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Pharmacology > Autonomics > Flashcards

Autonomics Flashcards

1
Q

Differentiate between the Sympathetic and Parasympathetic Nervous Systems.

A

SNS: Fight/Flight
PNS: Rest/Digest

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2
Q

In the sympathetic nervous system, preganglionic neurons are very _____ and end in ganglionic neurons very _____ to the spinal cord.

A

Short and close

Postganglionic neurons are long and travel further to site

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3
Q

In the parasympathetic nervous system, preganglionic neurons are very ______ and travel _____ distances.

A

Long and long

Post ganglionic neurons are shorter with short distances to travel

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4
Q

In the sympathetic nervous system; what neurotransmitter is present in the pre and post ganglions neurons and what receptors do they act on.

A

Pre ganglionic: Acetylcholine acts on the Nicotinic receptor
Post ganglionic: Norepinephrine acts on Adrenergeric (alpha and beta)receptors and Acetylcholine acts on Muscarinic (sweat glands)

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5
Q

In the parasympathetic nervous system; what neurotransmitter is present in the pre and post ganglions neurons and what receptors do they act on.

A

Pre ganglionic: Acetylcholine acts on Nicotinic receptors

Post ganglionic: Acetylcholine acts on Muscarinic receptors

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6
Q

In the somatic nervous system; what neurotransmitter is present in the neurons and what receptors does it act on.

A

Acetylcholine at the Nicotinic receptor

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7
Q

For sympathetic innervation neurons arise from:

A

Lumbar, thoracic regions.

Short pre, long post

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8
Q

For parasympathetic innervation neurons arise from:

A

Cranial, sacral

Long pre, short post

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9
Q

The primary neurotransmitter of the sympathetic nervous system is:

A

Norepinephrine

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10
Q

Catecholamines produced in neurons include:

A

Dopamine
Norepinephrine
Epinephrine

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11
Q

How can tyramine and MAOI’s lead to a hypertensive crisis?

A

Tyramine is metabolized by MAO, in the setting of taking an MAOI this does not happen. Excess tyramine displaces NE from vesicles, increased available NE, this can causes a hypertensive crisis.

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12
Q

Nonselective adrenoreceptors agonists include:

A

Norepinephrine
Epinephrine
Dobutamine

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13
Q

Non-selective alpha agonists include:

A

Oxymetazoline (afrin) and Tetrahydrozoline

Clinically these agents are used topically so alpha-1 effects usually predominate

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14
Q

Alpha-1 selective agonists include:

A

Phenylephrine and Pseudoephedrine

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15
Q

Alpha-2 selective agonists include:

A

Clonidine, guanabenz, guanfacine, alpha-methyldopa

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16
Q

Selectivity of alpha agonists phenylephrine and clonidine:

A

Phenylephrine a1>a2»»>B

Clonidine a2>a1»»>B

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17
Q

Selectivity of mixed alpha and beta agonists NE and epi:

A

NE: a1=a2 B1»B2
Epi: a1=a2; B1=B2

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18
Q

What are the main tissues alpha-1 agonist effect and what are their actions?

A 
Smooth muscle (innervated)=contraction 
Pupillary dilator muscle= contraction/dilate pupils
Pilomotor smooth muscle= erects hair
Prostate=contraction 
Heart=Increases forces of contraction
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19
Q

What are the main tissues alpha-2 agonist affect and what are their actions?

A

Negative feedback; sends message to decrease catecholamine release

Platelets=Aggregation
Adrenergic muscle terminals=Inhibits transmitter release
Some vascular smooth muscle= contraction
Fat cells= Inhibits lypolysis

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20
Q

B-selective adrenoreceptor agonists include:

A

Nonselective: Isoproterenol (Isuprel)- not used
B1 selective: Dobutamine, Xamoterol- not used
B2 selective: Metaproterenol, terbutaline, albuterol, salmeterol, formoterol, perbuterol, bitolterol

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21
Q

Selectivity of B agonists; dobutamine, isoproterenol, terbutaline/albuterol:

A

Dobutamine B1>B2»»»a
Isoproterenol B1=B2»»>a
Terbutaline/albuterol B2»B1»»a

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22
Q

Functional effects of B1 (tissue and action)

A

Heart= increases force and rate of contraction

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23
Q

Functional effects of B2 (tissues and actions)

A

Respiratory, uterine, vascular smooth muscle= Relaxation
Skeletal muscle= Promotes K uptake
Liver= Activates glycogenolysis

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24
Q

Functional effects of B3 (tissue and action)

A

Fat cells= lipolysis

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25
Selectivity of Dopamine agonists:
Dopamine: D1=D2>>B>>a Fenoldopam: D1>>D2
26
Functional effects of D1 and D2 (tissues and actions)
D1 Smooth muscle= dilates renal blood flow D2 Nerve endings= Modulates transmitter release
27
CV effects of sympathomimetics:
a1: vasoconstriction=incr. BP a2: neg. feedback=dec. BP b1: increased CO=incr. BP b2: peripheral vasodilation-dec. BP
28
What type of agonist would be used to accommodate for vision?
a1= causes mydriasis (pupil dilation)
29
How are a1, a2, and b1 used in regulation of intraocular pressure?
a1, a2=increased humoral outflow (=dec. pressure) | B1= increased production of aqueous humor (=dec. this to decrease pressure)
30
Respiratory effects of sympathomimetics:
a1=reduces mucosal secretion (decongestant) | b2= bronchial dilation
31
GI effects of sympathomimetics:
a2, b2= decreased peristalsis (direct smooth muscle relaxation) a2= decreased digestive secretions
32
GU effects of sympathomimetics:
Bladder- a1= contraction of urethral sphincter; b2 relaxation (decreases UOP) Erectile tissue- a1= facilitates ejaculation Uterus- B2= relaxation (inhibits labor)
33
Direct Acting Sympathomimetics: Catecholamines | Epinephrine:
a1: vasoconstriction B1: cardiac stimulation B2: vasodilation ex-anaphylaxis
34
Direct Acting Sympathomimetics: Catecholamines | Norepinephrine:
a1: vasoconstriction B1: cardiac stimulation ex-sepsis
35
Direct Acting Sympathomimetics: Catecholamines | Isoproterenol:
B1-cardiac stimulation
36
Direct Acting Sympathomimetics: Catecholamines | Dopamine:
Dose dependent D1/D2-renal vasodilation(lower dose) a1- vasoconstriction (higher dose) B1-cardiac stimulation (higher dose)
37
Direct Acting Sympathomimetics: Non-Catecholamines are not inactivated by ________.
COMT (enzyme that breaks down catecholamines) | =longer duration of action, better access into brain
38
Direct Acting Sympathomimetics: Non-Catecholamines: | a1 agonists:
Phenylephrine- mydriatic, decongoestant, pressor Methoxamine- increases BP Midodrine (ProAmatine)- postural hypotension Oxymetazoline tetrahydrozoline, xylometazoline- nasal and ocular decongestants
39
Direct Acting Sympathomimetics: Non-Catecholamines: | a2 agonists:
Clonidine- CNS receptors, decreases BP | Apraclonidine- ciliary receptors, reduces intraocular pressure
40
Direct Acting Sympathomimetics: Non-Catecholamines: B2 agonists:
Albuterol, terbutaline, pirbuterol, botolterol, metaproterenol- asthma, COPD Salmeterol, formorterol- long duration of action Ritodrine- relaxes uterus to delay premature labor
41
Indirect Acting Sympathomimetics:
Enhance the release of catecholamines Amphetamine-increases release of NE and dopa Methamphetamine- similar to amphetamine but higher CNS effects Methylphenidate (Ritalin), permoline (Cylert)- amphetamine variants used for ADHD
42
MOA of alpha antagonists:
a-receptor responds faster than B-receptor Blocks stimulatory effects of NE at a-receptor Reversible: Phentolamine Irreversible: Phenooxybenzamine
43
CV effects of a-antagonism:
a1: decreases PVR and lowers BP postural hypotension d/t failure of vasoconstriction upon standing up a2: (blocks negative feedback) Increase NE release from nerve terminals
44
GU effects of a-antagonism:
Blockade in prostate and bladder cause muscle relaxation and ease micturition
45
Phentolamine, phenoxybenzamine
a- antagonist vasodilation, lowers BP diabetic neuropathy, enhance male sexual function, reverse side effects of clonidine withdrawal
46
Prazosin (minipress), terazosin (Hytrin), doxazosin (Cardura), tamsulosin (Flomax)
a-antagonists | -Hypertension, BPH
47
Yohimbine
a-antagonist | Diabetic neuropathy, enhance male sexual function, reverse side effects of clonidine withdrawal
48
B antagonist CV effects:
Decreases CO, BP Increases Na+ retention Propranolol (antag) wins over epi= vasodilation>constriciton
49
B antagonist Resp effects:
Increases airway resistance
50
B antagonist ocular effects:
Decreases aqueous humor production
51
B antagonist metabolic effects:
Decreases carb metabolism which decreases insulin release Decreases renin secretion with decrease angiotensin II (lowers BP) Decreases Na+ excretion Decreases lipolysis
52
Timol:
B antagonist Used for glaucoma by decreasing aqueous humor production Topical ocular hypotensive agent
53
Betaxolol:
B antagonist | Used for glaucoma by decreasing aqueous humor production
54
______ is the only neurotransmitter working in the PSNS.
Acetylcholine
55
What is botulinum toxin's effect on Acetylcholine?
Prevents exocytosis of presynaptic vesicles which prevents release of Ach at nicotinic receptors/neuromuscular junction
56
Neostigmine and pyridostigmine:
AChE inhibitors Use in treating disease of the neuromuscular junction (myasthenia gravis) Neostigmine also increases smooth muscle motility to ease abdominal distension
57
Physostigmine (Isopto):
AChE inhibitor | Increases outflow of aqueous humor to treat glaucoma
58
Tacrine (Cognex), donepezil (Aricept), rivastigmine (Exelon), galantamine (Razadyne):
AChE inhibitors | Used to treat AD and other cognitive dysfunction
59
AE and CI of AChE inhibitors:
AE: Peripheral ACh effects of GI tract: N/V/D, anorexia, flatulence, abdominal cramping (dose dependent) CI: Unstable or severe cardiac disease (AV block), uncontrolled epilepsy, active PUD
60
Why is ACh not administered?
Broad activity and rapid hydrolysis of AChE
61
Methacholine:
Muscarinic Agonist Used to diagnose asthma Causes bronchoconstriction
62
Carbachol:
Muscarinic Agonist | Miosis and decreased intraocular pressure
63
Bethanechol:
Muscarinic Agonist | GI and urinary tract motility- post op and post-partum urinary retention, neurogenic bladder
64
Succinylcholine:
Nicotinic Agonist Resistant to AChE Induction of paralysis by means of depolarizing blockade Continuous activation of nicotinic receptor channels results in neuronal depolarization of blockade
65
What are muscarinic antagonists MOA?
By antagonizing muscarinic receptors they causes sympathetic responses to predominate
66
Atropine:
Muscarinic Antagonist Mydriasis for eye exams Reverse symptomatic brady Inhibits excessive salivation and mucus secretion during surgery Prevents vagal reflexes induced by surgical trauma of visceral organs
67
Scopolamine:
Muscarinic Antagonist Treats motion sickness Transdermal patch
68
Ipraroprium (Atrovent), tiotropium (Spiriva),
Muscarinic Antagonists Bronchodilators Used to treat COPD
69
Oxybutynin (Ditropan), tolterodine (Detrol)
Muscarinic Antagonists Used to treat overactive bladder Work at non-specific M-rc
70
Darifenacin (Enablex), Solifenacin (Vesicare)
Muscarinic Antagonists Used to treat overactive bladder M3 specific
71
AE and CI for Muscarinic Receptors:
AE: Anticholinergic effects Blurred vision, dry mouth, ileus, urinary retention, flushing, agitation, tachycardia CI: angle-closure glaucoma Use caution with elderly
72
MOA of Nicotinic Antagonists:
Prevent ACh binding to nicotinic receptors and subsequent muscle depolarization
73
Pancuronium, Vecuronium, Rocuronium:
Nicotinic receptors | Induce paralysis
74
What is the MOA of AChE inhibitors?
Elevates concentration of endogenously release ACh in the synapse =increases transmission at NM junction, increased parasympathetic tone, increases central cholinergic activity
75
Muscarinic Effects:
``` SLUG BAM Salivation, secretions, sweating Lacrimation Urination GI upset (vomiting, diarrhea) Brady, bronchoconstriction, bowel movement Abdominal cramps, Anorexia Miosis ```
76
Anticholinergic Effects:
``` ABCDS Anorexia Blurry vision Constipation, confusion Dry mouth Sedation, stasis of urine ``` Can'ts Cant: Pee, See, Spit, Shit
77
a-agonism Fight/flight properties:
``` Vasoconstriction Urethral constriction Dec. humoral outflow Prostate contraction Decreased peristalsis Platelet inhibtion ```
78
a- antagonism Rest/Digest properties:
``` Vasodilation Urethral relaxation Miosis Prostate relaxation Nasal congestion ```
79
b1 agonism Fight/Flight properties:
Increase CO/BP | Increased aqueous humor
80
b2 agonism Fight/Flight properties:
``` Bronchodilation Increase Na retention Peripheral vasodilation Decreased peristalsis Uterine relaxation ```
81
B1 antagonism : Rest/Digest properties:
Decrease CO/HR/BP | Decrease aqueous humor
82
B2/B3 antagonism: Rest/Digest properties:
Bronchoconstriction | Metabolic effects

Pharmacology (48 decks)

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