CPTP 2.9 ANS 2 Flashcards
What happens to adrenergic neurotransmitters after they are released?
The signal at the postjunctional effector site is rapidly terminated, because NE is either converted to inactive metabolites or is taken up by the neuron
Describe adrenergic receptor
- Respond to epinephrine, NE and dopamine
- Located in effector organs/ tissues of sympathetic system
- G-protein coupled receptors
- Slow (seconds) responses
Type of G-protein and its action in response to alpha 1 adrenoreceptor
Gq
Activates PLC
Type of G-protein and its action in response to alpha 2 adrenoreceptor
Gi
Inhibit adenylyl cyclase
Type of G-protein and its action in response to beta adrenoreceptors
Gs
Stimulate adenylyl cylase
What are the major effects mediated by A1 receptors?
PLC activated -> increased production of DAG and IP3 -> increase in calcium influx
- vasoconstriction (major effect)
- increased peripheral resistance
- increased BP
- relaxation of GI smooth muscle
What are the major effects mediated by A2 receptors?
inhibition of adenylyl cyclase -> decreased production of cAMP -> inhibition of further release of NE from the neuron
- inhibition of NE release
- inhibition of ACh release
- inhibition of insulin release
What are the major effects mediated by B1 receptors?
- increase HR (major effect)
- increased myocardial contractility (major effect)
- increased lipolysis
- increased release of renin
What are the major effects mediated by B2 receptors?
- bronchodilation (major effect)
- vasodilation
- decreased peripheral resistance
- hepatic and muscle glycogeolysis
Which one has higher affinity to each adrenoreceptor, NE or E?
A1 - NE
A2 - E
B1 - NE
B2 - E
Name the agonists that tend to act on each adrenoreceptor
A1 - phenylephrine
A2 - clonidine
B1 - Dobutamine
B2 - Salbutamol
Therapeutic uses of sympathomimetics (adrenergic agonist)
- cardiac arrest
- cardiogenic shock
- anaphylaxis
- asthma
- nasal decongestion
- increase duration of action of local anaesthetic
- premature labour
- hypertension, migraine
cardiac arrest - epinephrine (IV)
cardiogenic shock - dobutamine to increase myocardial contractility
anaphylaxis - epinephrine for bronchodilation and vasodilation
asthma - salbutamol for bronchodilation
nasal decongestion - phenylephrine
increase duration of action of local anaesthetic - epinephrine
premature labour - salbutamol (B2 receptors present in wall of uterus)
hypertension, migraine - clonidine
Name the adrenergic antagonists that act on each adrenoreceptor
A1 - Phenoxybenzamine, Doxazosin
A2 - Phenoxybenzamine
B1 - Propranolol, Bisopraolol
B2 - Propranolol
Clinical uses of alpha adrenergic antagonist in hypertension
Hypertension - A1 antagonist doxazosin causes vasodilation
Phaeochromocytoma - nonselective alpha antagonist phenoxybenzamine causes irreversible blockade of adrenoreceptors
Benign prostatic hyper
Clinical uses of alpha adrenergic antagonist in phaeochromocytoma
non-selective alpha antagonist phenoxybenzamine causes irreversible blockade of adrenoreceptors