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
2
Q
Composed of an ester group (Types of direct-acting cholinomimetics)
A
Choline esters
3
Q
__________ and __________ have methyl groups on the beta carbon; (Examples of choline esters) (MB)
A
Methacholine, Bethanechol
4
Q
__________ and __________ are carbamoyl esters; they are selective for muscarinic receptors (Examples of choline esters) (BC)
A
Bethanechol, Carbachol
5
Q
Choline esters are poorly __________ and __________ (AD)
A
Absorbed, Distributed
6
Q
Choline esters are excreted through __________
A
Rapid renal excretion
7
Q
Used for induction of miosis during ophthalmic surgery as ophthalmic solution (Examples of choline esters)
A
Acetylcholine
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
9
Q
Used for treatment of urinary retention; a prokinetic (Examples of choline esters)
A
Bethanechol
10
Q
Used for treatment of glaucoma and induction of miosis during surgery as ophthalmic solution (Examples of choline esters)
A
Carbachol
11
Q
Contains nitrogen-containing heterocyclic groups (Types of direct-acting cholinomimetics)
A
Cholinomimetic alkaloids
12
Q
Derived from Amanita muscaria (Examples of cholinomimetic alkaloids)
A
Muscarine
13
Q
Derived from Pilocarpus sp. (Examples of cholinomimetic alkaloids)
A
Pilocarpine
14
Q
Derived from Areca catechu (Examples of cholinomimetic alkaloids)
A
Arecoline
15
Q
Derived from Nicotiana tabacum (Examples of cholinomimetic alkaloids)
A
Nicotine
16
Q
Muscarine is poorly __________ and __________ but can still cross the BBB (AD)
A
Absorbed, Distributed
17
Q
Tertiary amines are rapidly __________ and crosses the BBB
A
Absorbed
18
Q
Cholinomimetic alkaloids are excreted through __________
A
Renal excretion
19
Q
Muscarine is a muscarinic alkaloid that is an __________
A
Agonist
20
Q
Pilocarpine is a muscarinic alkaloid that is a __________
A
Partial agonist
21
Q
An example of cholinomimetic alkaloid with both muscarinic and nicotinic activity is __________
A
Arecoline
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
23
Q
In the cardiovascular system, nicotine serves as a __________
A
Sympathomimetic
24
Q
In the gastrointestinal and genitourinary tract, nicotine serves as a __________
A
Parasympathomimetic
25
A quinuclidine derivative of acetylcholine; used for the treatment of xerostomia (Types of direct-acting cholinomimetics)
Cevimeline
26
Overdose from muscarinic agonists may be treated with __________
Atropine
27
Overdose from nicotinic agonists may be treated with __________ and __________ (AD)
Atropine, Diazepam
28
Bind to and inactivate acetylcholinesterase; thereby increasing acetylcholine (Types of cholinomimetics)
Indirect-acting cholinomimetics
29
Are derivatives of phosphoric acid; composed of a phosphate group (Types of covalent inhibitor, indirect-acting cholinomimetics)
Organophosphates
30
__________ and __________ are thiophosphate prodrugs (Examples of organophosphates) (MP)
Malathion, Parathion
31
Organophosphates are excreted through __________
Renal excretion
32
Organophosphates are rapidly absorbed and distributed, and crosses the BBB except __________
Echothiophate
33
Malathion and parathion are activated to the oxygen analogs, __________ and __________ (MP)
Malaoxon, Paraoxon
34
Used as an insecticide (Examples of organophosphates) (DMP)
Diisopropyl fluorophosphate (DFP), Malathion, Parathion
35
Used as nerve gases (Examples of organophosphates) (TSSV)
Tabun, Sarin, Soman, VX
36
Used for treatment of glaucoma (Examples of organophosphates)
Echothiophate (Phospholine iodide)
37
3 treatments for acute organophosphate toxicity (ADP)
Atropine, Diazepam, Pralidoxime/HI-6
38
Used for treatment of acute organophosphate toxicity; regenerates acetylcholinesterase before aging occurs
Pralidoxime
39
Contains an ester and amide group (Types of covalent inhibitor, indirect-acting cholinomimetics)
Carbamates
40
__________ and __________ are quaternary ammonium compounds (Examples of carbamates) (NP)
Neostigmine, Pyridostigmine
41
__________ and __________ are tertiary amines (Examples of carbamates) (PR)
Physostigmine, Rivastigmine
42
__________ has no amine group (Examples of carbamates)
Carbaryl
43
Carbamates are excreted by __________
Plasma esterases
44
Standard treatment of myasthenia gravis; used for paralytic ileus and bladder atony (Examples of carbamates)
Neostigmine
45
Standard treatment of myasthenia gravis; used for treatment of glaucoma, but pilocarpine is more effective (Examples of carbamates)
Pyridostigmine
46
Used for treatment of atropine toxicity and competitive neuromuscular blocker toxicity (Examples of carbamates)
Physostigmine
47
Used for treatment of Alzheimer's disease (Examples of carbamates)
Rivastigmine
48
Standard treatment of myasthenia gravis; used as alternative treatment of Alzheimer's disease (Examples of carbamates)
Ambenonium
49
3 carbamates used as insecticides (CPA)
Carbaryl, Propoxur, Aldicard
50
Contains a simple alcohol bearing a quaternary ammonium group (Types of noncovalent inhibitor, indirect-acting cholinomimetics)
Alcohols
51
Alcohols are excreted through __________
Rapid renal excretion
52
Alcohols are used for diagnosing myasthenia gravis in a test known as the __________
Edrophonium/Tensilon test
53
Characterized by muscle weakness due to generalized depolarization of NMJ; exacerbated by AChE inhibitors
Cholinergic crisis
54
Characterized by muscle weakness due to damaged nicotinic receptors at NMJ; improved by AChE inhibitors
Myasthenia gravis
55
3 other examples of noncovalent inhibitor, indirect-acting cholinomimetics (GDT)
Galantamine, Donepezil, Tacrine
56
Other noncovalent inhibitors are used for the treatment of __________
Alzheimer's disease
57
__________, a noncovalent inhibitor used for the treatment of Alzheimer's disease, can lead to hepatotoxicity
Tacrine
58
Are drugs that block muscarinic acetylcholine receptors, inhibiting PNS effects (Types of cholinolytics)
Antimuscarinic agents
59
____________ and __________ are antimuscarinic agents that are naturally occurring alkaloids (AS)
Atropine, Scopolamine
60
__________ derivatives are antimuscarinic agents that differ in disposition in the body or their duration of action (pharmacokinetics)
Semisynthetic
61
__________ derivatives are antimuscarinic agents that provides selectivity for certain muscarinic receptor subtypes (pharmacodynamics)
Synthetic
62
__________ is acquired from Atropa belladonna (Deadly nightshade) and Datura stramonium (Jimson-weed) (Examples of antimuscarinic agents)
Atropine
63
__________ is acquired from Hyoscyamus niger (Henbane) (Examples of antimuscarinic agents)
Scopolamine
64
Natural alkaloids and tertiary amines (examples of antimuscarinic agents) are well absorbed and distributed, and __________ the BBB
Crosses
65
Quaternary ammonium compounds (examples of antimuscarinic agents) are less absorbed and distributed, and __________ the BBB
Does not enter
66
Antimuscarinic agents work by __________ inhibition of muscarinic receptor
Competitive (reversible)
67
Atropine is __________ among muscarinic receptors and __________ for muscarinic receptors
Nonselective, Selective
68
Other antimuscarinic agents (not including atropine) is __________ among muscarinic receptors and ___________ for muscarinic receptors
Selective, Nonselective
69
Used for COPD (Examples of antimuscarinic agents) (ITAU)
Ipatropium, Tiotropium, Aclidinium, Umeclidinium
70
Used for overactive bladder (Examples of antimuscarinic agents) (POSTDFT)
Propiverine, Oxybutynin, Solifenacin, Trospium, Darifenacin, Fesoterodine, Tolterodine
71
Used for peptic ulcer disease/PUD (Examples of antimuscarinic agents)
Pirenzepine
72
Used to decrease secretion, motility, and tone in the GIT (Examples of antimuscarinic agents)
Glycopyrrolate
73
Used for IBS (Examples of antimuscarinic agents)
Dicyclomine
74
Used in attaining mydriasis and cyclopegia for eye examination (Examples of antimuscarinic agents) (HTC)
Homatropine, Tropicamide, Cyclopentolate
75
Used for motion sickness (Examples of antimuscarinic agents)
Scopolamine
76
Used for Parkinson's disease (Examples of antimuscarinic agents) (BTB)
Benztropine, Trihexyphenidyl, Biperiden
77
Used for reversal of organophosphate toxicity and cholinergic crisis (Examples of antimuscarinic agents)
Atropine
78
Characterized by xerostomia, constripation, blurred vision, dyspepsia, and cognitive impairment; due to antimuscarinic agent toxicity
Antimuscarinic agent overdose
79
A carbamate used for the treatment of antimuscarinic agent overdose
Physostigmine
80
Composed of synthetic amines; has a limited use due to nonselectivity (Examples of antinicotinic agents)
Ganglionic blockers
81
__________ causes early stimulation of ganglia by causing persistent depolarization
Nicotine
82
__________ and __________ causes competitive inhibition of neuronal nicotinic receptors on both parasympathetic and sympathetic ganglia (Examples of ganglionic blockers) (TT)
TEA, Trimethaphan
83
__________ causes noncompetitive inhibition of neuronal nicotinic receptors on both parasympathetic and sympathetic ganglia (Examples of ganglionic blockers)
Mecamylamine
84
__________ block channel after it opens (Examples of ganglionic blockers)
Hexamethonium
85
__________ is no longer used (Examples of ganglionic blockers)
Trimethaphan
86
__________ is the first drug effective for hypertension (Examples of ganglionic blockers)
Hexamethonium
87
Resemble acetylcholine; contains a quaternary ammonium group (Types of antinicotinic agents)
Neuromuscular blockers
88
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)
Depolarizing neuromuscular blockers
89
Involves depolarization; leads to muscle fasciculations and flaccid paralysis (Phases of depolarizing neuromuscular blocker MOA)
Phase I (Depolarizing)
90
Involves repolarization; leads to flaccid paralysis (Phases of depolarizing neuromuscular blocker MOA)
Phase II (Desensitizing)
91
Includes isoquinoline and steroid (Types of neuromuscular blockers)
Nondepolarizing neuromuscular blockers
92
A generic term for various South American arrow poisons; acquired from Strychnos sp.; also serves as a neuromuscular blocker
Curare
93
Nondepolarizing neuromuscular blockers work by __________ inhibition of nicotinic receptors
Competitive
94
__________ are used for surgical relaxation, endotracheal intubation, and treatment of convulsions
Neuromuscular blockers
95
Characterized by apnea, cardiovascular collapse, and anaphylaxis; due to neuromuscular blocker toxicity
Neuromuscular blocker overdose
96
3 carbamates used for neuromuscular blocker overdose that work for nondepolarizing blockers (NPE)
Neostigmine, Pyridostigmine, Edrophonium
97
__________ is used to treat neuromuscular blocker overdose by binding rocuronium and vecuronium
Suggamadex
98
__________ can trigger malignant hyperthermia due to uncontrolled release of Ca2+ from the sarcoplasmic reticulum
Succinylcholine
99
Characterized by contracture, rigidity, and heat production from skeletal muscle, resulting in severe hyperthermia; caused by succinylcholine
Malignant hyperthermia
100
Drug used as treatment for malignant hyperthermia due to succinylcholine
IV dantrolene
101
Cevimeline is used as treatment for xerostomia associated with __________ syndrome
Sjögren
