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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
Q

Muscarinic antagonists synthetic derivatives

A
  • Homatropine

* Ipratropium

26
Q

Nicotinic antagonists NMB examples

A
  • Tubocurarine

* Vecuronium

27
Q

Nicotinic antagonists ganglion blocking agents examples

A
  • Mecamylamine

* Trimethaptan

28
Q

Source of anti-muscarinic alkaloids

A
  • Atropine: Atropa belladonna, Datura stramonium

* Scopolamine: Hyocyamus niger

29
Q

MOA of anti-muscarinics

A
  • 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
Q

Effect of anti-muscarinics on CVS

A
  • Tachycardia: increased HR
  • No change to BP
  • Treatment of bradycardia due to MI or organophosphate poisoning
  • SE: palpitation
31
Q

Effect of anti-muscarinics on eye

A

• 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
Q

Effect of anti-muscarinics on GIT

A
  • 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
Q

Effect of anti-muscarinics on GI motility

A

• 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
Q

Effect of anti-muscarinics on respiratory tract

A
  • 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
Q

Effect of anti-muscarinics on respiratory tract (smooth muscle contraction)

A
  • Action: Inhibit smooth muscle contraction in larynx and bronchioles
  • Uses: prevent laryngospasm and bronchospasm in anaesthesia
36
Q

Effect of anti-muscarinics on Genito-urinary tract

A
  • 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
Q

Atropine in CNS

A
  • Benztropine, benzhexol: control of tremor in Parkinsonism
  • Scopolamine: prevention of motion sickness
  • SE: dizziness, light-headedness, fatigue
38
Q

Atropine other uses

A
  • Treatment of mushroom poisoning, organophosphate insecticide poisoning, exposure to chemical warfare agents (sarin)
  • Myasthenia Gravis: used with Neostigmine
39
Q

Ganglion stimulating agents

A
  • Nicotine, Lobeline, TMA

* Stimulates CNS

40
Q

Ganglion blocking agents examples

A
  • Hexamethonium
  • Mecamylamine
  • Trimethaphan
41
Q

Ganglion blocking agents effects

A
  • 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
Q

Ganglion blocking agents therapeutic uses

A
  • Acute hypertensive crisis

* Autonomic hyperreflexia

43
Q

Pyridostigmine use

A

Myasthenia gravis

44
Q

Succinylcholine use

A

Neuromuscular block (eg. tracheal intubation)

45
Q

Pilocarpine use

A

Acute narrow angle glaucoma

46
Q

Atropine use

A

Pre-anaesthetic medication, organophosphate insecticide poisoning, mushroom poisoning, eye examination

47
Q

Benztropine use

A

Parkinsonism

48
Q

Scopolamine use

A

Motion sickness

49
Q

Tubocurarine use

A

NMB (Nicotinic block)

Foundation 2 (11 decks)

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