRs of SGLT2 inhibitors?
Thrush
UTIs
Hypoglycaemia
What is the mode of action of Acarbose?
(Alpha glucose Inhibitors) - Decreases activity in the gut so less glucose is absorbed leading to delays in it entering the blood
What are the ADRs of Acarbose?
Flactulence
Diarrhoea
Loose stools
Large doses cause increase in ALT (Alanine Transaminase enzyme released when liver damaged)
What is the mode of action of Repaglinide?
(Meglitinide) - Similar mode of action as Sulphonylureas but have a shorter t1/2 and quicker action so can be taken before a meal
What is the mode of action of Pioglitazone?
(Thiazolidinediones/Glitazones) - Activates PPARs which alter gene transcription causing an increase in glucose sensitivity and a decrease in gluconeogenesis in the liver
What are the ADRs of Pioglitazone? (A Thiaxolidinedione/Glitazone)
Weight gain
Decrease bone production via osteoblasts
Water retention leading to oedema
What is always the first treatment in type II Diabetes?
Lifestyle changes
