Autonomic nervous system drugs Flashcards

1
Q

Sympathetic neuro-transmitters

A

Epinephrine (epi), norepinephrine (NE), dopamine

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2
Q

Parasympathetic neuro-transmitter

A

Acetylcholine (ACh)

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3
Q

Sympathetic receptors

A

Alpha-1, (alpha-2), beta-1, beta-2 adrenergic receptors

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4
Q

parasympathetic receptors

A

Cholinergic (nicotinic and muscarinic receptors)

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5
Q

Sympathetic physiological responses I

A

Vasoconstriction of vessel in skin and GIT→ moves blood to core organs
Increased BP
Increased HR and contractility
Increased RR
Bronchodilation

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6
Q

Parasympathetic physiological responses I

A

Relative vasodilation of peripheral blood vessels→ moves blood to skin +GI tract
Resting BP,HR, RR
(Bronchoconstriction)

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7
Q

Sympathetic Physiological responses II

A

Mydriasis (dilated pupils)
Decreased saliva, GI fluids, GI motility, urination

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8
Q

Parasympathetic Physiological responses II

A

Miosis (constricted pupils)
Increased saliva, GI fluids, GI motility, urination

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9
Q

3 mechanisms can occur for ANS drugs

A

Mimic neurotransmitters (and turn up a response; directly or indirectly)
Can increase the amount of naturally occurring neurotransmitter (enhance the natural response)
Some drugs bind to and block the receptors (turn off the response)

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10
Q

Drugs can be categorized by

A

Drugs act on either the SNS or PNS nervous system; never both
Also categorized as
Parasympathomimetics
Parasympatholytics
Sympathomimetics
Sympatholytic

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11
Q

4 classes of ANS drugs

A

Cholinergics
Anticholinergics
Adrenergics
Adrenergic blockers

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12
Q

Physiological effect of cholinergics

A

Turn up the PS response

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13
Q

physiological effects of anticholinergics

A

Turn down the PS response

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14
Q

Physiological effects of adrenergics

A

Turn up the sympathetic response

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15
Q

Physiological effects of adrenergic blockers

A

Turn down the sympathetic response

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16
Q

Cholinergic drugs do what

A

Drugs turn up the PS response by either
Mimic SCh (direct-acting)
Increase endogenous levels of ACh (indirect acting)
Action is increase binding to and turning on of cholinergic receptors

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17
Q

Overall effect of cholinergic drugs

A

Overall effect is to increase parasympathetic activity
Resting RR,HR,BP; decreased contractility, bronchoconstriction
Increased GI motility and GI secretions
Urination
Miosis, tearing

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18
Q

Ex of anticholinergics

A

Atropine
Glycopyrrolate

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19
Q

Ex of cholinergics

A

Organophosphates

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20
Q

Ex of adrenergics

A

Epinephrine sulphate
Epinephrine
Norepinephrine
Dobutamine

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21
Q

Ex of adrenergic blockers

A

Beta-blockers

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22
Q

Review of how the PSN response normally works

A

Electric signal moves down axon and causes ACh to be activated
ACh released in synapse
ACh binds to cholinergic receptors→ turns on cell→ PS response
The response is trend off when ACh-esterase (enzyme located in the synapse) breaks down ACh

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23
Q

Direct-acting cholinergic drugs

A

These drugs act like acetylcholine
They bind to and turn on cholinergic receptors
The drug eventually degrades or diffuses away from synapse

24
Q

Ex of Direct-acting cholinergic drugs

A

Bethanechol- drug used to stimulate urination
Cisapride- drug used to stimulate GI motility in cats with constipation

25
Indirect acting cholinergic drugs stop what
These drugs block the activity of the acetylcholinesterase enzyme This enzyme is normally located in the synaptic cleft and breaks down the neurotransmitter→ limits the PS response from going on too long or too much Blocking this enzyme causes the naturally occurring ACh to stay around for longer
26
Ex of Indirect acting cholinergic drugs
organophosphates
27
How the indirect acting cholinergic work
Work by blocking ACh-esterase and preventing ACh breakdown Result is ACh stays around longer (same as if increasing amounts of ACh that is present) Example: organophosphates
28
Organophosphates are
Class of incesticide Indirect-acting cholinergic drug If overdose or adverse reaction, can cause same effects in the host Most common form of toxicity world-wide
29
Organophosphates mechanism of action
(on the insect) Triggers activation of nicotinic receptors at neuromuscular junctions→ muscle spasms (skeletal muscle) leading to rigid paralysis Also increases PS tone→ severe bronchoconstriction
30
Anticholinergics bind to and block what
Drugs bind to and block cholinergic receptors
31
Anticholinergic drugs are
Commonly part of emergency drug kit Examples: atropine, glycopyrrolate Drug binds to cholinergic receptors and block ACh from binding Because the PNS system cannot be turned on the SNS dominates
32
effect of anticholinergics
Effect is PS responses cannot be tuned on; result is sympathetic response dominate Increased HR, contractility Peripheral vasoconstriction (increases BP) Bronchodilation Decreased GI motility, decreased GI secretions Urine retention Decreased secretions (tears, saliva, bronchosecretions)
33
Atropine is
Anticholinergic drug Binds to and blocks ACh receptors→ blocks PNS response
34
Physiological effects of atropine
Increased HR Blocks peripheral vasodilation (skin and GI) which results in increased BP and moves blood to support heart, lungs, kidney and brain Bronchodilation Mydriasis, decrease secretions
35
Clinical use of atropine
CPR drug (give IV) Given SQ as aprt of premedication or intra-op Supports heart rate and blood pressure Decreases airways secretions so easier to intubate Treating organophosphate toxicity Ophthalmic drops dilate pupils, decreases tearing
36
Glycopyrrolate is
Synthetic anticholinergic Mechanism of action is similar to atropine, but longer acting and less pronounced effects
37
Glycopyrrolate is used for
Used as part of pre-med or intra-op Supports HR and BP Decrease salivation and bronchial sections to easier to intubate Decreases gastric fluids so lessens reflux
38
How adrenergic drugs work
These drugs turn up the sympathetic response Works by binding to and turning on the adrenergic receptors Effect depends on which receptors are targeted
39
What does alpha-1 receptor do
blood vessels in skin and GIT; when activated, causes vasoconstriction of these vessels→ shifts blood flow so there is increased BP to heart/lung/brain
40
What does alpha-2 receptor do
Alpha-2: sedatives discussed in anesthesiology
41
What does beta-1 receptor do
Beta-1: heart muscle; increases HR and stroke volume
42
What does beta-2 receptor do
Beta-2: bronchioles; causes dilation to increase airflow and increases RR
43
2 classes of adrenergic drugs and what they do
Non-selective adrenergics -Bind to more than one adrenergic receptor→ broader effects -Ex. epinephrine, ephedrine Selective adrenergics -Only bind to one receptor→ more limited effects -Ex. beta-blockers
44
Epinephrine is
Non-selective adrenergic agonist Exact same as endogenous neurotransmitters Epinephrine has slight increased beta-1 activity compared to its activity on the other adrenergic receptors
45
Effect of epinephrine
Main effect: increased HR Also: causes peripheral vasoconstriction, increases airway diameter, pupil dilation
46
Clinical indications for epinephrine
CPR drug Cardiac resuscitation High dose IV, intratracheal every 2-5 min Anaphylaxis Low dose IV, SQ or IM depending in how emergent and what symptoms of anaphylaxis are Too rapid IV can cause arrhythmias
47
Ephedrine sulfate works on
Indirectly turns on sympathetic receptors By increasing amounts of norepinephrine in the body Longer lasting and less pronounced effects than epinephrine
48
Clinical indications of ephedrine sulfate
Use to produce bronchodilation (beta-2) Use to treat nasal congestion (alpha-1) Use for hypotension during anesthesia (alpha-1)
49
Adrenergic blockers are and work for
Drugs that bind to and block adrenergic receptors from being turned on Block sympathetic activation; parasympathetic responses dominate as a result Adrenergic blockers can be nonselective or selective
50
Effects of adrenergic blockers
Decreed HR, contractility, RR, vasodilation Bronshoconstriciton, increased bronchial secretions Increased GI motility and GI secretions Urination Miosis, tearing
51
Side effects of the ANS drugs occur if
Drug binds receptors in non-targeted tissues Ex. want to see its effect in the bladder, but drug also goes to the heart Drug binds more than one type of receptor Cholinergic drugs can also bind to nicotinic receptors at neuromuscular junction Selective adrenergic drugs may also bind unintentionally to other adrenergic receptors Ex. an alpha-1 specific adrenergic blocker may also block beta-1 and/or beta-2 receptors Most common at high doses
52
Side effects of cholinergics
Usually undesired or excessive parasympathetic responses Ex. cisapride is a cholinergic that increases GI motility. Side effects may include bradycardia or bronchoconstriction Also, unwanted activation of neuromuscular junctions
53
Side effects of anticholinergics
Usually undesired or excessive sympathetic response Includes; tachycardia, constipation, urine retention, dry mouth Also, unwanted inhibition of neuromuscular junctions
54
Side effects of adrenergics
Usually undesired or excessive sympathetic response Includes: tachycardia, arrhythmias, hypertension anxiety, excitability
55
Side effects of adrenergic blockers
Usually undesired or excessive parasympathetic responses Includes: bradycardia, hypotension, syncope, nausea, vomit, diarrhoea