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Intro to pharm

Physiology of PNS/cholinergics/adrenergics/fluid-electrolyte imbalance

QuestionAnswer
What are the two divisions of the nervous system? Central NS & Peripheral NS (includes somatic + autonomic: parasympathetic & autonomic: sympathetic)
What are three functions of the autonomic nervous system? regulates heart, secretory glands, & smooth muscles
What are the functions of the parasympathetic nervous system? (GI/bladder/eye) housekeeping (always "on"), slowing of heart rate, increased gastric secretion, emptying of bladder/bowel, focusing of the eye, constriction of pupil, contraction of bronchi
What are the functions of the sympathetic nervous system? (heart/lungs) fight or flight, increased heart rate & blood pressure, dilation of pupils, dilation of bronchi, shunt blood from skin-->muscle, mobilization of stored energy
The parasympathetic nervous system dominates except what? except the vascular system
What are the main components of the basic parasympathetic nervous system pathway? spinal cord, preganglionic neuron, ganglion, postganglionic neuron, various organs
What are the main components of the basic sympathetic nervous system pathway? spinal cord, preganglionic neuron-->ganglion-->postgangionic neuron-->various organs OR spinal cord-->"preganglionic neuron"-->adrenal medulla-->various organs
What are the main components of the basic somatic motor system pathway? spinal cord, motor neuron, skeletal muscle
Where do drugs work? at the ganglionic junction or effector organ
What are the neurotransmitters used in the parasympathetic nervous system? ACh (acetylcholine) at both junctions (ganglionic & at junction with organ)
What are the neurotransmitters used in the sympathetic nervous system? ACh (acetylcholine) at the ganglionic junction & at the adrenal medulla & at the junctions with sweat glands; NE (norepinephrine) at the junctions with various organs & the postgranglionic neuron; Epinephrine Epi) after adrenal medulla-->organ
What neurotransmitter is used in the somatic motor system? ACh(acetylcholine) between the motor neuron & skeletal muscle
What are three cholinergic (ACh) receptor subtypes? NicotinicN, NicotinicM, Muscarinic
What are the adrenergic (Epi & NE) receptor subtypes? Alpha1, Alpha2, Beta1, Beta2, dopamine
What are the receptor subtypes located in the parasympathetic nervous system? At the ganglionic junction, ACh binds to a nicotinicN receptor; At the organ junction, ACh binds to a muscarinic receptor
What are the receptor subtypes located in the sympathetic nervous system? At the ganglionic junction, ACh binds to a nicotinicN receptor; at the organ junction, NE binds to alpha or beta receptors; at the sweat gland junction, ACh binds to a muscarinic receptor; at the adrenal medulla-organ junction, Epi binds to alpha or beta
What receptor subtype is located in the somatic motor system? At the neuromuscular junction (motor neuron-skeletal muscle), ACh binds to a muscarinic receptor
Where are nicotinicN (cholinergic) receptor subtypes located? all autonomic nervous system ganglia & the adrenal medulla
What is the NicotinicN (cholinergic) receptor subtype response to receptor activation? stimulation of parasympathetic postganglionic nerves & release of epinephrine from the adrenal medulla
Where are nicotinicM (cholinergic) receptor subtypes located? at the neuromuscular junction
What is the NicotinicM (cholinergic) receptor subtype response to receptor activation? contraction of skeletal muscle
Where are muscarinic (cholinergic) receptor subtypes located? all parasympathetic target organs: eye, heart, lung, bladder, GI tract, sweat glands, sex organs, blood vessels
What is the muscarinic (cholinergic) receptor response to receptor activation in the eye? contraction of the ciliary muscle focuses the lens for near vision; contraction of the iris sphincter muscle causes miosis (decreased pupil diameter)
What is the muscarinic (cholinergic) receptor response to receptor activation in the heart? decreased heart rate
What is the muscarinic (cholinergic) receptor response to receptor activation in the lung? CONSTRICTION of bronchi, promotion of secretions
What is the muscarinic (cholinergic) receptor response to receptor activation in the bladder? promotes voiding
What is the muscarinic (cholinergic) receptor response to receptor activation in the GI tract? salivation, increased gastric secretions, increased intestinal tone & motility, defacation
What is the muscarinic (cholinergic) receptor response to receptor activation in the sweat glands? generalized sweating
What is the muscarinic (cholinergic) receptor response to receptor activation in the sex organs? erection
What is the muscarinic (cholinergic) receptor response to receptor activation in the blood vessels? vasodilation
Where are Alpha1 (adrenergic) receptor subtypes located? eye, arterioles (skin, viscera, mucous membranes), veins, sex organs (male), bladder neck & prostatic capsule
What is the Alpha1 (adrenergic) receptor response to receptor activation? eye:contraction of radial muscle of iris causes mydriasis (increased pupil size); arterioles (skin, viscera, mucous membranes): constriction; veins: constriction; male sex organs: ejaculation; bladder neck & prostatic capsule: contraction
Where are Alpha2 (adrenergic) receptor subtypes located? presynaptic nerve terminals (NOT ORGANS) (in CNS are postsynaptic)
What is the Alpha2 (adrenergic) receptor response to receptor activation? inhibition of neurotransmitter release
Where are Beta1 (adrenergic) recptor subtypes located? HEART, kidneys
What is the Beta1 (adrenergic) receptor response to receptor activation? heart: increased rate, increased force of contraction, increased AV conduction velocity; kidney: renin release
Where are Beta2 (adrenergic) receptor subtypes located? LUNGS, arterioles (heart, lung, skeletal muscle), bronchi, uterus, liver, skeletal muscle
What is the Beta2 (adrenergic) receptor response to receptor activation? arterioles (heart/lung/skeletal muscle): dilation; bronchi: dilation; uterus: relaxation; liver: glycogenolysis; skeletal muscle: enhanced contraction/glycogenolysis
Where are the dopamine (adrenergic) receptor subtypes located? kidney
What is the dopamine (adrenergic) receptor response to receptor activation? dilation of kidney vasculature
What is the specificity of epinephrine (which receptors won't it bind to)? no dopamine
What is the specificity of norepinephrine (which receptors won't it bind to)? no beta2 or dopamine
What is the specificity of dopamine (which receptors won't it bind to)? no alpha2 or beta2
What are the basic steps in the life cycle of ACh? choline + acetylcoenzyme A (acetyl CoA); STORED; destroyed by acetylcholinesterase (enzymatic degradation terminates transmission); uptake of choline
What are the basic steps in the life cycle of NE? precursors: amino acids; vesicles; reuptake (terminates transmission NOT enzymatic degradation); converted to Epi
What is the representative drug for muscarinic agonists? Bethanechol
What is the representative drug for muscarinic antagonists? atropine
What is the representative drug for ganglionic stimulating agents? nicotine
What is the representative drug for ganglionic blocking agents? Trimethaphan
What is the representative drug for neuromuscular blocking agents? d-Tubocurarine, succinylcholine
What is the representative drug for cholinesterase inhibitors? Neostigmine, physostigmine
What are the characteristics of muscarinic receptor subtypes? Location: sweat glands/blood vessels/all organs regulated by parasympathetic nervous system; effects of receptor activation: many/decreased heart rate/increased gland secretion/smooth muscle contraction; receptor agonists: Bethanechol/Cholinesterase inhib
What are the characteristics of NicotinicN receptor subtypes? Location: all ganglia of the autonomic nervous system; effects of receptor activation: promotes ganglionic transmission; receptor agonists: Nicotine/cholinesterase inhibitors-physosttigmine/neostigmine); receptor antagonists: Trimethaphan
What are the characteristics of NicotinicM receptor subtypes? location: neuromuscular junction; effects of receptor activation: skeletal muscle contraction; receptor agonists: nicotine/cholinesterase inhibitors: physostigmine/neostigmine; receptor antagonists: d-Tubocurarine, succinylcholine
What are some examples of muscarinic agonists (parasympathetic: mimic PSNS-decreased heart rate, increased sweating, voiding, salivation, pupil constriction)? Bethanechol: relieves urinary retention + side effects include hypotension, excessive salivation/gastric acid secretion, bronchoconstriction; Pilocarpine (glaucoma med); Acetylcholine (Michol- used with opthalmic surgery)
What are some characteristics of muscarinic antagonists? used for muscarinic poisoning (mushrooms/muscarinic agonists/cholinesterase inhibitors); example is Atropine; also used for preanesthetic + disorders of the eye + bradycardia + decrease intestinal motility + stabilize blood pressure
What are some symptoms of muscarinic poisoning (mushrooms/muscarinic agonists/cholinesterase inhibitors)? excessive sweating, tearing, hypotension
What are some possible side effects of muscarinic antagonists? dry mouth, blurred vision, elevation of eye pressure, constipation, tachycardia
What are some potential drug interactions for muscarinic antagonists? antihistamines, antipsychotics, antidepressants
What are some examples of muscarinic antagonists used for urge incontinence? Oxybutynin (Nitropan) & Tolterodine (Detrol)
What is a muscarinic antagonist used for motion sickness? Scopolamine
What is a muscarinic antagonist used for asthma? Ipatropium Bromide
What are some characteristics of antimuscarinic poisoning? treated with natural products/muscarinic antagonists/antimuscarinic properties; signs of poisoning: Hot as Hare + dry as bone + red as beet + blind as bat + mad as hatter (delerium is step further); use charcoal & physostigmine (inhibitor of acetylcholine
What are two reversible cholinesterase inhibitors? Neostigmine (Prostigmin) + Physostigmine (Antilirium)
What are some characteristics of Neostigmine (Prostigmin)? reversible cholinesterase inhibitor; binds to cholinesterase preventing it from catalyzing breakdown of ACh; used with myasthenia gravis; side effects: salivation, GI secretion, sweating; interactions: muscarinic antagonists, neuromuscular blockers; does
What are some characteristics of Physostigmine (Antilirium)? crosses membranes, drug of choice to treat Atropine poisoning
What are some characteristics of Myasthenia Gravis? fluctuating muscle weakness & rapid fatigue; drooping eyelids, difficulty swallowing, weakness of muscle, difficulty breathing; autoimmune-antibodies against nicotinicM receptors (can result in 70-90% decrease)
What are some characteristics of irreversible cholinesterase inhibitors? highly toxic (insecticides & nerve agents); glaucoma (only use for these: Echothiopate-phospholine iodide)
What are some characteristics of poisoning due to irreversible cholinesterase inhibitors? symptoms: profuse sweating/urination/bronchoconstriction/paralysis; treat with ventilation/atropine/Pralidoxime (Protopam)
What receptor subtype is blocked by neuromuscular blocking agents? block nicotinicM receptors (result in muscle relaxation)
What receptor subtype is blocked by ganglionic blocking agents? block nicotinicN (mostly replaced by newer drugs though)
During neuromuscular excitation-contraction depolarization, does positve charge go in or out? positive goes in during depolarization
During neuromuscular excitation-contraction repolarization, does positive charge pump in or out? during repolarization, positive pumps out
What are some characteristics of the non-depolarizing neuromuscular blocking agent Tubocurarine (curare)? mechanism of action: competes with ACh to bind to nicotinicM receptors; used for muscle relaxation during surgery, mechanical ventilation, endotrachial intubation, & electroconvulsive therapy; side effects: respiratory paralysis, hypotension; drug interac
What is the main thing to watch for when a patient has taken neuromuscular blocking agents? respiratory distress
What are some characteristics of the depolarizing neuromuscular blocking agent Succinylcholine (Anectine, Quelicin)? binds to nicotinicM receptors (& remains bound: constant depolarization); used for endotrachial intubation, electroconvulsive therapy, endoscopy; side effects: apnea, malignant hyperthermia, postoperative muscle pain, hyperkalemia; drug interactions: chol
What are some therapeutic uses for neuromuscular blocking agents? muscle relaxation during surgery, mechanical ventilation, electroconvulsive therapy, endotracheal intubation
What are some characteristics of ganglionic blocking agents? lack selectivity; example is Trimethaphan (Arfonad) which competes with ACh for binding to nicotinicN receptors; controlled hypertension in surgery, hypertensive crisis; side effects include antimuscarinic effects (dry mouth/blurred vision/elevation of ey
What are some characteristics of adrenergic agonists (sympathomimetics)? direct receptor binding, promotion of NE release (indirect), inhibition of NE uptake (indirect): termination, inhibition of NE inactivation (indirect): MAO, catecholamines & noncatecholamines
What are some characteristics of adrenergic agonists-catecholamines? Epinephrine, NE, Isoproterenol, Dopamine & Dobutamine; cannot give orally (MAO-liver, COMT-intestine); cannot cross BBB, brief duration of action; chemistry: catechol group + amine
What are some characteristics of adrenergic agonists-non-catecholamines? Ephedrine, Phenylephrine, & Terbutaline; given orally; penetrates BBB, longer duration of action
Which catecholamines activate alpha1 receptors? Dopamine, epinephrine, norepinephrine
Which noncatecholamines activate alpha1 receptors? phenylephrine, ephedrine
Which catecholamines activate alpha2 receptors? epinephrine, norepinephrine
Which noncatecholamines activate alpha2 receptors? ephedrine
Which catecholamines activate beta1 receptors? epinephrine, norepinephrine, isoproterenol, dobutamine, dopamine
Which noncatecholamines activate beta1 receptors? ephedrine
Which catecholamines activate beta2 receptors? epinephrine, isoproterenol
Which noncatecholamines activate beta2 receptors? ephedrine, terbutaline
Which catecholamines activate dopamine receptors? dopamine
Which nonchatecholamines activate dopamine receptors? none
What are the uses for alpha1 activation? vasoconstriction-hemostasis (Epi), nasal decongestion (phenylephrine & ephedrine), delay of anesthetic absorption (Epi), elevation of blood pressure (not primary drugs used), pupil dilation
What are some side effects of alpha1 activation? mostly relate to vasoconstriction, hypertension, necrosis, bradycardia
What are some uses for alpha2 activation? peripheral-inhibits NE release; CNS-reduce stimulation of adrenergic receptors
What are some uses for beta1 activation? cardiac arrest (helps to get contraction going), heart failure (increases force of contraction), shock (increase heart rate & blood flow), AV heart block (increase impulse conduction)
What are some side effects of beta1 activation? altered heart rate or rhythm, angina pectoris (insufficient oxygen compared to demand)
What are some uses for beta2 activation? asthma (bronchodilation), delay of preterm labor (relaxation of uterus)
What are some side effects of beta2 activation? hyperglycemia, tremor (most common)
What are some uses for dopamine activation? shock (dilation of kidney vasculature)
What are some characteristics of anaphylactic shock? hypotension, bronchoconstriction, edema, Epi (all receptors)
What are some characteristics of the catecholamine Epinephrine (Adrenalin, EpiPen)? binds to all receptors except dopamine (alpha 1&2, beta 1&2), used for anaphylactic shock, delay absorption of anesthetics, hemostasis, overcome AV heart block, pupil dilation, asthma
What are some side effects of the catecholamine epinephrine (adrenalin, epipen)? hypertensive crisis, dysrhythmias, angina, necrosis, hyperglycemia
What are some drug interactions for the catecholamine epinephrine (adrenaline, epipen)? MAO inhibitors, tricyclic antidepressants
What are some characteristics/side effects/drug interactions for the catecholamine norepinephrine (Levophed)? bind to alpha1, alpha2, beta1; used for hypotension & cardiac arrest; side effects: hypertensive crisis, dysrhythmias, angina, necrosis
What are some characteristics of the catecholamine Isoproterenol (Isuprel)? bind to beta1 & beta2; used for AV heart block, asthma, bronchospasm
What are some side effects of the catecholamine Isoproterenol (Isuprel)? dysrhythmias, angina, hyperglycemia
What are some drug interactions for the catecholamine Isoproterenol (Isuprel)? MAO inhibitors, tricyclic antidepressants
What are some characteristics of the catecholamine dopamine (Intropin)? bind to dopamine/alpha1/beta1 receptors, used for shock, heart failure, acute renal failure
What are some side effects of the catecholamine dopamine (Intropin)? tachycardia, dysrhythmias, angina, necrosis
What are some drug interactions for the catecholamine dopamine (Intropin)? MAO inhibitors, tricyclic antidepressants
What are some characteristics of the catecholamine Dobutamine (Dobutrex)? binds to beta1 receptors, used for heart failure, side effect is tachycardia, drug interactions with MAO inhibitors/tricyclic antidepressants/anesthetics
What are some characteristics of the noncatecholamine Terbutaline (Brethine)? binds to beta2 receptors, used for asthma & delay of preterm labor, side effect is tremor
What are the characteristics of the noncatecholamine Ephedrine? binds to alpha1, alpha2, beta1, beta2 receptors; mixed drug (direct activation of alpha/beta & indirect by releasing NE); used for nasal decongestion & narcolepsy
What are the side effects for the noncatecholamine Ephedrine? hypertensive crisis, dysrhythmias, angina, necrosis, hyperglycemia, insomnia
Which adrenergic antagonists (blocking agents) block both alpha1 and alpha2 receptors? Phentolamine, Phentoxybenzamine
Which adrenergic antagonists block only alpha1 receptors? Doxazosin, Prazosin, Terazosin, Tamsulosin
Which adrenergic antagonists block both beta1 & beta2 receptors? Carteolol, Carvedilol, Labetalol, Nadolol, Penbutolol, Pindolol, Propranolol, Sotalol, Timolol
Which adrenergic antagonists block only beta1 receptors? Acebutolol, Atenolol, Betaxolol, Bisoprolol, Esmolol, Metoprolol
What are some uses for alpha-adrenergic antagonists? hypertension, reversal of alpha1 agonist toxicity, benign prostatic hyperplasia, pheochromocytoma, Raynaud's Disease
What are some side effects of alpha-adrenergic antagonists? orthostatic hypotension, reflex tachycardia, nasal congestion
What are some characteristics of the alpha-adrenergic antagonist Prazosin (Minipress)? alpha1 blockers, used for hypertension & benign proststic hyperplasia; side effects: orthostatic hypotension, reflex tachycardia, nasal congestion
What are some characteristics of the alpha-adrenergic antagonist Phentolamine (Regitine)? alpha1 & alpha2 blockers, used for pheochromocytoma; side effects: orthostatic hypotension, reflex tachycardia, nasal congestion (same as Prazosin)
What are some general characteristics of beta-adrenergic antagonists? used for angina pectoris, hypertension, dysrhythmias, MI, heart failure; side effects (depend on receptor blocked): beta1-bradycardia/precipitation of heart failure/AV heart block; beta2-bronchoconstriction/inhibits glycogenolysis
What receptors does the beta-adrenergic antagonist Proprandolol (Inderal) block & what are its uses? blocks beta1 & beta2; used for hypertension, MI, angina
What are the side effects of the beta-adrenergic antagonist Propranolol (Inderal)? bradycardia, heart failure, inhibition of glycogenolysis, bronchoconstriction, CNS effects
What are the contraindications & drug interactions for the beta-adrenergic antagonist Propranolol (Inderal)? contraindications: diabetics, severe allergic reaction, heart failure, asthma, depression; drug interactions: calcium channel blockers, insulin
What receptor does the beta-adrenergic antagonist Metoprolol (Lopressor) block & what are its uses? blocks beta1; uses: hypertension, patients with asthma or diabetes & angina or MI
What are the side effects of the beta-adrenergic antagonist Metoprolol(Lopressor)? bradycardia, AV heart block
What are the contraindications for the beta-adrenergic antagonist Metoprolol (Lopressor)? heart failure, sinus bradycardia
What are the characteristics of the indirect acting antiadrenergic agent Reserpine (adrenergic neuron-blocking agent)? suppresses NE synthesis & displaces NE from vesicles, hypertension, side effects: depression/bradycardia/orthostatic hypotension; Guanethidine (Ismelin): no CNS effects b/c does not cross BBB
What are some characteristics of the centrally acting alpha2 agonist (indirect agent) Clonidine (Catapres)? activates alpha2 receptors to decrease transmitter release; used for hypertension & severe pain; side effects: drowsiness, dry mouth, rebound hypertension; other drugs: Guanabenz (Wytensin) & Guanfacine (Tenex)
What are some characteristics of the centrally acting alpha2 agonist (indirect agent) Methyldopa (Aldomert)? similar to clonidine except must be converted to methylNE; used for hypertension; side effects: hemolytic anemia & liver toxicity
What are some applications for diuretics? increase output of urine; hypertension; mobilization of fluid; prevent renal failure
What is the functional unit of the kidney? Nephron (including glomerulus, proximal convoluted tubule, loop of Henle, distal convoluted tubule, collecting duct)
What are some kidney functions? cleansing of extracellular fluid (ECF), maintenance of acid-base balance, excretion of metabolic wastes & foreign substances
What are three basic renal processes? filtration, reabsorption, active secretion
What are some characteristics of renal filtration? occurs at glomerulus, small molecules such as sodium/chloride (smaller amounts of bicarbonate, potassium ions), 125mL of filtrate per minute (180L per day), non-selective
What are some characteristics of renal reabsorption? very selective, 99% undergoes reabsorption, active transport, water follows passively, diuretics interfere
What are some characteristics of renal secretion? "pumps" for active secretion, located in proximal convoluted tubules, organic acids/organic bases
What are some characteristics of the reabsorption site: proximal convoluted tubule? 65% of Na+ & Cl-; all of bicarb & K+; water passively follows, isotonic, dilute urine
What are some characteristics of the reabsorption site: loop of Henle? descending loop: permeable to water, concentrated urine; ascending loop: 20% of Na+ & Cl-; NOT permeable to water, returns to original isotonic urine
What occurs in the distal convoluted tubule (early segment)? 10% of Na+ & Cl-; water passively follows
What occurs at the late distal convoluted tubule & collecting duct (distal nephron)? exchange of Na+ & Cl-; urine concentration by ADH (antidiuretic hormone), deficiency =diabetes
What are some characteristics of diuretics? blockade of Na+ & Cl- reabsorption; prevents reabsorption of water/retention; small blockade = large effect
What are some general adverse effects of diuretics? acid-base imbalance, disturbance of electrolytes, severe dehydration
What are the most effective diuretics? High-ceiling Loop diuretics (work in the loop of henle), such as Furosemide (Lasix)
What are some characteristics of Furosemide (Lasix)? blocks Na+ & Cl- reabsorption (some K+); high-ceiling loop diuretic, possible adverse effects: dehydration (headache/pain in chest, calves, pelvis), hypotension, hypokalemia-Digoxin toxicity, ototoxicity
What are some characteristics of Thiazide diuretics? block Na+ & Cl- reabsorption (K+), elevate uric acid & glucose, example is Hydrochlorothiazide (HydroDIURIL), which works at the early segment of distal tubule & depends on kidney function
What are some potential adverse effects of Hydrochlorothiazide (HydroDIURIL), a thiazide diuretic? dehydration (headache/pain in chest, calves, or pelvis), hypotension, hypokalemia-Digoxin toxicity, not for use during pregnancy
What are some characteristics of Potassium-sparing diuretics? modest increase in urine production, decrease in K+ excretion, aldosterone & non-aldosterone, examples: Spironolactone (Aldactone), Triamterene (Dyrenium), Amiloride (Midamor)
What are some characteristics of Spironolactone (Aldactone)? potassium-sparing diuretic, aldosterone antagonist, retains potassium & excretes sodium, adverse effects: hyperkalemia
What are some characteristics of Triamterene (Dyrenium)? potassium-sparing diuretic, non-aldosterone antagonist, direct inhibitor of potassium/sodium exchange, quicker than spironolactone, adverse effects: hyperkalemia
What are some characteristics of osmotic diuretics? creates osmotic force as undergoes minimal reabsorption, example: Mannitol (Osmitrol)
What are some characteristics of Mannitol (Osmitrol)? Intracranial pressure & intraocular pressure are uses, adverse effect is edema(don't use this drug to treat edema)
Created by: mpost51