L5 - Autonomic Nervous System 1 Flashcards
Breifly describe the structure of the ANS?
There’s 2 divisions: parasympathetic (PNS) and sympathetic (SNS).
PNS - pre-ganglionic nerves come from cranial or sacral nerves… post-ganglionic nerves release acetylcholine onto muscarinic receptors.
SNS - pre-ganglionic nerves come from thoracic or lumbar nerves…post-ganglionic nerve release noradrenaline onto adrenergic receptors (α and β)
How do postganglionic nerves of the ANS release neurotransmitters onto effector organs?
They enter the effector organs and form varcosities which contain neurotransmitters. These are released upon nerve action potential, which then activates receptors on the effector organs, inducing a response.
Where are M2 and M3 (muscarinic receptors) located, and when activated, what do they do?
M2 - heart, decreases heart rate
M3 - smooth muscle & glands, contract and secrete fluids
Where can we find α1 adrenoceptors, and what do they do when activated?
In vascular smooth muscle. When they’re activated they contract
Where are the 3 β-adrenoceptors located, and when activated what to they do?
β1 - Heart, increases heart rate and force of contraction
β2 - Smooth muscle, relaxation
β3 - Fat
What are some of the mechanisms by which drugs modulate ANS function?
Drugs can affect the ANS by:
- increasing or decreasing the levels of neurotransmitter
- activating neurotransmitter receptors
- blocking neurotransmitter receptors
What are adrenoceptor agonists?
They bind to and activate adrenoceptors, e.g. adrenaline, phenylephrine, salbutamol
- Other names: sympathomimetics or adrenomimetics (note the word “mime” = to copy)
- Can target one or more of the 5 subtypes
What do the direct effects of a given adrenoceptor agonist depend on?
- receptor selectivity of the drug
- adrenoceptor profile of the cell
- cellular response to receptor activation
Name a selective α1 adrenoceptor agonist and describe its effect.
Phenylephrine - primary effect = vasoconstriction.
used to decongest nasal passage by constricting blood flow
Name a selective β2 adrenoceptor agonist and describe its effect.
Salbutamol (known as ‘Ventolin’) - causes relaxation of smooth muscle of airways. (it relieves bronchoconstriction)
Name a selective α1 adrenoceptor antagonist and describe its effect.
Prazosin - reverses α1-mediated contraction of vascular smooth muscle causing vasodilation and lowers blood pressure.
Name a non-selective β adrenoceptor antagonist and describe its effect.
Propranolol - binds to and inhibits both β1 and 2.
β1 - decreases heart rate and contractility, reducing cardiac output and blood pressure.
β2 - exacerbate bronchoconstriction
Name a selective β1 adrenoceptor antagonist and describe its effect.
Metoprolol - decreases heart rate and contractility, reducing cardiac output and reduce blood pressure
What are some desirable pharmacodynamic actions of β-blockers?
β blockers are not all the same - there are vasodilatation effects, antioxidant activity, K+-channel blockade, partial agonist activity, and membrane stabilising activity.
Are Beta-1 receptors activated by noradrenaline, or adrenaline?
Noradrenaline. Beta-2 are activated by adrenaline