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Pharmacology- Test 1 Material > 04- Cholinergics > Flashcards

04- Cholinergics Flashcards

1
Q

atropine

A

cholinergic antagonist that is MUSCARINIC selective

  • no selectivity for Muscarinic sub-types
  • tertiary amine so easily cross BBB and cause CNS toxicity
  • quickly distributed after administration (30-60 min in CNS)
  • duration of action 5-10 hours
  • most sensitive tissues are salivary, bronchial, and sweat glands
  • has LONG-acting topical application used in eyes that elicits mydriasis and cycloplegia, relieves urinary incontinence, may be useful adjunct therapy for Parkinsonism, overcome poisoning by O-P or muscarine mushrooms, and can inhibit some vagal slowing of heart due to MI
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2
Q

homatropine

A

cholinergic antagonist that is MUSCARINIC selective

  • tertiary amine so can cross BBB (mainly used topically so this does not normally occur)
  • duration of action 2-4 hours
  • has INTERMEDIATE-acting topical application that is useful for eliciting mydriasis and cycloplegia (for eye exams)
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3
Q

scopolamine

A

cholinergic antagonist that is MUSCARINIC selective

  • quickly distributed after admin (30-60 min in CNS)
  • duration of action 5-10 hours
  • tertiary amine derivative primarily used for CNS effects (CNS depression manifested with drowsiness, amnesia, fatigue, dreamless sleep)
  • most effective treatment for motion sickness
  • side effects include sedation and dry mouth
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4
Q

methscopolamine (Pamine)

A

cholinergic antagonist that is MUSCARINIC selective

  • duration of action 5-10 hours
  • quaternary derivative of scopolamine so only used in PNS and lacks CNS effects
  • primarily used for GI diseases
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5
Q

trihexyphenidyl (Artane)

A

cholinergic antagonist that is MUSCARINIC selective

  • tertiary amine that readily crosses BBB and can cause CNS toxicity
  • duration of action 3-6 hours
  • useful adjunct therapy to dec. uncoordinated movement and excess salivation for Parkinsonism (main use) and extra-pyramidal side effects of anti-psychotics
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6
Q

cyclopentolate (Cyclogyl)

A

cholinergic antagonist that is MUSCARINIC selective

  • short acting (3-6hrs) topical application to induce mydriasis and cycloplegia
  • non-specific muscarinic blocker so can exhibit all associated effects of muscarinic blockade
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7
Q

ipratroprium (Atrovent)

A

cholinergic antagonist that is MUSCARINIC selective

  • aerosol, synthetic analog of atropine
  • quaternary derivative of atropine
  • bronchodilation, tachycardia, decreased salivation
  • minimizes mucociliary clearance effect and is useful for patients with airway problems (maintains airway fluidity)
  • specifically targeted when used as an inhalant and unable to cross membranes (so will only bronchodilate)
  • used for patients with COPD
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8
Q

tiotropium (Spiriva)

A

cholinergic antagonist that is MUSCARINIC selective

  • synthetic analog of atropine
  • serves as LONGER ACTING “topical” inhalation application that targets bronchodilation and specifically minimizes mucociliary clearance problems (maintains airway fluidity)
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9
Q

darifenacin (Enablex)

A

cholinergic antagonist that is M3 selective

  • slows micturition
  • aids in treatment of urinary urgency due to inflammatory bladder problems
  • may alleviate bladder spasm following urologic surgery
  • may precipitate urinary retention in men with prostatic hyperplasia
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10
Q

solifenacin (VESIcare)

A

cholinergic antagonist that is M3 selective

  • slows micturition
  • aids in treatment of urinary urgency due to inflammatory bladder problems
  • may alleviate bladder spasm following urologic surgery
  • may precipitate urinary retention in men with prostatic hyperplasia
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11
Q

tolterodine (Detrol)

A

cholinergic antagonist that is M3 selective

  • slows micturition
  • aids in treatment of urinary urgency due to inflammatory bladder problems
  • may alleviate bladder spasm following urologic surgery
  • may precipitate urinary retention in men with prostatic hyperplasia
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12
Q

mecamylamine (Inversine)

A

cholinergic antagonist that is NICOTINIC selective

  • acts as non-depolarizing competitive antagonist
  • secondary amine developed to improve absorption from GI tract following oral administration
  • Duration of action: 12 hours
  • CNS side effects include tremors, confusion, seizures, mania, depression
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13
Q

trimethaphan (Arfonad)

A

cholinergic antagonist that is NICOTINIC selective

  • acts as non-depolarizing competitive antagonist
  • sulfonium (positively charged sulfur group) developed for IV use (lasts minutes)
  • used during surgery to minimize blood loss in OR
  • monitor carefully for excessive hypotension and brain anoxia
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14
Q

succinylcholine

A
  • cholinergic antagonist that is DEPOLARIZING
  • non-competitive receptor agonist that opens Na+ channels and mimics effect of ACh
  • not substrate for AChE, but activity short because broken down by plasma cholinesterase
  • only depolarizing NM blocker
  • Phase I block (depolarizing): membrane remains depolarized and unresponsive inducing flaccid paralysis
  • Phase II block (desensitizing): membrane repolarizes but receptor is desensitized due to prolonged exposure to Succ.
  • cannot reverse action of succinylcholine***
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15
Q

curare (d-tubocurarine)

A

cholinergic antagonist that is NON-DEPOLARIZING

  • LONG-acting benzylisoquinoline that competes with ACh for binding to N2 receptor sites which prevents depolarization of membrane and flaccid paralysis
  • devoid of vagolytic and ganglionic blocking activity
  • may elicit some histamine release
  • poor lipid solubility so cannot cross BBB
  • can be reversed by AChE inhibitor which leads to more ACh at synapse which can compete off antagonist from receptor
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16
Q

atracurium (Tracrium)

A

cholinergic antagonist that is NON-DEPOLARIZING

  • competes with ACh for binding to N2 receptor sites which prevents depolarization of membrane and flaccid paralysis
  • poor lipid solubility so cannot cross BBB
  • can be reversed by AChE inhibitor which leads to more ACh at synapse which can compete off antagonist from receptor
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17
Q

cisatracurium (Nimbex)

A

cholinergic antagonist that is NON-DEPOLARIZING

  • INTERMEDIATE-acting benzylisoquinoline that competes with ACh for binding to N2 receptor sites which prevents depolarization of membrane and flaccid paralysis
  • devoid of vagolytic and ganglionic blocking activity
  • may elicit some histamine release
  • poor lipid solubility so cannot cross BBB
  • can be reversed by AChE inhibitor which leads to more ACh at synapse which can compete off antagonist from receptor
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18
Q

mivacurium (Mivacron)

A

cholinergic antagonist that is NON-DEPOLARIZING

  • SHORT-acting benzylisoquinoline that competes with ACh for binding to N2 receptor sites which prevents depolarization of membrane and flaccid paralysis
  • devoid of vagolytic and ganglionic blocking activity
  • may elicit some histamine release
  • poor lipid solubility so cannot cross BBB
  • can be reversed by AChE inhibitor which leads to more ACh at synapse which can compete off antagonist from receptor
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19
Q

pancuronium (Pavulon)

A

cholinergic antagonist that is NON-DEPOLARIZING

  • LONG-acting ammonio steroid that causes neuromuscular blockade by competing with ACh for binding to N2 receptor sites which prevents depolarization of membrane and flaccid paralysis
  • will have some muscarinic block leading to vagal blockade and tachycardia
  • poor lipid solubility so cannot cross BBB
  • can be reversed by AChE inhibitor which leads to more ACh which can compete off antagonist from receptor
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20
Q

vecuronium (Norcuron)

A

cholinergic antagonist that is NON-DEPOLARIZING

  • INTERMEDIATE-acting ammonio steroid that causes neuromuscular blockade by competing with ACh for binding to N2 receptor sites which prevents depolarization of membrane and flaccid paralysis
  • will have some muscarinic block leading to vagal blockade and tachycardia
  • poor lipid solubility so cannot cross BBB
  • can be reversed by AChE inhibitor which leads to more ACh which can compete off antagonist from receptor
21
Q

Cholinergic Antagonists

A

block the effects of ACh and ACh-like agonists from interacting with the various nicotinic and muscarinic receptors and prevent the normal physiological responses caused by these receptors

22
Q

Anti-Muscarinic (parasympatholytics) Agents

A

anticholinergic drugs that combine with muscarinic receptors (M1-M3) and prevent physiologic responses to ACh at post-ganglionic parasympathetic transmission sites

  • used when both mydriasis and cycloplegia are required
  • block vagal slowing of the heart due to antagonism of muscarinic receptors on SA and AV nodes
  • elicit bronchodilation and decreased secretions in airway
  • decrease smooth muscle motility and secretions in GI tract
  • decrease activity of salivary glands and thermoregulatory sweat glands
  • relax smooth muscle of genitourinary system
  • have anti-parkinson, anti-motion sickness and amnesic properties
23
Q

Anti-Nicotinic Agents

A

anticholinergic agents that block nicotinic receptors

  • ganglionic blockers (N1)
  • NMJ blockers (N2)
24
Q

Tertiary Amine

A

nitrogen forming 3 bonds and has a neutral charge

-derivatives can cross mucous membranes and BBB to exert effects on CNS

25
Q

Quaternary Ammonium

A

-positively charged nitrogen that forms 4 bonds
derivatives do not cross membrane boundaries due to poor lipid solubility from charged N group
-avoid CNS effects because does not cross BBB
-poor and unreliable oral absorption
-poor absorption across conjuctiva

26
Q

Why can’t we reverse a neuromuscular block created by succinylcholine (Succ) with neostigmine (Neo)?

A

neostigmine is an AchE inhibitor leading to increased Ach in the neuromuscular junction. Succ is a depolarizing neuromuscular blocker which acts as a Nm receptor agonist. Increasing the amount of Ach in the neuromuscular junction will augment and increase the depolarization further.

27
Q

edrophonium

A
  • Competitive inhibitor of cholinesterase (reversible, short-acting)
  • simple alcohol with Quaternary ammonium (binds to active site on AChE)
  • Major uses: myasthenia gravis, ileus, arrhthmias
  • Duration of action: 5-15 minutes
28
Q

carbaryl (Sevin)

A

Organophosphate insecticide. AChE inhibitor

29
Q

malathion

A

Organophosphate insecticide. AChE inhibitor

30
Q

parathion

A

Organophosphate insecticide. AChE inhibitor

31
Q

echothiophate

A
  • non-competitive inhibitor of cholinesterase (irreversible, long-acting)
  • organophosphate
  • major use: glaucoma
  • duration of action: 100 hours
32
Q

sarin

A

Nerve gas. AChE inhibitor.

33
Q

soman

A

Nerve gas. AChE inhibitor

34
Q

diisopropylfluorophosphate (DFP)

A

Organophosphate. Noncompetitive AChE inhibitor.

35
Q

Organophosphate derivatives

A

Noncompetitive inhibitors of cholinesterase. Insecticides react first with plasma cholinesterase. Nerve gases react more with AChE

36
Q

edrophonium

A
  • Competitive inhibitor of cholinesterase (reversible, short-acting)
  • simple alcohol with Quaternary ammonium
  • Major uses: myasthenia gravis, ileus, arrhthmias
  • Duration of action: 5-15 minutes
37
Q

neostigmine

A
  • competitive inhibitor of cholinesterase (reversible, short-acting)
  • carbamate
  • major uses: myasthenia gravis, ileus
  • duration of actionL 0.5-4 hours
38
Q

physostigmine

A
  • competitive inhibitor of cholinesterase (reversible, short-acting)
  • carbamate
  • major uses: glaucoma
  • duration of action: 0.5-2 hours
39
Q

pyridostigmine

A
  • competitive inhibitor of cholinesterase (reversible, short-acting)
  • carbamate
  • major uses: myasthenia gravis
  • duration of action: 4-6 hours
40
Q

diisopropylfluorophosphate (DFP)

A
  • non competitive inhibitor of cholinesterase (irreversible, long-acting)
  • organophosphate
41
Q

ambenonium

A
  • competitive inhibitor of cholinesterase
  • carbamate
  • major use: myasthenia gravis
  • duration of action: 4-8 hours
42
Q

bethanechol

A

-cholinergic agonist (synthetic choline ester)
-contains a methyl (CH3) and amine (NH2) group.
+methyl increases specificity for muscarinic receptors
+amine decreases substrate binding to AchE and pseudocholinesterase leading to an increased DOA.
-can be used in combination with neostigmine for post-op ileus.

43
Q

carbachol (Carbastat)

A

-cholinergic agonist (synthetic choline ester)
-contains amine group
+amine decreases substrate binding to AchE and pseudocholinesterase leading to an increased DOA.

44
Q

methacholine (Provocholine)

A

-cholinergic agonist (synthetic choline ester)
-contains a methyl group
+methyl increases specificity for muscarinic receptor

45
Q

muscarine

A
  • muscarinic receptor agonist (natural alkaloid)

- found in mushrooms

46
Q

pilocarpine

A
  • muscarinic receptor agonist (natural alkaloid).
  • sweat glands very sensitive to pilocarpine.
  • pilocarpine can be combined with an AchE inhibitor to treat acute closed angle glaucoma
  • can be used in increase salivation if xerostomia is present.
47
Q

nicotine

A

cholinergic agonist that is a natural alkaloid and NICOTINIC selective
Effects: increased HR, vasoconstriction, decreased mucus movement in the lungs, increased endogenous Epi.
-central stimulant effects: convulsions, coma, respiratory arrest, cardiac arrhythmia.

48
Q

varenicline (Chantix)

A
  • partial cholinergic nicotinic agonist.

- treatment for nicotine addiction

49
Q

What do we see clinically with parasympathetic stimulation?

A
  • decreased HR
  • decreased BP
  • bronchial constriction
  • increased salivation
  • increased GI motility
  • bladder relaxation
  • miosis

Pharmacology- Test 1 Material (8 decks)

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