lecture 6 Flashcards

1
Q

Autonomic Nervous System

A

involuntary: sympathetic/thoracolumbar outflow and parasympathetic/craniosacral outflow

two neuron pathway?

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2
Q

acetylcholine works on ________ receptors while norepinephrine mainly on ______

A

nicotinic; adrenergic

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3
Q

sympathetic releases _______. para releases _______

A

norepinephrine; acetylcholine

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4
Q

muscarinic receptors in the heart

A

M2 - coupled to G alpha i (inhibits adenylyl cyclase and decreases cAMP)

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5
Q

muscarinic receptors in the lungs

A

M3 - coupled to Gq (activates phospholipase C - calcium release thus contraction)

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6
Q

muscarinic stimulation of the parasympathetic nervous system in the lungs promotes _________

A

bronchoconstriction

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7
Q

muscarinic receptors (M1-M5) and what they do

A

GPCRs, M1, M3, and M5 all activate PLC (contraction of smooth muscle), M2 (ACh) is in the heart and slows conduction, decreasing contraction force of the heart

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8
Q

four adrenergic receptors

A

alpha1 (blood vessels), beta 1 (in heart), beta 2(in lungs, one in each), alpha 2 are presynaptic

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9
Q

cocaine and ecstasy will increase levels of norepinephrine how?

A

blocking the transporters, so it builds up in the vesicle

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10
Q

amphetamine-adderall for ADHD, or methyphenidate (ritalin) mechanism

A

tyramine displaces NE.

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11
Q

monoamine oxidase (MOAs) break down ________ and examples

A

tyramine, NE and dopamine
MAO A - phenelzine
MAO B - selegiline for parkinson’s

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12
Q

too much tyramine can cause

(wine and cheese effect)

A

hypertension

if you dont have enough MAOs to break it down you can die

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13
Q

actions of cocaine and amphetamines

A

c- blocks the DA (dopa) transporter, so DA that has been released stays out a lot longer

amph- reverses the DA transporter, so more DA is released and stays out longer, also blocks degradation of DA

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14
Q

amphetamines mechanism of action

A

normal dopaminergic synapse. amphetamine enters via DAT as a substrate. enters vesicles via VMAT1 to displace DA and inhibits MAO. DA concentration rises in the cytosol. DA is expelled into synapse via reverse transport.

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15
Q

“pleasure center” is the ____ in the brain

A

VTA (ventral tegmental area)

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16
Q

reward and mesolimbic dopamine

A

activation of reward pathway leads to increased dopamine in Nucleus Accumbens

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17
Q

DA usually released in a ______ way, and acts on __ receptors. Increasing activity (something important or a drug like coke), would release DA in a _____ way, and activates __ receptors.

A

tonic, D2; phasic, D1

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18
Q

all autonomic receptors are coupled to _____________

A

GTP binding proteins

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19
Q

alpha 1 (G-alpha-q)

A

smooth muscle contraction. activate phospholipase C –> intracellular calcium

cocaine eyes

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20
Q

alpha 2

A

brain.
inhibit adenylyl cyclase

21
Q

beta 1 (NE) (G alpha s)

A

increase heart rate, conduction velocity, and contractility.
SA, AV node and HIS-purkinje cells.
stimulate adenylyl cyclase

also found in the kidney for renin.

22
Q

beta 2 (G alpha s)

A

lung relaxation.
stimulate adenylyl cyclase.
cAMP –> PKA –> inactivates MLCK and decreases affinity for calcium/CaM

23
Q

alpha 1 receptors could increase blood pressure. why?

A

they release calcium, causing contraction and thus constriction of blood vessels

24
Q

presynaptic alpha2 receptors decrease release of ________

A

norepinephrine, bc the beta gamma subunit binds to the calcium channel inhibiting it

25
clonidine
produces bradycardia and hypotension to decrease BP
26
miosis (para)
pupillary constricion
27
mydriasis (sympathetic)
pupil dilation
28
sympathomimetics and examples
imitate the effects of the sympathetic nervous system, activating alpha or beta receptors or both (alpha-1) decongestants like phenylephrine (Sudafed) induce vasoconstriction of blood vessels in the nose (alpha-1) local anesthetics contain epinephrine to increase duration by causing vasoconstriction at site of injection (beta-2) bronchospasm and cardiac arrest- epinephrine (beta 2 and alpha 1) anaphylaxis - epinephrine relaxes bronchioles, increases BP cardiovascular collapse (alpha 1 and beta 1) - norepinephrine
29
anti asthmatic drugs include (broad)
bronchodilators, anti-inflammatory agents, leukotriene modifiers e.g. Spiriva
30
lipocortin-1
31
LTC4, LTD4, LTE4 constitute
slow reaching substance of anaphylaxis
32
leukotrine antagonist drugs
33
corticosteroids
help decrease inflammation by decreasing transcription of cytokines and increase lipocortin which inhibits PLA2 and thus the downstream production of inflammatory stuff
34
adrenergic agonists for asthma
albuterol! beta 2 receptors bronchodilator long acting salmeterol
35
advair
fluticasone and salmeterol steroid + b2 agonist longer acting
36
atrovent
ipatropium bromide inhibit muscarnic receptors anti-cholinergic
37
beta blockers
block beta-1 receptors to decrease the rate at which the heart works antihypertensive ischemic heart disease (chronic angina, reduces cardiac workload) arrythmias (vfib) e.g. metoprolol, atenolol
38
beta blocker side effects
bad dreams, cold exremities, decreased exercise tolerance, fatigue depression and impotence, heart failure
39
alpha sympatholytics (alpha blockers)
bind to alpha receptors to block the effects of endogenous agonists e.g. prazosin (minipress) for hypertension
40
targets of drugs with muscarinic action
exocrine glands, smooth muscles, cardiac tissue
41
cholinomimetics
mimic ACh receptor agonists direct acting: choline esters, alkaloids-plants; complex structure e.g. bethanechol (choline esters), pilocarpine (alkaloid) indirect acting: cholinesterase inhibitors, carbamates, phosphates
42
natural alkaloids
muscarine: poision in some mushrooms that causes hypotension, sweating, emesis, bradycardia, miosis, etc. pilocarpine (salagen): pure mucarinic agent in low doses used for dryness of mouth and constriction of pupils for glaucoma
43
clinical use of direct acting muscarinic agonists
glaucoma and gastric atony/urinary retention
44
indirect acting parasympathomimetics (acetylcholinesterase inhibitors)
45
toxic reactions
46
treatment of toxicity
47
anticholinergics/parasympatholytics
atropine
48
atropine actions
depresses salivation and bronchial secretions, bronchodilation, relax GI,
49
neuromuscular blocking drugs
non-depol: tubocurarine blocks NMJ depol: succinylcholine activate nicotinic acetylcholine receptors for muscle relaxtion