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57 Cards in this Set
- Front
- Back
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Autonomic Drugs used to treat?
8 general conditions |
Angina and Heart Failure
Glaucoma High BP Alzheimer's disease Benign prostatic hyperplasia Septic shock Asthma Anaphylactic shock |
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Autonomic NS
2 subdivisions? |
Sympathetic system
-Involves catecholamines and adrenergic receptors Parasympathetic system -Uses Ach and muscarinic receptors |
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NT used in both sympathetic and parasympathetic preganglionic fibers?
Acts on which receptor? |
Ach
Nicotinic Receptors |
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Sympathetic division arises from which region of the spinal cord?
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Thoracolumbar region
Stops at L2 (thanks amar!) |
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Sympathetic Fiber Organization
(4) |
Short preganglionic fiber
Synapse close to the cord Post-ganglionic fiber innervate target organs Post-ganglionic fiber releases NE |
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Exception to sympathetic fibers
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Preganglionic fibers of splanchnic nerve
Innervate adrenal medulla with preganglionic fibers* NT released = Ach |
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Preganglionic Fibers of Parasympathetic system arise from which section of the spinal cord?
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III, VII, IX, X cranial nerves
Sacral spinal cord |
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Characteristics of parasympathetic fibers
(4) |
Preganglionic fibers are long and synpase close to target organs
Short post-ganglionic fibers innervate target organs Release Ach Act on muscarinic receptors |
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Enteric NS characteristics
(4) |
-Connects sympathetic and parasympathetic system thru spinal and inferior vagal ganglia
-Sensory and motor nerves -Involved in contraction/relaxation of GI smooth muscle -Involved in secretory and absorption functions in GI epithelium |
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Myenteric Plexus
Function? Location? |
-Btw longitudinal smooth muscle and circular smooth muscle
-Contraction of two muscles |
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Submucosal Plexus
Function? Location? |
-Deep to circular smooth muscles
-Involved in mucus secretions |
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Drug Targets in Neurotransmission
(4) |
-Transmitter storage and release
-Postsynaptic receptors -Postsynaptic neuron activity -Removal or dissipation of NT via transporters or enzymes that metabolize the transmitter |
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Drugs cannot target which function of NT transmission? (1)
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-Cannot target nonelectrogenic functions such as quantal release
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Steps in Catecholamine synthesis
(4) |
-Tyrosine is hydroxylated to form DOPA via tyrosine hydroxylase
-DOPA is decarboxylated to form dopamine -Dopamine is hydroxylated to form NE -NE is methylated to form Epi |
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Rate limiting step in catecholamine synthesis
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-Tyrosine hydroxlase
-Conversion of tyrosine to DOPA |
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Adrenal Medulla's role in catecholamine synthesis
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-Has chromaffin granules rich in dopamine-beta hydroxylase
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Steps in NT release? (4)
Requirement for transmitter release? (3) |
-AP and Ca2+ entry required for vesicle docking and transmitter release
-ATP activity required for NT release* -Transmitter reuptake by the selective transporters -Metabolism via MAO (inside cell) or COMT (outside cell) |
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Steps in NE release?
(5) |
-Tyrosine is taken up with Na+ symporter and is converted to dopamine
-Dopamine is moved to vesicles or broken down by MAO -Taken up by VMAT into vesicles -Dopamine is converted to NE -NE is released into cleft and either metabolized by COMT or taken up by NET (DAT for dopamine) |
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Percentage of NE thats metabolized versus reuptake via NET?
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-70% is taken back up into cytoplasm
-30% metabolized |
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Preganglionic Sympathetic NT and receptor?
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-Ach
-Nicotinic receptor |
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Postganglionic Sympathetic Receptors
2 (2 subtypes) |
-Alpha adrenergic receptor
--Alpha 1 --Alpha 2 -Beta adrenergic receptor --Beta 1 --Beta 2 |
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Alpha-2 Receptor
Presynaptic subtype Targets? (1) Feedback? |
-Targets autonomic nerve terminals
-Negative feedback |
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Alpha-2 Receptor
Postsynaptic subtype Targets (3)? |
-Vascular smooth muscle
-Pancreas -Platelets |
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Beta-2 Receptor
Presynaptic type Targets? (1) Feedback? |
-Adrenergic nerve terminals
-Positive feedback |
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Beta-2 Receptor
Postsynaptic type Targets? (4) |
-Smooth muscle
-Respiratory system -Skeletal muscle -Liver (glycogenolysis) |
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M2 Receptor
Location? Targets? (1) Feedback? |
-Autonomic nerve terminals
-Negative feedback -Presynaptic |
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Alpha-1 Receptor
-Location? -Targets? (4) |
-Postsynaptic
-Smooth muscle -Sphincters -Heart -Liver -Contraction and glycogenolysis |
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Beta-1 Receptor
-Location? -Targets? (2) |
-Postsynaptic
-Heart (increase force and rate) -Juxtaglomerular cells (increase renin secretion) |
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Beta-3 Receptor
-Location? -Target? (1) |
-Postsynaptic
-Adipose tissue (lipolysis) |
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Steps in Ach neurotransmission
(5) |
-Synthesis via ChAT enzyme
-Transported into vesicles via proton anti-porter -Release due to AP and Ca2+ influx -Vesicles bind synaptic proteins and exocytosis releases vesicle content -Hydrolysis via AchE |
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Vesamicol
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Inhibits Ach transport into vesicles
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Time of action of Ach versus NE?
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-Ach is immediately metabolized
-NE is present in cleft for much longer |
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Botulinum Toxin
-MOA? |
-Binds vesicles so they cannot bind and release Ach
-Blocks Ach -Deadly |
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Physostigmine
-MOA? -Used in? (1) |
-Inhibits AchE
-Used in Alzheimer's disease |
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Hemicholinium
-MOA? |
-Inhibits Choline uptake
-Choline availability is rate-limiting step in Ach reaction |
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Nicotinic Receptor Characteristics
(3) |
-Ligand-gated, ionotropic
-Increased Na+ and K+ permeabililty -2 subtypes (Muscle = Nm; Neural = Nn) |
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Curare
-MOA? |
-Competitive NMJ blocker
-Does NOT affect Nn receptor -Does block Nm receptor |
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Reasons to block Nm receptor?
(4) |
-Surgery
-ET intubation -Mechanical ventilation -Diagnostic procedures -Paralyzes patient |
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Reasons to block Nn receptor?
(1) |
-Treat essential hypertension
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Muscarinic Receptors Characteristics
(2) |
-G-protein coupled
-5 subtypes (M1-M5) |
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M1, M3, M5
-MOA? |
-Activate phospholipase C
-Activate IP3-DAG pathway |
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M2 and M4 receptors MOA?
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-Inhibit adenylyl cyclase
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M1 Receptor
Location? (5) |
-Postsynaptic
-Smooth muscle (gut and respiratory system) -Glands (gastric and salivary) -Smooth muscle in eye -CNS neurons or nerve terminals |
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M2 Receptor
Location? (3) |
-CNS on neurons or nerve terminals
-Heart muscle -Presynaptically on nerve terminals |
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M3 Receptor
Location? (3) |
-Postsynaptic
-Smooth muscle (gut and respiratory system) -Glands (gastric and salivary) -Smooth muscle in eye |
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M4 Receptor
Location? (2) |
-CNS on neurons or nerve terminals
-Presynaptically on nerve terminals |
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M5 Receptor
Location? (2) |
-CNS on neurons or nerve terminals
-Cerebral arteries (action = dilation) |
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Atropine
-MOA? -Actions? (6) |
-Blocks ALL* muscarinic receptor subtypes
-Increase HR -Decrease secretions -Relax bronchi -Decrease bladder tone -Decrease GI tone and motility -Dilate pupil |
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Pirenzepine
-MOA? -Actions? (1) |
-Specifically blocks the M1 receptors
-Blocks gastric acid secretions thru blockade of the ganglionic neuron |
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Ipratropium
-MOA? -Actions? (1) |
-Blocks M3 receptors
-Reduces bronchospasm |
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Muscarinic Receptor agonists
-4 example drugs? |
-Acetylcholine
-Carbachol -Muscarine -Pilocarpine |
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Action of Muscarinic Receptor Agonists
(4) |
-Stimulate GI smooth muscle
-Stimulate exocrine gland secretion -Cause bronchoconstriction thru stimulation of bronchial smooth muscle -Pupil constriction when applied topically to eye |
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Pilocarpine
-MOA? -Use? (1) |
-Muscarinic Receptor Agonist
-Reduce intraocular pressure |
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Question from Lecture
What is the rate-limiting step in catecholamine synthesis? |
-Tyrosine Hydroxylase
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Question from Lecture
Which receptors provide negative feedback at autonomic terminals? |
-Alpha-2
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Question from Lecture
Which receptors are G-protein linked and inhibit adenylyl cyclase? |
M2
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Question from Lecture
A useful pharmacotherapy for a patient with increase ocular pressure is? (2) |
-Pilocarpine
-Beta-antagonist |
