Adrenergic Pharmacology Flashcards
What does post-autonomic ganglion neurotransmission depend on?
Catecholamines
Where is noradrenaline released from
sympathetic nerve fibre ends, often used in the intensive care unit
Where is adrenaline released from
adrenal glands (fight or flight, management of anaphylaxis
What is dopamine
The precursor for adrenaline and noradrenaline
Tyrosine -> DOPA -> Dopamine -> Noradrenaline -> Adrenaline
Alpha 1 receptor activation role
(NAd > Ad)
A1 activation = contracts smooth muscle= vasoconstriction, mainly in the skin and splanchnic (abdominal) beds
Noradrenaline is given IV for shock in ITU setting, or to overcome anaesthetic agents alpha blocking effects
However, adrenaline is stable and available intramuscularly, so useful in anaphylactic shock
Topical alpha activation useful in nasal decongestion (xylometazoline)
Alpha 2 receptor activation role
(NAd=Ad)
Mixed effects on vascular smooth muscle
Exist in brain
E.g., clonidine = alpha-2 agonist used in ADHD to help concentration - reduces vascular tone and reduces blood pressure
Alpha 1 blocker role and example
Lower blood pressure
e.g doxazosin (generally less frequently used than modern antihypertensives)
e.g phenoxybenzamine = phaeochromocytoma (catecholamine secreting tumour)
e.g. tamulosin for BPH
Alpha 2 blocker example
Tetracyclic antidepressants are A2 blockers
e.g mirtazapine
but antidepressant effect from other mechanism
Mainly used in research - no clinically useful applications yet found
Beta 1 receptors
Beta 1 receptor mainly in the heart, kidney and fat cells
Agonism leads to - Tachycardia, increased stroke volume, renin release (increase in vascular tone)
Lipolysis and hyperglycaemia
Beta 1 blockers role
Reduce heart rate
reduce stroke volume
reduce myocardial oxygen demand and help remodelling in heart failure or post-myocardial infarction
e.g. bisoprolol, propranolol
Caution in asthma
Beta blocker overdose treatment
Glucagon increases heart rate and myocardial contractility irrespective of the presence of beta-receptor blockers
Beta 2 receptor role
Bronchi - bronchodilation
Bladder wall - inhibits micturition
Uterus - inhibition of labour
Skeletal muscle - increase contraction speed (induces tremor)
Pancreas - insulin and glucagon secretion
Beta 2 agonist drugs
Salbutamol - useful in asthma and COPD
Side effects - tremor, hyperglycaemia (glucagon release) and tachycardia
Also used in tocolysis (delayed preterm labour)