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75 Cards in this Set
- Front
- Back
Where do axons of the somatic nervous system originate and what do they release? |
axons originate at the spinal cord and release ACh at neuromuscular junction
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Where do preganglionic neurons of the sympathetic nervous system originate and where do post-ganglionic neurons synapse?
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pre-ganglionic neurons originate from the thoracolumbar region of SC and synapse with post-ganglionic neurons close to the spinal cord
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Where do preganglionic neurons of the parasympathetic nervous system originate and where do they synapse with post-ganglionic neurons?
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Pre-ganglionic neurons originate from the cranialsacral region of SC and synpase with post-ganglionic neurons close to the effector tissue
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Neurons that release catecholamines are referred to as? What catecholamines are released at most post-ganglionic sympathtic neurons? CNS? Adrenal medulla? GI? kidney?
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Adrenergic! post-ganglionic sympathetic neurons release NE: CNS releases DA, NE; Adrenal medulla releases EPI; GI and kidney release DA
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Neurons that release ACh are called? And where are they found?
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Cholinergic foud in preganglionic symp and PS, post-gang PS, at neuromuscular junctions and in the CNS
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In general ___ receptors are excitatory and ___ receptors are inhibitory.
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alpha adrenergic receptors are excitatory; beta adrenergic receptors are inhibitory
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Where are alpha adrenergic receptors not excitatory?
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in the gut
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Where are beta adrenergic receptors not inhibitory?
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beta1 receptors are excitatory in the heart
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Presynaptic receptors are ____ and are acted on by ______ to decrease _______.
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alpha2 adrenergic receptors, released NE, further NE release
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Dopamine receptors produce _______ of renal, mesenteric and coronary vessels
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vasodilation
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Where are muscarinic receptors found?
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post-ganglionic PS in heart, glands, smooth muscle
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Where are nicotinic receptors found?
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pre-ganglionic symp and PS located in ganglia, neuromuscular junctions
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What receptors are found in the heart?
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B1
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What receptors are found in the blood vessels?
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alpha 1/2 - contriction and beta 1/2 - dilation
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What receptors are found in the GI tract?
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alpha and beta
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What receptors are found in the lung?
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B2
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What receptors are found in the eye?
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a1, b2
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What receptors are found in the urinary bladder?
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a1, b1
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What is NANC?
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Non-adrenergic, non-cholinergic = Nitric oxide
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Where is constitutive NO found?
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neurons and endothelial cells
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What effects does NO produce?
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vasodilation, bronchodilation, neurogenic control of penile erection, neuronal control of GI function
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What are sympathomimetics? sympatholytics?
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sympathomimetics=adrenergic agonists; sympatholytics=adrenergic antagonists
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What are parasympathomimetics? parasympatholytics?
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parasympathomimetics=direct and indirect cholinergic agonists, parasympatholytics=cholinergic antagonists
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What are ganglionic agonists and antagonists?
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non-specific
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Of xylazine, medtomadine and dexmedetomadine, which has cyp inhibition? which does not? which has species dosing variations?
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medetomadine has cyp inhibition; dexmedetomadine does not and xylazine has variations in dosing among different species
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What is the main difference between potentcy and efficacy?
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Potentcy can be changed by increasing dose while increasing dose will not affect a drug's relative efficacy
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What is a direct-acting drug?
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A drug that acts on the target receptor
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What is an indirect-acting drug?
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A drug that acts at the release site of the signal
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What are mixed-acting drugs?
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A drug that works at either release site or at receptor site
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Examples of Sympathomimetic drugs
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epinephrine, dopamine, dobutamine, isoproterenol, terbutaline, phenylpropalamine
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Examples of Sympatholytic drugs
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phenoxybenzamine, yohimbine, propanolol, atenolol
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What effects do sympathomimetic agents produce?
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peripheral excitatory and inhibatory actions, cardiac excitatory actions, glycogenolysis, fatty acid mobilization, ENS excitatory actions
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What are the mechanisms of action of sympathomimetics?
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direct stimulation of alpha & beta receptors; inhibit NE reuptake; increased release NE; inhibition of MAO (monoamine oxidase)
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What is the consequence of inhibition of NE reuptake into the presynaptic terminal?
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Increased NE levels in the synapse
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What is the consequence of inhibition of MAO?
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leads to accumulation of NE and EPI
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How are isoproterenol and norepinephrine related?
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Isoproterenol is a synthetic derivative of norepinephrine
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How are sympathomimetics generally administered and why?
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IV; because poorly absorbed PO due to rapid metabolism and SC, IM d/t vasoconstriction
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Do sympathomimetics cross the BBB?
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No
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How are sympathomimetics eliminated?
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Rapidly diffuse out of the synapse, uptake into presynaptic and effector cells, metabolized by MAO and COMT
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Of NE, EPI, ISO, DA, which is mixed acting? What are all the others?
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DA (dopamine) is mixed acting, and all others are direct-acting
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What tissue are alpha receptors found and what is the response to activation?
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Alpha receptors are found in the blood vessels and activation results in vasoconstriction
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What tissue are the beta1 receptors found and what is the response to activation?
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Beta1 receptors are found in the heart and activation results in positive inotropic and chronotropic effects
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What tissue are the beta2 receptors found and what is the response to activation?
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Beta2 receptors are found in the blood vessels and activation results in vasodilation
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Which sympathomimetic decreases blood pressure?
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Isoproterenol
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Which sympathomimetic increases peripheral resistance?
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Epinephrine
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What are some adverse effects of sympathomimetics?
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Anxiety, restlessness, excessive pressor responses, cardiac arrythmias, cerebral hemorrhage
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What are the theraputic indications of Epinephrine?
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bronchospasm, cardiac resuscitation, hypersensitivity, anaphylactic shock, vasoconstriction to prolong local anesthetics, localized hemorrhage
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What are the theraputic indications of Isoproterenol?
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cardiac stimulant in heart block, bronchospasm
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What are the theraputic indications of dopamine?
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hypotension/shock, acute heart failure
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Tell me all about Dobutamine
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direct alpha 1 agonist and antagonist, B1 agonist results in inotropic effects thus CO increased; for short-term tx of heart failure
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Let's talk about selective Beta2 agonists
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terbutaline, clenbuterol; direct B2 agonists; relax vasculature, uterine, bronchial smooth muscle; tx for bronchospasm and labor prevention (tocolysis)
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Important things about Phenylpropanolamine
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indirect agent that promotes release of endogenous NE that increases heart rate, contractility, blood pressure, peripheral resistance and smooth muscle contraction to tx incontinence and nasal decongestant
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Tell me all about yohimbamine
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competitive and selective antagonist of a2 receptors that stimulates CNS, increases HR, BP, insulin release; used for reversal of anesthesia/sedation induced by a2 agonists
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Tell me about Phenoxybenzamine
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irreversible inhibition of alpha receptors (a1>a2) that decreases peripheral resistance --> hypotension (reflex tachycardia); decreases urethral tone to tx urethral obstruction; dx pheochromocytoma and tx associated hypertension
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Important things about propanolol
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competitive and non-selective antagonist of B2 receptors that negatively affects HR, CO, conductance and automaticity; used to tx cardiac arrythmias, thyrotoxicosis and hypertension associated with pheochromocytoma
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What type of effects do parasympathomimetic agents produce?
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peripheral excitatory actions, cardiac inhibitory actions, rarely CNS excitatory actions
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What receptors mediate peripheral excitatory actions of parasympathomimetics?
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muscarinic receptors except nicotinic on skeletal muscles
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What receptors mediate cardiac inhibitory actions produced by parasympathomimetics?
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muscarininc receptors
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Why are CNS excitatory actions rare with parasympathomimetics? Which type may produce CNS excitatory actions?
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Rare d/t BBB, cholinesterase inhibitors may cause excitement followed by depression
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What are the mechanisms of action of parasympathomimetics?
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direct stimulation of muscarinic and nicotinic receptors; and indirect action involving inhibition of cholinesterases
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What are the attachment sites for ACh on acetylcholinesterase?
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esteratic site and anionic site
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How do AChE inhibitors prevent metabolism of ACh?
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AChE inhibitors prevent deacylation of ACh by binding to either or both the esteratic and/or anionic sites of AChE. May be reversible or irreversible.
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What binds irreversibly to only the esteratic site?
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organophosphates
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What do the effects of cholinergic agents depend on?
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Concentration used and whether ganglionic receptors are affected
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Lets talk about atenolol
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competitive and selective antagonist of B1 receptors that decrease HR, CO and BP for TX of cardiac arrythmias, hypertrophic cardiomyopathy, hypertension
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What is Bethanechol?
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choline ester related to ACh but more slowly metabolized produces muscarinic activity such as increased GI motility and secretion, urinary bladder contraction and sphincter relaxation used to stimulate bladder contractions
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Tell me about Pilocarpine
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natural alkaloid with direct muscarinic and nicotinic
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Let's talk about Neostigmine
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reversible, competitive inhibition of AChE via carbamylation producing increased GI motility & secretion, muscle fasciculations, miosis for reversal of tubocurarine-like neuromusclular blockade, paralytic ileus, atony of urinary bladder, myasthenia gravis
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What about edrophonium and pyridostigmine?
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reversible inhibition of AChE producing increased GI motility & secretion, muscle fascilutaions, miosis for reversal of turbocuranine-like neuromuscular block and dx (edrophonium) and tx (pyridostigmine) of myasthenia gravis
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Of edrophonium and pyridostigmine, which is short-acting and which is relatively long-acting?
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Edrophonium is short-acting and pyridostigmine is long-acting
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Let's chat about atropine
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plant alkaloid that competitively inhibits muscarinic receptors to produce mydriais, cylopeglia, tachycardia, decreased GI tone, decreased salivary, sweat & resp secretion, bronchodilation that is used for presnesthetic agent, bradycardia (sinus bradycardia, sinoatrial arrest, incomplete heart block), tx of anticholinesterase toxicity, myadriasis for eye exam
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What else can be used to induce myadriasis for eye exam?
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Tropicamide
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What is propantheline?
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antimuscarinic similar to atropine except it does not cross the BBB used for antipasmodic and antisecretory actions for diarrhea
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Tell me about glycopyrrolate
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antimuscarinic similar to atropine except it does not cross the BBB used as preanesthetic agent, tx for sinus bradycardia (SA arrest, incomplete AV block), and in conjunction with neostigmine for reversal of tubocurarine-like neuromuscular block
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What is pralidoxime?
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Selective antidote for organophosphate poisoning
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