Pharm drugs Flashcards
Primary mechanism
of action of metformin
Primary effect – metformin activates AMPK in hepatocyte mitochondria. This inhibits ATP production. This blocks gluconeogenesis and subsequent glucose output. It also blocks adenylate cyclase which promotes fat oxidation. Both help to restore insulin sensitivity.
Drug target of metformin
5′-AMP-activated protein kinase (AMPK)
in hepatocyte mitochondria
Main side effects of metformin
GI side effects (20-30% of patients)
e.g. Abdominal pain, decreased appetite, diarrhoea, vomiting)
Particularly evident when very high doses are given. A slow increase in dose may improve tolerability
examples of Dipeptidyl-peptidase 4 (DPP-4) inhibitors
sitagliptin
Primary mechanism of action of DPP-4
Primary effect - Work by inhibiting the action of DPP-4. This enzyme is present in vascular endothelium and can metabolise incretins in the plasma. Incretins (e.g. GLP-1) are secreted by enteroendocrine cells and help stimulate the production of insulin when it is needed (e.g. after eating) and reduce the production of glucagon by the liver when it is not needed (e.g. during digestion). Incretins also slow down digestion and decrease appetite.
DPP-4 drug target
DPP-4.
The primary site of DPP-4 inhibitor action is the vascular endothelium
main side effects of DPP-4
Upper respiratory tract infections (5% of patients) Flu-like symptoms e.g. headache, runny nose, sore throat Less common but serious: Serious allergic reactions/ avoid in patients with pancreatitis
Examples of sulphonylurea
gliclazide
Primary mechanism of action of sulphonylurea
Primary effect – Inhibit the ATP-sensitive potassium (KATP) channel on the pancreatic beta cell. This channel controls beta cell membrane potential. Inhibition causes depolarisation which stimulates Ca2+ influx and subsequent insulin vesicle exocytosis.
drug target for sulphonylurea
ATP-sensitive potassium channel
The primary site of SUs inhibitor action is the pancreatic beta cell
main side effects of sulphonylurea
weight gain is a likely side effect of hypoglycemia (2nd most common)
in clinic, BP above 140/90 will be given what
ABPM/HBPM
Above what blood pressure measured in clinic means pt need ABPM/HBPM
above 140/90
ABPM/HBPM- what to do under 135/85
monitor at least every 5 years
ABPM/HBPM- what to do 135/85-149/95
what stage hypertension?
start drug treatment if there is any of the following:
-target organ damage, CVD, renal disease, diabetes, at 10-year CVD risk 10%+
stage 1 hypertension
