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Foundation 2 > Cholinergic And Anticholinergic Drugs > Flashcards

Cholinergic And Anticholinergic Drugs Flashcards

1
Q

Cholinergic agonists types

A
  • Direct-acting cholinoreceptor stimulants

* Indirect-acting cholinomimetics (inhibit destruction of ACh)

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2
Q

Direct-acting cholinomimetic agonists

A
  • Cholinesters

* Cholinergic alkaloids

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3
Q

Cholinesters examples

A

ACh, methacholine, carbachol, betachol

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4
Q

Cholinergic alkaloids

A

Pilocarpine, arecoline, muscadine

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5
Q

Cholinesters therapeutic uses

A
  • GI disorders: Bethanechol for paralytic ileus, congenital megacolon
  • Urinary bladder disorders - neurogenic bladder
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6
Q

Alkaloid therapeutic uses

A
  • Xerostomia: orally for Sjögrand’s and head and neck radiation
  • Glaucoma: decrease IOP
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7
Q

Cholinergic agonists adverse effects

A
  • Abdominal cramps, belching
  • Flushing, syncope, sweating
  • Bronchospasm
  • Hypotension, bradycardia, heart block
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8
Q

Cholinergic agonists contraindications

A
  • Asthma
  • Hyperthyroidism
  • Coronary insufficiency
  • Peptic ulcer
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9
Q

Mushroom poisoning sources

A
  • Inocybe, clitocybe: muscarine

* Amanita Muscaria: muscimol, ibotenic acid

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10
Q

Mushroom poisoning symptoms

A
  • Salivation
  • Lacrimation
  • Vomiting
  • Headache
  • Colic
  • Diarrhoea
  • Bronchospasm
  • Hypotension
  • Shock
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11
Q

MOA of anti-cholinesterases

A

Anti-ChE agents cause accumulation of ACh at ALL sites of Cholinergic transmission

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12
Q

Myasthenia Gravis medication

A
  • Edrophonium: for diagnosis
  • Pyridostigmine: longer acting, preferred in patients whose muscles are weak on wakening
  • Neostigmine: poorly absorbed, lasts 4h, no CNS action, atropine given tgt
  • Distigmine: longest acting (SE: Cholinergic crisis)
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13
Q

Alzheimer’s disease medication

A
  • Tacrine
  • Donepezil
  • Rivastigmine
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14
Q

Intoxication by anticholinergic drugs medication

A

• Physostigmine

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15
Q

Reversal of non-depolarising NMB in anaesthesia

A

• Physostigmine

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16
Q

Acute glaucoma medication

A
  • Pilocarpine

* Physostigmine

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17
Q

Adverse effects of anti-cholinesterases

A
  • Increased muscarinic effects
  • Depolarising block
  • Cholinergic crisis
  • CNS: stimulation followed by inhibition (confusion, drowsiness, convulsion, coma)
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18
Q

Treatment of anti-ChE poisoning (organophosphate insecticide

A
  • Termination of exposure, removal of clothing, washing contaminated skin, gastric lavage
  • Maintenance of patient airway
  • Control of muscarinic effects: atropine
  • Cholinesterase reactivators: oximes
  • Supportive measures: oxygen
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19
Q

Atropine dosage

A
  • initial 2-4mg, repeated every 5 mins
  • May need 100 ampoules
  • Maintained for >72hours
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20
Q

Pralidoxime (PAM)

A
  • 1-2g IV over 5 mins, may repeat after 1 hour
  • Drug will reactive AChE enzyme, hasten recovery (most marked in NMJ)
  • Metabolised in liver, excreted in urine
  • Diacetyl monoxime (DAM) is an alternative
21
Q

Anticholinergic drugs classification

A

Muscarinic antagonist

Nicotinic antagonist

22
Q

Muscarinic antagonist classification

A
  • Natural alkaloids

* Synthetic derivatives

23
Q

Nicotinic antagonists classification

A
  • Neuro-muscular blockers

* Ganglion blocking agents

24
Q

Anti-muscarinic alkaloids

A
  • Atropine

* Scopolamine

25
Muscarinic antagonists synthetic derivatives
* Homatropine | * Ipratropium
26
Nicotinic antagonists NMB examples
* Tubocurarine | * Vecuronium
27
Nicotinic antagonists ganglion blocking agents examples
* Mecamylamine | * Trimethaptan
28
Source of anti-muscarinic alkaloids
* Atropine: Atropa belladonna, Datura stramonium | * Scopolamine: Hyocyamus niger
29
MOA of anti-muscarinics
* Compete with ACh for common binding site on muscarinic receptors, prevent muscarinic actions * No blockade of Nicotinic receptors * Atropine: little CNS action, Scopolamine: marked central effects
30
Effect of anti-muscarinics on CVS
* Tachycardia: increased HR * No change to BP * Treatment of bradycardia due to MI or organophosphate poisoning * SE: palpitation
31
Effect of anti-muscarinics on eye
• Action: mydriasis, cycloplegia • Uses: thorough examination of retina, optic disc Therapy of iridocyclitis, keratitis Alternated with miotics for breaking and preventing development of adhesion btwn iris and lens • SE: photophobia, blurred vision, precipitation of glaucoma
32
Effect of anti-muscarinics on GIT
* Decreased salivary secretion (treat sialorrhoea) (M3) * Decreased gastric secretion (M1), mucin, proteolytic enzyme secretion * useful for pre-anaesthetic medication, treatment of diarrhoea, acute pancreatitis
33
Effect of anti-muscarinics on GI motility
• Action: prolonged inhibition of motility in stomach, duodenum, jejunum, ileum, colon reduced tone and amplitude of contractions • Uses: intestinal colic, diarrhoea, IBS, diverticulitis Facilitate endoscopy, GI radiology • SE: constipation
34
Effect of anti-muscarinics on respiratory tract
* Action: Decreased secretion in both upper and lower respiratory tract * Uses: relieve acute rhinitis (coryza or hay fever), relax bronchial smooth muscle (bronchial asthma, COPD) (Ipratropium) * SE: viscid material hard to remove, can block airway, predispose to infection
35
Effect of anti-muscarinics on respiratory tract (smooth muscle contraction)
* Action: Inhibit smooth muscle contraction in larynx and bronchioles * Uses: prevent laryngospasm and bronchospasm in anaesthesia
36
Effect of anti-muscarinics on Genito-urinary tract
* Action: Relax smooth muscle contraction * Uses: renal colic (opioids), biliary colic, ureteric colic, enuresis in children (tolterodine), reduce urinary frequency in spastic paraplegia * SE: urinary retention
37
Atropine in CNS
* Benztropine, benzhexol: control of tremor in Parkinsonism * Scopolamine: prevention of motion sickness * SE: dizziness, light-headedness, fatigue
38
Atropine other uses
* Treatment of mushroom poisoning, organophosphate insecticide poisoning, exposure to chemical warfare agents (sarin) * Myasthenia Gravis: used with Neostigmine
39
Ganglion stimulating agents
* Nicotine, Lobeline, TMA | * Stimulates CNS
40
Ganglion blocking agents examples
* Hexamethonium * Mecamylamine * Trimethaphan
41
Ganglion blocking agents effects
* Blockade of sympathetic ganglia (vasodilation, hypotension, venous pooling, decreased cardiac output) * Blockade of parasympathetic ganglia (atropine like effects on heart, eye, urinary bladder, salivary glands)
42
Ganglion blocking agents therapeutic uses
* Acute hypertensive crisis | * Autonomic hyperreflexia
43
Pyridostigmine use
Myasthenia gravis
44
Succinylcholine use
Neuromuscular block (eg. tracheal intubation)
45
Pilocarpine use
Acute narrow angle glaucoma
46
Atropine use
Pre-anaesthetic medication, organophosphate insecticide poisoning, mushroom poisoning, eye examination
47
Benztropine use
Parkinsonism
48
Scopolamine use
Motion sickness
49
Tubocurarine use
NMB (Nicotinic block)

Foundation 2 (11 decks)

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