Pharmacology Flashcards
Gq
Contraction of vascular smooth muscle
a1
Gi
Inhibition of noradrenaline release
a2
Gs
Positive inotropic and chronotropic effect
B1
Gs
Relaxation of bronchial smooth muscle
B2
Gq
Increased gastric acid secretion
M1
Gi
Decreased HR
M2
Gq
Increased saliva
Visceral smooth muscle contraction
M3
Gs stimulates
Adenylyl cyclase
Gq
Stimulation of phospholipase C
Gi
Inhibition of adenylyl cyclase
Drug elimination rate independent of dose
Zero order kinetics
Drug elimination proportional to dose
First order kinetics
What is the steady state
Rate admin = rate elimination
Phase I metabolism
Oxidation, hydrolysis and reduction
Phase II metabolism
conjugation to make more hydrophilic
Examples of biguanides
Metformin
Action of biguanide
Decreases hepatic gluconeogenesis via AMP protein kinases
Increases peripheral uptake
Reduces carb absorption
Increases fatty acid oxidation
Indications for metformin
1st line T2DM
Protective against risks
WEIGHT LOSS
No hypoglycemia risk
Side effects of metformin
GI upset
Lactic acidosis
Sulfonylureas examples
Tolbutamide
Gliclazide
Sulfonurea action
Displaces Mg-ADP on SUR1 from Katp channel
B cell depolarises
Stimulates insulin release
Sulfonylurea indications
Add on T2DM
MODY ( HNF-1a)
Sulfonylurea side effects
Weight gain
HYPOglycemia
LFT derangement
Thiazolidione example
Pioglitazone
Thiazolinediones action
PPARy activator to:
Increase insulin signalling (more glucose uptake)
Increased uptake and metabolism of FAs (reduce resistance)
Thiazolinedione usage
Add on in T2DM (HbA1c reduced by 0.6-1.5%)
Contraindications of thiazolinediones
3-5kg weight gain
Fracture risk
Hepatotoxic
fluid retention
SGLT-2 inhibitors
Dapagliflozin
Canagliflozin
Empagliflozin
SGLT-2 inhibitor mechanism
blocks SGLT-2 to prevent glucose reabsoprtion in PCT
Uses
Add on T2DM
sglt-2 side effects
UTIs
Ketoacidosis
DPP4 inhibitors
‘gliptins’
DPP4 inhibitor action
inhibits DPP4 enzyme so GLP-1 and GLP can work longer
Increases insulin and decreases glucagon
DPP4 uses
alone/ add on to T2DM