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PH 113 - Pharmacology 1 > PRELIM 06 - Cholinergic Agonists and Antagonists > Flashcards

PRELIM 06 - Cholinergic Agonists and Antagonists Flashcards

1
Q

Cholinomimetics that bind to and activate nicotinic and muscarinic receptors (Types of cholinomimetics)

A

Direct-acting cholinomimetics

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2
Q

Composed of an ester group (Types of direct-acting cholinomimetics)

A

Choline esters

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3
Q

__________ and __________ have methyl groups on the beta carbon; (Examples of choline esters) (MB)

A

Methacholine, Bethanechol

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4
Q

__________ and __________ are carbamoyl esters; they are selective for muscarinic receptors (Examples of choline esters) (BC)

A

Bethanechol, Carbachol

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5
Q

Choline esters are poorly __________ and __________ (AD)

A

Absorbed, Distributed

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6
Q

Choline esters are excreted through __________

A

Rapid renal excretion

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7
Q

Used for induction of miosis during ophthalmic surgery as ophthalmic solution (Examples of choline esters)

A

Acetylcholine

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8
Q

Used for diagnosis of bronchial of bronchial airway hyperactivity in patients who do not have clinically apparent asthma (Examples of choline esters)

A

Methacholine

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9
Q

Used for treatment of urinary retention; a prokinetic (Examples of choline esters)

A

Bethanechol

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10
Q

Used for treatment of glaucoma and induction of miosis during surgery as ophthalmic solution (Examples of choline esters)

A

Carbachol

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11
Q

Contains nitrogen-containing heterocyclic groups (Types of direct-acting cholinomimetics)

A

Cholinomimetic alkaloids

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12
Q

Derived from Amanita muscaria (Examples of cholinomimetic alkaloids)

A

Muscarine

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13
Q

Derived from Pilocarpus sp. (Examples of cholinomimetic alkaloids)

A

Pilocarpine

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14
Q

Derived from Areca catechu (Examples of cholinomimetic alkaloids)

A

Arecoline

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15
Q

Derived from Nicotiana tabacum (Examples of cholinomimetic alkaloids)

A

Nicotine

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16
Q

Muscarine is poorly __________ and __________ but can still cross the BBB (AD)

A

Absorbed, Distributed

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17
Q

Tertiary amines are rapidly __________ and crosses the BBB

A

Absorbed

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18
Q

Cholinomimetic alkaloids are excreted through __________

A

Renal excretion

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19
Q

Muscarine is a muscarinic alkaloid that is an __________

A

Agonist

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20
Q

Pilocarpine is a muscarinic alkaloid that is a __________

A

Partial agonist

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21
Q

An example of cholinomimetic alkaloid with both muscarinic and nicotinic activity is __________

A

Arecoline

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22
Q

Used for treatment of glaucoma and xerostomia, and is used as a miotic agent as ophthalmic solution (Examples of cholinomimetic alkaloids)

A

Pilocarpine

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23
Q

In the cardiovascular system, nicotine serves as a __________

A

Sympathomimetic

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24
Q

In the gastrointestinal and genitourinary tract, nicotine serves as a __________

A

Parasympathomimetic

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25
Q

A quinuclidine derivative of acetylcholine; used for the treatment of xerostomia (Types of direct-acting cholinomimetics)

A

Cevimeline

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26
Q

Overdose from muscarinic agonists may be treated with __________

A

Atropine

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27
Q

Overdose from nicotinic agonists may be treated with __________ and __________ (AD)

A

Atropine, Diazepam

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28
Q

Bind to and inactivate acetylcholinesterase; thereby increasing acetylcholine (Types of cholinomimetics)

A

Indirect-acting cholinomimetics

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29
Q

Are derivatives of phosphoric acid; composed of a phosphate group (Types of covalent inhibitor, indirect-acting cholinomimetics)

A

Organophosphates

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30
Q

__________ and __________ are thiophosphate prodrugs (Examples of organophosphates) (MP)

A

Malathion, Parathion

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31
Q

Organophosphates are excreted through __________

A

Renal excretion

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32
Q

Organophosphates are rapidly absorbed and distributed, and crosses the BBB except __________

A

Echothiophate

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33
Q

Malathion and parathion are activated to the oxygen analogs, __________ and __________ (MP)

A

Malaoxon, Paraoxon

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34
Q

Used as an insecticide (Examples of organophosphates) (DMP)

A

Diisopropyl fluorophosphate (DFP), Malathion, Parathion

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35
Q

Used as nerve gases (Examples of organophosphates) (TSSV)

A

Tabun, Sarin, Soman, VX

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36
Q

Used for treatment of glaucoma (Examples of organophosphates)

A

Echothiophate (Phospholine iodide)

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37
Q

3 treatments for acute organophosphate toxicity (ADP)

A

Atropine, Diazepam, Pralidoxime/HI-6

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38
Q

Used for treatment of acute organophosphate toxicity; regenerates acetylcholinesterase before aging occurs

A

Pralidoxime

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39
Q

Contains an ester and amide group (Types of covalent inhibitor, indirect-acting cholinomimetics)

A

Carbamates

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40
Q

__________ and __________ are quaternary ammonium compounds (Examples of carbamates) (NP)

A

Neostigmine, Pyridostigmine

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41
Q

__________ and __________ are tertiary amines (Examples of carbamates) (PR)

A

Physostigmine, Rivastigmine

42
Q

__________ has no amine group (Examples of carbamates)

43
Q

Carbamates are excreted by __________

A

Plasma esterases

44
Q

Standard treatment of myasthenia gravis; used for paralytic ileus and bladder atony (Examples of carbamates)

A

Neostigmine

45
Q

Standard treatment of myasthenia gravis; used for treatment of glaucoma, but pilocarpine is more effective (Examples of carbamates)

A

Pyridostigmine

46
Q

Used for treatment of atropine toxicity and competitive neuromuscular blocker toxicity (Examples of carbamates)

A

Physostigmine

47
Q

Used for treatment of Alzheimer’s disease (Examples of carbamates)

A

Rivastigmine

48
Q

Standard treatment of myasthenia gravis; used as alternative treatment of Alzheimer’s disease (Examples of carbamates)

A

Ambenonium

49
Q

3 carbamates used as insecticides (CPA)

A

Carbaryl, Propoxur, Aldicard

50
Q

Contains a simple alcohol bearing a quaternary ammonium group (Types of noncovalent inhibitor, indirect-acting cholinomimetics)

51
Q

Alcohols are excreted through __________

A

Rapid renal excretion

52
Q

Alcohols are used for diagnosing myasthenia gravis in a test known as the __________

A

Edrophonium/Tensilon test

53
Q

Characterized by muscle weakness due to generalized depolarization of NMJ; exacerbated by AChE inhibitors

A

Cholinergic crisis

54
Q

Characterized by muscle weakness due to damaged nicotinic receptors at NMJ; improved by AChE inhibitors

A

Myasthenia gravis

55
Q

3 other examples of noncovalent inhibitor, indirect-acting cholinomimetics (GDT)

A

Galantamine, Donepezil, Tacrine

56
Q

Other noncovalent inhibitors are used for the treatment of __________

A

Alzheimer’s disease

57
Q

__________, a noncovalent inhibitor used for the treatment of Alzheimer’s disease, can lead to hepatotoxicity

58
Q

Are drugs that block muscarinic acetylcholine receptors, inhibiting PNS effects (Types of cholinolytics)

A

Antimuscarinic agents

59
Q

____________ and __________ are antimuscarinic agents that are naturally occurring alkaloids (AS)

A

Atropine, Scopolamine

60
Q

__________ derivatives are antimuscarinic agents that differ in disposition in the body or their duration of action (pharmacokinetics)

A

Semisynthetic

61
Q

__________ derivatives are antimuscarinic agents that provides selectivity for certain muscarinic receptor subtypes (pharmacodynamics)

62
Q

__________ is acquired from Atropa belladonna (Deadly nightshade) and Datura stramonium (Jimson-weed) (Examples of antimuscarinic agents)

63
Q

__________ is acquired from Hyoscyamus niger (Henbane) (Examples of antimuscarinic agents)

A

Scopolamine

64
Q

Natural alkaloids and tertiary amines (examples of antimuscarinic agents) are well absorbed and distributed, and __________ the BBB

65
Q

Quaternary ammonium compounds (examples of antimuscarinic agents) are less absorbed and distributed, and __________ the BBB

A

Does not enter

66
Q

Antimuscarinic agents work by __________ inhibition of muscarinic receptor

A

Competitive (reversible)

67
Q

Atropine is __________ among muscarinic receptors and __________ for muscarinic receptors

A

Nonselective, Selective

68
Q

Other antimuscarinic agents (not including atropine) is __________ among muscarinic receptors and ___________ for muscarinic receptors

A

Selective, Nonselective

69
Q

Used for COPD (Examples of antimuscarinic agents) (ITAU)

A

Ipatropium, Tiotropium, Aclidinium, Umeclidinium

70
Q

Used for overactive bladder (Examples of antimuscarinic agents) (POSTDFT)

A

Propiverine, Oxybutynin, Solifenacin, Trospium, Darifenacin, Fesoterodine, Tolterodine

71
Q

Used for peptic ulcer disease/PUD (Examples of antimuscarinic agents)

A

Pirenzepine

72
Q

Used to decrease secretion, motility, and tone in the GIT (Examples of antimuscarinic agents)

A

Glycopyrrolate

73
Q

Used for IBS (Examples of antimuscarinic agents)

A

Dicyclomine

74
Q

Used in attaining mydriasis and cyclopegia for eye examination (Examples of antimuscarinic agents) (HTC)

A

Homatropine, Tropicamide, Cyclopentolate

75
Q

Used for motion sickness (Examples of antimuscarinic agents)

A

Scopolamine

76
Q

Used for Parkinson’s disease (Examples of antimuscarinic agents) (BTB)

A

Benztropine, Trihexyphenidyl, Biperiden

77
Q

Used for reversal of organophosphate toxicity and cholinergic crisis (Examples of antimuscarinic agents)

78
Q

Characterized by xerostomia, constripation, blurred vision, dyspepsia, and cognitive impairment; due to antimuscarinic agent toxicity

A

Antimuscarinic agent overdose

79
Q

A carbamate used for the treatment of antimuscarinic agent overdose

A

Physostigmine

80
Q

Composed of synthetic amines; has a limited use due to nonselectivity (Examples of antinicotinic agents)

A

Ganglionic blockers

81
Q

__________ causes early stimulation of ganglia by causing persistent depolarization

82
Q

__________ and __________ causes competitive inhibition of neuronal nicotinic receptors on both parasympathetic and sympathetic ganglia (Examples of ganglionic blockers) (TT)

A

TEA, Trimethaphan

83
Q

__________ causes noncompetitive inhibition of neuronal nicotinic receptors on both parasympathetic and sympathetic ganglia (Examples of ganglionic blockers)

A

Mecamylamine

84
Q

__________ block channel after it opens (Examples of ganglionic blockers)

A

Hexamethonium

85
Q

__________ is no longer used (Examples of ganglionic blockers)

A

Trimethaphan

86
Q

__________ is the first drug effective for hypertension (Examples of ganglionic blockers)

A

Hexamethonium

87
Q

Resemble acetylcholine; contains a quaternary ammonium group (Types of antinicotinic agents)

A

Neuromuscular blockers

88
Q

Causes depolarization of membrane by opening channels in the same manner as ACh; has a longer duration of action than ACh (Types of neuromuscular blockers)

A

Depolarizing neuromuscular blockers

89
Q

Involves depolarization; leads to muscle fasciculations and flaccid paralysis (Phases of depolarizing neuromuscular blocker MOA)

A

Phase I (Depolarizing)

90
Q

Involves repolarization; leads to flaccid paralysis (Phases of depolarizing neuromuscular blocker MOA)

A

Phase II (Desensitizing)

91
Q

Includes isoquinoline and steroid (Types of neuromuscular blockers)

A

Nondepolarizing neuromuscular blockers

92
Q

A generic term for various South American arrow poisons; acquired from Strychnos sp.; also serves as a neuromuscular blocker

93
Q

Nondepolarizing neuromuscular blockers work by __________ inhibition of nicotinic receptors

A

Competitive

94
Q

__________ are used for surgical relaxation, endotracheal intubation, and treatment of convulsions

A

Neuromuscular blockers

95
Q

Characterized by apnea, cardiovascular collapse, and anaphylaxis; due to neuromuscular blocker toxicity

A

Neuromuscular blocker overdose

96
Q

3 carbamates used for neuromuscular blocker overdose that work for nondepolarizing blockers (NPE)

A

Neostigmine, Pyridostigmine, Edrophonium

97
Q

__________ is used to treat neuromuscular blocker overdose by binding rocuronium and vecuronium

A

Suggamadex

98
Q

__________ can trigger malignant hyperthermia due to uncontrolled release of Ca2+ from the sarcoplasmic reticulum

A

Succinylcholine

99
Q

Characterized by contracture, rigidity, and heat production from skeletal muscle, resulting in severe hyperthermia; caused by succinylcholine

A

Malignant hyperthermia

100
Q

Drug used as treatment for malignant hyperthermia due to succinylcholine

A

IV dantrolene

101
Q

Cevimeline is used as treatment for xerostomia associated with __________ syndrome

PH 113 - Pharmacology 1 (20 decks)

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