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Lehne Ch 13, Ch17 Physiology of PNS Flashcards

Physiology of PNS, intro to cholinergic drugs, intro to adrenergic drugs

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430854627To understand any particular PNS drug you need 3 types of info?(1) The type (or types) of receptor thru which the drug acts, (2) The normal response to activation of those receptors , (3) What the drug in question does to receptor function (ie, does it Inc/Dec receptor activation?)
430854628Activating Beta1Inc's cardiac output (by inc'g heart rate & force of contraction)
430854629Activating Beta2dilation of the bronchi & elevation of blood glucose
430854630The Peripheral Nervous System employs 3 neurotransmitters(1) acetylcholine, (2) norepinephrine, (3) epinephrine
430854631Acetylcholine is the transmitter released by - 5(1) ALL preganglionic neurons of the PNS, (2) ALL preganglionic neurons of the SNS, (3) ALL postganglionic neurons of the PNS, (4) ALL motor neurons to skeletal muscles, and (5) most postganglionic neurons of the SNS that go to sweat glands
430854632Norepinephrine is the transmitter released by ?Practically ALL postganglionic neurons of the SNS. The only exceptions are the postganglionic sympathetic neurons that go to sweat glands, which employ Ach as their transmitter.
430854633Epinephrine is the major neurotransmitter released by?Adrenal Medulla (the adrenal medulla also releases some NE)
430854634List the 3 Cholinergic receptor subtypes(1) NicotinicN, (2) NicotinicM, (3) Muscarinic
430854635ACh can activate ?All 3 Cholinergic receptor subtypes
430854636NicotinicN receptors are located?(1) Cell bodies of ALL Postganglionic Neurons of the PNS & SNS. (2) and the cells of the Adrenal Medulla
430854637Response to NicotinicN receptor activationStimulation of Parasympathetic & sympathetic postganglionic nerves & release of Epinephrine from the Adrenal Medulla
430854638Receptor Agonists for NicotinicNNicotine
430854639Receptor Antagonists for NicotinicNMecamylamine
430854640NicotinicM receptors are located?Skeletal muscle
430854641Response to NicotinicM receptor activationContraction of skeletal muscle
430854642Receptor Agonists for NicotinicMNicotine*(* The doses needed to activate nicotinicM receptors of the NMJs are much higher than the doses needed to activate nicotinicN)
430854643Receptor Antagonists for NicotinicMd-Tubocurarine, succinylcholine
430854644Muscarinic receptors are located?(1) All Organs regulated by the PNS (2) sweat glands (of the SNS) Muscarinic cholinergic receptors on blood vessels rqr addtl comment. These receptors are not assoc'd w/ the nervous system in any way. That is, no autonomic nerves terminate at vascular muscarinic receptors. However, regardless of their physiologic relevance, the cholinergic receptors on blood vessels do have pharmacologic significance. Why? Because drugs that are able to activate these receptors cause vasodilation, which in turn causes blood pressure to fall.
430854645Response to Muscarinic Receptor Activation(1) Eye: contraction of the ciliary muscle focus the lens for near vision (2) contraction of the Iris sphincter muscle causes miosis (dec'd pupil diam) (3) Heart : dec'd rate (4) Lung : constriction of bronchi (5) Bladder: promotion of secretions, contraction of detrusor inc's bladder pressure, relaxation of trigone & sphincter allows urine to leave (6) GI tract: Salivation, Inc'd gastric secretions, Inc'd intestinal tone, & mobility, Defecation (7) Sweat Glands: generalized sweating (8) Sex organs: Erection (9) Blood Vessels: Vasodilation
430854646Receptor Agonists for MuscarinicBethanecol
430854647Receptor Antagonists for MuscarinicAtropine
430854648List Adrenergic Receptor Subtypes(1) Alpha1 (2) Alpha2 (3) Beta1 (4) Beta2 (5) Dopamine
430854649Adrenergic receptors - alpha, beta, or both are located?(1) ALL Organs (except sweat glands) regulated by the SNS (2) & Organs regulated by Epinephrine released from the Adrenal Medulla
430854650Response of Alpha1 Peripheral Adrenergic Subtype(1) Eye: Contraction of radial muscle of iris (like spokes of wheel) causes mydriasis (Inc'd pupil sz) (2) Arterioles: Constriction (skin, viscera, mucous membranes (3) sex organs, male: Ejaculation (4) Prostate Capsule: Contraction (5) Bladder: Contraction of trigone & sphincter
430854651Response of Alpha2 Peripheral Adrenergic Subtype(1) Presynaptic nerve terminals: Inhibition of transmitter release (located on the nerve terminals and not on the organs innervated by the ANS)
430854652Response of Beta1 Peripheral Adrenergic Subtype(1) Heart: Inc'd rate, Inc'd force of contraction, Inc'd AV conduction velocity (2) Kidney: Release of renin (promotes synthesis of angiotensin, a powerful vasoconstrictor, helps elevated BP.
430854653Response of Beta2 Peripheral Adrenergic Subtype(1) Arterioles (heart, lung, & skeletal muscle) causes vasodilation (2) Bronchi: dilation (3) Uterus: Relaxation (4) Liver Glycogenolysis (5) Skeletal Muscle: Enhanced contraction, glycogenolysis
430854654Response of Dopamine Peripheral Adrenergic SubtypeKidney: dilation of kidney vasculature (In the CNS the dopamine receptors are of great therapeutic importance)
430854655List the 3 Adrenergic transmitters(1) Epinephrine (2) NE (3) dopamine
430854656Receptor specificity of adrenergic transmitters(1) Epinephrine can activate ALL Alpha & Beta receptors, but NOT dopamine receptors (2) NE can activate Alpha1, Alpha2, & Beta1 receptors, but NOT Beta2 or dopamine (3) Dopamine can activate Alpha1, Beta1, & Dopamine, but NOT Alpha2 or Beta2
430854657Adrenergic agonists produce their effects by activating adrenergic receptors. Since the SNS acts thru these same receptors, responses to adrenergic agonists & responses to stimulation of the SNS are very similar. Thus, adrenergic agonists are often called?sympathomimetics
430854658Adrenergic agonists fall into 2 major chemical classes:catecholamines & noncatecholamines
430854659Catecholamines & noncatecholamines differ in 3 important respects:(1) oral usability, (2) duration of action, (3) the ability to act in the CNS
430854660Catecholamines have 3 properties in common:(1) CANNOT be use orally, (2) brief duration of action, (3) CANNOT cross the blood-brain barrier (The actions of 2 enzymes monoamine oxidase (MAO) & catechol-O-methyltransferase (COMT) - explain why the catecholamines have short ½-lives and cannot be used orally. MAO & COMT are located in the liver & intestinal wall.
430854661List the 5 catecholamines:NE, Epinephrine, Isoproterenol, Dopamine, & Dobutamine
4308546623 catecholamines are only effective if admin'd by cont infusion?NE, dopamine, & dobutamine
430854663Catecholamines are polar molecules, and hence CANNOT ____?Cross the blood-brain barrier and thus have minimal effect on the CNS. The polar nature of the catecholamines are d/t the hydroxyl groups on the catechol portion of the molecule.
430854664Noncatecholamines have ethylamine in their structure, but do NOT contain?the catechol moiety that characterizes catecholamines.
4308546653 Noncatecholamines:(1) ephedrine, (2) albuterol, (3) phenylephrine
430854666Noncatecholamines differ from catecholamines in 3 important respects?(1)lack a catechol group so their ½ -lives are much LONGER, (2) Because they do NOT undergo rapid degradation by MAO & COMT they can be given ORALLY, (3) considerably less polar than catecholamines, and hence are more able to cross the blood-brain barrier.
430854667Receptor specificity is relative, not absolute. The ability of a drug to selectively activate certain receptors to the exclusion of others depends on the dosage:?(1) Low doses - selectivity is maximal, (2) As dosage Inc's - selectivity declines
430854668Receptor Specificity of Representative Adrenergic Agonists Catecholamines: Epinephrine?Alpha1, Alpha2, Beta1, Beta2
430854669Receptor Specificity of Representative Adrenergic Agonists Catecholamines: NE?Alpha1, Alpha2, Beta1
430854670Receptor Specificity of Representative Adrenergic Agonists Catecholamines: Isoproterenol?Beta1 & Beta2
430854671Receptor Specificity of Representative Adrenergic Agonists Catecholamines: Dobutamine?Beta1
430854672Receptor Specificity of Representative Adrenergic Agonists Catecholamines: Dopamine?Alpha1, Beta1 & Dopamine
430854673Receptor Specificity of Representative Adrenergic Agonists Noncatecholamines: Ephedrine?Alpha1, Alpha2, Beta1, Beta2
430854674Receptor Specificity of Representative Adrenergic Agonists Noncatecholamines: Phenylephrine?Alpha1
430854675Receptor Specificity of Representative Adrenergic Agonists Noncatecholamines: Albuterol?Beta1
430854676To understand the effects of any specific adrenergic agonist, all you need is 2 types of info:(1) identity of the receptors at which the drug acts (2) effects produced by activating those receptors. This will reveal a profile of drug action
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