Overview ANS

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jlolson83
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114558
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Overview ANS
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2011-11-08 02:03:11
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  1. ENS
    • 2 series of interconnected neuronal plexuses
    • Regulated by local network reflexes
    • Modulated by mostly PANS, some SANS
  2. ANS afferents
    • to insular cortex
    • PANS to right
    • SANS to left
  3. Methyl Mercury
    • Inhibit choline acetyl transferase (ChAT)
    • No ACh synthesis
  4. ChAT
    • choline acetyl transferase
    • choline and acetyl CoA to ACh
  5. VAT
    • vesicular ACh transporter
    • counter transports H+ with ACh and ATP to fill vesicles
  6. Vesamical
    • Inhibits VAT
    • No filling vesicles with ACh (and ATP)
  7. Botulinum toxin
    Inhibits SNARES (soluble attachment protein receptors)
  8. AChE
    • Acetyl-cholinesterase
    • Degrades ACh to choline and acetyl coA
    • Plasma version is butyrylcholinesterase
    • Inhibit by AChEIs
    • 2 binding sites (anionic and esteric) (both used by ACh)
  9. Hemicholinium
    • Inhibits choline transporter
    • Choline can't be taken back up into presynaptic neuron
  10. Tyrosine hydroxylase (TH)
    • Converts tyrosine to Dope (levodopa)
    • Inhibited by metyrosine
    • Rate limiting step
    • Tetrahydropterin BH4 is co-factor
  11. Aromatic amino acid decarboxylase (AAAD)
    • Converts levodopa to dopamine
    • Inhibited by carbidopa
    • Vitamin B6 is cofactor
  12. DA beta hydroxylase
    • Converts dopamine to norepinephrine
    • localized in NE terminals
  13. Phenyl-ethanolamine-N-methyl transferase
    • Converts norepinephrine to epinephrine
    • Present in adrenal medulla
  14. Vesicular monoamine transporter (VMAT)
    • Vesicular NE transporter
    • Counter-transports H+ with NE and ATP
    • Inhibited by reserpine
  15. Reserpine
    • Inhibits VMAT
    • No filling vesicles with NE
  16. Catechol-O-methyl transferase (CO
    MT
    • Biotransforms NE
    • Primary breakdown product is vanilla-mandelic acid (VMA)
    • Located in membrane of target cell, liver cells, etc
  17. Monoamine oxidase
    • MAO
    • Types A and B
    • Primary breakdown product is vanilla-mandelic acid (VMA)
    • Located in mitochondria within synapse, glia, etc
  18. NE transporter (NET)
    • Reuptake of NE into presynaptic neuron
    • Inhibited by tyramine, amphetamine, cocaine
  19. PENMT
    Circulates with epi and DA-beta-hydroxylase
  20. Bethanechol
    • Cholinomimetic
    • Quaternary amine
    • Full M1-M3 agonist, little N effect
    • increased secretions, sm m contraction, reduced heart rate
    • Used for urinary retention
    • Less affinity for AChE, so longer half time than ACh
    • Toxicity: bronchospasm
  21. General cholinomimetics
    • Bethanechol
    • Carbechol
    • Methacholine
    • (used in urinary retention)
  22. Specific M cholinomimetics
    • Muscarine
    • Pilocarpine
  23. Pilocarpine
    • Muscarinic cholinomimetics
    • alkaloid
    • quaternary
    • in certain mushrooms
    • very little N receptor activity
    • Increased secretions, sm m contraction, reduced heart rate
    • Used in glaucoma
    • Toxicity: bronchospasm
  24. Specific nicotinic cholinomimetics
    • Nicotine
    • Lobeline
  25. Nicotine
    • Specific N receptor cholinomimetic
    • Lipophilic, crosses membranes readily
    • Activates SANS and PANS and striated muscle
    • Used in smoking cessation
    • Increases dopamine via a4b2 nicotinic Nn receptors
    • Toxicity: increase GI activity, nausea, vomiting, diarrhea, increased BP, potential for seizures
  26. Varenicline
    • Chantix
    • Partial agonist of a4b2 nicotinic Nn receptor
  27. a4b2 nicotinic Nn receptor
    • Primarily in limbic system
    • Stimulated by nicotine and varenicline (chantix)
    • Heteroreceptor presynaptically reducing further dopamine release
  28. Acetylcholinesterase inhibitors
    • =indirect-acting cholinomimetics
    • 3 classes: alcohols, carbamates, organophosphates
  29. Alcohol AChE Inhibitors
    • Edrophonium
    • ACh competitive antagonist
    • Hangs out in active site
    • Reversible blockage lasts minutes
  30. Carbamate AChE Inhibitors
    • Neostigmine and Physostigmine
    • Processed like ACh but slower
    • Reversible blockade lasts hours
    • Overdose causes weakness by producing depolarization blockade
  31. Organophosphates
    • AChE Inhibitor
    • Echothiophate, Parathion, Malathion, Sarin, Soman, VX
    • Phosphorylate esteric AChE site
    • Irreversible after aged
  32. Nootropics
    • Specific AChEI for G1 and G4 isoenzyme
    • Alzheimer's treatment
    • Tacrine (comp, rev)
    • Donepezil (non-comp, rev)
    • Rivastigmine (comp, pseudorev)
    • Galantamine (rev, low potency, also non comp Nn agonist)
  33. SLUDGEM
    • PANS effects
    • Salivation
    • Lacrimation
    • Urination
    • Defecation
    • GI upset
    • Emesis
    • Miosis
  34. Vasoactive intestinal peptide
    • VIP
    • Colacalized in PANS terminals, relseased with higher frequency stimulation
  35. Cyclosporine
    • Anti-immune modulator
    • Applied topically to treat dry eye
    • Reduces activation of immune cells and their production of pro-inflammatory cytokines in tear ducts
  36. Urination - PANS and SANS split
    • PANS contracts detrusor by M3, M2 receptors inhibit NE release from SANS in detrusor
    • SANS relax detrusor by beta
  37. Eye effects of PANS
    • Miosis, accomodation, glaucoma
    • M3 mediates smooth muscle contraction to contract iris and ciliary muscle, opens angle of schlemm
    • M2 mediates NE release reduction
  38. Vascular bed ACh effects
    • vasoconstriction from circulating ACh
    • No ANS innervation
  39. Respiratory PANS effects
    M3 mediated smooth muscle contraction adn induced secretions
  40. Muscarinic Antagonists
    • Atropine
    • Scopolamine
    • Ipratropium
    • Oxybutynin
    • Tolterodine
    • Darifenacin, solifenacin, fesoterodine
    • Glycopyrrolate
  41. Atropine
    • Surmountable antagoinis of all M receptors
    • Used to reduce airway secretions in surgery
    • Used after mushroom poisoning/insecticide exposure
  42. Scopolamine
    • Anti motion sickness and to reduce airway secretions in surgery
    • Anti M with some anti Nn
  43. Ipratropium
    • COPD, asthma treatment
    • Anti M with some anti Nn
  44. Oxybutynin
    • M3 prefering antagonist
    • Manage bladder control
    • Short half life --> frequent dosing
  45. Tolterodine
    • M3 preferring antagonists
    • Manage bladder control
  46. Muscarinic antagonist effects
    • Reduce PANS
    • Sweat and salivary glands most affected and GI activity
    • CV effects compensated by reflexes
  47. Muscarinic antagonists toxicity and adverse effects
    • Hot as a hare: inability to swear - hot, dry skin
    • Blind as a stone: absence of accommodation
    • Mad as a hatter: CNS toxidrome - delusions with hallucinations
    • Dry to the bone: no bowel sounds, no spit, no tears, no sweat
  48. Muscarinic antagonist contraindications
    • Glaucoma
    • Obstructive GI and urinary systems
    • Intestinal atony
    • Dementia
  49. Non-depolarizing NMJ blockers
    • Nm antagonists
    • d-tubocurarine
    • Atracurium
    • Pancuronium
    • Rocuronium
    • Lead to weakness and eventually flaccid paralysis with increase dose
  50. D-tubocurarine
    • Non-depolarizing NMJ blocker
    • Nm antagonist
    • Stimulates release of histamine
  51. Succinylcholine
    • 2 ACh molecules
    • Full, specific Nn receptor agonist
    • First occupies receptor then desensitizes
    • Can release histamine and cause hypotension
    • Releases K+ from several sites leading to hyperkalemia
    • Broken down only by buyrylylcholinesterase
  52. NMJ toxins
    • a-Bungarotoxin (inhibits NMJ like curare)
    • a-latrotoxin (black widow spiders) (produces presynaptic relsease of neurotransmitters)
    • tick venoms (induce synaptic vesicle fusion)
  53. Ganglionic blockers
    • Relatively specific to Nn
    • Block all ANS outlfow
    • Limited clinical efficacy
    • Mecamylamine
    • Heexamethonium
    • Trimethaphan
  54. Trimethaphan
    • short acting ganglionic blocker
    • blocks Nn receptors
    • water soluble
  55. NE receptor preference
    a1 = a2 > b1 >>> b2
  56. Epi receptor preference
    b1 = b2 > a1 = a2
  57. Dopamine ANS role
    • vasodilates renal arterioles
    • direct inotropic effects
    • in chain ganglia small intensely fluorescent cells, regulates ACh release
  58. M1 MOA
    • enhance intracellular Ca
    • Regulate IP3 and DAG
  59. M3 MOA
    • enhance intracellular Ca
    • regulate IP3 and DAG
  60. M2 MOA
    • opens K+ channels
    • inhibits adenyulyl cyclase
  61. Nn and Nm MOA
    ionotropic, increasing Na+ channel conductance
  62. NE alpha 1 MOA
    • Increase intracellular Ca
    • regulates IP3 and DAG via Gq
    • Vascular sm m contraction, mydriasis, positive inotropy, bladder trigone and sphincter contraction, ENS sphincter contraction, arrector pili contraction, apocrine gland secretion, ejaculation
  63. NE alpha 2 MOA
    • Autoreceptor reducing future release of NE
    • Inhibits adenylyl cyclase via Gi
  64. NE beta 1 MOA
    • Enhances adenylyl cyclase
    • HEART
  65. NE beta 2 MOA
    • enchances adenylyl cyclase
    • can activate Gi
    • bronchioles, arterioles, liver
  66. NE beta 3 MOA
    • enhances andenylyl cyclase
    • LIPOCYTES
  67. Selectivity vs specificity
    • Selectivity: preference for one R over another
    • Specificity: 1000 fold higher affinity
  68. Tachyphylaxis
    Desensitization that occurs over a periord of time
  69. G-protein-coupled receptor kinase
    • GRK
    • Phosphorylates G-protein receptor after G-protein component has left
    • Then beta arrestins can jump on and target the receptor for internalization
  70. Alpha-1 selective drugs
    • Phenylephrine
    • Pseudoephedrine
    • Midodrine
    • Methoxamine
  71. Alpha-2 selective drugs
    • Clonidine
    • Methyldopa
    • Guanfacine
    • Guanabenz
  72. Beta non-selective drugs
    Isoproterenol
  73. Beta-1 Selective drugs
    Dobutamine
  74. Beta-2 selective drugs
    • Albuterol
    • Terbutaline
    • Metaproterenol
    • Pirbuterol
    • Salmeterol
    • Formoterol
  75. Phenylephrine
    • Alpha-1 selective agonist
    • smooth muscle contraction
    • used as decongestant, hypertensive, resolve priapism, induce mydriasis
    • Toxicity - hypertension issues, seizures
    • Significant first pass due to MAO-A
  76. Pseudoephedrine
    • Alpha-1 selective agonist
    • More CNS effects than phenylephrine
  77. Midodrine
    • Alpha-1 selective agonist
    • Prodrug to des-glymidodrine
    • Treats hypotension
  78. Methoxamine
    • Alpha-1 selective agonist
    • Similar to phenylephrine
    • Used for hypotension
  79. Clonidine
    • Alpha-2 selective agonist
    • sympatholytic effects
    • reduces NE release which can lead to hypotension
    • Used for AD/HD, CNS anxiety after opiate withdrawal, anti-hypertensive, sedative
  80. Isoproterenol
    • Non-specific beta receptor agonist
    • Asthma/COPD
    • High doses cause big BP increase
  81. Dobutamine
    • Beta-1 selective agonist
    • racemic mix complicates things
  82. Albuterol
    • Beta-2 selective agonist
    • like terbutaline, metaproterenol, and pirbuterol
    • R isomer is active
    • Vasodilate muscle arterioles, decreasing TPR and BP
    • ASTHMA, COPD
    • Tolerance issues
  83. Salmeterol and Formoterol
    • Beta-2 selective agonists
    • durations of actions up to 12 hours
  84. Terbutaline
    • Beta-2 Selective agonist
    • acute sc injection for ER treatment of asthma
  85. Amphetamine-like drugs
    • NE and DA re-uptake inhibitor
    • Substrate for NET, can result in ca-indep release
    • Blocks MAO

    • Increase HR and TPR
    • CNS effects
    • Effects of inc synaptic NE, DA, 5HT

    • Used as anorexient, AD/HD, narcolepsy, abuse
    • Dependence issues
    • Ceiling effect
  86. Amphtetamine-like drugs
    • Methamphetamine
    • Ephedrine
    • Psudoephedrine
    • Phenylpropanolamine
    • Phenmetrazine
    • Methylphenidate
    • Modafinil
    • Tyramine
  87. Cocaine and like drugs
    • Non-competitive inhibition of NET
    • (No Ca-indep release)
    • Caine properties

    like drugs: atomoxetine
  88. Non-specific alpha antagonists
    • Phenoxybenzamine
    • Phentolamine
  89. Alpha-1 selective antagonists
    • Prazosin
    • Tramsulosin
  90. Alpha-2 selective antagonist
    Yohimbine
  91. Non-specific beta antagonists
    • Propranolol
    • Nadolol
    • Pindolol
    • Sotolol
    • Carvedilol
    • Timolol
  92. Selective beta-1 antagonists
    • Metaprolol
    • Atenolol
    • Esmolol
  93. NE depleting agents
    • Guanethidine
    • Reserpine
  94. Phenoxybenzamine
    • Long acting non-spec alpha antagonist
    • Covalent binding alpha 1>>alpha 2
    • Significant orthostatic hypotension
    • Adverse effects: HR/CO up, nasal stuffiness, inhibit ejaculation
    • Used to manage pheochromocytoma
  95. Phentolamine and Tolazoline
    • Reversible, short acting non-specific alpha antagonist
    • alpha 1 = alpha 2
    • less sedation than phenoxybenzamine
    • used for surgical procedures for pheochromocytoma
  96. Prazosin
    • Alpha-1 selective drug
    • Profound vascular blocking effects leading to orthostatic hypotension
    • Like Tamsulosin, terazosin, doxazosin
    • Used to manage hypertension and for benign prostatic hyperplasia
  97. Yohimbine
    • Alpha-2 sselective drugs
    • Increase SANS activity during SANS activation
    • Treats orthostatic hypotension
  98. Propranolol, Nadolol, Timolol
    • Non-specific beta blockers
    • Treat hypertension, angina, chf, glaucoma
    • Beta-1 blockade reduces renin release
    • Beta-2 blockade prevents skel m vasodilation, bronchiole relax, glycogenolysis in liver
    • Beta-3 blockade prevents lipolysis
    • Watch out with asthmatics and type 1 diabetics
  99. Atenolol, metaprolol
    • Beta-1 selective antagonist
    • some beta-2 antag activity
    • Safer than non-spec to treat hypertension
  100. Esmolol
    • Beta-1 selective antagonist
    • ultrashort acting
    • used in icu to manage arrhythmias
  101. Pindolol
    • Partial non-specific agonist
    • Mildly reduces beta tone
  102. Carvedilol
    • Mixed antagonist
    • Used to manage CHF
  103. Guanethidine
    • NE depletor
    • Ligand for NET and VAT
    • Used as antihypertensive
  104. Lacrimal gland predominant tone and treatment options
    PANS

    • Liquid tears
    • Antibiotics
    • Cycosporine
  105. Glaucoma treatment options
    • M3 agonists increase aqueous outflow
    • Alpha-1 agonists induce mydriasis with facilitates aqueous humor outflow
    • Alpha-2 agonists reduce production of aquous humor
    • Beta blockers reduce production of aqueous humor
    • Carbonic anhydrase inhibitor reduces production of aqueous humor
    • PGF2a analogs facilite outflow
  106. Dorzolamide
    • Carbonic anhydrase inhibitor
    • Treats open and closed angle glaucoma by reducing aq humor production
  107. Treating congestion
    Use an alpha-1 agonist to induce vasoconstriction and reduce secretions
  108. Salivation tone and treatment
    • PANS
    • Dry mouth can be from lack of PANS secretions or too much SANS creating thick mucous
  109. Respiratory SANS effects
    Beta-2 receptors increase mucous clearance by increasing cliliary beat frequency

    Bronchiole smooth muscle is SANS controlled by Epi
  110. Cardiac versus vessel tone
    • Cardica is primarily PANS
    • Vessels = SANS (alpha-1 agonists increase tone, increasing TPR)(Beta-2 agonists reduce BP)
  111. Sweat glands tone and action
    • Eccrine sweat glands are SANS
    • ACh and M3 receptors
  112. Sildenafil Citrate
    • Viagra
    • Blocks PDE-5 so cGMP sticks around and erection stays
  113. Penis ANS
    Erection is PANS - ACh/M3 inc NO, act guanylate cyclase, making cGMP --> erection

    Ejaculation is SANS - alpha-1

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