Adrenergic Pharm Flashcards
Where do adrenergic drugs take effect?
SNS
- a and B receptors (NE) - cardiac muscle, smooth muscle, glands, nerve terminals
- D1 receptors (dopamine) - renal vascular smooth muscle
Where do cholenergic drugs take effect?
PNS
*MAChR (ACh) - cardiac muscle, smooth muscle, glands, nerve terminals, sweat glands
Are sweat glands under sympathetic or parasympathetic control?
Sympathetic
- but controlled by MAChR/ACh, and therefore affected by cholenergic drugs
- cholinomimetics and AChE inhibitors can induce sweating, anticholinergics can inhibit sweating
G protein and effects of
a1 receptors
Gq, increased IP3, DAG
*increased Ca actvates PKC
G protein and effects of
a2 receptors
Gi, decreased cAMP
*decreased PKA activity
G protein and effects of
B receptors
Gs, increase cAMP
*increased PKA activity
G protein and effects of
D1 receptors
Gs, increase cAMP
*increased PKA activity
G protein and effects of
D2 receptors
Gi, decrease cAMP
*decreased PKA activity
Phenylephrine MOA
a1 agonist
Clonidine MOA
a2 agonist
Dobutamine MOA
B1 > B2 agonist
Isoprotenol MOA
B1 = B2 agonist
Albuterol MOA
B2 > B1 agonist
Effects of a1 activation
*Phenylephrine, Norepinephrine
Vasoconstriction
*agonists can cause reflex bradycardia (phenylephrine, norepinephrine)
Effects of a2 activation
*Clonidine
Sympatholytic, decreased BP and HR
*also cause platelet aggregation
Effects of B1 activation
Increased HR and contractility, increased renin release
Effects of B2 activation
Respiratory, uterine and vascular smooth muscle relaxation
- K+ uptake in skeletal muscle
- Gluconeogenesis and glycogenolysis in liver
Effects of B3 activation
Relaxation of detrusor muscle
Effects of D1 activation
Dilates renal vasculature
Effects of D2 activation
modulates neurotransmitter release in brain
Effects of epinephrine
- Increased HR and contractility (B1)
- Increases SBP, decreases bronchial secretions (a1)
- Decreases DBP, relaxes bronchial SM, muscle tremor due to K+ uptake, liver glycogenolysis and gluconeogenesis (B2)
Adrenergic receptors found in the skin and mucous membranes
mostly a1