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76 Cards in this Set
- Front
- Back
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All preganglionic fibers release?
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ACh
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All ganglions are ___ receptors which have ___ as the NT?
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Nicotinic; ACh
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Sympathetic trunk found where? and release what NT?
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T1-L2; NE
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Parasympathetic found where? Release what NT?
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CN III, VII, IX, X; Sacral II - IV
ACh |
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Where are nicotinic receptors found?
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NMJ's; All pre-ganglionic; adrenal medulla
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What are the 2 exceptions to sympathetic releasing NE?
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Adrenal medulla and sweat glands;
Adrenals release EPI sweat glands are muscurinic ACh receptors |
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A class of drugs that blocks transport of choline into the nerve terminal
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hemicholiniums
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What is the rate limiting step in catecholamine synthesis? What drug inhibits it?
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Tyrosine to DOPA via Tyrosine hydroxylase;
Metyrosine |
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describe the formation of EPI from Tyrosine?
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Tyrosine - DOPA via Ty hydroxylase
DOPA - Dopamine via DOPA decarb Dopamine - NE via dopamine beta hydroxylase NE to EPI via PNMethyltransferase |
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enzyme for formation of acetylcholine from acetyl CoA and choline?
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cholineacetyl transferase
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2 types of cholinergic recptors
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nicotinic ; muscurinic
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What drugs blocks the nicotinic receptor in autonomic ganglia and adrenal medulla?
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Hexamethonium
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Is the NMJ blocked by hexamethonium?
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NO
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Where are M1-3 muscirinic receptors found?
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M1 = Brain and GI
M2 = Heart M3 = smooth muscle/glands Note CNS is in all of them |
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alpha receptors generally ___ contraction except in the ___
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increase; GI tract
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beta receptors generally ___ contraction, except in the ___?
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decrease; Heart
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a potent alpha-receptor blocker as well as sedative/antianxiety?
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promethazine
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beta-1 receptors found in the?
beta-2 receptors found in the? |
heart/GI
Lungs/bronchia/smooth muscle/uterus |
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Mydriasis
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pupil dilation d/t sympathetic stimulation
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miosis
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pupil constriction d/t parasympathetic stimulation
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All muscurinic receptors are ___ mediated?
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G-protein mediated
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parasympathetic stimulation of the heart will yield VC/VD?
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VD - leads to drop in BP and get rebound/reflex tachycardia
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Effects of cholinergic (parasymp) stimulation?
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SLUDGE
Salivation; lacrimation; urination, defecation, Emesis |
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Turn over time for AChE?
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150ms - located in the synaptic cleft
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Mechanism of Direct-acting cholinergic drugs? Indirect?
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Direct = activate cholinergic receptor
Indirect = inhibit AChE |
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Acetylcholine, carbachol, bethanecol, methacholine?
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Direct acting cholinergic drugs; Choline esters have quaternary ammonium group making them hydrophilic
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rate the hydrolzed ability of ACh, carbachol, bethanecol, methacholine
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Direct acting cholinergics
ACh >> methacholine > other 2 think about the name choline with ACh being #1 |
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muscarine, pilocarpine (non-selective), nicotine? Are they well absorbed? Are they lipophilic?
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"ine" = direct acting cholinergic
Yes, absorbed well Yes, so CNS toxicity is possible |
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Which one of the direct cholinergic drugs has effects at both nicotinic and muscarinic receptors?
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Pilocarpine
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Used for non-obstructive urinary retention; glaucoma; increase GI motility; miosis
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bethanecol - direct acting cholinergic (-chol) ending
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A potent, non-selective, long duration drug used to treat glaucoma
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carbachol (direct acting cholinergic)
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DOC for lowering ICP of glaucoma in emergency setting
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Pilocarpine (direct acting cholinergic)
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Treats Sjohren's; reversal of mydriasis d/t atropine; can enter CNS
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Pilocarpine (direct acting cholinergic)
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T/F - Indirect acting cholinergic drugs are more widely used and selective that direct?
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True
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Short acting drug used to diagnose myasthenia gravis
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Edrophonium
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3 types of drugs of indirect cholinergics?
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Simple alcohol (edrophonium in myasthenia gravis)
carbamic esters (neostigmine/physostigmine) Organic derivatives of phosphoric acid (echothiophosphate) |
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used in the chronic management of myasthenia gravis?
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Pyridostigmine, neostigmine, or ambenonium
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Used mainly for urinary retention to stimulate the GI tract? cannot enter CNS
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Neostigmine
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Can enter CNS! non-selective but antidote for anticholinergic blockade
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physostigmine
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DOC for alzheimer's disease?
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Donepezil
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Antidote for cholinergic crisis?
organophosphate poisoning and chemical warfare agents? |
Atropine
Pralidoxime both are irreversible inhibitors of aetylcholine so it can't compete |
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2 main anticholinergic drugs?
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atropine, scopolamine
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Useful in resuscitation and bradycardia?
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Atropine - anticholinergic
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Used to treat IBS? - colon spasm
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dicyclomine - anticholinergic
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not useful in asthma (beta2) but useful in COPD. (2)
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Ipratropium; Tiotropium (10x more potent)
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used as a sleep aid; motion sickness; but has amnestic effects; comes in a patch
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scopolamine
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Name the G-protein subunits for each receptor?
a1 a2 B1-3 |
a1 = Gq
a2 = Gi beta = Gs |
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T/F - EPI is non-selective for alpha/beta receptors because it stimulates both
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T
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A selective alpha 1 agonist but can activate beta as well at high doses; used in hypotensive states, nasal decongestant, can cause HTN crisis
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Phenylephrine
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selective alpha 2 agonist used to treat HTN and acts on the CV centers in the CNS?
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Clonidine
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a beta-1 selective agonist used in acute heart failure; increased cardiac contractions
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dobutamine
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non-selective beta agonist that can overstimulate heart while treating bronchoconstriction
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isoproterenol
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selective beta 2 agonist used to treat asthma/
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albuterol, salmeterol, formoterol
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DOC for acute allergic rxns
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epinephrine
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phentolamine, prazosin (alpha1 specific), terazosin, doxazosin
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alpha 1 receptor antagonists
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T/F - Terazosin is less selective than phentolamine (both are alpha1 receptor agonists)
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F - terazosin is more selective for alpha 1
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NorEPi and Dopamine reuptake inhibitor - nicotine antagonist as well
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Bupropion
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partial agonist of alpha4beta2; full agonist of alpha7; long half-life used smoking cessation?
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varenicline (chantix)
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does nicotine stimulate of inhibit the CNS response?
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stimulate - it's like acetylcholine
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The nAChR is a 5 membered complex of __ and ___ subunits
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alpha1-9
beta1-4 |
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Which types of nicotinic receptors are most abundant? Which are found in the NMJ? Neutral tissue?
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Alpha3/beta4
Alpha1/beta1 Alpha2-9/beta204 |
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fatal dose range for nicotine
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40-60mg
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a non-competitive nicotinic antagonist used to treat malignant HTN?
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Mecamylamine
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what do glucocorticoids block?
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arachidonic acid conversion to free arachidonic acid by phosphilipase A2
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What do NSAIDs block?
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Free arachidonic acid conversion to prostaglandins via cyclooxygenase
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potent anti-inflammatory and immunosupressive effects; reduce lymphoid cell count and DOC (class) for organ transplants
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Corticosteroids
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a specific T-cell immunity inhibitor with large interpatient variability
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cyclosporine
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standard prophylactic agent for GVHD and solid-organ transplants
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tacrolimus
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inhibits T-cell proliferation
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rapamycine
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inhibits b cell proliferation?
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Leflunomide
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The polyclonal antibody we need to know?
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antithymocyte globulin (thymocyte it's against it, duh)
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Monoclonal AB's
Murine has ___ in name Humanized has ___ in name Chimeric has ___ in name |
Muro (muromonab)
zu (daclizumab) xi (basiliximab) |
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IL-2 receptor antagonist used in renal transplants
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basiliximab (chimeric)
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recombinant IL-11; stimulates platelet production
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oprelvekin
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ACh esterase inhibitors? (4)
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Neostigmine, physostigmine, pyridostigmine, edrophonium
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cholinesterase inhbitor drug used for alzheimers
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rivastigmine, galantamine, donepezil, tacrine
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