Lectures 13 - 14: Cholinergic System 1 and 2 Flashcards

1
Q

Treatment of anticholinesterase overdoses.

A

Atropine

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2
Q

Can cause prolonged/excessive skeletal muscle paralysis

A

Gentamycin (aka aminoglycosides)

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3
Q

Treatment of Parkinson’s disease and tardive dyskinesia.

A

Benztropine

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4
Q

Block of choline uptake

A

Hemicholinium

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5
Q

Is also an antiemetic.

A

Scopolamine (Hyoscine)

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6
Q

Oxime Compounds (cholinesterase re-activators)

A

Pralidoxime

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7
Q

Antispasmodic: relax GI tract and bladder.

A

Atropine

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8
Q

Direct acting cholinergic agonists

A

Pilocarpine

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9
Q

High dose: excitation effect such as restlessness, disorientation and hallucinations.

A

Atropine

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10
Q

Actions of Muscarinic Antagonists (atropine, Benztropine, Ipratropium, Scopolamine (Hyoscine))

A

-Peripheral
● Block secretions (saliva, bronchial, GIT, etc.).
● Dilates pupil (mydriasis).
● Mydriasis can precipitate narrow angle glaucoma in the predisposed.
● Relaxes ciliary muscle to cause cycloplegia (lens fixed for far vision).
● Tachycardia (block of vagal influence).
● Blocks GIT motility (constipation).
● Relaxes bronchial smooth muscles.

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11
Q

Choline esters (longer duration than Ach)

A

Bethanechol

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12
Q

Blocks the rate-limiting step (uptake of choline into the neuron)

A

Hemicholinium

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13
Q

Muscarinic antagonists (no action on nicotinic receptors)

A

Atropine

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14
Q

Blocks nicotinic receptors on skeletal muscles

A

Gentamycin (aka aminoglycosides)

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15
Q

Antisecretory: block secretions in the upper and lower respiratory tracts prior to surgery.

A

Atropine

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16
Q

Long-acting reversible anticholinesterases

A

Neostigmine, Physostigmine

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17
Q

Block of Ach storage

A

Vesamicol

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18
Q

Induce reactivation of enzymes inactivated by phosphorylation.

A

Pralidoxime

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19
Q

Adverse Effects of Muscarinic Agonists (Acetylcholine, Pilocarpine, Bethanechol)

A

-Hypotension:
● Due to vasodilation :
Caused by the muscarinic receptor mediated release of NO from endothelium.
● Also due to decreased cardiac output:
due to decreased heart rate and force of contraction.
● Reflex tachycardia often overrides bradycardia.
-Bronchospasm:
● No significance in normal individuals, but may precipitate asthma in asthmatics.
-Others:
● Nausea, vomiting, GIT cramps, and diarrhea.

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20
Q

Actions of Acetylcholine

A

-Heart: decreases heart rate and cardiac output.
-Blood vessels: vasodilation and decrease in blood
pressure.
-GI tract: increases salivary secretion and stimulates
intestinal secretion and motility.
-Lungs: enhanced bronchiolar secretions and
bronchoconstriction.
-Genitourinary tract: increased tone of the detrusor
urinae muscle causing the expulsion of urine.
-Eye: muscle contraction for near vision and pupil
constriction (miosis).

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21
Q

Irreversible (Long-acting) Anticholinesterases:
Organophosphates
War gases and pesticides.

A

Ecothiophate

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22
Q

Treatment of paralytic ileus and bladder atony

A

Neostigmine

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23
Q

Block Ach release

A

Botulinum toxin

24
Q

Eye: persistent mydriasis

A

Atropine

25
Q

Muscarinic Antagonists

A

Ipratropium, Scopolamine (Hyoscine)

26
Q

Increase Ach release

A

Latrotoxin

27
Q

Therapeutic uses of Scopolamine (Hyoscine)

A
  • Treatment of motion sickness.

- Blocking short term memory and is used as an adjunct with anesthesia.

28
Q

Block of post-synaptic Ach receptors

A

Atropine

29
Q

Has no CNS effect at low doses.

A

Atropine

30
Q

Treatment of Alzheimer’s disease

A

Physostigmine

31
Q

Toxicity of Anticholinesterases (common with organophosphates)
(Ecothiophate, Neostigmine, Physostigmine):

A

-Acute
● Vomiting, colic and diarrhea.
● Constricted pupils that are unresponsive to light.
● Sweating and salivation.
● Bronchoconstriction.
● Bradycardia
● Agitation, confusion and respiratory depression. (Especially, physostigmine and organophosphates)
-Chronic
● Demyelination: sensory loss and respiratory paralysis

32
Q

Treatment of GIT cramps.

A

Scopolamine (Hyoscine)

33
Q

Treatment of Organophosphate Poisoning

A

Pralidoxime

34
Q

Anticholinesterases (Indirect-acting cholinergic agonists)

A

Ecothiophate, Neostigmine, Physostigmine

35
Q

Naturally occurring alkaloids (longer duration than Ach)

A

Pilocarpine

36
Q

Treatment of asthma and chronic bronchitis.

A

Ipratropium

37
Q

Greater action on the CNS than atropine and a longer duration of action.

A

Scopolamine (Hyoscine)

38
Q

Plant product

A

Scopolamine (Hyoscine)

39
Q

Treatment of myasthenia gravis

A

Neostigmine

40
Q

Contraindications of Muscarinic Agonists (Acetylcholine, Pilocarpine, Bethanechol)

A
  • Coronary insufficiency (worsened by hypotension).
  • Hyperthyroidism (may precipitate atrial arrhythmias).
  • Peptic ulcer.
  • Asthma.
41
Q

Used for glaucoma

A

Pilocarpine

42
Q

Treatment of atropine poisoning

A

Physostigmine

43
Q

Direct acting cholinergic agonists

A

Bethanechol

44
Q

Treatment of glaucoma

A

Ecothiophate, Physostigmine

45
Q

Selective muscarinic receptors

A

Pilocarpine, Bethanechol

46
Q

Adverse Effects of Muscarinic Antagonists (Atropine, Benztropine, Ipratropium, Scopolamine (Hyoscine) )

A
  • Urinary retention.
  • Dry mouth.
  • Blurred vision.
  • Tachycardia.
  • Constipation.
  • Confusion.
  • Myadriasis
  • contraindicated in people who are predisposed to glaucoma.
47
Q

Used for paralytic ileus and urinary retention

A

Bethanechol

48
Q

Reversal of competitive neuromuscular block

A

Neostigmine

49
Q

Is a depressant at therapeutic dose.

-Sedation, drowsiness, and amnesia.

A

Scopolamine (Hyoscine)

50
Q

Effects of Anticholinesterases (Ecothiophate, Neostigmine, Physostigmine)

A
-Peripheral
● Enhanced neuromuscular transmission.
● Increased GIT motility/bladder contraction.
● Bradycardia.
● Pupil constriction.
● Bronchoconstriction.
-Central
● General CNS stimulation (agitation and convulsion) followed by respiratory depression (death).
51
Q

Useful in Parkinsonism

A

Benztropine

52
Q

Can cause prolonged/excessive skeletal muscle paralysis

A

Gentamycin (aka aminoglycosides)

53
Q

Found in spider venom

A

Latrotoxin

54
Q

Alkaloid found in Atropa belladonna

A

Atropine

55
Q

Quaternary nitrogen compound

A

Ipratropium

56
Q

Clinical Uses of Muscarinic Antagonists

Atropine, Scopolamine (Hyoscine)

A
  • Surgery: as pre-anesthetic to inhibit salivary and bronchial secretions.
  • Antidote: in treatment of anticholinesterase poisoning.
  • Treatment of GIT cramps.
  • Treatment of Parkinson’s disease and tardive dyskinesia.
  • Treatment of sinus bradycardia after MI.