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52 Cards in this Set
- Front
- Back
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Binding of muscarinic receptors 1, 3, & 5 leads to cellular ___________ while 2 and 4 ___________ such activity.
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excitation, while 2 and 4 inhibit cellular excitability.
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The two primary chemical signals in the ANS?
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Acetylcholine & Norepinephrine
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Stimulation of the ___________ nervous system increases HR, BP. Diverts blood from skin and internal organs while increasing flow to skeletal muscle and heart and results in dilation of pupils and bronchioles.
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Sympathetic. The parasympathetic division opposes or balances its action.
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The ____________nervous system has the property of adjusting in response to stressful situations.
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Sympathetic, however, the Parasympathetic system is generally dominant in "rest and digest" situations.
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The adrenal medulla releases large quantities of ___________ into the blood and trace amounts of __________.
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EPINEPHRINE and norepinephrine
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When the baroreceptor in the aortic arch experienc a reduction, the afferent impulses to the brainstem are reduced. This causes an increase in Efferent impulses Via the ANS to increase peripheral resistance and cadiac output, resulting in increased BP. This is an example of a ___________.
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Relex arc. A response without involving consciousness.
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Agonist binding of M2 receptors on the heart and smooth muscles result in _________ cellular excitation.
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Decreased. Activation of this G protein linked receptor inhibits adenylyl cyclase and increases K+ conductance decreasing rate and force of contraction.
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Agonist binding of M1 receptors of the gastric parietal cells result in _________ cellular excitation.
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Increased. M1 & M3 trigger G-protein linked receptors activating Phospolipase C whose path increases intracellular Ca2+ hyperpolarizing the cell and increasing secretion, or contraction.
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M3 receptors are commonly found on _______, ________ and __________ effector organs.
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Bladder, exocrine glands and smooth muscle. Rememeber M3 excites intracellular function.
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Nicotinic receptors located at the neuromuscular junction are designated as ______while all others are designated as _____.
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Nm while all others are designated Nn.
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Acetylcholine is selective to ____and _______ receptors.
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Nicotinic and Muscarinic.
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Theraputic importance of Acetylcholine is __________.
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None, due to the multiplicity of its action and rapid degradation by acetylcholinesterase.
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Acetylcholine ______ heart rate and cardiac output.
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decreases. It mimics the effect of the parasympethetic Vagal nerve. Reduces SA node rate of fire.
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Acetylcholine ______ blood pressure.
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decreases. Muscarinic receptors in vascular endothelial cells increase intracellular Ca2+ which triggers the production of NO (Nitric Oxide) a endothelium-derived relaxing factor -> vasodilation.
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Acetylcholine ______ salivary secretion and _____ intestinal secretion and motility.
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Increases and Stimulates
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Bethanechol is a cholinergic agonist with affinity for the _____receptor.
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M3. Its major actions are on musculature of the bladder and GI tract.
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Bethanecol is clinically useful in the treatment of ___________.
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Postpartum, postoperative, nonobstructive urinary retention, neurogenic atony and megacolon. Bethanecol affinity is for M3 (M1,M3,M5 excite intracellular activity) increasing tone and motility of the GI and bladder. Bethanecol lacks nicotinic activity.
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The adverse effects of Bethanecol include......
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generalized cholinergic stimulation: sweating, salivation, vasodilation, nausea,abdominal pain, diarrhea and bronchospasms.
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Bethanecol has _____ duration of action.
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about a 1 hour.
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The cholinergic agonist Carbachol has both ____ and ____ receptor affinity.
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nicotinic and muscarinic.
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Carbachol is clinically useful in the treatment of ___________.
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Glaucoma. Because of its potency and long duration of action, it has little theraputic use.
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Pilocarpine has a therapeutic in treating___________.
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Glaucoma. It is the drug of choice in emergency lowering of intreocular pressure for both narrow and wide angle glaucoma.
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Pilocarpine has a duration action lasting ___________.
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up to one day. Atropine opposes the effects by blocking muscarinic receptors on the eye.
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Adverse effects of pilocarpine include _______and ________.
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Sweating and salivation. The tertiary amine does not carry a change which enables it to cross the BBB and cause CNS disturbances.
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Pilocarpine exhibits ________receptor activity.
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Muscarinic.
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Phytostigmine excerts its activity by binding with _______________.
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Acetylcholinesterase. It is a competitive substrate thus allowing the accumulation and potentiation of cholinergic activity.
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Phytostigmine is clinically useful in the treatment of _______________.
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Bladder and intestinal atony. . It is also used to treat overdoses of drugs with anticholinergic activities (atropine, phenothiazines and tri-cyclic anti-depressants.
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Phytostigmine exhibits a duration of action of __________.
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2 - 4 hours.
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The adverse effects of Phytostigmine include ____________ on the CNS, _____________on cardiac function and ____________ on skeletal muscule.
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Convulsion, bradycardia and paralysis. However these are rarely seen at therapeutic doses.
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Neostigmine, unlike phytostigmine has a _______ amine and does not effect the CNS.
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Quaternary. The extra bond provides the nitrogen its positive charge rendering it incapable of penetrating the BBB.
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Neostigmine is used to stimulate the ________and ________.
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Bladder and GI tract.It is also used in symptomatic treatment of myasthenia gravis and as an antidote for Turbocurarine and other neuromuscular blocking agents.
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Neostigmine has a _________ duration of action.
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30 minutes to 2 hours.
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Adverse effects of Neostigmine include__________.
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those of generalized cholinergic stimulation. Salivation, flushing, decreased blood pressure, nausea, abdominal pain, diarrhea, and bronchospasms.
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Pridostigmine and Ambenomium is similar to _____________. However they have a longer duration of action.
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Neostigmine.
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Demecarium is the first line treatment for ____________.
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Chronic open-angle glaucoma closed-angle glaucoma after irredectomy. It is also used in diagnosis and treatment of accomodative esotropia (cross-eyes when focusing).
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Edrophonium is used in the diagnosis of _______________.
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myasthenia gravis (autoimmune disease against nicotinic receptors). Given a IV injection leads to a rapid increase in muscle strength. 10-20 min. duration of action.
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Scopolomine is clinically useful in the teatment of _______________.
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Motion sickness. Its amnesic effects also makes it a useful adjunt in anethetics.
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While peripheral effects are similar, Scopolamine has a _________effect on the CNS than atropine
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Greater effect. This characteristic contributes to its amnesic and euphoric effects rendering this drug subject to abuse.
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Of the nicotinic ganglionic blockers only ___________ depolarizes the receptor prior to antagonizing the receptor.
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Nicotine.
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Cyclopentolate, Torpicamide and Atropine are cholinergic antagonost commonly used in_____________________.
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Opthalmology. To produce mydriasis and cycloplegia prior to refraction.
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Tubocurarine, pancuronium, mivacurium, metocurine and doxacurium are all ________________ competitive blockers.
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Nondepolarizing. Their quaternary amines in their bulky ring structure makes them orally ineffective, unable to pass the BBB and leave the body unchanged via urinary excretion.
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α adrenoceptor order of affinity for catecholamines.
_____>>_______>>________ |
Epinephrine>>Norepinephrine>>Isoproterenol
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β adrenoceptor order of affinity for catecholamines.
_____>>_______>>________ |
Isoproterenole>>Epinephrin>>Norepinephrine
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α1 adrenoceptor stimulation increases cytoplasmic _______through the G-Protein linked activation of _______________.
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Ca2+ through a G-Protein linked activation of phospolipase C. The result is the constriction of smooth muscle tissue.
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α2 receptors control ___________ and __________.
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Adrenergic neuromediation and insulin (down regulate) output. In neuromediation, these receptors assert an inhibitory action to the ongoing release of norepinephrine at the pre-synaptic nerve ending.
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Adrenoceptor _________ can be found on pre-synaptic parasympathetic neurons.
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α2. The release of norepinephrine into surrounding tissue acts as a local mediator of the parasympathetic and sympathetic nervous systems.
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α1 & α2 adrenoceptors are G-protein linked receptors. α1 stimulation cascade involves the second messanger ____________ while α2 involves _____________.
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α1 -> phospolipase C
α2-> cAMP α2 stimulation leads to the inhibition of ATP ->cAMP thus stopping the release of additonal norepinephrine. |
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vacalature to skeletal muscle have both α1 & β2 receptors, however ______ receptors predominate.
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β2. Conversly, in the heart β1 predominates.
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As a generalization _______stimulation produces vasoconstriction and increase in total peripheral resistnce and blood pressure.
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α1
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As a generalization _______stimulation causes cardiac stimulation.
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β1
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As a generalization _______stimulation produces vasodialation (skeletal vascular) and bronchiolar relaxation.
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β2
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As a generalization _______stimulation causes inhibition of Ach, Noepinephrine and insulin.
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α2
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