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581 - Pharmacology I > Exam 3 - ANS & Cholinergic Agonists > Flashcards

Exam 3 - ANS & Cholinergic Agonists Flashcards

1
Q

Two nervous divisions

A
  • PNS: between periphery and CNS

- CNS: brain/spinal cord

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2
Q

CNS components

A
  • Brain: process input/output

- Spinal cord: conduit between body and brain

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3
Q

PNS divisions

A
  • Efferent: carry away from CNS
  • Afferent: carry sensory to CNS
  • Sensory = afferent
  • Motor = efferent
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4
Q

Afferent division

A
  • sensory
  • reflex arcs
  • provide sensory signals for efferent to respond to
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5
Q

Efferent division

A
  • divides into ANS and SNS
  • ANS: autonomic control
  • SNS: conscious control
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6
Q

Somatic Nervous System (SNS)

A
  • voluntary
  • sensory and motor neurons
    • sensory: signals to CNS
    • motor: can only stimulate, not inhibit
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7
Q

Neuromuscular junction

A
  • Ach is neurotransmitter
    • ionotropic: excites skeletal muscles
  • AChE degrades Ach in the junction
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8
Q

ANS vs Endocrine

A
  • ANS: electrical impulses and neurotransmitters

- Endocrine: hormonal signals

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9
Q

ANS divisions

A
  • Enteric: brain of gut
  • Parasympathetic: rest/digest
  • Sympathetic: fight/flight
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10
Q

ANS motor division paths

A 
Preganglionic
- cell body in CNS
Postganglionic:
-cell body in middle ganglion
-terminates at effector organ
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11
Q

Neurotransmitter substances

A
  • BOTH preganglionic: Ach
  • Para post: Ach
  • MOST symp post: NE
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12
Q

Parasympathetic neurons arise from:

A

Cranial and sacral regions

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13
Q

Sympathetic neurons arise from

A

Thoracic and lumbar regions

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14
Q

Fiber lengths

A
  • Symp pre: short
  • Symp post: long
  • Para pre: long
  • Para post: short
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15
Q

Nicotinic receptor

A
  • binds to Ach
  • in between pre and postganglionic fibers
    • aka presynaptic junction
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16
Q

Enteric system

A
  • part of ANS
  • GI / pancreas / gallbladder
  • made up of myenteric and submucosal
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17
Q

Sympathetic nervous system

A
  • continually active: vascular tone
  • adjusts to stressful situations
  • up HR/BP/Blood flow to skeletal and heart
  • dilation of pupils/bronchioles
  • diffuse response: all at same time
  • adrenal medulla releases Epi and NE
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18
Q

Parasympathetic nervous system

A
  • maintain homeostasis
  • drop HR
  • constrict bronchioles/pupils
  • Discrete response: not all at same time
    • SLUDD
    • salivate/lacrimate/urinate/digest/defecate
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19
Q

Location of ganglia in symp vs para

A
  • Symp: near spinal cord

- Para: in or near organ

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20
Q

Distribution of symp vs para

A
  • Symp: wide

- Para: limited

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21
Q

Glands with only sympathetic innervation

A
  • sweat glands
  • adrenal medulla
  • kidney
  • pilomotor muscles
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22
Q

BP is controlled by

A

Sympathetic nervous system

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23
Q

CNS and the ANS

A
  • reflex arcs

- emotions can influence ANS

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24
Q

Signaling between cells

A
  • hormones
  • local mediators (don’t enter blood)
  • neurotransmitters (Ach and NE)
  • all bind to receptors
    • too hydrophilic to pass through
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25
Q

Inotropic

A

Ion channel opens

26
Q

Metabotropic

A

Binding + 2nd messenger system

27
Q

Ach

A 
- cholinergic neurons
used for:
- somatic system
- preganglionic of ANS
- postganglionic of para
28
Q

Cholinergic receptors

A
  • nicotinic

- muscarinic

29
Q

NE and Epi

A
  • adrenergic neurons
    Used in:
  • postganglionic of symp (all except sweat)
30
Q

Adrenergic receptors

A
  • Alpha 1 and 2

- Beta 1 and 2

31
Q

Midbrain and medulla

A
  • important processing part of brain

- integrates ANS/sensory input/endocrine system

32
Q

Primary controlled variable in CV function

A
  • MAP

- autonomic drugs can really affect MAP

33
Q

Effects of slow infusion of NE

A
  • adrenergic
  • vasoconstrictor
  • positive chronotrope (up HR)
  • positive ionotrpe (up contractility)
  • MAP and HR should go way up…..but…
    • increase in SVR and MAP….but decrease in HR
    • due to integration of cerebral cortex (response mech)
    • mech is barroreceptors
    • not true for transplant patients (no innervation of vagus)
34
Q

Autoreceptor

A
  • Neuron responds to chemical it releases
  • inhibitory
  • like NE
  • presynaptic
35
Q

Heteroreceptor

A
  • neuron responds to chemicals released from other neurons that synapse with nerve ending
  • inhibitory
  • some vagal nerve fibers inhibit NE release
  • presynaptic
36
Q

Postsynaptic regulation

A
  • can up or down regulate receptors
  • receptors can be desensitized to previous activity
  • transmitter can act on more than one type of receptor:
    • one may inhibit
    • one may excite
    • means of regulation
37
Q

Ach sites of action

A
  • Preganglionic adrenal medulla
  • Preganglionic symp and parasympth
  • postganglionic para
  • postganglionic sweat glands
  • skeletal muscles of somatic
38
Q

Step 1 of cholinergic neurotransmission

A
  • Choline into neuron via Na cotransport
  • choline + acetyl coenzyme A = Ach
    • Choline acetyltransferase does this
  • uptake of choline is rate limiting step
39
Q

Step 2 of cholinergic neurotransmission

A 
- Ach packed into vesicles via active transport
Vesicles contain:
- Ach
- ATP
- proteoglycan
40
Q

Step 3 of cholinergic neurotransmission

A
  • release of Ach into cleft
  • voltage gated Ca channels open when action potential arrives….Ca moves in…vessicle fuses with membrane….Ach released
41
Q

Step 4 of cholinergic neurotransmission

A
  • Ach binds to target receptors to get response

- Ach also binds to pre-synaptic membrane to prevent over-release

42
Q

Step 5 of cholinergic neurotransmission

A
  • Ach degraded in cleft via AchE

- Ach cut into choline and acetate

43
Q

Step 6 of cholinergic neurotransmission

A
  • Na cotransport brings choline back into neuron
44
Q

Muscarinic receptors

A
  • high affinity for muscarine
  • G protein coupled
    Innervates:
  • smooth muscle
  • cardiac muscle
  • glandular tissue
  • mimics effect of parasympathetic
  • aka parasympathomimetic
45
Q

Muscarinic subtypes

A
  • 5 exist and all 5 on neuron
  • other locations besides neuron:
    • M1: gastric
    • M2: cardiac and smooth muscle
    • M3: bladder and smooth muscle
46
Q

Muscarinic activation

A
  • rest and digest responses
  • constrict at high dose
  • dilate vessels at low dose
47
Q

Nicotinic receptors

A
  • high affinity for nicotine
  • ligand gated ion channels (ionotropic)
  • low [ ]: stimulates receptor
  • high [ ]: inhibits receptor
    Located in:
    -CNS
    -adrenal medulla
    -autonomic ganglia
    -NMJ muscles
48
Q

Direct acting drug

A
  • bind to receptor
49
Q

Indirect acting drug

A
  • Blocks AChE
  • provoke response at ALL cholinoreceptors
  • short acting
50
Q

Nicotine

A
  • direct acting nicotinic agonist

- easily absorbed / lipophilic

51
Q

Carbachol aka Miostat

A
  • direct acting muscarinic AND nicotinic agonist
  • non selective… so can’t be used systemically
    • otherwise too broad of effect
  • produces constriction of eye during surgery
  • reduce pressure in glaucoma or post surgery
52
Q

Bethanechol / Urecholine

A
  • direct acting muscarinic agonist
  • produces urination
  • short action
  • acts on smooth muscle of bladder
53
Q

Pilocarpine / Salagen

A
  • direct acting muscarinic agonist
  • less potent but can penetrate CNS
  • used on eye for miosis and reduce pressure
  • stimulates sweat, tears, saliva
  • research for Alzheimer’s
  • For Sjögren’s syndrome (dry mouth/no tears)
54
Q

Edrophonium / Enlon

A
  • indirect acting reversible cholinergic agonist
  • acts for 10-20 min
  • diagnoses myasthenia gravis
    • chronic neuromuscular disease
    • negative effect on nicotinic receptors ion NMJ
  • not long term treatment
55
Q

Physostigmine

A
  • indirect acting reversible cholinergic agonist
  • acts for 30 min - 2 hours
  • treats glaucoma / anticholinergic overdose
56
Q

Neostigmine

A
  • indirect acting reversible cholinergic agonist
  • like physostigmine but cannot enter CNS
  • greater effect on skeletal
  • antidote for NMJ blockers
  • management of myasthenia gravis
57
Q

Pyridostigmine

A
  • indirect acting reversible cholinergic agonist
  • chronic management for myasthenia gravis
  • lasts for 4-6 hours
58
Q

Organophospahtes

A
  • indirect acting IRREVERSIBLE cholinergic agonist
  • permanently deactivates AchE
    Actions:
  • cholinergic stimulation
  • paralysis
  • convulsions
  • breathing difficulties
  • once used topically for glaucoma
59
Q

Organophosphate poisoning

A

SLUDGE
-salivation/lacrimation/urination/diarrhea/GI upset/emesis
Example:
- Sarin gas:
-eye pain/drooling/SOB/SLUDGE/weakness/headache

60
Q

Organophosphate poison therapy

A

Pralidoxime / 2-PAM

  • reactivate AchE
  • no CNS entering

Atropine

  • competitively binds to muscarinic receptor
  • can get into CNS
  • no direct effect on AchE

581 - Pharmacology I (6 decks)

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