Adrenergic System Flashcards
Phosphatidylinositol 4,5-bisphosphate (PIP2) is cleaved into two second messengers:
diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3).
Mechanism of alpha 1 action
•Binding of agonist
•Activation of Gprotein
•Activation of phospholipase C…..cleaving of PIP2 to DAG and IP3
•Release of intracellular Calcium
•Activation of protein kinase C and calcium calmodulin complex which activates MLCK
•MLCK phosphorylate mlc leading to contraction
Beta 1 receptors are primarily found in the
Heart
What is the effect of beta 2 receptor activation in the bronchi
Bronchodilation- relaxation of smooth muscles
Isoprenaline is a ……… receptor agonist and has no effect on ……….. receptor
Beta
Alpha
Examples of a direct acting alpha 1 agonist
Methoxamine
Phenylephrine
Meturamin
Mephenteramine
Use of direct acting alpha 1 agonist
•Nasal decongestion
•Management of hypotension due to overdose
•Blood pressure elevation during spinal anaesthesia
•Combined with local anesthetics to prolong effect
•Mydraitic agents
Example of direct acting alpha 2 agonist
Brimonidine
Apraclonidine
Clonidine
Guanabenz
Guanfacine
A side effect of alpha 2 agonists
Sexual dysfunction
Rebound htn
Bradycardia
An example of a B1 agonist is
Dobutamine
…………….. is a non selective beta agonist
Isoprenaline
Beta 2 agonists Include
Salbutamol
Terbutaline
Fenoterol
Albuterol
Levalbuterol
The indirect acting sympatomimetics are
Amphetamine
Metamphetamine
Methylphenidate
Cocaine
Ephedrine
Example of an alpha 2 selective blocker used to improve sexual performance
Yohimbine
Non selective alpha receptor blockers
Phenoxybenzamine
Phentalamine
Alpha 1 receptor inhibitors
Prazosin
Doxazosin
Terazosin
Trimazosin
Alpha receptor antagonists are used to treat
Pheochromocytoma
Chronic HTN
Hypertensive emergencies
HTN due to pheochromocytoma
Symptoms of BPh
Beta 1 selective antagonists are
Metoprolol
Atenolol
Alprenolol
Esmolol
Non selective beta blockers
Propanalol
Nadolol
Pindolol
Timolol
Selective beta 2 blockers
Butoxamine
Beta blockers are used in the treatment of
HTN
IHD
Heart failure
Neuronal uptake is inhibited by
Tricyclic antidepressants
Tyrosine hydroxylase is inhibited by
Metyrosine
Direct acting sympathomimetics
Metaraminol
Mephentamine
Methoxamine
Phenylephrine
Epinephrine