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149 Cards in this Set
- Front
- Back
what is the kinetic effect of a competitive inhibitor? noncompetitive inhibitor?
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competitive inhibitors increase the Km and non competitive's decrease the Vmax
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volume of distribution s 4-8L. Where?
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blood
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volume of distribution is large, i.e. over body weight. Where?
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tissues
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how do you calculate clearance?
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(Rate of drug elimination)/
(plasma drug concentration) = Vd X Ke |
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What happens in Phase I metabolism?
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it is reduced, oxidized or hydrolyzed. Becomes slightly polar and H2O soluble but still active.
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what happens in 2nd pass metabolism?
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conjugation: glucuronidation, acetylation, sulfation making it polar and inactive usually
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what happens with a Gq receptor activation?
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activates phospholipase C to cleave PIP2 to DAG and IP3.
IP3 increases calcium concentration DAG increases Protein Kinase C |
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What happens with GS receptor activation?
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activates adenylyl cyclase which increases ATP-->cAMP which then increases PKA
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What happens with Gi receptor activation?
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it decreases adenylyl cyclase activity
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name the NE release modulatory receptors (on the presynaptic neuron)
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M2, AngII, alpha2
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blocks uptake of choline
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hemicholinium
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blocks Ach transport into the vesicle
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vesamicol
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blocks Ach release
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botulinum
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blocks Tyrosine--> DOPA
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metyrosine
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blocks DA from going into the vesicle
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Reserpine
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blocks NE release at the exocytosis stage
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guanethidine
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actions of amphetamines
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increases NE release and decreases NE reuptake
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block NE reuptake
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cocaine, amphetamines, TCA's
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name the cholinomimetics that are direct agonists?
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bethanechol, carbachol, Pilocarpine, methacholine
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name the cholinomimetics that are indirect agonists
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neostigmine, pyridostigmine, physostigmine, edrophonium
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neostigmine - class?
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cholinomimetic indirect agonist
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pyridostigmine - class?
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cholinomimetic indirect agonist
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physostigmine - class?
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cholinomimetic indirect agonist
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edrophonium class?
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cholinomimetic indirect agonist
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pilocarpine class?
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cholinomimetic - direct agonist
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methacholine class?
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cholinomimetic - direct agonist
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Bethanechol class?
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cholinomimetic - direct agonist
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carbachol class?
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cholinomimetic - direct agonist
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What happens if you take to many anti-Ach esterase?
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DUMBBELSS:
Diarrhea urination miosis bronchospasm bradycardia excitement of skel. muscle/CNS lacrimation sweating salivation |
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Treatment for anti-Ach esterase OD
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Atropine and Dialidoxamine
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Atropine - class?
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muscarinic antagonist
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benztropine class?
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muscarinic antagonist
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Scopolamine class?
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muscarinic antagonist
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Ipratropium class?
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muscarinic antagonist
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used to produce mydriasis and cyclopegia on eyes?
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atropine
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used for CNS symptoms of Parkinson Disease
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benztropine
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muscarinic antagonist used for motion sickness
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scopolamine
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muscarinic antagonist used for Asthma and COPD
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ipratropium
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increased temperature, increased pulse, dry mouth, flushed skin, disorientation.
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Atropine
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What's hexamethonium?
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nicotinic antagonist
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whats hexamethonium used for?
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ganglionic blocker to prevent vagal reflexes in experiments
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receptor selectivity of epinephrine?
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same for all alphas and beta's unless low dose then beta 1's
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receptor selectivity of Norepinephrine?
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alpha's>Beta one.
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receptor selectivity of Isoproterenol?
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ONLY Beta's
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receptor selectivity of Dopamine
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D1=D2 > beta> alpha
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receptor selectivity of phenylephrine?
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alpha1>alpha2
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receptor selectivity of albuterol and salmeterol?
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selective beta 2 agonists
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use of epinephrine?
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anaphylaxis, glaucoma, asthma, hypotension
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use of NE
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hypotension but it decreases renal perfusion
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use of isoproterenol
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used RARELY for AV block
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use of dopamine
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shock and heart failure
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use of dobutamine
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shock, heart failure, cardiac stress testing
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use of phenylephrine
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pupillary dilation, vasoconstriction, nasal decongestion
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use of albuterol and salmeterol?
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albuterol for acute asthma and salmeterol for long term
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MOA of clonidine?
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centrally acting alpha 2 agonist that decreases central adrenergic outflow
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use of clonidine?
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HTN, esp. w/ renal disease
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difference between phenoxybenzamine and pentolamine.
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phenoxybenzamine is irreversible and pentolamine is reversible
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use of phenoxybenzamine and phentolamine?
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alpha blockage in pheochromocytoma
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selective alpha one blockers?
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-zosin's
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Prazosin MOA
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alpha one blocker
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use of Prazosin
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alpha one blocker for HTN, urinary retention in BPH
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mirtazapine MOA
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alpha 2 blocker
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selective alpha 2 blocker?
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mirtazapine
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how do beta blockers decrease HTN
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decrease CO, decrease renin secretion
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how do beta blockers decrease renin secretion
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by blocking JGA cell beta receptors
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how do beta blockers help with SVTwhich ones?
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decrease AV conduction velocity
propranolol and esmolol |
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adverse CV effects of beta blockers?
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bradycardia, AV block, CHF
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non selective beta blockers?
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propranolol and labetalol
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beta one selective antagonists?
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Esmolol, Atenolol, Metoprolol
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nonselective alpha and beta antagonists?
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carvedilol and labetalol
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where are t cells found in the lymph node
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paracortex
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what goes on in the follicle of a lymph node?
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primary follicles are dense and inactive/dormant. the secondary follicles have pale centers and are active
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where are t cells found in the spleen
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periarterial lymphatic sheath and the red pulp
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what happens in splenic dysfunction and why?
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increased susceptibility to encapsulated organisms because their is decreased IgM leading to decreased complement activation and C3b opsonization
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what is going on in the thymus?
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in the cortex it is dense with immature T cells. in the medulla it is pale with mature T cells.
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where do positive and negative selection take place?
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corticomedullary junction
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what is positive selection of T cells
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when MHC's are selected for
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what is negative selection of T cells
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making sure they aren't reactive to self antigens.
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what is innate immunity? who are the players?
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receptors recognize pathogens fast and specific.
PMN's, macrophages, dendritic cells, NK cells, complement |
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What is adaptive immunity? who are the players?
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receptors recognize pathogens and under go V(D)J recombination during development.
T cells, B cells, circulating antibody |
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what cytokine is responsible for Th1 proliferation
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IL12
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cytokine for Th2 proliferation?
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IL4
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IL 10 inhibits?
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Th1
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IFN gamma inhibits?
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Th2
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what cytokines do Th2's make?
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IL4, IL5, IL10
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how are viral antigens presented
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they are loaded onto MHC I in rER and presented to CD8 cells
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role of NK cells
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if absence or down regulation of MHC I they kill - usually tumor cells or virally infected cells
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cytokines that enhance NK cell activity?
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IL12, IFN beta, IFN alpha
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explain the steps of Th cell activation
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APC phagocytoses foreign body
presented and recognized on MHCII Costimulatory signal from B7 (on APC) interaction with CD28 (onT helper) |
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explain steps of Tc cell activation
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MHC I presenation and recognition by Tc's
IL2 from T helper cell activates the Tc cell to kill the virus infected cell |
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what is used for B cell class switching
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IL4, IL5, IL6 all from Th2 cell
CD40 receptor activation by CD40 ligand on helper t cell |
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when talking about immunoglobulins what is the difference between isotype and idiotype
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isotype refers to the Ig class like IgG or IgA whereas idiotype refers to the antigen it recognizes
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what is one property of IgM that makes it well suited for the immediate response
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it can be a pentamer shape which allows it to bind to 5 different antigens and keep them at bay until humoral response can evolve
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ANA associated w/
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SLE
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SLE specific autoantibodies
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anti-smith and anti-dsDNA
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antihistones
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drug induced lupus
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anti-IgG
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aka Rheumatoid Factor
Rheumatoid arthritis |
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anticentromere
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scleroderma (CREST)
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anti-Scl-70
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(anti-DNA topoisomerase I)
Scleroderma (diffuse) |
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antimitochondrial
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primary biliary cirrhosis
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antigliadin
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celiac
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anti basement membrane
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goodpasutre's
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anti desmoglein
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pemphigus vulgaris
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antimicrosomal
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hashimoto's
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anti-jo-1
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polymyositis or dermatomyostits
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Anti-SS-A
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anti-Ro
Sjogrens |
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Anti-SS-B
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anti-la
Sjogren's |
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anti smooth muscle
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autoimmune hepatitis
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anti-glutamate decarboxylase
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DM I
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c-ANCA
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Wegener's granulomatosis
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p-ANCA
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vasculitides besides Wegener's
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recurrent bacterial infections after 6 months
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Bruton's agammaglobulinemia - decreased IgG due to opsonization defect
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Bruton's agammaglobulinemia defect
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X linked Recessive - Defective BTK whic his a tyrosine kinase gene so B cell differentiation and maturation are blocked
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severe pyogenic infections early in life?
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Hyper IgM Syndrome
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Defect of Hyper IgM syndrome
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Defective CD40L on helper t cells = inaibility to class switch
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how is the vancomycin related 'red man syndrome' different from HSN type I?
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it involves histamine release w/o production of IgE antibodies.
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nonlinear mesangial deposits on immunofluorescence?
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IgA nephropathy
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RBC's, casts in urine, decreased complement, lumpy bumpy electron dense deposits in glomerulus
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Post-strep glomerulonephritis
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subendothelial DNA-anti-DNA ICs
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Diffuse proliferative glomerulonephritis due to SLE or MPGN
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split basement membrane
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Alport's syndrome
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nerve disorders, ocular disorders, deafness, nephritic syndrome
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Alport's Syndrome
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spike and dome on EM
diffuse capillary and GBM thickening on LM |
membranous glomerulonephritis
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foot process effacement only
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minimal change disease
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mesangial expansion, GBM thickening, nodular glomerulosclerosis
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diabetic glomerulopathy
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tram track appearance w/ subendothelial IC's.
Type II w/ dense deposits? |
membranoproliferative glomerulonephritis
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treatment of multiple sclerosis
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IFN beta
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IFN beta made by:
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connective tissue fibroblasts
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increased protein (IgG) in CSF, oligoclonal bands, periventricular plaques
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Multiple sclerosis
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periventricular plaques in MS are from what?
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areas of oligodendrocyte loss and reactive gliosis
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what antibodies bind antigen?
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IgG and IgM
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what holds light chains and heavy chains together in an antibody
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disulfide bonds
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deficient IgA makes someone more susceptible to what?
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infections at mucosal surfaces
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IgM can bind how many antigens in circulation? on B lymphocytes?
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pentamer in circulation - each of which can bind two antigens = 10
monomer on B cell so two |
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what is the most important cytokine mediator in septic shock?
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tumor necrosis factor
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TNF is secreted from what?
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macrophages to cuase vascular leakange --> fluid extravasation and hypotension
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recurrent viral infections are a sign of ? why?
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T lymphocyte dysfunction
play a particularly important role in the response to viral infections. |
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important cytokine for t lymphocyte growth and differentiation?
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IL2
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IL2 from where
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helper T lymphocytes secreted
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function of IFN gamma
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stimulates macrophages
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plays a role in dampening the immune response
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TGF beta
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how does TGF beta dampen immune response in RA?
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inhibits T lymphocyte activation and proliferation, inhibits TNF secretion
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two primary opsonins fro defense against bacteria?
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C3b and IgG
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what is mostly responsible for defense against Gram negative bacteria?
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Membrane attack complex made of C5-C8 guide the polymerization of C9's to form pores in the membrane allowing ions and small molecules to enter cell and allow it to lyse
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recurrent pyogenic infections, eczema and thrombocytopenia?
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Wiskott Aldrich Syndrome w/ inability to mount IgM response
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cerebellar ataxia, spider angiomas - disease? what's missing?
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Ataxia-telengiectasia - also IgA deficiency
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recurrent streptococcal and staphylococcal infections. possible partial albinism?
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chedak higashi.
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chediak higashi defect?
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defective phagolysosome formation.
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why is there partial albinism in w/ chediak higashi?
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melanosomes are derivatives of lysosomes.
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associated risks for Goodpasure's syndrome?
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cigarette smoking and expsure to hydrocarbon solvents
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