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Exam #2 - Sympathomimetics
N/A
40
Pharmacology
Graduate
10/06/2009

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Term
Intra-synaptic Adrenergic Receptors in Sympathetic Pathway
Definition
alpha-1 or beta-1 receptors
Term
Extra-synaptic Adrenergic Receptors in Sympathetic Pathway (usually found on end organs, obtained by systemic circulation)
Definition
alpha-2 or beta-2 receptors
Term
Adrenal Medulla & Pheochromocytoma cells
Definition
places of NE & Epi production
Term
Adrenergic Post-ganglionic Synapse Reuptake Pump
Definition
removes both normally-released NE and circulating NE & Epi from synaptic cleft, requiring very high levels of each to stimulate alpha-1 & beta-1 receptors
Term
Monoamine Oxidase (MAO)
Definition
enzyme that inactivates NE & Epi, resulting in deaminated metabolites
Term
Monoamine Oxidase Inhibitors (MAOIs)
Definition
persons taking this type of drug will likely experience more intense effects of many sympathomimetic drugs which are otherwise inactivated by this enzyme
Term
General Effect of Alpha-Adrenergic Receptors on Smooth Muscle Sites
Definition
constriction of smooth muscle
Term
General Effect of Beta-Adrenergic Receptors on Smooth Muscle Sites
Definition
dilation or relaxation of smooth muscle
Term
General Effect of Beta-Adrenergic Receptors on Production Sites
Definition
production sites are stimulated, creating a response
Term
Overall normal resting level of sympathetic nerve activity (SNA)
Definition
activity level at 10-20% of maximum
Term
Reason for raised resting level of SNA
Definition
maintains certain critical body functions at optimum levels (i.e. BP & temp.); ALSO, level of activity can be rapidly adjusted up or down by centers in the brain, attempting to hold important bodily functions constant
Term
Baroreceptors
Definition
receptors in walls of carotid arteries & aortic arch that sense small, but significant changes in BP
Term
Thermoreceptors
Definition
receptors in brain & skin that tell the brain to redistribute SNA going to vessels near the surface of the body & to vessels in the inner core in an attempt to shift blood one way or the other to regulate body temperature
Term
Raynaud's Disease
Definition
a condition that causes some areas of your body — such as your fingers, toes, tip of your nose and your ears — to feel numb and cool in response to cold temperatures or stress; the arteries that supply blood to your skin narrow, limiting blood circulation to affected areas
Term
Epinephrine (Adrenalin, EpiPen, Primatene Mist)
Definition
direct-acting sympathomimetic mixed agonist that stimulates all alpha & beta-receptors alike; treats circulatory shock, anaphylactic shock, bronchoconstriction & bronchospasm, cardiac arrest, bradycardia due to A-V block, mixed with local anesthetics to prolong local anesthesia (alpha-receptors)
Term
Low IV rates of Epi cause
Definition
drug (& amount) that causes a decrease in diastolic BP; increases systolic & pulse pressure; increases heart rate
Term
High IV rates of Epi
Definition
drug (& amount) that increases diastolic, mean, and systolic pressures
Term
Norepinephrine (Levophed)
Definition
direct-acting sympathomimetic mixed agonist that acts on alphas & beta-1 receptors much more than beta-2s; used in neurogenic & septic shock; supports BP during spinal anesthesia
Term
Low IV rate of NE
Definition
drug (& amount) that increases systolic, diastolic, & mean BPs
Term
High IV rates for NE
Definition
drug (& amount) that increases all systolic, diastolic, & mean BPs
Term
isoproterenol (Isuprel)
Definition
direct-acting sympathomimetic mixed agonist that acts mainly on beta receptors; bronchodilator for asthma; treats A-V blocks along with bradyarrhythmias; used to assist in tilt-table tests for diagnosis of unexplained syncopes
Term
Low & High IV Rates of Isoproterenol
Definition
drug (& amount) that decreases diastolic & mean BPs while increasing pulse pressure and heart rate
Term
Low Dose of Dopamine
Definition
drug (& amount) that stimulates D receptors in GI & renal arterial smooth muscle, selectively increasing blood flow to GI & kidney
Term
Intermediate Dose of Dopamine
Definition
drug (& amount)that stimulates D receptors & beta-1 receptors, increasing blood flow to GI & kidney and also stimulating cardiac contractility & rate due to stimulation of cardiac beta-1 receptors
Term
Higher Doses of Dopamine
Definition
drug (& amount of) stimulates D receptors in GI & kidney arterial smooth muscle, beta-1 receptors at cardiac & arterial smooth muscle cells, as well as alpha-1 receptors; alpha-1 stimulation blunts effects of lower concentrations of drug in GI & kidney and together, with stimulation of all other vascular alpha-1s, raises substantially mean arterial BP du to overall increase in total peripheral vascular resistance
Term
Therapeutic Uses for Dopamine (DA, Intropin)
Definition
drug used to treat cardiogenic (beta-1) shock, neurogenic (alpha-1) shock, and septic shock (beta-1, alpha-1s); treat patients with congestive heart failure who may be refractory to other therapy; treats bradycardia in non-cardiac arrest patients who are unresponsive to other treatments
Term
dobutamine (Dobutrex)
Definition
selective beta-1 agonist that is a mix of 2 stereoisomers; one is an alpha-1 agonist and the other a potent beta-1 agonist plus alpha-1 antagonist; net effect is a fairly selective beta-1 stimulator that increases cardiac contractility & thus increases cardiac output & pulse pressure but does not incrase diastolic or mean BP
Term
Therapeutic Uses of dobutamine (Dobutrex)
Definition
drug used to treat CHF & certain forms of shock (cardiogenic); sometimes used to stimulate heart during emergence from surgery
Term
albuterol (Proventil), metaproterenol (Alupent), pirbuterol (Maxair), salmeterol (Serevent), terbutaline
Definition
drugs that are selective beta-2 agonists with some beta-1 agonist activity; bronchodilators used as "rescue" inhalers in treatment of COPD and asthmatics and prevention of exercise-induced bronchospasms
Term
salmeterol (Serevent)
Definition
selective beta-2 agonist that is used as a bronchodilator; has the longest duration of action
Term
terbutaline
Definition
selective beta-2 agonist that is used as a bronchodilator; also used to manage premature labor by causing beta-2-mediated uterine relaxation
Term
phenylephrine (Neo-Synephrine)
Definition
drug that is a selective vascular alpha-1 agonist; when given IV, raises diastolic & mean BP but with more reflex bradycardia than NE; when used IV, used to maintain diastolic & mean BP during spinal & other anesthesia, also rarely used to treat paroxysmal supraventricular tachycardia; used topically to treat hemorrhoids; used to treat nasal congestion; a mydriatic agent (dilates pupil at dilator muscle); poor oral absorption
Term
midodrine (ProAmatine)
Definition
a selective alpha-1 agonist prodrug with better oral absorption than sister drug; treats orthostatic hypotensive symptoms; being investigated for possible treatment of urinary incontinence (alpha-1 receptors on urinary sphincters, constricts sphincters keeping urine in bladder)
Term
cocaine
Definition
indirect-acting sympathomimetic that inhibits NE reuptake at sympathetic nerve terminals, leaving NE available to postsynaptic receptors; a good local anesthetic that can exert its own vasoconstriction effects at site of local injection; rarely still used for pain relief & reducing epistaxis while doing intubation of trachea; topical anesthetic for mucous membranes; good absorption through nasal mucosa; very poor oral absorption due to 100% first-pass effect
Term
psuedoephedrine (Sudafed)
Definition
indirect acting sympathomimetic durg that stimulates release of NE from sympathetic nerve endings independent of nerve action potentials but also stimulates adrenergic receptors directly; used to treat nasal & bronchial congestion, promotes nasal & sinus drainage
Term
Oral administration
Definition
preferred form of taking selective alpha-1 & beta-2 direct-acting agonists & indirect-acting drugs except for cocaine; readily absorbed and has a duration of action of several hours
Term
Parenteral Administration
Definition
preferred form of giving cocaine & other direct-acting agonists (Epi, NE, isoproterenol, DA, dobutamine) but their actions only last a few minutes due to rapid inactivating mechanisms
Term
tolerance
Definition
significant problem that occurs during long-term adminstration of any sympathomimetic drug; adrenergic receptors able to down-regulate when exposed too long to too much agonist concentration
Term
"Extensions of Therapeutic Effects"
Definition
side effects of sympathomimetics that involve too much stimulation of the same type of receptors intended to mediate all or part of therapeutic effect: 1) treating cardiac contractility after an acute MI may lead to more O2 deficit, tachycardia, and/or arrhythmia; 2) prevention of hypotension during surgery & ending up with severe hypertension; 3) local dermal tissue necrosis when IV alpha-agonist for systemic therapy accidentally ends up in surrounding superficial tissue
Term
"Lack of Sufficient Receptor Selectivity"
Definition
side effects of sympathomimetics that involves stimulation of receptors other than those that mediate therapeutic effect: 1) attempting to prevent premature labor & ending up with a tachycardia in both mother & fetus; 2) inhaling albuterol and ending up with marked tachyarrhythmias; 3) giving DA to increase renal blood flow & decreasing it instead
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