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62 Cards in this Set
- Front
- Back
Parasympathetic neurons- pre and post ganglionic neuron NT's and receptors
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pre-ganglionic- Ach, nicotinic
post-gangionic- Ach, muscarinic |
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Adrenal gland- NT and receptor
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NT- Ach, nicotinic
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Sympathetic NS- sweat glands- pre and post ganglionic neuron NT's and receptors
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preganglionic- ACh, nicotinic
postganglionic- ACh, muscarinic |
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Sympathetic NS- Skeletal muscle- NT- and receptor
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Ach, nicotinic
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SNS- catecholamine synthesis pathway
(tyrosine -->epinephrine. How?) |
Tyrosine
Dopa Dopamine Norepinephrine Epinephrine |
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What's the function of the alpha 1 adrenoreceptor?
What system? |
think CONTRACTION!
smooth muscle contraction intestinal/bladder sphincter contraction pupilary dilator muscle contraction Sympathetic NS |
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What is the function of the alpha 2 adrenoreceptor?
What system? |
In brain stem. Negative feedback.
Decreased SNS outflow, insulin release decrease sympathetic nervous system outflow and blood pressure Sympathetic NS |
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What is the function of the beta 1 adrenoreceptor? What system?
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increased HR/contractility/renin/lipolysis
Sympathetic NS |
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What is the function of Beta 2 adrenoreceptor?
What system? |
Dilator!
vasodilation/bronchodilation, decreased uterine tone BUT increased HR/contractility/renin/lipolysis/insulin release Sympathetic NS |
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Muscarinic and nicotinic receptors are receptors for what kind of NT?
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actetylcholine
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What is the function of M1 receptors? What type of receptor, what system?
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muscarinic receptors, parasympathetic nervous system
largely for CNS and enteric nervous system! |
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What is the function of M2 receptors? What type of receptor, what system?
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Muscarinic receptors, parasympathetic NS
this one is for parasympathetic innervation of the heart Think decreased heart rate and atrial contractility |
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What is the function of M3 receptors? What type of receptor, what system?
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M3, muscarinic, parasympathetic
increased exocrine gland secretions, like sweat or gastric acid more peristalsis, more blader contractions endothelial vasodilation bronchoconstriction pupillary sphincter muscle contraction ciliary muscle accommodation |
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What is the post ganglionic NT for most sympathetic neurons?
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norepinephrine/noradrenaline
1. sweat is Ach 2. adrenals are Ach because they release epinephrine |
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Pupil constriction is associated with what NS?
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PNS, muscarinic receptors, M3
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What are the Nm and Nn nicotinic receptors associated with, respectively ?
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Nm= neuroMuscular junction
Nn= autoNomic ganglia |
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What's special about nicotinic acetylcholine receptors?
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They are ion channel receptors! Others are not.
Don't use receptors! |
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How does the second messenger cellular signaling work for all receptors besides nicotinic acetylcholine receptors?
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G protein coupled receptors, effector, second messenger (cAMP), cellular response
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What is the function of Gs g-protein coupled receptors?
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Gs= stimulating receptor, increase cAMP, increase pKA
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What is the function of Gi g-protein coupled receptors?
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inhibiting receptor, decreases cAMP, decreases PKA
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What is the function of Gq g protein coupled receptors?
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uses different second messenger, uses protein kinase C, more direct effect, separate pathway that directly increases calcium from ER
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*!This one's a hard one! Give the type of G protein coupled receptor for all the different kinds of receptors!
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Alpha1= q
Alpha2= i Beta1=s Beta2/3=s M1=q m2=i M3=q D1=s D2= i H1=q H2= s V1=q V2=s |
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What's the function of D1 receptors
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relaxes renal smooth muscles
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What's the function of D2 receptors
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modulates NT release, especially in brain
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What's the function of H1 receptors
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increased nasal/bronchial mucus, increased pain/itching
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What's the function of H2 receptors?
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increased gastric acid secretion
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What's the function of V1 receptors?
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increased vascular smooth muscle contraction
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What's the function of V2 receptors?
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increased free water absorption in kidney
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What is the function of Choline Acetyl Transferase?
What is the function of Acetylcholine Esterase? Where are they? |
CAT combines Choline and Acetyl CoA to make Acetyl Choline- CHOLINE SYNTHESIS in cholinergic receptro
ACheE breaks down Acetylcholine into Choline and Acetate- ACETYLCHOLINE BREAKDOWN, in synapse! |
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What is myasthenia gravis?
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antibodies block Ach, receptors, treatment is to try to overcome receptors with more Ach
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Is acetylcholine an agonist or antagonist of muscarinic receptors?
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Agonist!
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What would be a good class of NT agonists/ antagonists to use for
open angle claucoma, urinary retention, gastroparesis, and Sjögren’s*syndrome? |
Muscarinic agonists!
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What is pilocarpine? How does it work? What does it do, anyway?
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M3 receptor agonist,
eye drops for open-angle glaucoma, makes circular muscles contract to get pupils smaller, stimulations ciliary muscles |
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What's going on here?
• Blind*as*a*bat,** • mad*as*a*ha`er,** • red*as*a*beet,** • hot*as*Hades,** • dry*as*a*bone,** • the*bowel*and*bladder*lose* their*tone,** • and*the*heart*runs*alone* |
A muscarinic blockade!
Anticholinergic |
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What class of agonists/antagonists would be good to use for
respiratory (decrease bronchial secretion) asthma parkinson's disease motion sickness diarrhea pesticide poisoning mushroom poisonin sarin gas poisoning? |
Muscarinic antagonists!
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What are acetylcholinesterases, and where might you find them?
Contrast this with pseudocholinesterases! |
"true cholinesterase," found in neurons and RBC's
psuedocholinesterases are in plasma and other tissues |
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How does sarin gas work?
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War agent that is a cholinesterase inhibitor, increases Ach availability, functions as an Ach "agonist"
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myasthenia*gravis*
What class of medications might be good for treating the following conditions? • openeangle*glaucoma* • overdose*reversal* • insec;cide* • poor*GI*mo;lity* • parasympathe;c*failure* • Demen;a*e.g.*donepezil*(Aricept)* |
Cholinesterase inhibitors!
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What is the mechanism of action of sevin/carbaryl?
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it's a pesticide, a slowly reverisble cholinesterase inhibitor
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What would be a good mechanism of emergency treatment of acetylcholinesterase inhibitor poisoning
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Atropine- blocks muscarinic receptor effects
pralidoxime- separates organophosphate from Acetylcholinesterase inhibitor |
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What does Pralidoxime (2-PAM) do in the case of acetylcholinesterase inhibitor poisoning?
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separates organophosphate from AChE inhibitor
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Adrenergic receptors, alpha1 and alpha2. What do they each do?
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alpha 1- on vascular smooth muscle, for vasoconstriction
alpha 2- presynaptic adrenergic nerve terminals, and vascular smooth muscle, they work for inhibition of norepinephrine release and vasoconstriction |
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What do beta 2 adrenergic receptors on vascular smooth muscle do?
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vasodilation!
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What do beta 2 adrenergic receptors on bronchial smooth muscle do?
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bronchodilation!
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What do beta 2 adrenergic receptors on liver cells do?
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stimulate glycogenolysis
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What receptors do these drugs target/stimulate, on what continuum?
• Norepinephrine* • Epinephrine* • Dopamine* • αeMethyldopa* • Clonidine* • Dexmedetomidine* |
they target alpha adrenergic receptors!
Spectrum alpha1>>alpha2 • Norepinephrine* • Epinephrine* • Dopamine* • αeMethyldopa* • Clonidine* • Dexmedetomidine* alpha2>>>alpha1 |
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Effects of α1 Adrenergic Stimulation
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Vasoconstriction
Increase blood pressure pupils dilate (contract iris muscles |
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Effects of α2 Adrenergic Stimulation
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decreased sympathetic outflow
decreased norepinephrine release vasoconstriction |
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Effects of β1- Adrenergic stimulation
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increased heart rate! more AV node contracting!
more renin from kidney, higher BP! |
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Effects of β2- Adrenergic stimulation
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bronchodilation
uterine relaxation relaxation of bladder decreased motility of GI tract increased glucose metabolism of GI tract relaxation of smooth muscle |
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Dopamine is a precursor of ????
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dopamine-->norepinephrine-->epinephrine
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What is epinephrine's precursor?
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dopamine-->norepinephrine-->epinephrine
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What is norepinephrine's precursor?
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dopamine-->norepinephrine-->epinephrine
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Epi/epinephrine/ adrenaline
What receptors does it hit? What does low dose IV target? What does high dose IV target? |
Hits ALL (α1,*α2,*ß1,*ß2) receptors!
Low dose IV - more beta effect High dose IV- more alpha effect, especially alpha 1 (vasoconstriction!) |
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Norepinephrine/NE/noradrenaline
What receptors does it hit? What's the net effect? |
Hits all receptors EXCEPT for BETA 2! (α1,*α2,*ß1)
Net effect ↑HR, ↑ BP |
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Isoproterenol
What receptors does it hit? What's the net effect? When would you use it in treatment? |
Synthetic epinephrine analogue
ONLY hits beta receptors! No alpha receptor effects! Good for patients with low heart rates! Great for patients with a heart block before pacemaker can be implanted, or systolic dysfunction and low HR, like after cardiac surgery |
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Dopamine!
What receptors does it hit? What does low dose IV target? What does medium dose IV target? What does high dose IV target? |
Dopamine is a precursor of norepinephrine!
At low doses it hits dopamine receptors, we call it "renal dose dopamine" hits renal vascular beds, diuretic at medium dose, hits beta 1, norepinephrine release, so then beta 1 and some alpha 1 are activated at high dose- alpha 1! vasoconstriction! great for hypotension and shock! |
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Dobutamine!
This is a synthetic analogue of what? What receptors does it hit? What does low dose IV target? What does medium dose IV target? What does high dose IV target? |
DOPAMINE analog, better for patietns who have heart failure!
stimulates beta1, beta2, and alpha1 (minimally), doesn't affect dopamine receptors |
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Phenylephrine! What does it stimulate? What is it for?
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Phenylephrine is a selective alpha1 agonist!
paradoxically decreases heart rate because beta 1 is not stimulated |
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Let's talk about the baroreflex!
When/how activated? What does it do? |
Input- reduced BP from the carotids and aortic arch
Output- increased heart rate, increased vasoconstriction |
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Let's talk about the bezold-jarisch reflex!
When/how activated? |
Triggered by mechanoreceptors in heart and chemoreceptorsin the inferior wall
it lowers HR and causes vasodilation |
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What is the diving reflex?
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elicited by coldness on forehead, decreases oxygen/energy demand!
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