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55 Cards in this Set
- Front
- Back
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Sympathetic originates from:
Parasympathetic originates from: |
S-thoracolumnar division
P-craniosacral division (3, 7, 9, 10) |
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Rate limiting step for:
Cholinergic transmission Adrenergic transmission |
C- Choline intake
A- Tyrpsine Hydroxylase Both use Na symport pumps and proton antiport pumps |
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Biosynthesis of Catecholamines
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1) Tyrosine
Tyrosine Hydroxylase 2) Dopa Dopa decarboxylase 3) Dopamine Dopamine B-hydroxylase 4) Norepinephrine Phenylethanolamine-N-methyl transferase 5) Epinephrine |
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Metabolism of Catecholamines:
Epi NE DA |
Epi- 3- methoxy-4-hydroxymandelic acid (VMA)
EN- 3- methoxy-4-hydroxymandelic acid (VMA) DA- Homovanillic Acid |
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Location and function of:
Catechol-O-Methyltransferase (COMT) Monoamine oxidase (MAO) |
Catechol-O-Methyltransferase (COMT)- in cytoplasm of liver cells; adds methyl group
Monoamine oxidase (MAO)- on surface of mitochondria; adds oxygen |
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ANS controlled by
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Hypothalamus
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Discrete vs Integrated
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Discrete- controlled by SNS or PSN
Integrated- controlled by both SNS and PSN |
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Somatic vs Autonomic
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Somatic- no ganglia, myelinated neurons, only Acn
Autonomic- ganglia, pre and post ganglionic neuron, unmylinated, Preganglionic-Ach, Post ganglionic (NE- sympathetic, Ach- parasympathetic) |
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although both pre and post ganglionic use Ach as neurontransmitter for sweat glands, it is still considered Sympathetic
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FYI
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Effect of the following non-adrenergic non-cholinergic trasnmission (NANC):
NPY ATP Dopamine Enkephalin Galanin |
NPY- inhibit secretion of water and electrolytes by the gut
ATP- inhibits release of Ach and NE Dopamine- post-sympathetic transmitter in renal blood vessels Enkephalin- inhibit Ach release- inhibit peristalsis Galanin- appetite satiety |
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Effect of the following non-adrenergic non-cholinergic trasnmission (NANC):
CCK cGRP GABA GRP |
CCK- cotransmitter in excitatory neuromuscular ENS
cGRP- cardiac stimulant GABA- relaxant effect on gut GRP-excitatory neuron to neuron junction in ENS |
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Effect of the following non-adrenergic non-cholinergic trasnmission (NANC):
NO Serotonin Substance P VIP |
NO- inhibitory ENS, important in sphincters
Serotonin-excitatory neuron to neuron junc. in ENS Substance P- vasodilator/sensory neuron transmitter in the ENS VIP- vasodilator and cardiac stimulant |
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Nicotinic vs Muscarinic
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N- ligand-gated ion channels; 2 Ach bind, then Na influx; located in ganglia and adrenal
M- Gprotein activates 2nd messengers; located in skeletal muscle NMJ |
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Autorecepters:
Nicotinic with Ach Muscarinic with Ach Alpha with Ne |
Nicotinic with Ach +
Muscarinic with Ach - Alpha with Ne - |
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Heterocepters:
Beta with Epi Alpha with Ne |
Beta with Epi +
Alpha with Ne - |
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Potency of adrenergic agonist:
alpha Beta |
Alpha- E> NE> Isoproteranol
Beta- Isoproteranol>E> NE |
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General effect of:
Alpha binding Beta binding |
A- Excitation
B- Inhibition (except B1 Heart increase) |
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M1
M2 M3 |
M1- increase Ca
M2- decrease cAMP and K efflux M3- increase Ca |
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Nn
Nm |
Nn- Na/K depolarization
Nm- Na/k depolarization |
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alpha 1
alpha 2 |
alpha 1- increase Ca
alpha 2- decrease cAMP |
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Beta 1
Beta 2 Beta 3 |
all increase cAMP
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Name the Choline esters and what they are used for
What do they all have in common? |
1. Acetylcholine- cataract removal
2. Carbachol- anterior eye surgery; also stimulates nicotinic 3. Bethanechol- treats non-obstructive urinary retention; M1 selective, can be administered systemically 4. Methacholine- used to diagnose asthma ALL quaternary amines |
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Physiological Actions of choline esters on:
Eye Glands Cardiovascular GI Tract Urinary Tract |
Physiological Actions of choline esters on:
Eye- miosis (constriction), allows aqueous humor to flow out into canal of schlem Glands- increase secretion of saliva, mucous, sweat Cardiovascular- lowers HR, loweres conduction rate, lowers force of contraction, vasodilation when contact with NO GI Tract- increases motility Urinary Tract- causes urination, detrusor muscle contracts |
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Natural Alkaloids
(name anything special about them) |
Muscarine
Pilocarpine- only one given therapeutically, more lipisoluble, long term can cause hypertension Oxotremorine |
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Effects of High stimulation of Muscarine
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S- salvation
L- lacrimation U- urination D- defication Hallucinations |
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Effects of High levels of nicotine
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GI- nausea, vomiting
Glands- increase salvation Cardiac- hypertension CNS- convulsions, coma skeletal muscle- paralysis |
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Nicotinic Receptor Agents
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Nicotine (agonist at first, but antagonist in the end)
Lobeline DMPP |
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AChE Inihibitors
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Edrophonium- Short
Neostigmine, physostigmine- medium Organophosphates, dyflos, ecothiopate- Irreversible |
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What are these used for?
Edrophonium Physostigmine Neostigmine Pyridostigmine Ambemonium/Demecarium Pentavalent Ecothlophate, DFP, Isoflurophate |
What are these used for?
Edrophonium- diagnosis of Ms Physostigmine- treats open angle gluacoma Neostigmine- Treats MG Pyridostigmine- most common used treatment for MG, also prophylaxis during gulf war Ambemonium/Demecarium- treats MG and glaucoma Pentavalent- used as war gas or pesticide Ecothlophate, DFP, Isoflurophate- used to treat MG, highly lipophilic |
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Define Myasthenia Gravis
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auto-immune disorder, loss of nicotinic Ach receptors from the NMJ. AchE inhibitors increase response of MG.
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Alzheimer's Disease
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decrease in choline acetyltransferase which lowers the amount of Ach in CNS
sensitive to CNS toxicities of drugs with anti-muscarinic effects |
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Centrally acting AchE inhibitors
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Tacrine (Cognex)
Donepezil (Aricept) Rivastigmine (Exelon) Galantamine (Reminyl) |
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What does PAM do?
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reactivates AchE, most effective in NMJ, not CNs because of charged nitrogen
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Three types of Cholinergic Receptor Antagonists and their main targets
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1. Anti-muscarinic agents- inhibits PSN
2. Ganglionic Blockers- inhibits nicotinic SNS and PSN 3. Neuromuscular Blockers- inhibits signals to skeletal muscle |
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Side effects of Atropine
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D- dry mouth
U- urinary retention C- constipation T- tachycardia |
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How do Anti-Muscarinic agents work?
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inhibit PSN
just affects muscarinic receptors reduces parasymapthetic stimulation, hence AKA Parasympatholytic |
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What does Atropine treat?
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irritable bowel syndrome
urinary incontinence to decrease salivation prevent bradycardia and hypotention reverses AchE inhibitor toxicity |
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How do Ganglionic Blocker work?
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inhibit nicotinic SNS and PSN
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How do Neuromuscular Blockers work?
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inhibit signals sent to skeletal muscle
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Chain effect from M3 stimulation on endothelial cells by Choline Esters
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M3
NO cGMP PKG K efflex/ prevents Ca2 influx Smooth muscle relaxation and Hyperpolarization |
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Drug Interactions with Anti-muscarinic agents
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Tricyclic antidepressants
histamine H1 blockers CNS depressents MAO inhibitors |
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Contraindications for Anti-muscarinic agents
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prostatic hypertrophy
closed angle glaucoma cardiac disease MG |
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Anti-Muscarinic Agents and their effects
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Atropine- treats irritable bowel syndrome
Scopolamine- more pronounced effects, significant CNS effects, more pronounce sedation and amnesia, prevents MOTION SICKNESS Ipratopium bromide (Atrovent)- inhalant that relaxes bronchials Cyclopentolate (Cyclogy) and Tropicamide (Mydriacyl)- used for mydriasis and paralysis; shorter duration |
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Pirenzepine
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muscarinic antagonist for M1 receptor used for peptic ulcers
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Clinical uses for Parasympatholytics
cardiovascular eye Neurological Respiratory Gastrointestinal |
Clinical uses for Parasympatholytics
cardiovascular- treats bradycardia eye- dilates pupil Neurological- prevents motion sickness Respiratory- Asthma Gastrointestinal- relax GI tract ans suppress secretion; used to facilitate endoscopy and GI radiology |
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Ganglionic Blockers treat what?
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short term treatment for hypertension, to minimize bleeding, for acute dissecting aneurysm of the aorta
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Examples of Ganlgionic Blockers
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Tetraethylammonium
Hexamethonium- blocks Na entry Mecamylamine- can be ionized or unionized, can cross BBB, competiviley block ganglionic nicotinic receptors Trimethaphan- charged, must be given parenterally, does not enter CNS, competitively block ganglionic nictotinic receptors |
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What is the predominant tone for:
Arterioles Veins Heart iris Ciliary muscle GI tract Urinary bladder Salivary glands Sweat glands |
What is the predominant tone for:
Arterioles- Sympathetic (adrenergic) Veins- Sympathetic Heart- Parasympathetic iris- Parasympathetic Ciliary muscle- Parasympathetic GI tract- Parasympathetic Urinary bladder- Parasympathetic Salivary glands- Parasympathetic Sweat glands- Sympathetic |
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Neuromuscular Blockers used for what?
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for surgical procedures to maintain muscle paralysis, adjuncts to anesthesia for skeletal muscle relaxation
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Drugs that block Choline uptake (2)
Drugs that Block Ach release (3) |
Drugs that block Choline uptake (2)- Hemicholinium, Triethylcholine
Drugs that Block Ach release (3)- aminoglycoside antibiotics, botulinum toxin, B-bungarotoxin |
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Non-Depolarizing neuromuscular blocking agents
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tubocurarine (medium)
gauamine pancuronium (long) atracurium (short)- spontaneous elimination vecuronium (medium) |
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Depolarizing neuromuscular blocking agents
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Succinylcholine
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Characteristics of Non-Depolarizing Blockers
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-Have 1 or more Tertiary amines
-given IV, can't cross into CNS -volume of distribution=blood volume -rapidly excreted -competitve antagonists |
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Side effects of Non-depolarizing blockers
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Histamine release
Hypotension bronchoconstriction |
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Phase 1 and 2 of Depolarizing Blockers
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Phase 1- continuous depolarization until muscle becomes unresponsive to additional stimulation
Phase 2- membrane repolarizes, but Ach can't activate receptor because they are desensitized; can cause rapid release of K+ |
