DRUGS AFFECTING CHOLINERGIC TRANSMISSION Flashcards
(229 cards)
1
Q
Compounds that possess affinity for cholinergic receptors but exhibit no intrinsic activity
A
Cholinergic antagonists
Anticholinergics
Cholinolytics
Parasympatholitic agents
2
Q
Agents that mimic the sympathetic division
A
sympathomimetic agents
3
Q
Blocks the action of sympathetic division
A
sympatholitic agents
4
Q
What receptor play an essential role in regulating the functions of organs innervated by the ANS to maintain homeostasis?
A
Muscarinic Receptors
5
Q
mAChR stimulation results in at least 2 events:
A
Inhibition of adenylyl cyclase
Activation of phospholipase C and subsequent biosynthesis of secondary messengers.
6
Q
These are called neural muscarinic receptors
A
M1 receptors
7
Q
In addition to CNS, these receptors are located in exocrine glands and autonomic ganglia
A
M1
8
Q
These receptors affects K+ and Ca2+ levels in heart tissue
A
M2 receptors
9
Q
These are cardiac muscarinic receptors
A
M2
10
Q
These receptors when hyperpolarized, will result to bradycardia
A
M2
11
Q
These receptors are found in smooth muscles, in the parietal cells in the G1 and when stimulated, cause gastric secretion
A
M1
12
Q
Act through Gi protein to reduce adenylate cyclase activity and lower cAMP levels in cardiac cells
Lower cAMP levels decrease the amount of free Ca2+ in cardiac cells and slows down the heart rate.
A
M2
13
Q
These are glandular muscarinic receptors
A
M3
14
Q
These receptors are found in exocrine glands and smooth muscles
A
M3
15
Q
These receptors are mediated through G-protein activation of PLC to form IP3 and DAG
A
M3
16
Q
These receptors when stimulated, causes release of EDRF or known as nitrous oxide ~ vasodilation
A
M3
17
Q
Like M2 receptors, act through Gi protein to inhibit adenylate cyclase
A
M4
18
Q
These receptors regulates dopamine release at terminals within the striatum
A
M5
19
Q
These receptors have direct regulatory action on K+ and Ca2+ ion channels
A
M4
20
Q
True or False
Dilation of airways of the respiratory tract is the effect of acetylcholine
A
False - constriction
21
Q
True or False
Inhibition of contraction of the heart and relaxation of smooth muscle of blood vessels is an effect of acetylcholine
A
true
22
Q
Nicotinic receptors are found where?
A
skeletal neuromuscular junction
adrenal medulla
autonomic ganglia
23
Q
Both ganglionic neuronal (NN) and neuromuscular (somatic muscle) (NM) nAChRs are classified as what type of ion channel receptors?
A
ligand gated ion channel receptors
24
Q
True or False
nAChR creates a transmembrane ion channel (the gate), and the acetylcholine (ligand) serves as the gatekeeper by binding with nAChR ~ to modulate the passage of ions, Na+ and K+, through the channel.
A
true
25
Depolarizes the end plate ~ which results in muscular contraction at a ____________________
neuromuscular junction (N1)
26
Responses of acetylcholine mimetics or muscarinic agonists include:
Smooth muscle ______________
Vaso________
__________ secretion of exocrine glands
Pupillary __________
____________ heart rate and force of contraction
contraction
dilation
increased
constriction
decreased
27
TRUE OR FALSE
Acetylcholine lacks specificity for nicotinic and muscarinic receptors
True
28
Even if acetylcholinesterase is parenterally administered, action is fleeting as a result of hydrolysis by _______________________________
butyryl cholinesterase (plasma cholinesterase)
29
Is acetylcholine absorbed across lipid membranes? Why or Why not?
Acetylcholine is not absorbed across lipid membranes since it is a quaternary amine (charged molecule)
30
How many atoms should be between the nitrogen and the terminal hydrogen atom for maximal muscarinic potency?
no more than 5 atoms
31
What enantiomer of methacholine is equipotent with acetylcholine?
S (+) methacholine
32
What enantiomer of methacholine is 20-fold less potent with acetylcholine?
R (-) enantiomer
33
What enantiomer of methacholine is hydrolyzed slowly
S (+) methacholine
33
What enantiomer of methacholine is a weak inhibitor of AChE
R (-) enantiomer
34
Is less electrophilic and more stable than carboxylate esters to hydrolysis.
Carbonyl carbon
35
What do you call the esters derived from carbamic acid?
Carbamates
36
Modification of the Acyloxy group is the replacement of the acetoxy functional group with a functional group resistant to _____________.
hydrolysis
37
STRUCTURE ACTIVITY RELATIONSHIP FOR MUSCARINIC AGONIST ACTIVITY
Molecule must possess a ____________ capable of bearing a positive charge, preferably a quaternary ammonium salt
nitrogen atom
38
STRUCTURE ACTIVITY RELATIONSHIP FOR MUSCARINIC AGONIST ACTIVITY
For maximum potency, the size of the alkyl groups substituted on the nitrogen should (exceed, not exceed) the size of a methyl group
not exceed
39
STRUCTURE ACTIVITY RELATIONSHIP FOR MUSCARINIC AGONIST ACTIVITY
The molecule should have an __________, preferably an ester-like oxygen,
oxygen atom
40
STRUCTURE ACTIVITY RELATIONSHIP FOR MUSCARINIC AGONIST ACTIVITY
There should be a ___________ between the O2 and N2 atom
2-carbon unit
41
Another name of methacholine
acetyl b-methacholine
42
Brand name of Methacholine chloride
Provocholine
43
These agent has a selective muscarinic agonist with very little activity at nicotinic receptors
Methacholine chloride
44
What is the route of administration of methacholine and what condition will it diagnose?
via inhalation used to diagnose asthma
45
Brand name of Carbachol
Isopto Carbachol
46
It is a carbamate analog of acetylcholine
Carbachol
47
Does carbachol exhibits affinity for both muscarinic and nicotinic receptors?
YES
48
Carbachol is used in the treatment of what conditions?
glaucoma and induction of miosis
49
It has a weak anticholinesterase activity
Carbachol chloride
50
This muscarinic agent is more resistant to hydrolysis
Carbachol chloride
51
It is a carbamate analog of methacholine
Bethanechol chloride
52
Brand name of Bethanechol Chloride
Urecholine
53
Bethanechol chloride is selective to what receptors?
muscarinic receptors
54
Uses of Bethanechol Chloride
tx of postsurgical and postpartum urinary retention and abdominal distention
55
Route of administration of Bethanechol chloride
oral
56
What receptor is Pilocarpine Hydrochloride has affinity for?
M3
57
Pilocarpine Hydrochloride can be formulated as?
tablet
ophthalmic solution
gel
58
Pilocarpine hydrochloride is used in the treatment of
xerostomia
Sjogren syndrome
mucositis following chemotherapy
59
This muscarinic agent penetrate the eye and miotic of choice for open-angle glaucoma
Pilocarpine Hydrochloride
60
Alkali hydrolysis give what pharmacologically inactive compound?
hydroxy acid (pilocarpic acid)
61
Base catalyzed epimerization at ____ in the lactone give what stereoisomer?
C3
Isopilocarpine (inactive stereoisomer of pilocarpine)
62
It is a nonclassical muscarinic agonist
Cevimeline Hydrochloride
63
What derivative has Cevimeline has?
Quinuclidine derivative
64
Quinuclidine derivative has affinity to what muscarinic receptors?
M1 - CNS
M3 - lacrimal and salivary glands
65
What conditions is Cevimeline Chloride used?
Xerostomia
Sjogren syndrome
66
Elimination half life of Cevimeline
3 to 5 hours
67
Inhibition of the rapid hydrolysis by AChE _____________ the concentration of acetylcholine in the synapse ~ production of both muscarinic and nicotinic effects.
increases
68
Therapeutically used to improve muscle strength in myasthenia gravis
ACETYLCHOLINESTERASE INHIBITORS
69
Used in open angle glaucoma (through contraction of ciliary muscle and sphincter) to decrease IOP
ACETYLCHOLINESTERASE INHIBITORS
70
Recently used for the treatment of symptoms of Alzheimer’s disease
ACETYLCHOLINESTERASE INHIBITORS
71
Used extensively as insecticides and as chemical warfare agents
ACETYLCHOLINESTERASE INHIBITORS
72
What process regenerate the active form of AChE and acetic acid.
Hydrolysis
73
If the enzyme is acylated by a functional group like ______ or _______ that is more stable toward hydrolysis, enzyme remains inactive for a longer period of time.
carbamyl or phosphate
74
True Or False
Acylated enzyme cannot bind to another molecule of acetylcholine
True
75
Those compounds that are substrates for and react with AChE to form an acylated enzyme
REVERSIBLE ACETYLCHOLINESTERASE INHIBITORS
76
Those compounds that bind to AChE with greater affinity than acetylcholine but do not react with the enzyme as a substrate.
REVERSIBLE ACETYLCHOLINESTERASE INHIBITORS
77
Aryl carbamate AChEIs (e.g. physostigmine) bind to the catalytic site of AChE by _______________ of the carbamoyl group forming a “carbamylated enzyme”.
transesterification
78
Regeneration of active AChE by hydrolysis of the carbamylated enzyme is much _________ than hydrolysis of acetylated enzyme.
slower
79
Inhibits AChE by acting as a substrate and carbamylating the enzyme
Physostigmine
80
More lipophilic than any other AChEIs
Physostigmine
81
Uses of physostigmine
Used in ophthalmology for the treatment of glaucoma
Used to treat overdoses of compounds possessing anticholinergic effects (e.g. atropine and antidepressants)
82
Brand name of Neostigmine
PROSTIGMIN
83
A reversible AChEI that lacks central activity
Neostigmine
84
Elimination half life of Neostigmine
15 to 90 minutes
85
Indications of Neostigmine
Indicated for the prophylaxis of post operative abdominal distention and urinary retention, myasthenia gravis and reversal of neuromuscular
blockade
86
Brand name of Pyridostigmine
Mestinon
87
Closely related structure to neostigmine that incorporates the charged N into a pyridine ring.
Pyridostigmine
88
A reversible AChEI that has longer duration of action and a lower incidence of side effects
Pyridostigmine
89
Elimination half life of Pyridostigmine
1 to 2 hours
90
It is also administered parenterally to reverse the effects of nondepolarizing neuromuscular blocking agents
Pyridostigmine
91
A reversible, carbamate-derived AChEI
Carbaryl (Sevin)
92
Used as an insecticide for use on houseplants and vegetables and for the control of fleas and ticks on pets.
Carbaryl (Sevin)
93
A reversible AChEI that is a quarternary ammonium-substituted phenol
EDROPHONIUM CHLORIDE (ENLON®, REVERSOL®)
94
Does not carbamylate AChE but inhibits AChE in a reversible manner
EDROPHONIUM CHLORIDE (ENLON®, REVERSOL®)
95
It has a direct cholinomimetic effect at skeletal muscle Used IV for the diagnosis of myasthenia gravis (to increase muscle strength)
EDROPHONIUM CHLORIDE (ENLON®, REVERSOL®)
96
Elimination half life of Edrophonium Chloride
1.3 to 2.4 hours
97
IM: Reversal of effects of nondepolarizing blocking agents
EDROPHONIUM CHLORIDE (ENLON®, REVERSOL®
98
Structural changes of the brain accompanied by neurotransmitter dysfunction involving reduction in ACh, 5-HT, NE, dopamine and glutamate.
Alzheimer's Disease
99
First observable symptom of Alzheimer's Disease
Impairment of short-term memory
100
An aminoacridine; is a nonclassical inhibitor that binds to both AChE and butyrylcholinesterase
TACRINE HYDROCHLORIDE
(COGNEX®)
101
Why is the use of Tacrine Hydrochloride limited?
due to hepatotoxicity
102
Elimination half life of Tacrine Hydrochloride
1.5 to 4 hours
103
A “nonclassical”, centrally acting, reversible, noncompetitive AChEI for the treatment of mild-to-moderate AD and dementia
DONEPEZIL (ARICEPT®)
104
No potential for hepatotoxicity
DONEPEZIL (ARICEPT®)
105
Has a longer elimination half-life
DONEPEZIL (ARICEPT®)
106
A centrally selective, arylcarbamate AChEI for oral administration in the treatment of AD.
RIVASTIGMINE TARTRATE (EXELON®)
107
Inhibits both plasma cholinesterase and acetylcholinesterase
RIVASTIGMINE TARTRATE (EXELON®)
108
Inhibits AChE for up to 10 hours due to the slow hydrolysis of the carbamylated enzyme
Pseudo-irreversible AChEI
RIVASTIGMINE TARTRATE (EXELON®)
109
How much is the oral bioavailability of Rivastigmine?
40%
110
Exhibits a low potential of hepatotoxicity and drug-drug interactions due to lack of hepatic metabolism by CYP450 enzymes
RIVASTIGMINE TARTRATE (EXELON®)
111
A reversible inhibitor of AChE, but does not appear to inhibit butyrylcholinesterase
GALANTAMINE HYDROBROMIDE (RAZADYNE®)
112
Galantamine hydrobromide is what time of amine? Does it cross the BBB?
Tertiary Amine
Yes
113
Uses of Galantamine Hydrobromide
For mild-to-moderate AD and dementia
114
It allosterically binds to nAChRs giving it a dual cholinergic action
Not associated with hepatotoxicity
GALANTAMINE HYDROBROMIDE (RAZADYNE®)
115
What esters are very stable to hydrolysis?
Phosphate esters
116
Rate of hydrolysis is much ________ (measured in hours) for the phosphorylated enzyme
slower
117
Led to derivatives of _______________, _________________, ___________ that are effective inhibitors of AChE
phosphoric, pyrophosphoric and phosphonic acids
118
Phosphorylated AChE can undergo a process known as ____________
aging
119
is the result of hydrolysis of one or more of the phosphoester bonds while leaving the AChE phosphorylated ~ less likely to regenerate
aging
120
One of which is ______ (GB) ~ phosphorylates AChE, one aging reaction takes place and the enzyme becomes refractory to regeneration
sarin
121
What are nerve agents?
deadly phosphorus-derived chemical warfare
122
What are other organophosphate nerve acting agents?
Tabun and Soman
123
Found therapeutic application for the treatment of glaucoma and strabismus
ECHOTHIOPHATE IODIDE (PHOSPHOLINE IODIDE)
124
treatment for Isoflurophate toxicity?
atropine sulfate and magnesium sulfate
125
Isoflurophate has been used for the treatment of ____
glaucoma
126
Stable in peanut oil for a period of 1 year
ISOFLUROPHATE, USP
127
True Or false
Isoflurophate must be handled with extreme caution ~ contact should be avoided as it can be absorbed readily through the skin
True
128
Phosphoester AChEIs exhibit _____________ properties
cataractogenic
129
An irreversible AChEI that should be reserved for patients who are refractory to other forms of treatment.
ECHOTHIOPHATE IODIDE (PHOSPHOLINE IODIDE)
130
These irreversible AChEI are extermely lipophilic and extereme caution should be practiced in the presence of humans to prevent inhalation of the vapors or skin absorption
Insecticidal AChEI
131
are rapidly bioactivated to afford the corresponding oxoderivatives (phosphate esters) which are quite potent.
Thiono-compounds
132
Symptoms of Insecticidal AChEI
Nausea and vomiting
Excessive sweating and salivation
Miosis
Bradycardia, low blood pressure and difficulty of respiration
133
Organophosphate insecticide of low toxicity
Malathion
134
malathion generally cause poisoning only by _____ of large doses
ingestion
135
Parathion, or methylparathion, cause poisoning by ________ or ________ absorption.
inhalation or dermal
136
Used both as an aerial insecticide and clinically as a mitocide for topical treatment of hair and scalp lice infestations
MALATHION (OVIDE®)
137
Low transdermal absorption
Bioactivated to a toxic phosphate ester metabolite (in insects)
MALATHION (OVIDE®
138
Used as an agricultural insecticide and is a weak cholinesterase inhibitor
PARATHION
139
A metabolite of parathion in insects that is more potent inhibitor of cholinesterase
paraoxon
140
Not hydrolyzed by alkalis or water but is hydrolyzed by acids.
SCHRADAN
141
Used as a systemic insecticide for plants, being absorbed in plants without appreciable injury.
Insects feeding on the plant are incapacitated.
SCHRADAN
142
is a strong nucleophile that efficiently cleaves
phosphate esters and significantly increases the rate of reactivation of AChE.
Hydroxylamine (NH2OH)
143
Reaction of hydroxylamine with aldehydes and ketones affords _________, which possess the desired nucleophilic oxygen atom.
oximes
144
________________________ (2-PAM, 2-pyridine aldoxime methyl chloride) – clinically effective as an antidote for poisoning by phosphate ester AChEIs
Pralidoxime chloride
145
Nucleophilic attack of the oxime oxygen results in breaking of the ester bond between the __________ and the __________
Products: __________________
serine oxygen and phosphorous atom
Regenerated active form of AChE and phosphorylated 2-PAM
146
Route of administration of Pralidoxime Chloride
Parenterally ( SC, IM, IV)
147
How many hours after exposure of irreversible AChEI PRALIDOXIME CHLORIDE be given to have little reactivation of AChE
36
148
Have high binding affinity for mAChRs but exhibit no intrinsic activity
ACETYLCHOLINE ANTAGONISTS: MUSCARINIC ANTAGONISTS
149
ANTICHOLINERGIC TOXIDROME (Symptoms)
Mydriasis
Confusion, Delirium
Flushing, Dilation
Dry skin, Lack of diaphoresis
Fever, Hyperthermia
Bowel/urinary retention
150
1st compound shown to block the effects of muscarine
ATROPINE
151
Clinical uses of atropine
Treatment of bradycardia
Preoperative agent to reduce secretions prior to surgery
Management of parkinsonism
Cycloplegic agent (in ophthalmology)
Mydriatic agent
Decreases the muscarinic cholinergic symptoms in organophosphate poisoning
Lacrimation
Salivation
Sweating
Bradycardia
Breathing problems
152
Atropine is contraindicated in patients with _________
glaucoma
153
Elimination half life of Atropine
4 hours (in adults) and 6.5 hours (in children)
154
Scopolamine is marketed as _____________
Hydrobromide salt (less deliquescent)
155
Scopolamine is used in the treatment of?
uveitis, iritis, parkinsonism
156
Both atropine and acetylcholine are esters of amino alcohols, but they differ mainly on the ______ of the acyl portion ~ which was a major factor in blocking action.
size
157
Most potent antagonists were those that possessed ____________________________________________
two lipophilic ring substituents on the α-carbon of the ester moiety
158
Substituents R1 and R2 should be _________ or __________ rings for maximal antagonist potency.
carbocyclic or heterocyclic
159
R3 substituent can be a _________, ______________, a _________, or a __________________.
hydrogen atom
hydroxyl group
hydroxymethyl group
carboxamide
160
What substituent will make this antagonist more potent
hydroxyl or hydroxymethyl group
161
The X substituent in the most potent anticholinergic agents is an ________ ~ but is not an absolute necessity for muscarinic antagonist activity.
ester
162
The N substituent is a ____________ in the most anticholinergic agents ~ not a requirement because tertiary amines also possess antagonist
activity
quaternary ammonium salt
163
Alkyl substituents of anticholinergics are usually what?
methyl, ethyl, propyl, isopropyl
164
Tertiary amines possess antagonistic activity by binding to the receptor in what form?
cationic form
165
Length of the alkyl chain: from 2 to 4 carbons. The most potent anticholinergic agents have ___________ in this chain.
two methylene units
166
What are the different Amino alcohol Esters (synthetic cholinergic blocking drugs)
Dicyclomine HCl, Ipratropium Bromide, Tiotropium Bromide, Glycopyrrolate, Oxybutynin
167
Uses of Dicyclomine HCl
Dysmenorrhea
Pylorospasm
Biliary dysfunction
168
An anticholinergic that binds more firmly to M1 and M3
Dicyclomine HCl
169
Used for its spasmolytic effect on various smooth muscle spasms, particularly those associated with the GI tract.
Dicyclomine HCl
170
A quaternary ammonium derivative of atropine.
IPRATROPIUM BROMIDE (ATROVENT®)
171
Used in inhalation therapy to produce dilation of bronchial smooth muscle for acute asthmatic attacks
IPRATROPIUM BROMIDE (ATROVENT®)
172
Onset of action of Ipratopium Bromide
5 to 15 minutes
173
Antimuscarinic agent that is used in an inhalation device to deliver the drug into the lungs.
Indicated for the treatment of COPD, including chronic bronchitis and emphysema.
TIOTROPIUM BROMIDE (SPIRIVA®)
174
Daily dose of TIOTROPIUM BROMIDE (SPIRIVA®)
18 micrograms
175
It has a spasmolytic effect on the musculature of the GI tract as well as the genitourinary tract.
GYLCOPYRROLATE
176
It diminishes gastric and pancreatic secretions and the quantity of perspiration and saliva
GYLCOPYRROLATE
177
A cholinergic antagonist that is more potent on M1 than on M2 and M3 receptors
GYLCOPYRROLATE
178
By competitively blocking the muscarinic receptors, it has direct spasmolytic effects on bladder smooth muscle.
Use results to less urinary incontinence, urgency, and frequency
OXYBUTYNIN
179
Oxybutynin acts on what receptors?
M1, M2, M3
180
What are the different Amino ethers (synthetic cholinergic blocking drugs)
BENZTROPINE MESYLATE (COGENTIN®)
ORPHENADRINE CITRATE
181
Tremor and rigidity in parkinsonism are relieved by this agent
BENZTROPINE MESYLATE (COGENTIN®)
182
Has anticholinergic, antihistaminic, and local anesthetic properties.
BENZTROPINE MESYLATE (COGENTIN®)
183
Does not produce central stimulation but instead exerts the characteristic sedative effect of the antihistamines.
BENZTROPINE MESYLATE (COGENTIN®)
184
Closely related to diphenhydramine structurally but has much lower antihistaminic activity and much higher anticholinergic action.
ORPHENADRINE CITRATE
185
Symptomatic treatment of Parkinson’s disease
ORPHENADRINE CITRATE
186
What are the different anticholinergic Aminoethers?
BENZTROPINE MESYLATE (COGENTIN®
ORPHENADRINE CITRATE
187
Only weak effects on smooth muscle, eye and secretory glands
It does reduce voluntary muscle spasm, however, by a central inhibitory action (similar to atropine)
ORPHENADRINE CITRATE
188
What are the different anticholinergic AMINOALCOHOLS?
BIPERIDEN (AKINETON®)
TOLTERODINE
189
Drug is used in Parkinson’s disease and helps to eliminate akinesia, rigidity and tremor
BIPERIDEN (AKINETON®
190
Relatively weak visceral anticholinergic but a strong nicotinolytic.
It has a strong musculotropic action
BIPERIDEN (AKINETON®)
191
Biperiden is contraindicated in all forms of __________
Epilepsy
192
Is an antimuscarinic agent that acts on M2 and M3 muscarinic subtypes.
Results in a reduction of the smooth muscle tone, allowing for greater volume of urine to be stored in the bladder ~ less urinary incontinence, urgency and frequency.
TOLTERODINE
193
What are the different anticholinergic AMINOAMIDES?
TROPICAMIDE (MYDRIACYL®)
SOLIFENACIN
194
Anticholinergic for ophthalmic use
TROPICAMIDE (MYDRIACYL®)
195
Onset of action of Tropicamide
20-25 minutes
196
As with other mydriatics, however, pupil dilation can lead to increased intraocular pressure and is contraindicated in patients with glaucoma.
TROPICAMIDE (MYDRIACYL®)
197
Competitive antagonist for M1, M2 and M3 receptor subtypes ~ more pronounced as a M3 antagonist.
Selectivity of ____________________ for bladder muscarinic receptors over salivary receptors is superior to the effects observed with oxybutynin.
SOLIFENACIN
198
All therapeutically useful nicotinic antagonists are _______________________
competitive antagonists
199
Two subclasses of nicotinic antagonists:
Skeletal neuromuscular blocking agents
Ganglionic blocking agents
200
Depolarizes the end plate ~ which results in muscular contraction at a neuromuscular junction
Another is the continuation of a nerve impulse at the autonomic ganglia
NICOTINIC RECEPTORS
201
1st known neuromuscular blocking drug
Tubocucarine
202
South American natives using these plant extracts as arrow poisons.
Curare
203
The correct structure of tubocurarine, has only ___________; the other nitrogen is a _________
one quaternary ammonium nitrogen
tertiary amine salt
204
________________________ having _____ quaternary ammonium salts separated by _______ carbons ~ was a requirement for neuromuscular blocking activity
Bis-quarternary ammonium compound
2
10 to 12
205
nAChRs possessed ________, both of which have to be occupied for neuromuscular blocking activity
two anionic-binding sites
206
What are specific depolarizing neuromuscular blocking agents?
DECAMETHONIUM BROMIDE
SUCCINYLCHOLINE CHLORIDE (ANECTINE®)
207
One of the first neuromuscular blocking agents synthesized
DECAMETHONIUM BROMIDE
208
Maximal neuromuscular blockade occurred with 10 to 12 unsubstituted methylene groups
DECAMETHONIUM BROMIDE
209
– 6 methylene groups; a nicotinic antagonist at
autonomic ganglia (ganglionic blocking agent).
Hexamethonium
210
A depolarizing neuromuscular blocking agent that represents a dimer of acetylcholine bonded through α-carbon atom of each.
SUCCINYLCHOLINE CHLORIDE (ANECTINE®)
211
Rapidly hydrolyzed and rendered inactive both in aqueous solution and by plasma esterases.
SUCCINYLCHOLINE CHLORIDE (ANECTINE®)
212
Used for the rapid induction of neuromuscular blockade
Primarily used to produce muscle relaxation during endotracheal intubation or endoscopic procedures
SUCCINYLCHOLINE CHLORIDE (ANECTINE®)
213
What are specific non-depolarizing neuromuscular blocking agents?
D-TUBOCURARINE
METOCURINE (METUBINE IODIDE)
214
Given IV and has a relatively long duration of action
preparations contain _________(potentiate allergic reactions)
Most potent inducer of histamine release
D-TUBOCURARINE
215
Reaction of d-tubocurarine with methyl iodide afford _________
metocurine iodide
216
4-fold more potent than d-tubocurarine
Has a long duration of action and eliminated via kidneys
METOCURINE (METUBINE IODIDE)
217
An ideal neuromuscular blocking agent would be a ____________ that is metabolically inactivated and rapidly eliminated.
non-depolarizing compound
218
What are the different aminosteroid neuromuscular blocking agents
PANCURONIUM BROMIDE (PAVULON®)
VECURONIUM BROMIDE (NORCURON®)
PIPECURONIUM BROMIDE (ARDUAN®
ROCURONIUM BROMIDE (ZEMURON®)
219
A long-acting agent, more active than tubocurarine
Can increase heart rate and blood pressure
Avoided in patients with coronary artery disease
PANCURONIUM BROMIDE (PAVULON®
220
Removal of methyl group from the quaternary piperidinium group at position 3 of pancuronium
Has an advantage of not inducing histamine release at normal doses
Not exhibiting significant CV effects
3,17-dihydroxymetabolite – prolonged neuromuscular blockade
VECURONIUM BROMIDE (NORCURON®)
221
A long-acting neuromuscular blocking agent, exhibits minimal cardiovascular effects
Can be used in patients with CAD, but neuromuscular blockade is prolonged in patients with renal failure.
PIPECURONIUM BROMIDE (ARDUAN®)
222
An intermediate-acting agent
Rapid onset of action
Does not appear to cause significant histamine release
ROCURONIUM BROMIDE (ZEMURON®)
223
TETRAHYDROISOQUINOLINE-BASED NEUROMUSCULAR BLOCKING AGENTS ????
ATRACURIUM BESYLATE (TRACRIUM®)
MIVACURIUM CHLORIDE (MIVACRON®)
DOXACURIUM CHLORIDE (NUROMAX®)
224
Is a nondepolarizing neuromuscular blocker
Duration of action is slightly longer than succinylcholine
ATRACURIUM BESYLATE (TRACRIUM®)
225
What type of elimination does Atracurium Besylate undergo?
Hofmann elimination
226
Not metabolized in the liver ~ useful in patients with hepatic or renal disease
ATRACURIUM BESYLATE (TRACRIUM®)
227
Hydrophilic, has a small volume of distribution
Distributed primarily to extracellular fluids
Short-acting
Rapidly hydrolyzed
MIVACURIUM CHLORIDE (MIVACRON®)
228
Mixture of three trans-trans stereoisomers
is hydrophilic, has a small volume of distribution
Distributed primarily to extracellular fluids.
DOXACURIUM CHLORIDE (NUROMAX®
