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Dr. Louis - 9/21/09 - ANS Receptor Review
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129
Pharmacology
Professional
09/27/2009

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Cards

Term
2 Divisions of the Nervous System
Definition
  • Central - Brain, Spine
  • Peripheral - somatic, autonomic
Term
Autonomic N.S. consists of 2 types of innervation:
Definition
  • parasympathetic (CranioSacral CNS outflow)
  • Sympathetic (ThoracoLumbar CNS outflow)
Term
Discription of the Parasympathetic innervation
Definition
Feed or Breed
Term
Description of the sympathetic innervation
Definition
Fight or Flight
Term
Preganglionic Fiber
Definition
nerve fiber before the synapse, not located on the motor neuron
Term
Synapse/Synaptic Cleft
Definition
The space between the preganglionic fiber and the cell body of the post ganglionic fiber
Term
Ganglia
Definition
Where 2 nerves come together, the junction between the pre and post ganglionic nerve.
Term
Nerve Terminal Ending
Definition
End of the post-ganglionic nerve or the end of the motor neuron
Term
Neuro-Effector junction
Definition
The space between the nerve terminal ending and the effector tissue
Term
Neuro-muscular junction
Definition
the space between the motor neuron and the skeletal muscle endplate
Term
Peripheral Cholinergic Receptor locations (3)
Definition
  • Ganglionic (Nn) - at the post-ganglion cell body
  • Effector Site of the PS (muscarinic)
  • Effector Site of the skeletal muscle endplates (Nm)
Term

Peripheral Adrenergic Receptor Locations

 

Definition
  • Effector Tissue - Alpha 1, Beta 1,2,3
  • Prejunctional (autoregulatory) - Alpha 2

 

Term
Prejunctional (autoregulatory) receptors
Definition
regulate the amount of neurotransmitter (NE) released by the adrenergic nerve. When the concentration of NE builds up, it triggers the receptors to reduce the release of NE because there is already too much.
Term
Function of Alpha 2 receptor Agonist
Definition
decreases the amount of neuro transmitter because it over saturates the Alpha-2 receptors with agonist.
Term
Function of Alpha 2 antagonist
Definition
doesn't allow the alpha 2 receptors to regulate, therefore the release of neurotransmitter increases.
Term
Definition of dually innervated effector tissues
Definition

innervation by both divisions of the ANS; antogonistic in nature

 

Ex. One slows and the other speeds up.

Term
Types of Receptors located in the ciliary muscle of the eye
Definition
  • parasympathetic cholinergic innervation-muscarinic - causes the pupil to constrict when innervated
  • causes myosis
Term
Muscles within the eye
Definition
  • ciliary
  • radial
  • sphincter
Term
Receptor types in the radial muscle of the eye
Definition
  • sympathetic adrenergic innervation of the alpha-1 receptor
  • causes pupil dilation - mydriaisis

 

Term
Receptor types of the sphincter muscle of the eye
Definition
  • parasympathetic cholinergic innervation - muscarinic
  • causes pupil constriction - myosis
Term
effect of muscarinic receptor agonist on the eye
Definition
  • causes parasympathetic stimulation thereby causing the pupils to constrict
  • myosis
Term
effect of alpha-1 agonist on the eye
Definition
  • sympathetic stimulation of the alpha 1 receptor resulting in dilation of the pupil
  • mydriaisis
Term
effect of a muscarinic antagonist on the eye
Definition
  • causes mydriasis
Term
Effect of a alpha-1 antagonist on the eye
Definition
  • causes pupil to decrease
  • myosis
Term
Receptor types of the heart and their functions
Definition
  • PS - muscarinic, causes decrease in HR
  • sympathetic - beta-1, causes increase in HR
Term
effect of muscarinic receptor antagonist on the heart
Definition
causes tachycardia
Term
effect of a muscarinic agonist on the heart
Definition
cuases bradycardia
Term
effect of a beta-1 receptor antagonist on the heart
Definition
causes bradycardia
Term
Types of receptors located in the GI tract and their functions
Definition
  • PS - muscarinic, causes increase in GI motility
  • S - alpha-1, causes decrease in GI motility
Term
effect of a muscarinic agonist on the GI tract
Definition
promotes acid secretion and digestion/motility
Term
effect of an alpha-1 antagonist on the GI tract
Definition
promotes digestion - dangerous for people with peptic ulcers
Term
Type of receptors in the salivary glands and effects of drugs on them
Definition
  • PS - muscarinic - MAJOR innervation
  • muscarinic agonist - promotes salivation
  • muscarinic antagonist - produces dry mouth (xerostomia)
Term
Types of receptors in the penis
Definition
  • alpha - 1
  • muscarinic
Term
Bladder muscles
Definition
  • Detrusor
  • Sphincter
  • Trigone
Term
Receptor Types of the Urinary Bladder
Definition
Parasympathetic muscarinic
Term
Effect of a muscarinic agonist in the bladder
Definition

detrusor - contract

sphincter - relax

trigone - relax

Term
Effect of a muscarinic antagonist of the bladder
Definition
urinary retention
Term
Receptor types of the Arterioles
Definition
  • alpha-1
  • beta-2
  • muscarinic
  • histamine
Term
Effect of an alpha 1 agonist on the arterioles
Definition
vasoconstriction
Term
effect of an alpha 1 antagonist on the arterioles
Definition
vasodilation
Term
effect of a beta-2 agonist on the arterioles
Definition
vasodilation
Term
effect of B-2 antagonist
Definition
nothing - its not innervated
Term
Adrenal chromafin tissue receptors are called ____ and are stimulated by which system (PS or S) and by what neurotransmitter?
Definition
nicotinic, Sympathetic, ACh
Term
Lungs - alveolar smooth muscle receptor types
Definition
  • beta 2
  • muscarinic
  • histamine
Term
effect of a B2 agonist and muscarinic agonist on the alveolar smooth muscle of the lungs
Definition

B-2 agonist - relaxation

 

muscarinic agonist - constriction, increased secretions

Term
effect of B2 or muscarinic antagonist on the alveolar smooth muscle of the lungs
Definition
decreased secretions (muscarinic antagonist)
Term
types of receptors located in the secretory glands of the lungs
Definition
muscarinic
Term
effect of a muscarinic agonist on the secretory glands of the lungs
Definition
increased secretions
Term
effect of a muscarinic antagonist on the secretory glands of the lungs
Definition
decreased secretions
Term
receptor types of the kidneys
Definition
beta - 1
Term
effect of a B-1 agonist on the kidney
Definition
increased release of renin to produce angiotensin
Term
effect of a b-1 antagonist on the kidney
Definition
decreased renin release
Term
Receptor type in the arteriolar smooth muscle
Definition
  • alpha 1
  • muscarinic
  • beta - 2
  • histamine

 

Term
effect of a muscarinic, beta 2 and histamine agonist on arteriolar smooth muscle
Definition
vasodilation 
Term
receptor types in uterine smooth muscle
Definition
  • alpha 1
  • beta 2
Term
effect of an alpha agonist on uterine smooth muscle
Definition
contraction
Term
effect of a Beta-2 agonist on uterine smooth muscle
Definition
relaxation
Term
receptor types in the liver
Definition
Beta - 2
Term
effect of a beta 2 agonist on the liver
Definition
  • glycogenolyis
  • glycolysis
Term
receptor type found in adipose tissue
Definition
Beta 2 and 3
Term
effect of a B-2 agonist on adipose tissue
Definition
lipolysis to generate production of Acetyl CoA (energy)
Term
Neurotransmitter
Definition
  • synthesized in nerve
  • released in response to nerve action potential
  • diffuse across synapse to interact with receptor
Term
Neurohormone
Definition
  • chemical substance released
  • travels through blood stream
  • then interacts with receptor tissue to produce effects
Term
Acetylcholine released from where on the lollipop?
Definition
  • pre-ganglionic fibers
  • post-ganglionic fiber of the PS
  • motor neuron
  • CNS
Term
Norepinephrine released from where on the lollipop?
Definition
Post ganglionic adrenergic fiber
Term
Epinephrine released from where?
Definition
Neuro hormone released by adrenal chromafin tissue
Term
Prime receptor affinity of Acetylcholine
Definition
  • nicotinic
  • muscarinic
Term
Prime receptor affinity of Norepinephrine
Definition
  • Alpha - 1
  • Beta - 1
Term
prime receptor affinity of Epinephrine
Definition
  • Alpha 1
  • Beta 1
  • Beta 2
  • Beta 3
Term
Acetyl choline is produced by what 2 substrates utilizing what enzyme?
Definition
choline + Acetyl CoA, Choline acetylase
Term
Acetyl choline is broken down by what enzyme?
Definition
Acetylcholinesterase
Term
Most important mechanism limiting the duration of action of ACh?
Definition
Acetylcholinesterase - breaks down ACh
Term
phenylalanine hydroxylase catalyzes the production of?
Definition
Tyrosine
Term
Tyrosine Hydroxylase does what?
Definition
catalyzes the hydroxylation of tyrosine to create DOPA
Term
DOPA decarboxylase does what?
Definition
decarboxylates DOPA into dopamine
Term
Dopamine Beta hydroxylase does what?
Definition
hydroxylates dopamine into NorEpinephrine
Term
Dopamine is a?
Definition
neurotransmitter in the CNS and PNS; called a cotransmitter (released with the neurotransmitter)
Term
PNMT
Definition
in adrenal glands, PNMT adds a methyl group to norepinephrine to give you EPI
Term
Catecholamine synthetic pathway
Definition
  • phenylalanine
  • tyrosine
  • DOPA
  • Dopamine
  • Norepinephrine
  • Epinephrine (only in the adrenal medulla)
Term
Catacholamine Degradative Enzymes
Definition
  • Monoamine Oxidase (MAO)
  • Catecholamine-O-methyl transferase (COMT)
Term
MAO
Definition
  • located in the adrenergic nerve
  • important for degrading catecholamines which are in the adrenergic nerve or taken back up into the adrenergic nerve
Term
COMT
Definition
  • degrades catecholamines that are released into the neuro-effector junction
Term
Effect of drugs that inhibit MAO
Definition
  • cause an increase in catecholamines in the adrenergic nerve
Term
Effect of drugs that inhibit COMT
Definition
  • inhibit the breakdown of dopamine in the CNS
  • important for Parkinson's treatment
Term
The most important mechanism limiting the actions of NE
Definition

Re-uptake - taking NE back into the nerve; produce the biggest effect to the dose response curve

 

inhibitors of NE re-uptake enhance the effect of NE

Term
Effect of an Alpha 1 agonist on the carotid sinus reflex
Definition
  • vasoconstriction
  • hypertension
  • reflexbradycardia
Term
Effect of an Alpha 1 antagonist on the carotid sinus reflex
Definition
  • vasodilation
  • hypotension
  • reflex tachycardia
Term
Effect of B-1 agonist on the carotid sinus reflex
Definition
  • tachycardia
Term
Beta 1 agonist on the heart causes what effects?
Definition
  • tachycardia
  • +inotropic
  • +chronotropic
Term
effect of alpha agonist on the penis
Definition
ejaculation
Term
effect of muscarinic agonist on the penis
Definition
erection
Term
Receptor types of the lacrimal glands
Definition
muscarinic
Term
effect of muscarinic agonist on the lacrimal glands
Definition
secretion (tears)
Term
types of receptors in the skin
Definition

alpha 1

muscarinic

Term
alpha agonist causes the ____ muscles of the skin to do what?
Definition
piloerector - constrict; hair stands up.
Term
receptor type in the sweat glands
Definition
muscarinic - innervated by the sympathetic system
Term
receptor affinities for isoproterenol
Definition
Beta 1,2,3
Term
Adrenergic alpha 1 receptor agonist potency (EPI, NE and ISO)
Definition
Epi>NE>ISO
Term
Beta 1 receptor agonist potency
Definition
ISO>EPI=NE
Term
Beta 2 receptor agonist potency
Definition
ISO>EPI>>>>>>>>NE
Term
MABP =
Definition
PR x CO
Term
Drug Vulnerable Mechanisms (8)
Definition
  • Axons
  • synthesis of neurotransmitters
  • release
  • neuronal neurotransmitter storage
  • catecholamine reuptake
  • agonist
  • antagonist
  • inhibition of degradation
Term
Tetrodotoxin
Definition
  • local anesthetic
  • interferes with the movement of ions along the neuronal membrane which interferes with the movement of impoulses.
  • not used often, often in conjunction with vasoconstrictor

 

Term
Hemicholinium
Definition
  • inhibits the synthesis of ACh
  • inhibits the uptake of choline into the cholinergic nerve
Term
metyrosine
Definition
  • inhibits tyrosine hydroxylase in order to inhibit the synthesis of epinephrine
  • used in patients with pheochromacytoma
Term
Botulinus Toxin
Definition
  • inhibits the release of ACh
  • locally used for botox
  • reduces the contractile response of muscles
Term
Carbachol
Definition
  • promotes the release of Ach from cholinergic nerves
  • the ACh must be replenished in order for the carbochol to work
  • Indirect acting parasympathomimetic
Term
Tyramine
Definition
  • promotes the release of NE from adrenergic nerves
  • dependent on the adrenergic nerve to be intact
  • a drug that destroys the adrenergic nerve would make it hard for Tyramine to work
  • Indirect Acting Sympathomimetic
Term
Reserpine
Definition
  • adrenergic neuron blocker
  • works in the CNS and PNS
  • taken into the adrenergic nerve and causes impairment of the neuronal storage of NE and dopamine
  • results in more deamination of NE by MAO and less available for release in response to nerve action potential
Term
Guanethidine
Definition
  • adrenergic neuron blocker
  • charged - so no CNS effects
  • inhibits the release of NE and causes impairment of the storage of NE
Term
Cocaine
Definition
  • inhibts catecholamine re-uptake
  • synergizes the effect of NE (greater effect from NE)
  • sympathomimetic like effect
Term
Tricyclic Antidepressant
Definition
  • inhibit the re-uptake of NE and seratonin in the CNS
Term
6 OH Dopamine
Definition
  • destroys adrenergic nerve
  • makes it hard for a drug like Tyramine to work
Term
Alpha -1 Agonists - name three
Definition
  • Phenylephrine - synthetic sympathomimetic; mimics the effect of NE on alpha receptors
  • NE
  • EPI - most potent alpha agonist
Term
Clonidine
Definition

Alpha 2 agonist

 inhibits the release of NE via autoregulatory agonism. Not an adrenergic neuron blocker

Term
Beta-1 agonist (4)
Definition
  • NE - causes tachycardia and + inotropism
  • EPI - increase HR and BP;
  • ISO - non-selective B agonist,
  • Dobutamine - prototype B1 agonist - tachycardia and +inotropism
Term
Beta - 2 agonists (2)
Definition
  • EPI
  • ISO
  • ex. albuterol - causes bronchodilation
Term
Methacoline
Definition
Muscarinic agonist - not broken down as readily/quickly as ACh
Term
Nicotinic agonist example
Definition
  • nicotine
Term
hexamethonium
Definition
  • ganglionic blocker
  •  nicotinic sub n antagonist;
  • used for emergency BP lowering;
  •  non-selective
Term
D-tubercurare
Definition
  • nicotinic sub m antagonist
  • causes skeletal muscle paralysis
Term
Atropine (type)
Definition
  • muscarinic antagonist

 

Term
phenoxybenzamine
Definition
  • alpha 1 antagonist
  • mixed antagonist
Term
Yohimbine
Definition
  • alpha 2 receptor antagonist
  • no therapeutic value yet
Term
Atenolol and its indications
Definition
  • beta-1 antagonist (beta blocker)
  • used for glaucome, protection against MI and HTN
Term
Propranolol
Definition
  • non-selective B-blocker (Beta 1-3)
  • has membrane stabilizing effect which is beneficial for protection against MI or arrhythmia.
  • membrane stabilizing effect not beneficial for glaucoma treatment - stabilizing the eye membrane would make the eye less sensitive to particles - producing damage without you knowing they were there
Term
Neostigmine
Definition
  • Acetylcholinesterase Inhibitor
  • increases ACh at muscarinic and nicotinic receptors
  • effects limited to PNS
Term
Tranylcypromine
Definition
  • Monoamine oxidase Inhibitor
  • inhibit the degredation of NE
  • not really used anymore
Term
muscarinic receptor agonist in the skin causes what?
Definition
sweating
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