Pharmacology - Intro to ANS Drugs (Exam 2) Flashcards
What makes up the ANS
sympathetic and parasympathetic nervous systems
CNS =
brain + spinal cord
Somatic nervous system is for ________ movements while the ANS is for _________ movements
voluntary (skeletal muscle); involuntary
Origin of somatic nervous system
all levels of the brain and spinal cord
Origin of ANS - sympathetic
thoracic and lumbar level of spinal cord
Origin of ANS - parasympathetic
brain (cranial nerve nuclei) and sacral spinal cord
Describe length of preganglionic and postganglionic fibers of SNS
Short preganglionic
Long postganglionic
Describe length of preganglionic and postganglionic fibers of PNS
Long preganglionic
Short postganglionic
Preganlionic fibers of SNS synapse on 3 different ganglia. Name them
1) paravertebral
2) prevertebral
3) terminal
What are the paravertebral ganglion of the SNS? What are their targets?
Superior cervical ganglion (head and neck)
Superior, middle, and inferior ganglia (heart)
What are the prevertebral ganglion of the SNS? What are their targets?
Celiac
Superior mesenteric
Inferior mesenteric
(stomach, small intestine, colon)
What is the target of the terminal ganglion of the SNS?
Bladder
Rectum
Preganglionic fibers of the PNS arise from which cranial nerve nuclei?
CN III, VII, IX, and X
Preganglionic fibers of the PNS arise from which region of the spinal cord?
Sacral region
CN III has which ganglion? Where is it located?
Ciliary ganglion: in the orbit
CN VII has which ganglia? Where are they located?
Submandibular and sublingual ganglion: in submandibular and sublingual glands
Pterygopalatine ganglion: in lacrimal gland and mucus-secreting glands
CN IX has which ganglion? Where is it located?
Otic ganglion: parotid gland
Where are ganglia of CN X located?
Heart
Viscera of thorax and abdomen
What do neurons from sacral segments form?
Pelvic nerves
What ganglia do pelvic nerves synapse in? Where are these ganglia located?
Terminal ganglia: uterus, bladder, rectum, sex organs
Which system is “fight or flight” - a protecting mechanism to help cope with stress or get away from it?
Sympathetic nervous system
Which system is involved with E activities? Name these activities
Sympathetic nervous system
Exercise
Excitement
Emergency
Embarassment
What symptoms are illustrated by a person who is threatened (sympathetic nervous system - fight or flight)?
Heart rate increases
Breathing rate increases
Skin is cold/sweaty
Pupils dilate
Which system is “rest and digest” - to maintain essential body functions, digestive processes, and elimination of wastes?
Parasympathetic nervous system
Which system is involved with D activities? Name these activities
Parasympathetic nervous system
Digestion
Defecation
Diuresis
What symptoms are illustrated by a person who relaxes after a meal (parasympathetic - rest and digest)?
Heart rate decreases
Breathing rate decreases
Skin is warm
Pupils constrict
GI activity increases
Sympathetic output is _______
Diffuse
Each sympathetic preganglionic fiber branches to make synapses with many ganglionic neurons
Divergence
Each ganglion cell may receive several preganglionic fibers
Convergence
Sympathetic preganglionic fibers can give rise to ___________ fibers, innervating more than one ________ distributed in many parts of the body
postganglionic; organ
T/F: the SNS functions as a unit
True
Parasympathetic output is _________
Discrete
Parasympathetic postganglionic neurons are not __________. They are directed to a _________ organ
branched; specific
Discrete parasympathetic fibers are activated __________, and the system functions to affect _______ ______
separately; specific organs
The parasympathetic nervous system is organized for ________ and ______ activities
discrete; localized
T/F: most visceral organs are innervated by only the parasympathetic nervous system
False! They are innervated by both SNS and PNS
We can describe the relationship between parasympathetic and sympathetic nervous systems as?
dynamic antagonisms
(precisely controls visceral activity)
Sympathetic fibers __________ heart and respiratory rates, and __________ digestion and elimination
increase; inhibit
Parasympathetic fibers __________ heart and respiratory rates, and __________ digestion and elimination
decrease; increase
Put the steps of synaptic transmission in the correct order
1. fusion of vesicles containing neurotransmitters with membrane and release of neurotransmitter into synaptic cleft
2. AP is generated causing depolarization.
3. Ca2+ enters the cell
4. Transmitters diffuse across cleft and bind to receptors on postsynaptic membrane to induce a response in postsynaptic neuron.
2, 3, 1, 4
Which neurotransmitters are released from sympathetic and parasympathetic preganglionic fibers?
Achetylcholine (ACh) for both
What does ACh from sympathetic and parasympathetic preganglionic fibers bind to?
Nicotinic receptors
Which neurotransmitters are released from sympathetic and parasympathetic postganglionic fibers?
Sympathetic: NE
Parasympathetic: ACh
What does NE from sympathetic postganglionic fibers bind to?
Adrenergic receptors
What does NE from parasympathetic postganglionic fibers bind to?
Muscarinic receptors
What are 4 parts of adrenergic neurotransmission?
Catecholamine synthesis
Adrenergic transmission
Adrenergic receptors
Catecholamine fate
Enzyme that converts phenylalanine -> tyrosine
phenylalanine hydroxylase
Enzyme that converts tyrosine -> dihydroxyphenylalanine
tryosine hydroxylase
Enzyme that converts dihydroxyphenylalanine -> norepinephrine
aromatic L-amino-acid decarboxylase
Enzyme that converts norepinephrine -> epinephrine
phenylethanolamine-N-methyltransferase
Enzyme that converts dopamine -> norepinephrine
dopamine beta hydroxylase
Put the steps of adrenergic neurotransmission in order:
1. Tyrosine is transported into adrenergic ending & converted to dopa by tyrosine hydroxylase and then to dopamine
2. AP causes influx of Ca2+ which causes vesicle to fuse with plasma membrane and NE is released.
3. Dopamine is transported into vesicles and converted to NE by dopamine-B-hydroxylase
4. Transmitter activates receptors in postsynaptic membrane.
1, 3, 2, 4
What are the 2 types of adrenergic receptors?
Alpha (a1, a2)
Beta (B1, B2, B3)
Where are adrenergic receptors located?
Postganglionic sympathetic junctions where NE is released from postganglionic sympathetic nerves
This adrenergic receptor is responsible for smooth muscle contraction (blood vessel constriction, radial muscle in iris contraction, GI and bladder sphincter contraction)
alpha 1
This adrenergic receptor is found on the presynpase and responsible for negative feedback and inhibiting neurotransmitter release
alpha 2
This adrenergic receptor is found on the heart (increase heart rate and contractility) and kidney (renin release)
Beta 1
This adrenergic receptor is responsible for relaxation of visceral smooth muscle (dilate skeletal muscle blood vessels, relax bronchial smooth muscle, relax intestinal and bladder function)
Beta 2
This adrenergic receptor is responsible for lipolysis in fat cells and detrusor muscle relaxation
Beta 3
What happens to NE at adrenergic junctions?
most NE is removed from the synaptic cleft through reuptake to presynpatic neruons
What happens to cytoplasmic NE that is not transported into synaptic vesicles?
Degraded by monoamine oxidase
Put the steps of cholinergic transmission in order:
1. Ach is hydrolyzed by acetylcholine-esterase; terminating the action of the neurotransmitter
2. Ach binds to and activates postsynaptic Ach receptors
3. Once synthesized, Ach is transported into and packaged into vesicles
4. Ach is synthesized from acetyl CoA and choline through catalytic action of of choline acetyl transferase
5. AP triggers influx of Ca2+ and facilitates fusion of vesicles w/ terminal membrane and causes release of Ach into synaptic space.
4, 3, 5, 2, 1
Where are muscarinic receptors located? What are they innervated by?
Effector cells (heart, smooth muscle, secretory glands)
Innervated by postganglionic parasympthatic nerves
How many subtypes of muscarinic receptors are there?
5 (M1-M5)
What kind of receptors are muscarinic receptors?
G protein coupled receptors
Where are nictonic receptors located?
Postganglionic nerve cell bodies in all autonomic ganglia, medulla, and skeletal muscle in the somatic nervous system
What kind of receptors are nicotinic receptors?
Ligand gated ion channels
Locations of M1, M2, and M3 (subtypes of muscarinic receptors)
M1: stomach and enteric system
M2: heart
M3: eye, glands, lungs, and vascular endothelium
What happens when M1 receptors are stimulated?
Increased secretions along GI tract
What happens when M2 receptors are activated?
Decreased contracility of heart/heart rate
What happens when M3 receptors are stimulated?
-Circular muscle contraction (pupillary constriction)
-Excretions from nose, tears from eyes, defecation, and urination
-Bronchoconstriction
How many subtypes of dopamine receptors are there?
5 (D1-D5)
What kind of receptors are dopamine receptors?
G protein coupled receptors
Where do dopamine receptors play important roles?
CNS
Where are some D4 receptors found?
Heart
What do D4 receptors in the heart do?
Increase myocardial contractility and cardiac output
Do NOT change heart rate
Dopamine receptors can be present in the nephron of the kidney. What is the action of these receptors?
Diuresis and natriuresis
Which cells in the kidney have the highest density of dopamine receptors?
Proximal tubule epithelial cells
Where are purinergic nerves found?
GI tract, vasculature, lungs, bladder, and CNS
ATP is stored in vesicles in purinergic nerve endings and activates ______ receptors when released
P2 (purinergic receptor)
ATP can be broken down to adenosine. Adenosine activates what kind of receptors?
P1 (adenosine receptor)
How many types of P1 receptors are there?
4
How many groups of P2 receptors are there?
2
Adenosine can regulate the release of ________ through a feedback mechanism
NE
ATP acts as a _________________ with NE and Ach
co-transmitter
Release of more than one neurotransmitter from the same nerve terminal may result in __________ or _________ actions
synergistic; opposite
Various peptide ____________ are released with classic ANS transmitters
co-transmitters
When co-transmitter release occurs, substances may have slightly different
functions, one functioning as _________________ and the other acting as a ____________________. They may also act cooperatively as transmitters to elicit physiologic response
neurotransmitter and neuromodulator
This type of receptor acts directly on the channel protein
Ion channel-linked receptor
Ion channel-linked receptors are also __________ receptors
nicotinic
How are G protein-linked receptors (GPCRs) coupled to the ion channel?
Through a G protein
What does coupling a G protein to a GPCR modulate?
Formation of diffusible 2nd messengers
What are some of the other 2nd messenger systems?
-cGMP
-Ca2+
-Calmodulin
-Nitric oxide
-Prostanoids
-Peptides
What 2 things contribute to the regulation of blood pressure?
Spinal cord
Brainstem
The main integration center for the ANS is the _______.
hypothalamus
Name the 4 mechanisms of action of agonism
- Receptor agonists (direct)
- Facilitate release
- Block reuptake
- Affect metabolism
Drugs that enhance neurotransmission
Agonists
Name the 5 mechanisms of action of antagonism
- Inhibit synthesis
- Inhibit release
- Disrupt vesicular transport and storage
- Receptor antagonists (direct)
- Affect metabolism
Drugs that inhibit neurotransmission
Antagonists
What type of drugs are agonists and antagonists?
Autonomic drugs
What type of drugs are sympathomimetics and sympatholytics?
Sympathetic drugs
Drugs that enhance or mimic noradrenergic transmission
Sympathomimetic
Drugs that reduce noradrenergic transmission
Sympatholytic
Name the 3 mechanisms of action of sympathomimetics
- Facilitate release
- Block reuptake
- Receptor agonists
Name the 4 mechanisms of action of sympatholytics
- Inhibit synthesis
- Disrupt vesicular transport and storage
- Inhibit release
- Receptor antagonists
Drugs that enhance cholinergic transmission
Parasympathomimetic
Drugs that inhibit cholinergic transmission
Parasympatholytic
What type of drugs are parasympathomimetic and parasympatholytic?
Parasympathetic drugs
Name the 3 mechanisms of action of parasympathomimetic drugs
- Nicotinic receptor agonist
- Muscarinic receptor agonist
- Cholinesterase inhibitor
Name the 6 mechanisms of action of parasympatholytic drugs
- Inhibit vesicular ACh transport
- Inhibit exocytotic release
- Nicotinic receptor antagonists
- Muscarinic receptor antagonists
- Inhibit high-affinity choline transport
- Inhibit pyruvate dehydrogenase
What is the key neurotransmitter facilitating the preganglionic synpase in the SNS and PNS?
ACh
What is the neurotransmitter released from PNS postganglionic neurons?
ACh
What is the neurotransmitter released from SNS postganglionic nerves?
NE
How does NE produce its effects?
Activating alpha and/or Beta adrenergic receptors on organs and tissues
How does ACh produce its effects?
Activating nicotinic or muscarinic receptors on nerves, organs, or tissues
What contributes to significant regulatory effects of autonomic function?
CNS
What do medications that affect the ANS often mimic or block the actions of?
Ach or NE