Pharm Exam 1 Flashcards

1
Q

Direct acting agonist

A

Class: Cholinomimetics

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2
Q

AChE inhibitors

A

Class: Cholinomimetics

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3
Q

Cholinergic antagonist

A

Class: Anticholinergics

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4
Q

Neuromuscular blockers

A

Class: Anticholinergic

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5
Q

Acetylcholine

A

direct acting Cholinergic Agonist

Muscarinic

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6
Q

Bethanechol

A

direct acting Cholinergic Agonist

Muscarinic

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7
Q

Pilocarpine

A

direct acting Cholinergic Agonist

Muscarinic

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8
Q

Nicotine

A

direct acting Cholinergic Agonist

Nicotinic

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9
Q

Varenicline

A

direct acting Cholinergic Agonist

Nicotinic

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10
Q

Neostigmine

A

AChe/Cholinesterase Inhibitor

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11
Q

Pyridostigmine

A

Ache/Cholinesterase Inhibitor

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12
Q

Physostigmine

A

Ache/Cholinesterase Inhibitor

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13
Q

Edrophonium

A

Ache/Cholinesterase Inhibitor

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14
Q

Donepezil

A

Ache/Cholinesterase Inhibitor

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15
Q

Organophosphates

A

Ache/Cholinesterase Inhibitor

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16
Q

Pralidozime

A

Poisoning tx

Cholinesterase Inhibitor

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17
Q

Atropine

A

Cholinergic Antagonist

Muscarinic

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18
Q

Diphenoxylate-atropine

A

Cholinergic Antagonist

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19
Q

Scopolamine

A

Cholinergic Antagonist

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20
Q

Tropicamide

A

Cholinergic Antagonist

Muscarinic

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21
Q

Ipratropium

A

Cholinergic Antagonist

Muscarinic

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22
Q

Tolterodine, Fesoterodine, Darifenacin, Solifenacin

A

Cholinergic Antagonist

Muscarinic

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23
Q

Oxybutynin

A

Cholinergic Antagonist

Muscarinic

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24
Q

Dicyclomine

A

Cholinergic Antagonist

Muscarinic

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25
OnabotuliniumtoxinA
Botox Cholinergic Antagonist (Muscarinic)
26
Succinycholine
Depolarizing Nueromuscular Blocker
27
Direct Acting Agonists and Cholinesterase Inhibitors are what class:
Cholinomimetics
28
Cholinergic Antagonists and Neuromusc blockers are what class:
Anticholinergics think "antagonist" and "blockers" are ANTIcholinergics
29
Muscarinic effects on the heart
stimulates M2 receptors in the SA node effects primarily SA, AV, and Atrial Slows conduction thru AV node
30
Acetylcholine
decreases HR and decreases BP
31
Ach
M3 receptors on endothelium increase NO --> increase cGMP --> vasodilation experimentally driven very short effect bc Ach has such a short half life
32
Ach
stimulates both Muscarinic and Nicotinic receptors no clinical use (short half life)
33
Ach effect
IV infusion: similar to parasympathetic stimulation EXCEPT: decrease BP
34
Ach pharmacokinetics
hydrolyzed by AchE (Very quickly)
35
Bethanechol (Urecholine) Mechanism
Non specific Muscarinic agonist with highest effect in urinary bladder and GI tract
36
Bethanechol (Urecholine) Use
Muscarinic DOC for: increasing GI motility, treating Urinary retention
37
Bethanechol (Urecholine) Pharmacokinetics
Quart ammon ion (has charge) does not enter brain bc BBB does not allow any charged ions
38
Pilocarpine (IsoptoCarpine) Mechanism
Non specific Muscarinic agonist
39
Pilocarpine (IsoptoCarpine) Use
Topical: Acute angle glaucoma (last agent used) Oral: Xerostomia (dry mouth)
40
Pilocarpine (IsoptoCarpine) Adverse Effects
Topical: Blurred vision Oral: Sweating Both: HA/brow ache
41
Overall Adverse effects of Muscarinic Agonists
N/V/D, abd cramp, bladder tightness, sweating, salivation, bronchoconstriction, constricted pupils, blurred vision
42
Contraindications to Muscarinic Agonists
Asthma/COPD Peptic Ulcer Bowel Obstruction Coronary insuff
43
Toxicity of Muscarinic Agonists
Mushroom poisoning : muscarine | SLUDGE
44
SLUDGE side effects of Mushroom poisoning
``` Salivation Lacrimation Urination Defecation Gastric distress Emesis ```
45
Bronchoconstriction d/t Muscarinic poisoning
Treat with atropine (antagonist) and albuterol (beta agonist) to reverse
46
Sympathetic effects of Nicotine
HTN, tachycardia alternating with vagal bradycardia
47
Parasymp effects of Nicotine
N/v/d, urination
48
Varenicline (Chantix) Mechanism
Partial agonist on the nicotinic receptor | subtype that stimulates reward system in the brain by releasing Dopamine
49
Varenicline (Chantix) Use
Smoking cessation (provide some nicotine stimulation to decrease craving)
50
Varenicline (Chantix) Adverse Effects
Nightmares Psychoses Suicidal ideation
51
AChE inhibitors
all ganglia activated, so both Parasympathetic and Sympathetic . nerves are stimulated
52
Parasympathetic dominates the heart effects of AChE Inhibitors
Ach release increased (ganglia) and prolonged (heart) cardiac M2 receptors are stimulated more Bradycardia
53
AChe Inhibitors effect on BP
``` little effect no cholinergic (Ach) innervation ``` (BP is only stimulated by sympathetic system)
54
Myasthenia Gravis
Autoimmune Antibodies bind to Nicotinic Ach receptors and REDUCE the receptor number able to respond to Ach not enough Ach can be released to stimulate the low receptor number
55
Neostigmine and Pyridostigmine Mechanism
Form covalent bond with AchE enzyme and BLOCK it
56
Neostigmine and Pyridostigmine Pharmacokinetics
Hydrolyzed slowly Quat ammon ion- meaning does NOT enter brain
57
Neostigmine and Pyridostigmine Use
Most common used for Myasthenia Gravis Reverse neuromuscular block after surgery Postop/neurogenic ileus or atony of urinary bladder
58
Neostigmine and Pyridostigmine Adverse Effects
Muscarinic SE, although pt generally becomes tolerant
59
Physotigmine Pharmacokinetics
Tertiary amm compound- ENTERS CNS
60
Physotigmine Use
systemic use rare: used in Muscarinic Antagonist poitoning (Atropine)
61
Edrophonium Pharmacokinetics
VERY short acting (5-10 min), reversible, must be INJECTED similar to Neo and Pyrido, but more short acting
62
Edrophonium Use
to diagnose and determine tx dose for Myasthenia gravis To reverse neuromuscular blockade after surgery
63
Donepezil Pharmacokinetics
Well absorbed orally and CAN enter CNS
64
Donepezil Use
Alzheimer's dz
65
Finding the right dose of Neostigmine or Pyridostigmine by testing with Edrophonium
Add Edro on top of the Neo/Pyrido If strength improves: need to increase Neo/Pyrido dose If strength worsens: dose is too high, need to decrease (if dose is too high, causing desensitization)
66
Predominant tone is usually parasympathetic under what receptor
M3
67
Muscarinic receptors work via:
G proteins secondary cascade that we don't need to know details about fo this exam
68
Nicotinic receptors work via
ligand gated Na+ channel rapid desensitization
69
Muscarinic effects on eye
Miosis (contraction of circular muscle) Accomodation for near vision Opens angle, decrease pressure
70
Muscarinic agonists can help what in the eye?
Glaucoma, help decrease pressure
71
Muscarinic effects on the heart
slow conduction via SA node M2 receptors
72
Ach
stimulates both M and N receptors Decrease BP
73
Bethanechol (Urecholine)
highest effect on bladder and GI tract used to: increase GI motility and treat Urinary retention charged (no enter to brain)
74
Pilocarpine (IsoptoCarpine)
Applied topically for acute angle glaucoma (last resort though) Treat Xerostomia (Dry mouth) SE: blurred vision, sweating, HA
75
Contraindications to Muscarinic Agonists
Asthma, COPD, Peptic ulcer, Bowel obstruction, Coronary insufficiency/heart dz
76
Nicotine activates
both para and symp neurons has para and symp effects para: n/v/d, urination symp: HTN, tachy alt with vagal brady
77
Varenicline (Chantix)
smoking cessation PARTIAL agonist on Nicotinic receptor
78
Varenicline (Chantix) bad side effects
nightmare, psychose, SI
79
Neostigmine and Pyridostigmine
most common drug for Myasthenia Gravis Also used to: reverse neuromuscular blockade post surgery, and for postop/neurogenic ileus or atony of bladder
80
Physostigmine
Used in Muscarinic antagonist poisoning
81
Edrophonium
test dose for Neo and Pyrid short acting, injected and to reverse neuro blockade
82
Donepezil
Alzheimer's dz
83
Organophosphates
long lasting effect soman, sarin, tabun, VX
84
AChE Inh Toxicity
SLUDGE Salivation, lacrimation, urination, defecation, gastric distress, emesis Miosis, sweating, bronchoconstrict, n/v/d CNS: confusion, ataxia,s lurring, convulsions, coma Neuromusc stimulation followed by blockade --> paralysis --> respiratory arrest --> Death
85
Tx of Organophosphate AcHe inh poisoning
Atropine until pupils dilate 2-PAM (Pralidozine) if less than 3-4 hrs since exposure Diazepam (Valium) for convulsions
86
Many drugs block Muscarinic receptors:
``` Old antihistamine (Benadryl) Antidepressants Antipsychotics GI meds Eyedrops Plants ``` *poisoning fairly common
87
Nicotinic Receptor
Acetylcholine Nondepolarizing blocker Depolarizing blocker
88
Norepinephrine
Catecholamine
89
Epinephrine
Catecholamine
90
Isoproterenol
Catecholamine
91
Catecholamines
Norepi, Epi, Isoproterenol
92
Alpha 1 Agonists
Phenylephrine, Pseudoephedrine (Sudafed), Oxymetazoline (Afrin)
93
Phenylephrine
Alpha-1 agonist
94
Pseudoephedrine (Sudafed)
Alpha-1 agonist
95
Oxymetazoline (Afrin)
Alpha-1 agonist
96
Alpha-2 agonists
Clonidine, Methyldopa, Tizanidine
97
Clonidine
Alpha-2 agonist
98
Methyldopa
Alpha-2 agonist
99
Tizanidine
Alpha-2 agonist
100
Beta-1 agonist
Dobutamine
101
Beta-2 agonist
Albuterol
102
Beta-3 agonist
Mirabegron
103
Dopamine Agonist
Dopamine | Fenoldopam
104
Dopamine
Dopamine agonist
105
Fenoldopam
Dopamine agonist
106
Tx for Organophosphate poisoning
Atropine (until pupils dilate) 2-PAM (if 3-4hr since exposure) Diazepam "Valium": convulsions
107
How does 2-PAM work
A strong nucleophile | pulls the Organophosphate away from the AcHe preventing the "aging"
108
"aging" of organophosphate
the breaking of the phosphorus-oxygen bond, making the resulting bond to the AChE irreversible (AChE is now inactive)
109
Atropine
Muscarinic Antagonist it lessens normal parasympathetic effects, therefore has effects like sympathetic would
110
Atropine uses
prevent excessive Vagus nerve stimulation during surgery
111
Atropine uses
reverse bradycardia
112
Atropine uses
Treat diarrhea (combined with an opoid)
113
Atropine uses
block Muscarine effects - pesticide or nerve gas poisoning - muscarine poisoning (mushrooms)
114
Scopolaine (transferm scop)
crosses BBB For motion sickness
115
Tropicamide (mydriacil)
topical, short acting, used to DILATE pupils for EYE EXAM Cycloplegia side effect- can't see near vision
116
Ipratropium (atrovent)
Immediate lung bronchodilation not absorbed into sytemic, only works in the lungs!! To treat: COPD, sometimes in Asthma attacks
117
Tolterodine, Fesoterodine, Darifenacin, Solifenacin
M3 selective | To treat overactive bladder
118
Oxybutynin (ditropan)
To treat bladder spasms
119
Dicyclomine (bentyl)
to treat diarrhea- dominant IBS (with abdominal cramping)
120
Botox
``` Blocks release of Ach Used for: -urinary incontinence -chronic migraine -wrinkles ``` can cause Asthenia: speech, swallowing, numbness, ptosis- loss of TONE
121
Overall Adverse Effects of Muscarinic Antagonists
``` Dry mouth and eyes Mydriasis, cycloplegia Tachy Decreased GI motility Urinary retention ``` With high doses: hot and dry skin, decreased sweating
122
Contraindications of Muscarinic Antagonists
Acute- angle glaucome (bc M antagonists increase ocular pressure) Benign Prostate Hyperplasia (bc M antagonists cause urinary retention)
123
Atropine overdose
Hot, dry, blind, red face, agitation
124
Tx for Atropine overdose
Supportive Physostigmine to increase Ach levels in brain (helps to rescue the brain Muscarinic effects) bc Ach acts on M receptors in brain
125
Nicotinic receptor
quick depolarizing effects!!
126
Nondepolarizing NMJ blockers | none on drug list, understand mechanism
They are Ach antagonists Bind to Ach's place but do not emit a response. Solely paralysis
127
How do you reverse a Non depolarizing NMJ blocker?
Just add AcHe inhibitor | out compete the blocker
128
Nondepolarizing blockers
No CNS effects used for anesthesia in surgery
129
Depolarizing blocker
Succinylcholine opens up the channel: initial depolariztion and contraction THEN, blocks the channel: paralysis
130
Succinylcholine use
Tracheotomy or Intubation anesthesia | short procedures bc it's fast acting
131
Succinylchoine
longer lasting than Ach but still short acting IV only rapid onset: <90 sec Rapid recovery: 5-10 min hydrolyzed by plasma pseudocholinesterase
132
Amphetamine
Adderall
133
Methylphenidate
Ritalin
134
Methamphetamine
Desoxyn
135
Ach release onto Vagus nerve is responsible for
SLOWING heart down
136
Amphetamine
Adderall
137
Methylphenidate
Ritalin
138
DOC for ADHA
Amphetamine (Adderall) and Methylphenidate (Ritalin)
139
Do not eat Tyramine rich foods with
MAOIs | depression meds
140
INDIRECT acting adrenergic effectors
act on PRESYNAPTIC neuron to increase synthesis, cause release, inhibit reuptake/catabolism
141
examples of INDIRECT adrenergic effectors
Cocaine, Tyramine, Amphetamine, MAOIs
142
DIRECT acting adrenergic effectors
act on receptors on the TARGET TISSUE to mimic sympathetic stimulation
143
Denervation
Stops INDIRECT acting (bc damaging the pre-synaptic neuron which needs to be intact for these to work) May enhance DIRECT acting (bc receptor up regulation happens)
144
alpha 1 receptor
excitatory | specific agonist: phenylephrine
145
alpha 2 receptor
inhibitory PRE-synaptic specific agonist: Clonidine
146
All beta receptors
excitatory | Isoprot > NE and Epi
147
beta 1 receptor
spec agonist: Dobutamine
148
beta 2 receptor
spec agonist: Albuterol
149
beta 3 receptor
spec agonist: Mirabegron
150
D 1 receptor
excitatory | spec agonist: Fenoldopam
151
NE
acts on alpha 1 and beta 1 equally way down the road, acts on beta 2
152
NE use
RARELY used to increase BP in severe hypotensive crisis
153
NE pharmacokinetics
IV only | very short action
154
NE adverse effects
can cause Severe Vasoconstriction at infusion site (can necrose)
155
Epi (Adrenalin)
activates ALL adrenergic receptors Affinity: beta 1 and 2 first, then way down the road alpha 1
156
Epi (Adrenalin) use
Treat anaphylactic shock Decrease diffusion of injected drugs Glaucoma eye drops Emergency tx for cardiac arrest
157
Epi (Adrenalin) CV effects
Remember stimulates beta receptors first
158
Epi (Adrenalin) CV effects
bottom line: most clinical situations will be high dose- where alpha receptors are ultimately activated and Baroreceptor reflex slows the HR
159
Epi (Adrenalin) CV effects
low dose: HR stays high, only beta receptors activated | high dose: alpha receptors are reached, baroreflex kicks in, HR is slowed down
160
Epi (Adrenalin) adverse effects
Tremor, HA, inc BP, Tachy Angina in pts w/Heart dz Vasoconstriction can cause severe HTN and tissue necrosis
161
Epi (Adrenalin) contra-indications
Those taking Beta Blockers- will lead to severe HTN
162
Phenylephrine (Neofrin) mechanism
alpha 1 selective agonist
163
Phenylephrine (Neofrin) use
Vasoconstriction (increased BP but baroreflex takes HR back down) Hypotensive emergency Decongestant Mydriasis (topical)- eye exam
164
Phenylephrine (Neofrin) adverse effects
Rebound effect decongestant | Prolonges use: ischemic changes in mucous membranes
165
Phenylephrine (Neofrin) contraindications
Those w HTN and BPH
166
Pseudoephrine (Sudafed) mechanism
alpha 1 agonist | similar and more effective than phenylephrine
167
Oxymetazoline (Afrin) use
topically to cause vasoconstriction in eye and nares - decreases eye redness - decongestant
168
Oxymeazoline (Afrin) caution
closed angle glaucoma | HTN
169
Clonidine and Methyldopa
NOT 1st line drugs
170
Clonidine and Methyldopa
alpha 2 agonist | INHIBITORY- decrease sympathetic output from CNS
171
Clonidine and Methyldopa use
treat HTN (Methyldopa is one of recommended Pregnancy HTN drugs) Decrease addict cravings Decrease hot flashed Pre-anesthesia to dry up secretions
172
Clonidine and Methyldopa pharmacokinetics
Both oral | Clonidine offered as patch too
173
Clonidine and Methyldopa adverse effects
Xerostomia (dry mouth) Sedation Erectile Dysfx
174
Other adverse effects of Methyldopa
Hemolytic anemia w/pos coombs test Hepatotoxic Increased prolactin secretion --> gynecomastia and lactation
175
Contraindications to Clonidine and Methyldopa (alpha 2 agonists)
Not recommended for monotherapy Sudden withdrawal of Clonidine --> HTN crisis Avoid getting patch hot --> hypotension
176
Tizanidine mechanism
Alpha-2 agonist (inhibitory) | BUT less effect than Clonidine and Methyldopa
177
Tizanidine use
Reduce muscle spasticity in neuro conditions
178
Tizanidine pharmacokinetics
Short duration- used when spasticity muscle control is imp
179
Tizanidine adverse effects
Asthenia (dose related weakness, fatigue, tiredness)
180
Isoproterenol mechanism
very potent selective B1 and B2 agonist
181
Isoproterenol use
Emergency tx for cardiac arrest and complete heart block
182
Isoproterenol adverse effects
large doses: tachycardia, palpitations, arrhythmia
183
Dobutamine mechanism
beta 1 agonist
184
Dobutamine use
increase cardiac contractility and output often used in cardiac stress test
185
Dobutamine pharmacokinetics
given IV, short half life of ~2 min
186
Dobutamine adverse effect
if pt HTN, BP may increase if given too quickly
187
Albuterol (Ventolin)
beta 2 agonist
188
Albuterol (Ventolin) use and pharmacokinetics
Asthma | given orally or inhaled
189
Albuterol (Ventolin) adverse effects
HA, Tachycardia, tremor
190
Mirabegron mechanism
beta 3 agonist
191
Mirebegron use
Tx of overactive bladder
192
Mirebegron adverse effects
HTN, sinus tachycardia, nausea, HA, diarrhea, constipation, dizzy
193
Dopamine
DA agonist
194
Dopamine use
low dose- D1 receptors- renal vasodilation med dose- beta 1 receptors- ionotropic high dose- alpha receptors- vasoconstriction
195
Dopamine use
short term tx of severe refractory HF (useful if an increase in BP is needed)
196
Dopamine pharmacokinetics
IV | Metabolized by monoamine oxidase (MAO)
197
Fenoldopam mechanism
D1 agonist
198
Fenoldopam use
Emergency HTN situation- causes dilation of renal vascular beds which decreases BP
199
Fenoldopam pharmacokinetics
given IV, short half life of ~5 min
200
Fenoldopam adverse effects
Reflex tachy, HA, flushing
201
Indirect acting sympathomimetics (give "symp like" effects)
Amphetamine (Adderall) Methamphetamine (Desoxyn) Methylphenidate (Ritalin)
202
Mechanism of Indirect acting
Increase release of NE from neurons, esp in the CNS taken into neuron by NET, DISPLACES the neurotransmitter in vesicle causing it to be released
203
Why is methamphetamine a drug of abuse
more central actions and fewer peripheral effects
204
Amphetamine (Adderall) and Methylphenidate (Ritalin) use
CNS stimulants used for ADHD and narcolepsy
205
Amphetamine (Adderall) and Methylphenidate (Ritalin) adverse effects
Tremor, tachycardia, HTN Psychosis Also: restless, aggression, HA, angina, cerebral hemorrhalge, convulsions
206
Cocaine
Indirect acting sympathomimetic
207
Cocaine mechanism
inhibits re-uptake of DA and NE
208
Cocaine use
local anesthetic and powerful vasoconstrictor, rarely used for naroph surgery
209
Cocaine adverse effects
severe HTN and stroke Tachycardia--> arrhythmia and MI long term- cocaine induced psychoses
210
Cocaine and Amphetamine (Adderall) synergism
because cocaine prevents the reuptake of NE, and Amphetamine displaces more into the cleft
211
Tyramine (food component) mechanism
increase catecholamines from nerve terminals
212
Tyramine pharamcokinetics
rapidly hydrolyzed by Monoamine Oxidase (MAO) in GI tract and Liver Tachyphylaxis will develop (diminishing response)
213
Tyramine Contraindication
In pts treated for depression with MAOI (mao inhibitors) --> severe HTN crisis
214
Prazosin (Minipress)
highly selective alpha 1 antagonist
215
Prazosin (Minipress) use
Men who have BPH and HTN
216
Phenoxybenzamine
IRREVERSIBLe, non specific alpha antagonist
217
Phentolamine
nonspecific alpha antagonist
218
Tamsulosin (Flomax)
alpha 1 antagonist [different bc its more selective for alpha1A subtype (prostate) rather than alpha1B (blood vessels)]1
219
Tamsulosin (Flomax) use
BPH more selective for the prostate