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N929 Pharmacology > Exam 1 > Flashcards

Exam 1 Flashcards

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1
Q

Key Characteristics of Autonomic Nervous System

A

regulates involuntary response (smooth muscle, muscle, glands and heart)
2-neuron pathways
diffuse vs. discrete responses
dual innervation- opposing antagonistic effects
reflex responses
predominant, basal activity/control

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2
Q

Exceptions to Dual Innervation

A 
adrenal medulla (sympathetic)
most sweat glands (sympathetic only)
blood vessels (sympathetic only)
-basal tone 
-receptor distribution determines response
pilorector muscle
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3
Q

Parasympathetic Tone is dominant in what systems?

A

cardiac, bronchial smooth muscle, GI tract, urinary tract, salivary glands

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4
Q

Sympathetic tone is dominant in what systems?

A

sweat glands and arterioles/veins

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5
Q

Adrenal Medulla

A 
sympathetically innervated
only one neuron
postsynaptic neuroendocrine cells
secrete epi/norepi into blood
mimics sympathetic stimulation
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6
Q

sweat glands

A

sympathetic innervation
post ganglionic neuron is cholinergic (not adrenergic)
Ach is NT
receptor at effector tissue is muscarinic

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7
Q

Enteric Nervous system innervates the

A

GI tract

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8
Q

Steps of Neurotransmission

A

synthesis
storage
release (vesicles fuse w/ nerve terminal)
action
termination (reuptake, enzyme degradtion, and diffusion)

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9
Q

Cholinergic Transmission

A 
synthesis from choline, acetyl-CoA
storage in vesicles
action potential triggers Ca2+ entry, then interacts with SNARE protein on vesicle leading to fusion of vesicle and opening/release of Ach
binding to receptor
termination of action
recycle choline
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10
Q

what blocks cholinergic transmission?

A

botulinum toxin blocks

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11
Q

AchE

A

acetylcholinesterease

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12
Q

Major Types of Receptors

A

Ligand Gated Ion Channel
GPCR
Transmembrane w/ linked enzymatic domain
Intracellular receptor

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13
Q

Muscarinic Cholinergic Receptor

A

GCPR
5 subtypes, 2 subgroups
autonomic effector tissues (heart, endothelium, smooth muscle, glands) CNS
endogenous ligand: Ach
Activation mimics post ganglionic parasympathetic neuron stimulation
diverse cellular responses to M agonist
current drugs aren’t very selective

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14
Q

Nicotinic Cholinergic Receptor

A

ligand gated Na K depolarizing channel
major subtypes: NicM NicN
located: autonomic ganglia, skeletal muscle innervated by somatic nerves and CNS
Ach binds causing conformational changes, channel opens and + charged ions pulled through channel
depolarization of post synaptic cell

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15
Q

Where are cholinergic receptors?

A 
M1 CNS
M2 heart
M3 Smooth muscle, glands, endothelium, eye (circular, ciliary m)
M4 CNS
M5 CNS
NicN ANS ganglia, adrenal medulla, CNS
Nicm: Skeletal muscle NMJ
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16
Q

Key Points of Acetylcholine

A

roles in peripheral and central NS

many NT sites (NMJ, ANS ganglia, effector jux of postganglionic parasympathetic neurons and CNS)

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17
Q

Acetylcholine Termination of Action

A

Termination action: AchE
Receptors: Muscarinic, NicotinicN and NicotinicM
Drug Targets:

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18
Q

Receptors of Acetylcholine

A

Muscarinic, NicotinicN and M

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19
Q

Drug Targets of Acetylcholine

A

Ach Synethesis, storage, release AchE

Muscarinic and nicotinic receptors

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20
Q

Drug uSes of Ach

A

heart, eye, lung, GI GU NMJ and CNS

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21
Q

Adrenergic Neurotransmission

A

synthesis of NE (catecholamine)
uptake/storage vesicles
release w/ action potential (indirect adrenergic drugs)
rec binding
termination of action: reuptake via NET (NE transporter)

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22
Q

Catecholamine from

A

AA tyrosine

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23
Q

Alpha Adrenergic Receptors

A

GPCR
ligands: NE, Epi and Dopamine
3 subtypes alpha1 and alpha2

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24
Q

Alpha 1 found in

A

smooth mucle

eye

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25
Alpha 2 is
mainly presynaptic
26
Activation of Alpha 1
excitatory | increases Ca2+, calmodulin activity, increase actin-myosin interaction, smooth muscle contraction
27
Activation of Alpha 2
inhibitory | decreases cAMP, decrease NE release
28
Beta Adrenergic Receptor
B1 B2 B3 GCPRs Gs activation of adenyl cyclase to increase cAMP increase kinase activation and phosphorylation
29
Beta Adrenergic Effector tissue
autonomic | heart kidney liver smooth muscle skeletal muscle and fat cells
30
Where are Alpha 1 adrenergic receptors located?
``` smooth muscle GU sphincters most vascular (skin, splanchnic) eye (radial msucle) heart liver ```
31
Where are alpha 2 adrenergic receptors located?
presynaptic nerve terminal platelets pancreatic beta cell
32
Where are beta2 adrenergic receptors located?
``` smooth muscle (bronchiolar, uterine, etc.) vascular smooth muscle skeletal muscle beds liver skeletal muscle heart ```
33
Where are beta 1 adrenergic receptors located?
heart | kidney JG cells
34
Where are beta 3 cells located?
adipose tissue
35
Key Points of NE in the peripheral nervous system
roles in peripheral and CNS (excitatory) catecholamine NT termination of action: reuptake back into presynaptic neuron, diffusion, metabolism- minor role (MAO/COMT) Noradrenergic receptors (GCPR, negative feedback limits response)/alpha1/alpha2/beta1-3 Drug Targets: NE synethesis, storage, reuptake, metabolism, receptor Drug uses: cardiovascular, respiratory
36
Dopamine has roles in
peripheral and CNS
37
Dopamine is a catecholamine NT
precursor of NE and E | at effector JXNm sympathetic renal vascular smooth muscle
38
TOA of Dopamine
neuronal reuptake by DA transporter | MAO breakdown
39
MAO A
periphery
40
MAO B
CNS
41
COMT
minor role
42
Dopamine Receptors
``` GCPR, cAMP 2nd messanger D1 class: increases cAMP D2 class (d2-d4): decreases cAMP ```
43
Dopamine in the periphery (d1)
vasodilation in renal mesenteric, coronary vasculature
44
Dopamine in the periphery (d2)
presynaptic, modulates NT release
45
Dopamine as a drug (low dose)
vasodilation
46
Dopamine as a drug (intermediate)
+ inotrope (B1)
47
Dopamine as a drug (high)
vasoconstriction (alpha1)
48
Other NT utilized by PNS
``` NO vasoactive intestingal peptide calcitonin gene related peptide neuropeptide Y substance P serotonin others ```
49
PDE5
phosphodiesterase 5; the enzyme that breaks down the 2nd messengar
50
eNOS
endothelial nitric oxide synthase; enzyme that makes nitric oxide from L-arginine
51
Iris
``` pupillary control iris radial (mydrasis) Sympathetic NS Iris circular (miosis) Parasympathetic NS ```
52
Ciliary
focus lens Parasympathetic- accomodate near vision increase outflow aqueous humor
53
Ciliary Body
aqueous humor production | increase secretion of aqueous humor via epithelium (sympathetic)
54
Aqueous Humor
intraocular pressure
55
adrenergic
describes neurons or receptors that use NE, or drugs that mimic sympathetic nerve stimulation
56
Alpha adrenergic
adrenergic receptor activated by NT NE
57
beta adrenergic
adrenergic receptor activated by NT NE
58
Catecholamine
molecule class that contains a caetchol and amine gorup, includes Epi, NE and dopamine
59
Cholinergic
describes neurons or receptors that use Ach or drugs that mimic parasympathetic nerve stimulation
60
Epipherine
adrenalin, produced in adrenal medulla, also NT in CNS
61
ganglion
a cluster of nerve cell bodies
62
muscarinic receptor
cholinergic receptor of PSNS
63
Nicotinic receptor
cholinergic receptor
64
NE
noradrenalin, NT at sympathetic effector tissues in periphery, some produced in adrenal medulla also in CNS
65
Preganglionic
situated before the ganglion
66
Postganglionic
situated after the ganglion
67
Characteristics of SNS
``` originated in the thoracolumbar 2 neurons peripheral ganglia preganglia -short post ganglia- long divergence- diffuse receptor on post gang- adrenegic/ muscarinic receptor on target tissue: sweat glands/ adrenal` ```
68
Characteristics of PSNS
``` Central Nervous and below and above scaral region 2 neurons ganglia locations: SC and CNS Pre- long, post short discrete divergence receptors: muscarinic, nicotinic, ```
69
Sympathomimetics
drugs with an effect that mimic stimulation of SNS or adrenal medullary discharge
70
Symopatholytics
drugs that antagonize the sympathetic nervous system
71
three ways sympathomimetics stimulate SNS
directly on adrenoreceptors indirectly by stimulating release of noradrenaline from nerve endings combination of both mechanisms
72
Direct acting Cholinergic Drugs | receptor agonist
acetylcholine muscarine pilocarpine bethanechol
73
Direct Acting Cholinergic Direct (Nicotinic Agonist)
Acetylcholine nicotine succinylcholine varenicline
74
Indirect Acting (AchE inhibitors)
Edrophonium neostigmine pyridostigmine, physostigmine donepezil
75
Indirect Acting AchEi (irreversible)
echothiopate
76
Other Cholinergic Agonist Drugs
increased muscarinic activity lack acetate ester function AChE does not hydrolyze
77
MOA of AChE Inhibitor Drugs
Goal: to increase Ach in cleft and increase half life bind to active site and inhibit AChE Indirect Muscarinic and nicotinic effects
78
Indirect Reversible AchE inhibitor Drugs
alcohol (edrophonium) | Carbamate (neostigmine)
79
Indirect Irreversible AchE inhibitor Drugs
echothiophate
80
AchE inihbitors are reversible if
the drug covalently bonds
81
Short Duration Reversible AchE inhibitors
edrophonium
82
Medium Duration Reversible AchE inhibitors
neostigimine, pyridostigmine, physostigmine
83
AchE Effects
increases Ach amplifies effects at cholinergic synapses indirect stimulant of nicotinic receptors by increasing Ach
84
Clinical Uses of AchE
``` reversal of NM blockade by ND drug MG diagnosis and treatment glaucoma GI- ileus Postop Urinary Retention Alzheimer's Disease Non-therapeutic insecticide ```
85
AchE Inhibitor drug effect on ANS
bradycardia, bronchoconstriction, increase secretions, increase GI motility, hypotension, miosis (accomdation for near vision)
86
AchE Inhibitor drug effect on NMJ
reverses NM block by ND NMR blocker improves transmission MG large doses can depolarize block
87
AchE Inhibitor drug effect on CNS
therapeutic- dementia tx toxicity- excitation Depression follows
88
Edrophonium DOA, Main Site of Action, Onset, Notes
``` alcohol, quaternary amine, very polar Reversible blockade Injectable IV IM use for reversal Onset 30-60seconds, duration 10 mins NMJ, used for MG diagnosis ```
89
Neostigmine DOA, Main Site of Action, Onset, Notes
``` medium NMJ used IV to reverse used as oral treatment in MG visceral side effects carbamate, quaternary amine, moderately polar hydrolyzed by AchE, labile covalent bond IV, orally active Onset: 10-30 mins DOA 2-4 hours ```
90
Physostigmine
carbamate, tertiary amine, non-polar CROSSES BBB hydrolyzed by AchE labile covalent bond oral, IV/IM, useful for anticholinergic toxicity onset 3-8 mins, duration 1 hour medium, Peripheral, used as eye drops for glaucoma treatment
91
Pyridostigime
Medium NMJ used orally in treatment of myasthenia gravis better absorbed than neostigmine and has longer DOA
92
Cholinergic Crisis
``` DUMB BELLS diarrhea, diaphoresis urination miosis Bradycardia Bronchoconstriction Excitation (skel m., CNS) lacrimination salivation sweating ```
93
Cholinergic Toxicity can occur
as a muscarinic toxicity treat with atropine and AChE toxicity ( too much Ach from blocking too much inhibitor) antidote: atropine/pralidoxime
94
Muscarinic Agonist Drugs
``` acetylcholine carbechol methacholine bethanecol muscarine pilocarpine oxotremorine cevimeline ```
95
Bethanecol is utilized for
treatment of bladder and GI hypotonia
96
Pilocarpine is used for
glaucoma
97
Cevimeline is used for
sjogen's syndrome
98
Drug effects of Muscarinic Agonist (parasympomimic)
``` decrease HR/BP bronchoconstriction increased salivation/ lacrimination increase GI motility Miosis decrease intraocular pressure, accommodation for near vision bladder contracts ```
99
Effects and Clinical use of Muscarinic agonist
glaucoma (contract ciliary body, increase aqueous outflow humor) postop ileus post op urinary retention xerostomia (dry mouth)
100
Effects of Muscarinic Agonist Type
``` salivation lacrimination urination diarrhea gi upset emesis ```
101
Do not use cholinergic drugs if
``` GI/GU obstruction CV disease Respiratory disease (asthma, COPD) ```
102
Effects of Nicotinic neuron Agonist
stimulation of post ganglionic neuronal activity | CNS stimulation
103
Clinical Use of Nicotinic neuron Agonist
Smoking cessation
104
Adverse effects of Nicotinic Neuron Agonist
CNS stimulation skeletal muscle depolarization/blockade HTN, increase HR, N/V and diarrhea
105
Effects of Nicotinic muscle Agonist
activation of NM endplates | contraction
106
Clinical Use of Nicotinic NMJ agonist
depolarizing skeletal muscle paralysis
107
Muscarinic Antagonist Drugs (nonselective)
atropine glycopyrrate scopolamine
108
Nicotinic Antagonist (NicotinicN)
ganglionic blocker | hexamethonium
109
Nicotinic Antagonist (NaChRM)
atracurium, cisatracurium, vecuronium, rocuronium, pancuronium
110
Muscarinic Receptor Antagoinst Effects
``` increase HR bronchodilation decrease GI motility GU constipation and retention Decrease sweat and glandular release pupillary dilation CNS sedation ```
111
Clinical Uses of Muscarinic Receptor Antagonist
``` motion sickness parkinson's disease exam requiring mydriasis cyclopegia decrease lung secretions COPD asthma GI hypermotility urinary urgency treatment of bradycardia anesthetic premed cholinergic poisoning achE inhibitor toxicity ```
112
Atropine Characteristics
``` tetriary amine lipophilic crosses BBB half-life about 4 hours injection (IV IM) opthalamic utilized for opthalmic, bradycardias, antidote vs cholinergic agonist, pre-op inhibits secretions adjunct for NM block reversal ```
113
Scopolamine Characteristics
``` tertiary amine crosses BBB CNS effects- amnesia, sedation half- life 1-4hr (IV) onset 10 mins duration 2 hours transdermal patch injection uses for motion sickness, post op NV preop- amnesia, sedation, antiemetic decrease secretions ```
114
Glycopyrrolate Characteristics
``` quaternary amine, decreases CNS effects half life about 1 hour onset 1 min duration (7 hours) IV oral uses include pre-op, cardiac dysrhythmia (vagal reflex association) adjunct for NM blockade ```
115
Muscarinic Antagonist/Anticholinergic Effects
Dry as a bone, hot as a pistol, red as a beet, blind as a bat, mad as a hatter
116
Potential concerns of Muscarinic Antagonist/Anticholinergic
``` hyperthermia glaucoma prostatic hypertropy CV (arrhythmias, ischemia, HF, HTN) ileus, ulerative colitis ```
117
Medication classes with anticholinergic effects
``` antihistamines antispasmodics antiparkinson's skeletal muscle relaxants antipsychotics antidepressants antimuscarinics for urinary incontinence ```
118
Nicotinic Receptor Antagonist Effects
competitive antagonism at skeletal muscle | Non-depolarizing
119
Nicotinic M Receptor Antagonist Clinical Uses
Skeletal muscle relaxation for surgical, intubation, ventilation control
120
Nicotinic N Receptor Antagonist Effects
Blocks ganglionic output
121
Nicotinic N Receptor Antagonist CLinical uses
hypertensive emergency (no longer in use)
122
Mechanisms of Adrenergic drugs
indirect mixed multiple sites of action (release of NE from nerve terminal, activate adrenergic receptors, broader actions) direct receptor antagonist
123
Alpha 1 second messengers and effectors
phospholipase C activation increase inositol trisphosphate increase diacylglycerol increase Ca2+
124
Alpha 1 potency order
NE, E, iso
125
Alpha 1 Selective Agonist
phenylpherine | methoxamine
126
Alpha 1 Selective antagonist
prazosin | doxazocin
127
Alpha 2 second messengers and effectors
decrease cAMP, decrease Ca channels, increase K channels
128
Alpha 2 potency order
E, NE, ISO
129
Alpha 2 selective agonist
clonidine
130
Alpha 2 selective antagonist
yohimbine | idazoxan
131
Beta 1/2/3 second messengers and effectors
increase cAMP
132
Beta 1 potency
ISO>NE>E
133
Beta 2 potency
ISO > E> NE
134
Beta 3 potency
ISO> NE=E
135
Beta 1 selective agonist
dobutamine | xamoterol
136
Beta 1 selective antagonist
atenolol | metoprolol
137
Beta 2 selective Agonist
``` salbutamol terbutaline salemetrol formoterol clenbuterol ```
138
Beta 2 selective antagonist
butoxamine
139
Beta 3 selective agonist
mirabegron
140
Ephedrine
displaces/releases stored catecholamine NT some agonist activity on alpha and beta receptors noncatecholamine extended duration herbal source-ma hung
141
Amphetamine
displaces/releases stored catecholamine NT secondary inhibits catetcholamine reuptake (NET, DAT) uses in ADHD, narcolepsy, appetite suppression
142
Cocaine
blocks NE reuptake (inhibits NET & DAT transporters) | Blocks sodium channels- local anesthetic actions
143
Tyramine
displaces/releases stored catecholamines | not a drug, in fermentated foods, role in drug food interacitons of MAO inhibitors
144
Tricyclic Antidepresants, SNRI
block NE re-uptake (inhibits NET transporter)
145
Monamine Oxidase inhibitors (MAOis)
prevents breakdown of catecholamines in presynaptic terminal- catecholamine accumulation in vesicles MAOA metabolizes NE MAOB metabolizes DA
146
tranylcypromine and phenelzine
nonselective inhibits MAOA and MAOB
147
Selegiline and rasagiline
selective MAOB inhibitors
148
Most drugs are non-catecholamines
longer acting | oral adminsitration
149
Epinephrine Receptor and Uses
``` Alpha 1 alpha 2 beta 1 beta 2 beta 3 low doses- beta effects high doses: alpha effects Anaphylaxis, w/ local anesthetics, cardiac arrest ```
150
Norepinpherine Receptors and Uses
Alpha 1 and Beta 1 | shock
151
Isoproterenol Receptors and Uses
Beta 1 and Beta 2 | acute asthma, cardiac stimulant
152
Dopamine Receptors and Uses
low dose: renal, mesenteric, coronary vascular beds med doses: beta 1 higher doses: alpha 1 shock, HF and increase blood flow to kidney
153
Dobutamine Receptors and Uses
b1 primarily | acute HF
154
Cardiac Effects of NE
decrease pulse increase SBP and DBp Increases PVR
155
Cardiac Effects of Epi
increases HR increases SBP/ decreases DBP decreases PVR
156
Cardiac Effect of Isoproterenol
increases HR increases SBP/ decreases DBP decreases PVR
157
Predominant effects of Adrenergic Receptor agonist | Alpha 1
``` vasoconstriction smooth muscle (except GI) trophic effect (BPH) GI/GU sphincters contract Eye-mydriasis ```
158
Predominant effects of Adrenergic Receptor agonist | Beta 1
increase HR, increase contractility effects on rhythm kidney renin trophic effect- hypertrophy
159
Predominant effects of Adrenergic Receptor agonist | Alpha 2
decrease NE release (presynaptic) CNS inhibit sympathetic outflow platelet aggregation decrease insulin in pancreas
160
Predominant effects of Adrenergic Receptor agonist | Beta 2
``` bronchodilation vasodilation most smooth muscle (relaxes) skeletal muscle contracts (tremor) GI/GU relax uterine smooth muscle relax glycogenolysis ```
161
Alpha 1 agonist effects
increase vascular tone, increase PVR/BP and eyes dilate
162
Alpha 1 agonist clinical uses
shock | OTC: decongestants, ophthalamic hyperemia
163
Alpha 2 agonist clinical uses
hypertension
164
Alpha 2 effects
decrease NE release
165
Dexmedetomidine
selective alpha 2 receptor agonist (CNS actions) suppresses sympathetic NS activity sedative effects analgesic effects decrease HR, decrease SVR, decrease BP Respiratory less RR decrease TV tolerance, tachyphylaxis, premed, adjunct to general anesthesia,
166
Beta 1 Agonist Effects
increase HR, AV node conduction, increase force and renin release
167
Beta 1 Clinical Uses
ACUTE heart failure
168
Beta 2 agonist effects
relaxation or lung, uterus, vascular and liver
169
Beta 2 clinical uses
asthma, COPD, preterm labor
170
Potential concerns with adrenergic agonist
``` CV disease cerebrovascular disease other vasoconstriction related diabetes (increase blood glucose) IV extravasation risks thyroid disease ```
171
Nonselective alpha adrenergic receptors Blockers
phenoxybenzamine | phentolamine
172
Alpha 1 adrenergic receptors Blockers
prazosin
173
Alpha 2 adrenergic receptor Blockers
yohimibine
174
Nonselective Beta Blocker
propanolol
175
Beta 1 Receptor Blocker
Metoprolol | esmolol
176
Alpha Receptor Antagonist Effects
smooth muscle relaxation, decrease pVR, decrase BP
177
Alpha receptor antagonist Clinical uses
hypertension BPH pheochromocytoma
178
Adverse Effects of Alpha Receptor Antagonist
increase HR, first dose effect | orthostatic HTN and syncopy
179
Beta Receptor Antagonist Effects
decrease HE, decrease force of contraction | decrease renin release, anti-rhythmic effects
180
Clinical uses of beta receptor antagonist
htn, angina pectoris, arrhythmia, myocardial infaraction, thyrotoxicosis, heart failure, infantile hemangioma, glaucoma, migrane, prophylaxis, anxiety
181
Potential concerns of Adrenergic Antagonist
respiratory disease cardiovascular diabetes (may potentiate hypoglycemia and mask sign/sym) thyroid disease

N929 Pharmacology (16 decks)

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