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Pharm H&N, lecture 10

Quiz yourself by thinking what should be in each of the black spaces below before clicking on it to display the answer.
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Question
Answer
show 60% water, 40% ICF, 20% ECF  
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show anti histamine Histamine type 1 receptor inverse agonist  
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Cimetidine   show
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show increase urine flow  
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show decrease BP, anti-hypertensive block Ca channels  
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sildenafil   show
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cholinergic nicotinic receptor type   show
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-caine   show
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show anti-anxiety drugs open Cl channels  
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tolbutamide -amide   show
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show nitric oxide causes vasodilation via opening K channels  
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show Gs increases cAMP  
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alpha 2 mechanism   show
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alpha 1 mechanism   show
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show tyrosine kinase recruits glucose transporters to cell membrane from intracellular reserves  
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Aspirin   show
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show competitive inhibitor of COX (cyclooxygenase)  
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show ibuprofen, acetaminophen  
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Caffeine   show
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Theophylline   show
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PDE inhibitors   show
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sildenafil   show
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enalapril -april   show
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ciproflaxacin   show
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fluoxetine   show
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chloroquine   show
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show replace a dysfunctional gene, create continuous production of deficient protein, target specific cells, maximize compliance  
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Gene therapy vectors   show
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show -capable of integrating in both dividing and nondividing cells -can insert a large piece of DNA -Not integrative, so effect is transient  
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show Full agonist only binds to active receptors  
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show Prevents receptor activation, reduces max response  
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Inverse agonist vs antagonist   show
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show LD50/ ED50 Bigger is better  
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show "The Queen Likes Digging Low" Low therapeutic index Theophylin (asthma), Quinine (anti-arrhythmic), Lithium (bipolar), Digoxin (cardiac)  
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succinylcholine   show
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show non-depolarizing NMJ blocker, half life 1 hours, patients come off by achetylcoline esterase inhibitor and muscarinic antagonist  
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show non-depolarizing NMJ blocker, half life 1 hours, patients come off by achetylcoline esterase inhibitor and muscarinic antagonist  
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show competitive inhibitor of ach at muscarinic receptors, blocks M2 muscarinic receptors; increase HR by blocking vagal affect on SA node (dec HR at low levels), decrease secretion, decrease mictutition, decrease accomodation; can enter CNS; can treat nerve  
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show inc HR, inc CV, mydriasis, cycloplegia (inability to focus), dec GI motility, dec secretions, urinary retention; include atropine, scopolamine, glycopyrollate, scopolamine; ipratroprium for bronchiodilation in COPD  
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Depolarizing NMJ antagonist   show
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Non-depolarizing NMJ antagonist   show
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bring patient off *d-tubocurarine* and *gallamine*   show
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show autosomal dominant disorders with rapid increase temp and serum potassium in response to inhalation anesthesics or muscle relaxants (succinylholine) increase in Ca, muscle contraction; treat with ice & dantrolene to block Ca from SR  
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PAM   show
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Sarin   show
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Cholinergic agonist/ cholinomimetics   show
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show inc HR, inc CV, mydriasis, cycloplegia (inability to focus), decrease GI motility, dec secretions, urinary retention; include atropine, scopolamine, glycopyrollate to dec secretions; scopolamine for motion sickness; ipratropprium for bronchiodilation in C  
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show block constriction (dilation) via blocking muscarinic receptor on central airways, muscarinic receptor constant rate through aging, e.g. ipratropium  
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show bronchodilation via activating beta 2 receptors in small peripheral airways, incrases adenyl cyclase, incraeses cAMP to promote relaxation, beta 2 receptors in airways reduce with age, e.g. albuterol  
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Xanthines   show
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show adrenergic agonist on beta 2 receptors, bronchodilation for asthma and COPD with side effect of chest pain  
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Ipratroprium   show
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Theophylline   show
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show patches, treats motion sickness  
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show 1) treat symptoms 2) provide cholinesterase inhibitor eg psysotigmine, in small doses 3) blankets for cold and diazepam for seizure control  
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Ganglionic blockers   show
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show drugs that bind competitively to nicotinic receptor, classified as de-polarizing or non-depolarizing  
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show binds Nm receptor, opens channel in end plate, depolarizes endplate, and blocks receptor so desensitized to effect of ach, produces skeletal muscle transient fasciculations followed by flaccid paralysis; eg succinylcholine  
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Non-depolarizing NMJ antagonist   show
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Malignant hyperthermia   show
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show treats malignant hypothermia  
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show prevents release of acetylcholine in synaptic terminal by cleaving SNAP 25 to  
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show competitive inhibitor of ach at M2 muscarinic receptors; increase HR by blocking vagal affect on SA node (dec HR at low levels), dec secretion, decrease mictutition, decrease accomodation; can enter CNS; treat nerve gas (excess Ach)  
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show b1 (b2) Increased heart rate & M2 Decreased heart rate  
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show b1 (b2) Increased contractility & M2 Decreased contractility  
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ANS on AV node   show
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ANS on His-Purkinje   show
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ANS on Ventricles   show
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show blood supply increases, decreases, or same due to a1/b2 receptor rato & local demand)  
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show a1 Constriction, b2 dilation* ; No PS innervation  
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ANS on Veins   show
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show pupil dilation mydriasis via sympathetic for far vision; Constriction & accommodation via parasympathetic for near vision, reading  
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ANS on Radial muscle-iris   show
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show no sympathetic innervation, PS stimulation causes Contraction / miosis M3  
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show b2 relaxation (far vision), Contraction (reading) M3  
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show b2 relaxes – bronchodilation, M3 bronchoconstriction  
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show decreases –a2 inhibition, b2 relaxation, PS increases motility, increases secretions  
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ANS on GI Sphincters   show
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ANS on GI Secretions   show
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ANS effect on Bladder   show
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ANS on bladder Detrusor muscle   show
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sympathetic effect on Pancreas   show
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ANS effect on b-cells producing insulin in pancraes   show
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ANS effect on a-cells producing glucagon in pancreas   show
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ANS effect on Liver   show
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ANS effect on Gluconeogenesis   show
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show sympathetic on b2 – increase glycogenolysis, PS increase glycogen synthesis  
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show sympathetic a1 inactivation of insulin receptors by dephosphorylation to increase blood glucose, PS insulin receptors activated  
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show sympathetic stimuation causes breakdown of triglycerides, supply fatty acids to rest of the body  
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show symp on b1, b3 lipolysis, PS stimulates fat synthesis, storage  
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show b1 – rennin secretion goes up  
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show b1 – ADH secretion goes up  
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Where are MOST of the beta 1 receptors located in our body   show
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show Temperature control & Sweat glands by acetylcholine  
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What is the effect of an alpha 2 agonist on blood glucose levels   show
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show decrease  
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What is effect of prednisone on a. Blood pressure, b. Blood glucose levels, c. Blood lipid levels, d. Weight e. Blood CRH levels f. Blood Cortisol levels g. Blood ACTH levels h. Ability to fight infections i. Fluid retention   show
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show homeostasis  
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show _two  
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All preganglionic neurons release _______, which binds to ____ receptors on the postganglionic neurons   show
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show catabolic, thoarcolumbar, many  
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show anabolic, craniosacral, few  
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Within the parasympathetic system, the postganglionic fibers release __, which interacts with ____ receptors   show
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show norepinephrine, α or β  
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show _norepinephrine___  
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show _epinephrine__  
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Acetylcholine is synthesized from ___ and ____. It's action is terminated by _____ (enzyme name)   show
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What is the rate-limiting step in the synthesis of epinephrine   show
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show reuptake  
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show parasympathetic  
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show blood vessels (symp only, alpha 1 constrict and beta 2 relaxation), skin (symp only, beta 1?), radial/ dilator muscle (symp only, alpha 1 mydriasis or dilation), and sphincter/ constrictor muscle (PS only, M3 miosis or pupil constriction)  
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In the eye, the sympathetic nervous system innervates the __________ muscle, which causes _____________, or ___________. The parasympathetic nervous system innervates the ____________ muscle, which causes ________________, or __________   show
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show heart  
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show constriction of blood vessels, constriction of GI sphincters, constriction of urinary sphincter, inactivation of insulin receptor in liver causing blood glucose increase,  
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Activation of ß2 receptors causes _____________ of smooth muscle   show
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show beta 2 selective stimulant  
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Why do drugs that increase acetylcholine transmission, such as anticholinesterases, promote sympathetic as well as parasympathetic responses   show
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show blocks cholinergic  
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Adrenomimmetics   show
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Direct adrenomimmectis   show
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show cause release of NE, eg tyramine, ephedrine, amphetamin  
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Cathecolamine reuptake inhibitors   show
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show increase catecholamine levels by inhibiting breakdown  
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Adrenergic receptors   show
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Norepinephrine   show
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Epinephrine   show
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show primarily beta2 to dilate, at high levels of epinephrine, alpha1 to constrict blood vessels  
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show to achieve vasoconstriction through alpha1 receptors to keep anesthetic local  
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show acts on adrenergic beta but not alpha, large group on amine nitrogen increases affinity for beta receptor, same effects as epinephrine except not dilate pupils, not constrict blood vessels to skin, not contract GI & bladder sphincters  
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show epinephrine has strongest effect on glucose level because it acts on alpha1&2, beta 2 of pancreas to decrease insulin and increase glucagon, while norepinephrine doesnt act on beta2 and isoproterenol doesn't acts on alpha  
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Dopamine   show
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show alpha1 predominates on veins, so epinephrine and norepinephrine constrict veins to increase BP, alpha1 & beta2 together in capillaries  
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show dose dependent; at low dose, activates beta2 for dilation, and high dose, activates alpha1 for constriction  
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show increase to heart, lungs and skeletal muscles, brain stays same, decrease to skin, GI, and genitals  
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Norepinephrine effect on heart   show
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Epinephrine effect on heart   show
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isoproterenol effect on heart   show
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presynaptic autoreceptors   show
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