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Sympathetic Nervous System
Dr. Elstad's Pharmacology Final Exam 2011
138
Pharmacology
Professional
12/08/2011

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Term
Effects of alpha 1 on smooth muscle
Definition
contraction
Term
Effects of alpha 1 on pupillary dilator muscle
Definition
contraction (dilates pupil)
Term
effects of alpha 1 on pilomotor smooth muscle
Definition
erects hair
Term
effects of alpha 1 on prostate
Definition
contraction
Term
effects of alpha 1 on heart
Definition
increases force of contraction
Term
effects of alpha 2 on platelets
Definition
aggregation
Term
Effects of alpha 2 on adrenergic and cholinergic nerve terminals
Definition
inhibition of transmitter release
Term
Effects of alpha 2 on some vascular smooth muscle
Definition
contraction
Term
Effects of alpha 2 on fat cells
Definition
inhibition of lipolysis
Term
Effects of beta 2 on respiratory, uterine, and vascular smooth muscle
Definition
promotes smooth muscle relaxation
Term
effects of beta 2 on skeletal muscle
Definition
promotes potassium uptake
Term
effects of beta 2 on human liver
Definition
activates glycogenolysis
Term
effects of D1 receptor on smooth muscle
Definition
dilates renal blood vessels
Term
effects of D2 on nerve endings
Definition
modulates transmitter release
Term
Direct-acting sympathomimetics
Definition
Bind to adrenergic receptors
Term
Indirect-acting sympathomimetics
Definition
Cause release of NE from nerve endings, All indirect-acting drugs are substrates for uptake-1
Term
Examples of indirect-acting sympathomimetics
Definition
Amphetamine, Methamphetamine, Methylphenidate, Tyramine
Term
Positive response after reserpine treatment
Definition
direct-acting
Term
no effect after reserpine treatment
Definition
indirect-acting
Term
partial effect after reserpine treatment
Definition
mixed-acting
Term
Effects of beta 2 and alpha 1 on the bladder
Definition
Beta 2 - relaxation, Alpha 1 - tightens sphincter to prevent urination
Term
effects of skin if Alpha 1 agonist binds to alpha 1 receptor
Definition
vasoconstriction in blood vessels in skin
Term
Effect of blood flow in skeletal muscle by activating beta 2 and alpha 1 receptors in physiological doses
Definition
Beta 2 is activated first, vasodilation, blood flow in skeletal muscles in high
Term
Effects of blood flow in skeletal muscle when activating alpha 1 and beta 2 receptors under higher doses
Definition
Activate alpha 1 and cause vasoconstriction.
Term
Effects of high doses of epinephrine on blood pressure
Definition
drives up blood pressure
Term
MAO and COMT effects
Definition
Degrade catecholamines (catechol, phenylethylamine,norepinephrine, epinephrine, isoproterenol, dopamine)
Term
Effects of epinephrine administered orally
Definition
not effective- cannot cross gut
Term
Effects of epinephrine administered subcutaneously
Definition
slow absorption- vasoconstriction in skin by alpha receptor (lower blood flow)
Term
effects of epinephrine administered intramuscularly
Definition
more rapid- causes vasodilation increasing flow
Term
effects of inhaled epinephrine
Definition
localized- lipophobic nature of epinephrine
Term
Cardiac output x Peripheral vascular resistance
Definition
blood pressure
Term
Cardiac effects of epinephrine
Definition
+ inotropic effects, + chronotropic effects (beta 1)
Term
vascular effects of epinephrine
Definition
redistribution of blood flow, cutaneous vasoconstriction, blood flow in skeletal muscles
(physiological dose= dilate blood vessels, high dose= constrict vessels)
Term
Epinephrine Reversal
Definition
Reversal of blood pressure caused by prior administration of an alpha-adrenergic antagonist
Term
Use of beta 2 agonist on uterine smooth muscle
Definition
can be used to delay delivery of the baby
Term
effects of beta 2 receptor on bladder smooth muscle
Definition
relaxes detrusor muscle
Term
effects of alpha 1 receptor on bladder smooth muscle
Definition
contracts trigone and sphincter muscles
Term
Respiratory effects of beta 2 and alpha 1 activation
Definition
Beta 2- bronchodilation and inhibition of Ag-induced release of inflammatory mediators from mast cells
Alpha 1- decreases bronchial secretion
Term
insulin effects of alpha 2 receptor in pancreas activation
Definition
inhibits insulin release --> blood glucose increases
Term
insulin effects of beta 2 receptor in pancreas
Definition
enhances insulin release --> blood glucose decreases
Term
dominating receptor in pancreas
Definition
Alpha 2
Term
Beta 2 receptor in pancreas effects on glucagon secretion
Definition
increase in glucagon secretion, increase in blood glucose
Term
metabolic effect of epinephrine in glucose uptake by peripheral tissues
Definition
glucose uptake is decreased
Term
epinephrine metabolic effect on glycogenolysis
Definition
increases glycogenolysis (breaks down glycogen into glucose) - beta 2
Term
effects of epinephrine on lipolysis
Definition
increased lipolysis- increases fatty acids, beta 3 receptor activation
Term
serious side effects (toxicities) of epinephrine
Definition
cerebral hemorrhage (caused by elevated blood pressure), cardiac arrhythmia (caused by beta 1 receptor)
Term
effects of administering epinephrine to someone taking a nonselective beta blocker
Definition
exaggerated response- shoots up response (patient may die from cerebral hemorrhage)
Term
epinephrine effects on local anesthetics
Definition
prolongs actions of local anesthetics- alpha 1 receptor
Term
epinephrine effects on cardiac rhythm
Definition
can restore cardiac rhythm (beta 1 receptor)
Term
epinephrine effects on bleeding surfaces
Definition
topical hemostatic agent on bleeding surfaces (alpha 1 causing vasoconstriction)
Term
epinephrine effects on open-angle glaucoma
Definition
treatment of open-angle glaucoma (alpha 2 decreases aqueous formation, alpha 1 increases aqueous outflow)
Term
Olipivefrin HCl
Definition
prodrug put on eyeball, gets metabolized into epinephrine after crossing cell membrane
Term
effects on someone on an MAO inhibitor
Definition
prolonged effects of catecholamines because they will not be metabolized as quickly
Term
Receptors activated by Norepinephrine
Definition
Alpha 1, Alpha 2, Beta 1
Term
Epinephrine vs. Norepinephrine (which has greater alpha activation)
Definition
Epinephrine is more potent activator at alpha receptor than NE
Term
Renin effects by epinephrine and norepinephrine
Definition
both stimulate renin release
Term
blood pressure and pulse pressure effects from norepinephrine
Definition
systolic and diastolic pressure are increased, pulse pressure usually increased -- involve activation of beta 1 cardiac receptor
Term
TPR effect from norepinephrine
Definition
TPR is increased -- alpha 1 receptor activated
Term
Norepinephrine metabolic effects
Definition
hyperglycemia, similar to EPI. (no beta 2 so you cannot increase insulin, you do not get the stimulation of glucagon release-- also do not increase glycogenolysis)
Term
Uterine effects from norepinephrine
Definition
increased frequency of contraction of pregnant human uterus
Term
Toxicites of NE
Definition
similar to EPI but less pronounced and less frequent.
most common- anxiety, respiratory difficulty, awareness of a slow forceful heart beat, transient headache

overdoses- severe hypertension, violent headache, photophobia, stabbing retrosternal pain, pallor, intense sweating, vomiting
Term
Therapeutic uses of NE (Levophed)
Definition
hypotension and shock
Term
Effects of MAO inhibitor on dopamine
Definition
will be prolonged because it is not metabolized as quickly
Term
dopamine effect on kidney
Definition
vasodilation- improve kidney function. important in patients who are renally compromised
Term
high doses of dopamine effects on heart
Definition
tend to stimulate beta 1 receptors, increase strength of contraction of heart, positive inotropic effect
Term
Mixed acting effects of dopamine
Definition
causes release of NE from nerve terminals
(therefore these effects can be blocked by tricyclic antidepressant or cocaine)
Term
half life of dopamine
Definition
half life is short- effects quickly disappear
Term
therapeutic use of dopamine
Definition
treatment of shock (hypotension)
Term
clinical roles of Beta adrenergic sympathomimetic
Definition
treatment of bronchoconstriction- beta 2
cardiac stimulants- beta 1
Term
Isoproterenol (Isuprel)
Definition
nonselective beta sympathomimetic
(can activate beta 1, 2 and 3)
much stronger agonist than epi at beta 1 and 2 receptors.
no alpha activity
Term
Isoproterenol structure
Definition
has catelcholamine in its structure- not an endogenous catelcholamine.
(effects will be prolonged by an MAO inhibitor)
Term
cardiovascular effects of nonselective beta sympathomimetic
Definition
decrease TPR - beta 2
increase HR- beta 1
increase CO- beta 1
net effect: decrease blood pressure
Term
Drug toxicities of nonselective beta sympathomimetic
Definition
palpitations, tachycardia, arrythmias, myocardial necrosis, flushed skin
Term
smooth muscle effects of nonselective beta sympathomimetic
Definition
bronchial relaxation- beta 2
GI smooth muscle relaxation- beta 2
Term
insulin effects of nonselective beta sympathomimetic
Definition
insulin secretion increases- beta 2 (blood glucose decreases)
Term
fatty acid effect of nonselective beta adrenergic sympathomimetic
Definition
free fatty acid release increases because of beta 3
Term
energy production effect of nonselective beta adrenergic sympathomimetic
Definition
increased energy production- beta 2
(increased glycogenolysis, increased glucagon release, increased blood glucose)
Term
therapeutic uses of nonselective beta adrenergic sympathomimetic
Definition
stimulate HR in patients with bradycardia- beta 1
treatment of asthma- beta 2
treatment of shock -beta 1
Term
dobutamine (dobutrex)
Definition
beta 1 selective sympathomimetic
Term
structure of dobutamine
Definition
resembled dopamine structurally (dobutamine and dopamine are the 2 most widely used beta 1 agonists, but their use is limited to emergency i.v. therapy)
Term
Cardiovascular effects of Dobutamine
Definition
Dose related-
low doses- selective beta 1 agonist
high doses- acts on beta 2 receptors with mild effects on alpha receptors
less peripheral vasoconstriction produced than if EPI is administered
Term
A person with an enlarged heart that is not functioning properly to provide the body with enough blood- what is the best drug to use?
Definition
Dobutamine- helps with congestive heart failure because it doesn't increase heart rate much but increases CO.
Term
therapeutic uses of Dobutamine
Definition
Treatment of cardiac decompensation that may occur after cardiac surgery or in patients with congestive heart failure or acute myocardial infarction
Term
Major use of Beta 2 selective adrenergic sympathomimetic
Definition
treatment of asthma
(bronchodilation, decreased release of leukotrienes and histamine from mast cells, increased mucociliary function, decreased microvascular permeability, inhibition of phospholipase A2, decreased arachidonic acid metabolism)
Term
Examples of Beta 2 selective adrenergic sympathomimetics
Definition
metaproterenol, terbutaline, albuterol,levalbuterol, pirbuterol, salmeterol, formoterol, arformoterol,indacaterol,ritodrine
Term
Toxicities of beta 2 selective adrenergic sympathomimetics
Definition
Skeletal muscle tremor (beta 2)
feelings of restlessness, apprehension, anxiety, tachycardia and arrythmias
increase glycogenolysis (beta 2 outsider of lungs)
Term
Cardiovascular toxicity effects from MAO inhibitors and tricyclic antidepressants
Definition
Toxicities are increased because of the enhanced NE effects
Term
general effects of alpha 1 selective adrenergic agonists
Definition
vasoconstriction, increased TPR, BP is maintained or increased
Term
General clinical uses of alpha 1 selective adrenergic sympathomimetics
Definition
treatment of hypotension, treatment of shock.
Term
Phenylephrine and Methoxamine
Definition
Direct-acting alpha 1 selective adrenergic agonists
Term
Mephentermine and Metaraminol
Definition
Mixed-acting alpha 1 selective adrenergic agonist
Term
Primary use of selective alpha 2 agonists
Definition
hypertension (they activate alpha 2 receptors in CNS that can cross the blood brain barrier. Suppresses sympathetic outflow from CNS)
Still causes vasoconstriction in smooth muscles.
Term
Examples of alpha 2 selective agonists
Definition
Clonidine, Apraclonidine, Guanfacine, Guanabenz, Methyldopa, Dexmedetomidine

(inhibit or paralyze sympathetic nervous system)
Term
Pharmocological effects of Clonidine
Definition
Decreased blood pressure, decreased heart rate
Term
Toxicities of Clonidine
Definition
Dry mouth, sedation, sexual dysfunction, marked bardycardia, contact dermatitis
Term
Therapeutic uses of Clonidine
Definition
FDA approved = treatment of hypertension and ADHD
non-FDA approved= decrease GI motility, treatment of withdrawal symptoms in narcotic and nicotine addicts, relieve menopausal hot flashes, treatment of neuropathic pain, anaesthetic uses, treatment of insomnia
Term
Amphetamines
Definition
Amphetamine (oral), Dextroamphetamine (oral), hydroxyamphetamine (ophthalamic)
= miscedllaneous adrenergic agonist
Term
pharmacological effects of amphetamines
Definition
indirect-acting sympathomimetic + CNS effects
(main effects on CNS, mainly cardiovascular effects because of CNS effects)
Term
cardiovascular effects of amphetamines
Definition
increased BP, heart rate reflexly slowed, cardiac arrythmias w/ large doses, cardiac output is generally not increased with therapeutic doses, cerebral blood flow does not change w/ therapeutic doses
Term
Amphetamines effect on appetite
Definition
decreased appetite (used to treat obesity)
Term
Toxicities of Amphetamines
Definition
psychotic effects, fatigue and depression, cardiovascular effects, excessive sweating, GI symptoms, fatal poisoning: convulsions and coma
Term
Treatment of obesity, narcolepsy, and ADHD
Definition
Amphetamines
Term
classified as a schedule II drug under federal regulations
Definition
Methamphetamine (Desoxyn)
Term
Ephedrine
Definition
Miscellaneous adrenergic agonist. Mixed-acting sympathomimetic + CNS effects
Term
Pharmacological effects of Ephedrine
Definition
Increased HR and CO, Increased TPR, Increased BP, Urinary Retention, Bronchodilation, Potent CNS stimulant

(can activate all 4 receptors)
Term
Toxicities of Ephedrine
Definition
Risk of hypertension and cardiac arrhythmias, insomnia, tachyphylaxis (tolerance) with repetitive doses
Term
Therapeutic uses of Ephedrine
Definition
bronchodilators in patients with asthma, promotion of urinary continence, treatment of hypotension associated with spinal anesthesia, nasal degonestant, past uses as CNS stimulant (narcolepsy and depression)
Term
Methylphenidate (Ritalin)
Definition
used in treatment of narcolepsy and ADHD
Term
Sympatholytics
Definition
Drugs that are competitive antagonists at alpha or beta adrenergic receptors
Term
Direct-acting sympatholytics
Definition
act peripherally on adrenergic neurotransmission at pre- or postsynaptic sites
Term
Indirect-acting sympatholytics
Definition
act centrally in the CNS
Term
Pharmacological effects of alpha 1- adrenergic antagonists
Definition
inhibit CV effects of endogenous catecholamines and exogenous sympathomimetics, vasodilation, decreased TPR, decreased BP, baroreceptor reflex increased in HR and CO
Term
Alpha 2 adrenergic antagonists CV pharmacological effects
Definition
increased release of NE from nerve endings, increased sympathetic outflow from CNS
Term
Actions of alpha adrenergic antagonists (in addition to CV effects)
Definition
decreased resistance to urinary outflow, inhibit contraction of bronchial smooth muscle, inhibit platelet aggregation, decreased glycogenolysis, increased insulin release from pancreas, decreased blood glucose
Term
Phenoxybenzamine
Definition
nonselective, irreversible alpha blocker
Term
pharmacological effects of phenoxybenzmine
Definition
vasodilation, decreased TPR, increased CO, orthostatic hypotension, ability to respond to hypovolemia and anesthetic-induced vasodilation is impaired
Term
Therapeutic uses of Phenoxybenzamine
Definition
treatment of pheochromocytoma, management of benign prostatic obstruction, management of autonomic hyperreflexia in patients with spinal cord transection
Term
Adverse side effects of Phenoxybenzamine
Definition
orthostatic or postural hypotension, reflex tachycardia
Term
similar agent of Pheoxybenzamine
Definition
Phentolamine (Regitine)
Term
Prazosin (Minipress)
Definition
Selective alpha 1 blocker
Potent inhibitor of cyclic nucleotide phosphodiesterases (increases cAMP)
Term
Examples of related agents to Prazosin (Minipress)
Definition
Terazosin, Doxazosin, Tamsulosin, Alfuzosin
Term
Pharmacological effects of Prazosin
Definition
decreased TPR, increased vasodilation, decreased VR, decreased cardiac preload (little tendency to increase CO and HR)
Term
Therapeutic uses of Prazosin
Definition
Major use: treatment of hypertension
Treatment of congestive heart failure
treatment of benign prostate hyperplasia
Term
Yohimbine (Aphrodyne)
Definition
Selective alpha 2 blocker
Term
Uses of Yohimbine
Definition
Little clinical usefulness (limited benefit in treating male erectile dysfunction), potention for treating orthostatic hypotension (promotes NE release via blockade of presynaptic alpha2 receptors
Term
cardiovascular effects of beta adrenergic receptor antagonists
Definition
decreased HR, negative inotropic effects, short term use - decreased CO, increased TPR, long term use- TPR returns to initial values
Term
pulmonary system effects of beta adrenergic receptor antagonists
Definition
in patients with asthma or COPD, blockade of beta 2 receptors in bronchial smooth muscle can lead to life threatening bronchoconstriction
Term
metabolic effects of beta adrenergic receptor antagonists
Definition
changes in metabolism of carbohydrates and lipids, potentially decrease pancreatic insulin release, increase blood glucose, may adversely affect recovery from hypoglycemia in insulin-dependence diabetics, decrease release of fatty acids from adipose tissue
Term
Propranolol
Definition
beta adrenergic receptor antagonist
prototype- used in the treatment of hypertension and angina
Term
examples of beta adrenergic antagonists
Definition
nadolol, timolol, pindolol, sotalol, carteolol
Term
examples of beta 1 selective receptor antagonists
Definition
metprolol, atenolol, esmolol, acebutolol, betaxolol, bisoprolol, nebivolol
Term
butoxamime
Definition
beta 2 selective adrenergic receptor antagonist
Term
CV toxic side effects of beta antagonists
Definition
may induce CHF in susceptible individuals, may cause or exacerate heart failure in compromised individuals, may cause bradycardia and life threatening radyarrhythmias, cold extremeties- worsening of PVD, development of Raynaud's phenomenon, Consequences of abrupt discontinuation after long term use- exacerbation of angina, increased risk of sudden death
Term
toxic side effects of pulmonary function- beta antagonists
Definition
life threatening increase in airway resistance
Term
toxic side effects of central nervous system- beta antagonists
Definition
fatigue, sleep disturbances (insomnia, nightmares) depression
Term
toxic side effects of metabolism -- beta antagonists
Definition
blunt recognition of hypoglycemia by patients, delay recovery from insulin-induced hypoglycemia, increased plasma triglycerides
Term
CV diseases therapeutic uses- beta antagonists
Definition
treatment of hypertension, treatment of ventricular arrhythmias, treatment of acute myocardial infarction and prevention of recurrences
Term
non-CV therapeutic uses of beta blockers
Definition
treatment of symptoms of hyperthroidism, prophylaxis of migraine headaches, control of acute pain, treatment of glaucoma, treatment of alcohol withdrawal
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