Pharm H&N, lecture 10
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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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