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PH ORGMED LEC > DRUGS AFFECTING CHOLINERGIC TRANSMISSION > Flashcards

DRUGS AFFECTING CHOLINERGIC TRANSMISSION Flashcards

1
Q

Compounds that possess affinity for cholinergic receptors but exhibit no intrinsic activity

A

Cholinergic antagonists
Anticholinergics
Cholinolytics
Parasympatholitic agents

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2
Q

Agents that mimic the sympathetic division

A

sympathomimetic agents

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3
Q

Blocks the action of sympathetic division

A

sympatholitic agents

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4
Q

What receptor play an essential role in regulating the functions of organs innervated by the ANS to maintain homeostasis?

A

Muscarinic Receptors

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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.

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6
Q

These are called neural muscarinic receptors

A

M1 receptors

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7
Q

In addition to CNS, these receptors are located in exocrine glands and autonomic ganglia

A

M1

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8
Q

These receptors affects K+ and Ca2+ levels in heart tissue

A

M2 receptors

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9
Q

These are cardiac muscarinic receptors

A

M2

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10
Q

These receptors when hyperpolarized, will result to bradycardia

A

M2

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11
Q

These receptors are found in smooth muscles, in the parietal cells in the G1 and when stimulated, cause gastric secretion

A

M1

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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

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13
Q

These are glandular muscarinic receptors

A

M3

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14
Q

These receptors are found in exocrine glands and smooth muscles

A

M3

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15
Q

These receptors are mediated through G-protein activation of PLC to form IP3 and DAG

A

M3

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16
Q

These receptors when stimulated, causes release of EDRF or known as nitrous oxide ~ vasodilation

A

M3

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17
Q

Like M2 receptors, act through Gi protein to inhibit adenylate cyclase

A

M4

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18
Q

These receptors regulates dopamine release at terminals within the striatum

A

M5

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19
Q

These receptors have direct regulatory action on K+ and Ca2+ ion channels

A

M4

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20
Q

True or False

Dilation of airways of the respiratory tract is the effect of acetylcholine

A

False - constriction

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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

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22
Q

Nicotinic receptors are found where?

A

skeletal neuromuscular junction
adrenal medulla
autonomic ganglia

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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

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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

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25
Q

Depolarizes the end plate ~ which results in muscular contraction at a ____________________

A

neuromuscular junction (N1)

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26
Q

Responses of acetylcholine mimetics or muscarinic agonists include:

Smooth muscle ______________
Vaso________
__________ secretion of exocrine glands
Pupillary __________
____________ heart rate and force of contraction

A

contraction
dilation
increased
constriction
decreased

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27
Q

TRUE OR FALSE

Acetylcholine lacks specificity for nicotinic and muscarinic receptors

A

True

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28
Q

Even if acetylcholinesterase is parenterally administered, action is fleeting as a result of hydrolysis by _______________________________

A

butyryl cholinesterase (plasma cholinesterase)

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29
Q

Is acetylcholine absorbed across lipid membranes? Why or Why not?

A

Acetylcholine is not absorbed across lipid membranes since it is a quaternary amine (charged molecule)

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30
Q

How many atoms should be between the nitrogen and the terminal hydrogen atom for maximal muscarinic potency?

A

no more than 5 atoms

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31
Q

What enantiomer of methacholine is equipotent with acetylcholine?

A

S (+) methacholine

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32
Q

What enantiomer of methacholine is 20-fold less potent with acetylcholine?

A

R (-) enantiomer

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33
Q

What enantiomer of methacholine is hydrolyzed slowly

A

S (+) methacholine

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33
Q

What enantiomer of methacholine is a weak inhibitor of AChE

A

R (-) enantiomer

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34
Q

Is less electrophilic and more stable than carboxylate esters to hydrolysis.

A

Carbonyl carbon

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35
Q

What do you call the esters derived from carbamic acid?

A

Carbamates

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36
Q

Modification of the Acyloxy group is the replacement of the acetoxy functional group with a functional group resistant to _____________.

A

hydrolysis

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37
Q

STRUCTURE ACTIVITY RELATIONSHIP FOR MUSCARINIC AGONIST ACTIVITY

Molecule must possess a ____________ capable of bearing a positive charge, preferably a quaternary ammonium salt

A

nitrogen atom

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38
Q

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

A

not exceed

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39
Q

STRUCTURE ACTIVITY RELATIONSHIP FOR MUSCARINIC AGONIST ACTIVITY

The molecule should have an __________, preferably an ester-like oxygen,

A

oxygen atom

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40
Q

STRUCTURE ACTIVITY RELATIONSHIP FOR MUSCARINIC AGONIST ACTIVITY

There should be a ___________ between the O2 and N2 atom

A

2-carbon unit

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41
Q

Another name of methacholine

A

acetyl b-methacholine

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42
Q

Brand name of Methacholine chloride

A

Provocholine

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43
Q

These agent has a selective muscarinic agonist with very little activity at nicotinic receptors

A

Methacholine chloride

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44
Q

What is the route of administration of methacholine and what condition will it diagnose?

A

via inhalation used to diagnose asthma

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45
Q

Brand name of Carbachol

A

Isopto Carbachol

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46
Q

It is a carbamate analog of acetylcholine

A

Carbachol

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47
Q

Does carbachol exhibits affinity for both muscarinic and nicotinic receptors?

A

YES

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48
Q

Carbachol is used in the treatment of what conditions?

A

glaucoma and induction of miosis

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49
Q

It has a weak anticholinesterase activity

A

Carbachol chloride

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50
Q

This muscarinic agent is more resistant to hydrolysis

A

Carbachol chloride

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51
Q

It is a carbamate analog of methacholine

A

Bethanechol chloride

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52
Q

Brand name of Bethanechol Chloride

A

Urecholine

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53
Q

Bethanechol chloride is selective to what receptors?

A

muscarinic receptors

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54
Q

Uses of Bethanechol Chloride

A

tx of postsurgical and postpartum urinary retention and abdominal distention

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55
Q

Route of administration of Bethanechol chloride

A

oral

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56
Q

What receptor is Pilocarpine Hydrochloride has affinity for?

A

M3

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57
Q

Pilocarpine Hydrochloride can be formulated as?

A

tablet
ophthalmic solution
gel

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58
Q

Pilocarpine hydrochloride is used in the treatment of

A

xerostomia
Sjogren syndrome
mucositis following chemotherapy

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59
Q

This muscarinic agent penetrate the eye and miotic of choice for open-angle glaucoma

A

Pilocarpine Hydrochloride

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60
Q

Alkali hydrolysis give what pharmacologically inactive compound?

A

hydroxy acid (pilocarpic acid)

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61
Q

Base catalyzed epimerization at ____ in the lactone give what stereoisomer?

A

C3
Isopilocarpine (inactive stereoisomer of pilocarpine)

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62
Q

It is a nonclassical muscarinic agonist

A

Cevimeline Hydrochloride

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63
Q

What derivative has Cevimeline has?

A

Quinuclidine derivative

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64
Q

Quinuclidine derivative has affinity to what muscarinic receptors?

A

M1 - CNS
M3 - lacrimal and salivary glands

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65
Q

What conditions is Cevimeline Chloride used?

A

Xerostomia
Sjogren syndrome

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66
Q

Elimination half life of Cevimeline

A

3 to 5 hours

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67
Q

Inhibition of the rapid hydrolysis by AChE _____________ the concentration of acetylcholine in the synapse ~ production of both muscarinic and nicotinic effects.

A

increases

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68
Q

Therapeutically used to improve muscle strength in myasthenia gravis

A

ACETYLCHOLINESTERASE INHIBITORS

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69
Q

Used in open angle glaucoma (through contraction of ciliary muscle and sphincter) to decrease IOP

A

ACETYLCHOLINESTERASE INHIBITORS

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70
Q

Recently used for the treatment of symptoms of Alzheimer’s disease

A

ACETYLCHOLINESTERASE INHIBITORS

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71
Q

Used extensively as insecticides and as chemical warfare agents

A

ACETYLCHOLINESTERASE INHIBITORS

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72
Q

What process regenerate the active form of AChE and acetic acid.

A

Hydrolysis

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73
Q

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.

A

carbamyl or phosphate

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74
Q

True Or False

Acylated enzyme cannot bind to another molecule of acetylcholine

A

True

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75
Q

Those compounds that are substrates for and react with AChE to form an acylated enzyme

A

REVERSIBLE ACETYLCHOLINESTERASE INHIBITORS

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76
Q

Those compounds that bind to AChE with greater affinity than acetylcholine but do not react with the enzyme as a substrate.

A

REVERSIBLE ACETYLCHOLINESTERASE INHIBITORS

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77
Q

Aryl carbamate AChEIs (e.g. physostigmine) bind to the catalytic site of AChE by _______________ of the carbamoyl group forming a “carbamylated enzyme”.

A

transesterification

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78
Q

Regeneration of active AChE by hydrolysis of the carbamylated enzyme is much _________ than hydrolysis of acetylated enzyme.

A

slower

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79
Q

Inhibits AChE by acting as a substrate and carbamylating the enzyme

A

Physostigmine

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80
Q

More lipophilic than any other AChEIs

A

Physostigmine

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81
Q

Uses of physostigmine

A

Used in ophthalmology for the treatment of glaucoma
Used to treat overdoses of compounds possessing anticholinergic effects (e.g. atropine and antidepressants)

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82
Q

Brand name of Neostigmine

A

PROSTIGMIN

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83
Q

A reversible AChEI that lacks central activity

A

Neostigmine

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84
Q

Elimination half life of Neostigmine

A

15 to 90 minutes

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85
Q

Indications of Neostigmine

A

Indicated for the prophylaxis of post operative abdominal distention and urinary retention, myasthenia gravis and reversal of neuromuscular
blockade

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86
Q

Brand name of Pyridostigmine

A

Mestinon

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87
Q

Closely related structure to neostigmine that incorporates the charged N into a pyridine ring.

A

Pyridostigmine

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88
Q

A reversible AChEI that has longer duration of action and a lower incidence of side effects

A

Pyridostigmine

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89
Q

Elimination half life of Pyridostigmine

A

1 to 2 hours

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90
Q

It is also administered parenterally to reverse the effects of nondepolarizing neuromuscular blocking agents

A

Pyridostigmine

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91
Q

A reversible, carbamate-derived AChEI

A

Carbaryl (Sevin)

92
Q

Used as an insecticide for use on houseplants and vegetables and for the control of fleas and ticks on pets.

A

Carbaryl (Sevin)

93
Q

A reversible AChEI that is a quarternary ammonium-substituted phenol

A

EDROPHONIUM CHLORIDE (ENLON®, REVERSOL®)

94
Q

Does not carbamylate AChE but inhibits AChE in a reversible manner

A

EDROPHONIUM CHLORIDE (ENLON®, REVERSOL®)

95
Q

It has a direct cholinomimetic effect at skeletal muscle Used IV for the diagnosis of myasthenia gravis (to increase muscle strength)

A

EDROPHONIUM CHLORIDE (ENLON®, REVERSOL®)

96
Q

Elimination half life of Edrophonium Chloride

A

1.3 to 2.4 hours

97
Q

IM: Reversal of effects of nondepolarizing blocking agents

A

EDROPHONIUM CHLORIDE (ENLON®, REVERSOL®

98
Q

Structural changes of the brain accompanied by neurotransmitter dysfunction involving reduction in ACh, 5-HT, NE, dopamine and glutamate.

A

Alzheimer’s Disease

99
Q

First observable symptom of Alzheimer’s Disease

A

Impairment of short-term memory

100
Q

An aminoacridine; is a nonclassical inhibitor that binds to both AChE and butyrylcholinesterase

A

TACRINE HYDROCHLORIDE
(COGNEX®)

101
Q

Why is the use of Tacrine Hydrochloride limited?

A

due to hepatotoxicity

102
Q

Elimination half life of Tacrine Hydrochloride

A

1.5 to 4 hours

103
Q

A “nonclassical”, centrally acting, reversible, noncompetitive AChEI for the treatment of mild-to-moderate AD and dementia

A

DONEPEZIL (ARICEPT®)

104
Q

No potential for hepatotoxicity

A

DONEPEZIL (ARICEPT®)

105
Q

Has a longer elimination half-life

A

DONEPEZIL (ARICEPT®)

106
Q

A centrally selective, arylcarbamate AChEI for oral administration in the treatment of AD.

A

RIVASTIGMINE TARTRATE (EXELON®)

107
Q

Inhibits both plasma cholinesterase and acetylcholinesterase

A

RIVASTIGMINE TARTRATE (EXELON®)

108
Q

Inhibits AChE for up to 10 hours due to the slow hydrolysis of the carbamylated enzyme
Pseudo-irreversible AChEI

A

RIVASTIGMINE TARTRATE (EXELON®)

109
Q

How much is the oral bioavailability of Rivastigmine?

A

40%

110
Q

Exhibits a low potential of hepatotoxicity and drug-drug interactions due to lack of hepatic metabolism by CYP450 enzymes

A

RIVASTIGMINE TARTRATE (EXELON®)

111
Q

A reversible inhibitor of AChE, but does not appear to inhibit butyrylcholinesterase

A

GALANTAMINE HYDROBROMIDE (RAZADYNE®)

112
Q

Galantamine hydrobromide is what time of amine? Does it cross the BBB?

A

Tertiary Amine
Yes

113
Q

Uses of Galantamine Hydrobromide

A

For mild-to-moderate AD and dementia

114
Q

It allosterically binds to nAChRs giving it a dual cholinergic action
Not associated with hepatotoxicity

A

GALANTAMINE HYDROBROMIDE (RAZADYNE®)

115
Q

What esters are very stable to hydrolysis?

A

Phosphate esters

116
Q

Rate of hydrolysis is much ________ (measured in hours) for the phosphorylated enzyme

A

slower

117
Q

Led to derivatives of _______________, _________________, ___________ that are effective inhibitors of AChE

A

phosphoric, pyrophosphoric and phosphonic acids

118
Q

Phosphorylated AChE can undergo a process known as ____________

A

aging

119
Q

is the result of hydrolysis of one or more of the phosphoester bonds while leaving the AChE phosphorylated ~ less likely to regenerate

A

aging

120
Q

One of which is ______ (GB) ~ phosphorylates AChE, one aging reaction takes place and the enzyme becomes refractory to regeneration

A

sarin

121
Q

What are nerve agents?

A

deadly phosphorus-derived chemical warfare

122
Q

What are other organophosphate nerve acting agents?

A

Tabun and Soman

123
Q

Found therapeutic application for the treatment of glaucoma and strabismus

A

ECHOTHIOPHATE IODIDE (PHOSPHOLINE IODIDE)

124
Q

treatment for Isoflurophate toxicity?

A

atropine sulfate and magnesium sulfate

125
Q

Isoflurophate has been used for the treatment of ____

A

glaucoma

126
Q

Stable in peanut oil for a period of 1 year

A

ISOFLUROPHATE, USP

127
Q

True Or false

Isoflurophate must be handled with extreme caution ~ contact should be avoided as it can be absorbed readily through the skin

A

True

128
Q

Phosphoester AChEIs exhibit _____________ properties

A

cataractogenic

129
Q

An irreversible AChEI that should be reserved for patients who are refractory to other forms of treatment.

A

ECHOTHIOPHATE IODIDE (PHOSPHOLINE IODIDE)

130
Q

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

A

Insecticidal AChEI

131
Q

are rapidly bioactivated to afford the corresponding oxoderivatives (phosphate esters) which are quite potent.

A

Thiono-compounds

132
Q

Symptoms of Insecticidal AChEI

A

Nausea and vomiting
Excessive sweating and salivation
Miosis
Bradycardia, low blood pressure and difficulty of respiration

133
Q

Organophosphate insecticide of low toxicity

A

Malathion

134
Q

malathion generally cause poisoning only by _____ of large doses

A

ingestion

135
Q

Parathion, or methylparathion, cause poisoning by ________ or ________ absorption.

A

inhalation or dermal

136
Q

Used both as an aerial insecticide and clinically as a mitocide for topical treatment of hair and scalp lice infestations

A

MALATHION (OVIDE®)

137
Q

Low transdermal absorption
Bioactivated to a toxic phosphate ester metabolite (in insects)

A

MALATHION (OVIDE®

138
Q

Used as an agricultural insecticide and is a weak cholinesterase inhibitor

A

PARATHION

139
Q

A metabolite of parathion in insects that is more potent inhibitor of cholinesterase

A

paraoxon

140
Q

Not hydrolyzed by alkalis or water but is hydrolyzed by acids.

A

SCHRADAN

141
Q

Used as a systemic insecticide for plants, being absorbed in plants without appreciable injury.
Insects feeding on the plant are incapacitated.

A

SCHRADAN

142
Q

is a strong nucleophile that efficiently cleaves
phosphate esters and significantly increases the rate of reactivation of AChE.

A

Hydroxylamine (NH2OH)

143
Q

Reaction of hydroxylamine with aldehydes and ketones affords _________, which possess the desired nucleophilic oxygen atom.

A

oximes

144
Q

________________________ (2-PAM, 2-pyridine aldoxime methyl chloride) – clinically effective as an antidote for poisoning by phosphate ester AChEIs

A

Pralidoxime chloride

145
Q

Nucleophilic attack of the oxime oxygen results in breaking of the ester bond between the __________ and the __________

Products: __________________

A

serine oxygen and phosphorous atom

Regenerated active form of AChE and phosphorylated 2-PAM

146
Q

Route of administration of Pralidoxime Chloride

A

Parenterally ( SC, IM, IV)

147
Q

How many hours after exposure of irreversible AChEI PRALIDOXIME CHLORIDE be given to have little reactivation of AChE

A

36

148
Q

Have high binding affinity for mAChRs but exhibit no intrinsic activity

A

ACETYLCHOLINE ANTAGONISTS: MUSCARINIC ANTAGONISTS

149
Q

ANTICHOLINERGIC TOXIDROME (Symptoms)

A

Mydriasis
Confusion, Delirium
Flushing, Dilation
Dry skin, Lack of diaphoresis
Fever, Hyperthermia
Bowel/urinary retention

150
Q

1st compound shown to block the effects of muscarine

A

ATROPINE

151
Q

Clinical uses of atropine

A

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
Q

Atropine is contraindicated in patients with _________

A

glaucoma

153
Q

Elimination half life of Atropine

A

4 hours (in adults) and 6.5 hours (in children)

154
Q

Scopolamine is marketed as _____________

A

Hydrobromide salt (less deliquescent)

155
Q

Scopolamine is used in the treatment of?

A

uveitis, iritis, parkinsonism

156
Q

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.

A

size

157
Q

Most potent antagonists were those that possessed ____________________________________________

A

two lipophilic ring substituents on the α-carbon of the ester moiety

158
Q

Substituents R1 and R2 should be _________ or __________ rings for maximal antagonist potency.

A

carbocyclic or heterocyclic

159
Q

R3 substituent can be a _________, ______________, a _________, or a __________________.

A

hydrogen atom
hydroxyl group
hydroxymethyl group
carboxamide

160
Q

What substituent will make this antagonist more potent

A

hydroxyl or hydroxymethyl group

161
Q

The X substituent in the most potent anticholinergic agents is an ________ ~ but is not an absolute necessity for muscarinic antagonist activity.

A

ester

162
Q

The N substituent is a ____________ in the most anticholinergic agents ~ not a requirement because tertiary amines also possess antagonist
activity

A

quaternary ammonium salt

163
Q

Alkyl substituents of anticholinergics are usually what?

A

methyl, ethyl, propyl, isopropyl

164
Q

Tertiary amines possess antagonistic activity by binding to the receptor in what form?

A

cationic form

165
Q

Length of the alkyl chain: from 2 to 4 carbons. The most potent anticholinergic agents have ___________ in this chain.

A

two methylene units

166
Q

What are the different Amino alcohol Esters (synthetic cholinergic blocking drugs)

A

Dicyclomine HCl, Ipratropium Bromide, Tiotropium Bromide, Glycopyrrolate, Oxybutynin

167
Q

Uses of Dicyclomine HCl

A

Dysmenorrhea
Pylorospasm
Biliary dysfunction

168
Q

An anticholinergic that binds more firmly to M1 and M3

A

Dicyclomine HCl

169
Q

Used for its spasmolytic effect on various smooth muscle spasms, particularly those associated with the GI tract.

A

Dicyclomine HCl

170
Q

A quaternary ammonium derivative of atropine.

A

IPRATROPIUM BROMIDE (ATROVENT®)

171
Q

Used in inhalation therapy to produce dilation of bronchial smooth muscle for acute asthmatic attacks

A

IPRATROPIUM BROMIDE (ATROVENT®)

172
Q

Onset of action of Ipratopium Bromide

A

5 to 15 minutes

173
Q

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.

A

TIOTROPIUM BROMIDE (SPIRIVA®)

174
Q

Daily dose of TIOTROPIUM BROMIDE (SPIRIVA®)

A

18 micrograms

175
Q

It has a spasmolytic effect on the musculature of the GI tract as well as the genitourinary tract.

A

GYLCOPYRROLATE

176
Q

It diminishes gastric and pancreatic secretions and the quantity of perspiration and saliva

A

GYLCOPYRROLATE

177
Q

A cholinergic antagonist that is more potent on M1 than on M2 and M3 receptors

A

GYLCOPYRROLATE

178
Q

By competitively blocking the muscarinic receptors, it has direct spasmolytic effects on bladder smooth muscle.

Use results to less urinary incontinence, urgency, and frequency

A

OXYBUTYNIN

179
Q

Oxybutynin acts on what receptors?

A

M1, M2, M3

180
Q

What are the different Amino ethers (synthetic cholinergic blocking drugs)

A

BENZTROPINE MESYLATE (COGENTIN®)
ORPHENADRINE CITRATE

181
Q

Tremor and rigidity in parkinsonism are relieved by this agent

A

BENZTROPINE MESYLATE (COGENTIN®)

182
Q

Has anticholinergic, antihistaminic, and local anesthetic properties.

A

BENZTROPINE MESYLATE (COGENTIN®)

183
Q

Does not produce central stimulation but instead exerts the characteristic sedative effect of the antihistamines.

A

BENZTROPINE MESYLATE (COGENTIN®)

184
Q

Closely related to diphenhydramine structurally but has much lower antihistaminic activity and much higher anticholinergic action.

A

ORPHENADRINE CITRATE

185
Q

Symptomatic treatment of Parkinson’s disease

A

ORPHENADRINE CITRATE

186
Q

What are the different anticholinergic Aminoethers?

A

BENZTROPINE MESYLATE (COGENTIN®
ORPHENADRINE CITRATE

187
Q

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)

A

ORPHENADRINE CITRATE

188
Q

What are the different anticholinergic AMINOALCOHOLS?

A

BIPERIDEN (AKINETON®)
TOLTERODINE

189
Q

Drug is used in Parkinson’s disease and helps to eliminate akinesia, rigidity and tremor

A

BIPERIDEN (AKINETON®

190
Q

Relatively weak visceral anticholinergic but a strong nicotinolytic.
It has a strong musculotropic action

A

BIPERIDEN (AKINETON®)

191
Q

Biperiden is contraindicated in all forms of __________

A

Epilepsy

192
Q

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.

A

TOLTERODINE

193
Q

What are the different anticholinergic AMINOAMIDES?

A

TROPICAMIDE (MYDRIACYL®)
SOLIFENACIN

194
Q

Anticholinergic for ophthalmic use

A

TROPICAMIDE (MYDRIACYL®)

195
Q

Onset of action of Tropicamide

A

20-25 minutes

196
Q

As with other mydriatics, however, pupil dilation can lead to increased intraocular pressure and is contraindicated in patients with glaucoma.

A

TROPICAMIDE (MYDRIACYL®)

197
Q

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.

A

SOLIFENACIN

198
Q

All therapeutically useful nicotinic antagonists are _______________________

A

competitive antagonists

199
Q

Two subclasses of nicotinic antagonists:

A

Skeletal neuromuscular blocking agents
Ganglionic blocking agents

200
Q

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

A

NICOTINIC RECEPTORS

201
Q

1st known neuromuscular blocking drug

A

Tubocucarine

202
Q

South American natives using these plant extracts as arrow poisons.

A

Curare

203
Q

The correct structure of tubocurarine, has only ___________; the other nitrogen is a _________

A

one quaternary ammonium nitrogen
tertiary amine salt

204
Q

________________________ having _____ quaternary ammonium salts separated by _______ carbons ~ was a requirement for neuromuscular blocking activity

A

Bis-quarternary ammonium compound
2
10 to 12

205
Q

nAChRs possessed ________, both of which have to be occupied for neuromuscular blocking activity

A

two anionic-binding sites

206
Q

What are specific depolarizing neuromuscular blocking agents?

A

DECAMETHONIUM BROMIDE
SUCCINYLCHOLINE CHLORIDE (ANECTINE®)

207
Q

One of the first neuromuscular blocking agents synthesized

A

DECAMETHONIUM BROMIDE

208
Q

Maximal neuromuscular blockade occurred with 10 to 12 unsubstituted methylene groups

A

DECAMETHONIUM BROMIDE

209
Q

– 6 methylene groups; a nicotinic antagonist at
autonomic ganglia (ganglionic blocking agent).

A

Hexamethonium

210
Q

A depolarizing neuromuscular blocking agent that represents a dimer of acetylcholine bonded through α-carbon atom of each.

A

SUCCINYLCHOLINE CHLORIDE (ANECTINE®)

211
Q

Rapidly hydrolyzed and rendered inactive both in aqueous solution and by plasma esterases.

A

SUCCINYLCHOLINE CHLORIDE (ANECTINE®)

212
Q

Used for the rapid induction of neuromuscular blockade
Primarily used to produce muscle relaxation during endotracheal intubation or endoscopic procedures

A

SUCCINYLCHOLINE CHLORIDE (ANECTINE®)

213
Q

What are specific non-depolarizing neuromuscular blocking agents?

A

D-TUBOCURARINE
METOCURINE (METUBINE IODIDE)

214
Q

Given IV and has a relatively long duration of action

preparations contain _________(potentiate allergic reactions)
Most potent inducer of histamine release

A

D-TUBOCURARINE

215
Q

Reaction of d-tubocurarine with methyl iodide afford _________

A

metocurine iodide

216
Q

4-fold more potent than d-tubocurarine
Has a long duration of action and eliminated via kidneys

A

METOCURINE (METUBINE IODIDE)

217
Q

An ideal neuromuscular blocking agent would be a ____________ that is metabolically inactivated and rapidly eliminated.

A

non-depolarizing compound

218
Q

What are the different aminosteroid neuromuscular blocking agents

A

PANCURONIUM BROMIDE (PAVULON®)
VECURONIUM BROMIDE (NORCURON®)
PIPECURONIUM BROMIDE (ARDUAN®
ROCURONIUM BROMIDE (ZEMURON®)

219
Q

A long-acting agent, more active than tubocurarine
Can increase heart rate and blood pressure
Avoided in patients with coronary artery disease

A

PANCURONIUM BROMIDE (PAVULON®

220
Q

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

A

VECURONIUM BROMIDE (NORCURON®)

221
Q

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.

A

PIPECURONIUM BROMIDE (ARDUAN®)

222
Q

An intermediate-acting agent
Rapid onset of action
Does not appear to cause significant histamine release

A

ROCURONIUM BROMIDE (ZEMURON®)

223
Q

TETRAHYDROISOQUINOLINE-BASED NEUROMUSCULAR BLOCKING AGENTS ????

A

ATRACURIUM BESYLATE (TRACRIUM®)
MIVACURIUM CHLORIDE (MIVACRON®)
DOXACURIUM CHLORIDE (NUROMAX®)

224
Q

Is a nondepolarizing neuromuscular blocker
Duration of action is slightly longer than succinylcholine

A

ATRACURIUM BESYLATE (TRACRIUM®)

225
Q

What type of elimination does Atracurium Besylate undergo?

A

Hofmann elimination

226
Q

Not metabolized in the liver ~ useful in patients with hepatic or renal disease

A

ATRACURIUM BESYLATE (TRACRIUM®)

227
Q

Hydrophilic, has a small volume of distribution
Distributed primarily to extracellular fluids
Short-acting
Rapidly hydrolyzed

A

MIVACURIUM CHLORIDE (MIVACRON®)

228
Q

Mixture of three trans-trans stereoisomers
is hydrophilic, has a small volume of distribution
Distributed primarily to extracellular fluids.

A

DOXACURIUM CHLORIDE (NUROMAX®

PH ORGMED LEC (1 decks)

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