Adrenergic Pharmacology Flashcards
Define ‘Adrenergic’.
Relating to nervous system cells involving neurotransmitters (i.e. adrenaline or noradrenaline)
List the points of sympathetic outflow.
- Short pre-ganglionic axons
- Long post-ganglionic axons
- Adrenal medulla
What is released by the post-ganglionic sympathetic nerve terminals?
Noradrenaline, ATP and sometimes other co-transmitters such as NPY
What is transferred to the sweat glands?
ACh
What are the effects of beta(1) - and beta(2) - adrenoceptors?
beta(1) - stimulatory and innervated
beta(2) - inhibitory; non-innervated; circulating adrenaline
Where are innervated beta-adrenoceptors found?
- Heart
- Juxtaglomerular apparatus - release of renin
- Adipose Tissue Brown; lipolysis
Where are non-innervated beta-adrenoceptors found?
- Bronchial Smooth Muscle
(i. e. in the treatment of asthma) - Uterine Smooth Muscle
(i. e. treatment of premature labour)
3.Skeletal muscle vasculature
Describe the main metabolic effects of activation adrenoceptors.
beta(2) - adrenoceptor activates adenylate cyclase (AC)
Describe the adrenoceptor-related process involved in the liver, muscles, pancreas and adipocytes
Liver: glycogenolysis
(glycogen –> glucose)
alpha-1 release of K+ (hyperkalaemia)
Muscle: hyperlactic acidaemia
(glycogen –> lactic acid)
+ activation of Na+/K+ ATPase
decreased Blood K+ (hypokalaemia)
Pancreas: insulin release;
alpha-2 (-ve); beta-3?
Adipocytes: lipolysis;
FFA; beta-3
What are the subdivisions of alpha-adrenoceptors?
alpha-1 - post-junctional/synaptic (heteroreceptor)
alpha-2 - pre-junctional/synaptic (autoreceptors)
What kind of feedback is related to alpha-2 and beta-2?
alpha-2 - negative feedback
beta-2 - positive feedback
Which adrenoceptors is adrenaline selective for?
alpha-1
alpha-2
beta-1
beta-2
Which adrenoceptors is noradrenaline selective for?
alpha-1
alpha-2
beta-1
Which adrenoceptors is isoprenaline selective for?
beta-1
beta-2
What are the effects of adrenoceptors on the heart?
beta-1 - increase force and rate
What are the effects of adrenoceptors on the blood vessels?
alpha-1 - constrict
alpha-2 - constrict
beta-2 - dilate
What are the effects of adrenoceptors on the bronchi?
beta-2 - dilate
What are the effects of adrenoceptors on the GI tract (motility and tone)?
alpha-1 - decrease
alpha-2 - decrease
beta-2 - decrease
What are the effects of adrenoceptors on the uterine smooth?
beta-2 - relax
What are the effects of adrenoceptors on the bladder detrusor?
beta-2 - relax (beta-3)
What are the effects of adrenoceptors on the bladder sphincter?
alpha-1 - contract
What are the effects of adrenoceptors on the eye (radial muscle)?
alpha-1 - contract
What are the effects of adrenoceptors on the skeletal muscle?
beta-2 - tremor
What are the effects of adrenoceptors on the kidney?
beta-1 - renin release
What are the effects of adrenoceptors on the liver?
alpha-1 - glycogenolysis (minor)
beta-2 - glycogenolysis
What are the effects of adrenoceptors on the fat cells?
beta-1 - lipolysis (beta-3)
What are the effects of adrenoceptors on the mast cells?
beta-2 - inhibition of histamine release
What are the effects of adrenoceptors on the platelets?
beta-2 - aggregation
Give an example of a clinical effect of an alpha(1) - adrenoceptor agonists
Phenylephrine, used as nasal congestant
What are the clinical effects of adrenaline?
BP - effet depends on dose Skeletal muscle - tremor Uterine smooth muscle - relax Mast Cell - "stabilisation" Bronchial smooth muscle - relax CNS effects - foreboding
Give some examples of clinical uses of adrenaline.
- Anaphylactic shock - “physiological antagonism”
- Glaucoma
- Cardiac arrest (cardiopulmonary resuscitation)
- prolongation of the action of local anaesthetics
Adrenaline use in anaphylactic reactions
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