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PDA Block 1 > Cholinergics > Flashcards

Cholinergics Flashcards

1
Q 
Muscarinic Receptors
Eye:
Heart:
Lung:
Bladder:
GI tract:
Sweat Glands:
Blood Vessels:
A

Eye: Contraction of the ciliary muscle focus lens for near vision; Contraction of the iris sphincter muscle
Heart: Decreased rate
Lung: Constriction of bronchi; secretion
Bladder: Voiding
GI tract: Salivation; Increased gastric secretion; increased intestinal motility
Sweat Glands: Generalized sweating
Blood Vessels: Vasodilation

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2
Q

Nicotinic Receptors
Nm:
Nn:
CNS:

A

Nm: Skeletal muscle - End-plate depolarization
Nn: Autonomic ganglia and Adrenal medulla - depolarization and firing of post-ganglionic neurons; Depolarization and secretion of catecholamines
CNS: Control of neurotransmitter release

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3
Q

Cholinergic Agonists and Antagonists

A 
Muscarinic Receptor Agonists
Acetylcholinesterase inhibitors
- Reversible inhibitors
- Irreversible inhibitors
Muscarinic Receptor Antagonists
Ganglionic Blocking Agents
Neuromuscular Blocking Agents
- Competitive blockers
- Depolarizing blockers
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4
Q

Muscarinic Agonists

A

Direct agonists of muscarinic receptors; produce effects similar to activating post-ganglionic parasympathetic nerves (parasympathomimetics)

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5
Q

Choline Esters

A

Acetyclcholine; Bethanechol

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6
Q

Bethanechol
Primarily Effects:
Therapeutic Uses:

A

Primarily effects G.I/G.U systems

Therapeutic Uses: Orally or subcutaneous treatment for urinary retention in the absence of obstruction

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7
Q

Alkaloids

A

Muscarine; Pilocarpine

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8
Q

Pilocarpine - Therapeutic Effects

A
  • Orally for xerostomia

- Miotic agent used opthalmically to treat wide-angle glaucoma as well as emergency treatment for narrow-angle glaucoma

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9
Q

Bethanechol and Pilocarpine: Route of administration

A

Not IV
Oral (bethanechol, pilocarpine) or Subcutaneous (Bethanechol)
Opthalmic: pilocarpine, acetylcholine

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10
Q

Bethanechol and Pilocarpine: Side Effects

A

Salivation, Lacrimation, Urination, Defacation, Gastrointestinal upset, Emesis (SLUDGE)
Also… Hypotension, bradycardia and blurred vision
Toxicity: treated with muscarinic receptor antagonist (atropine)

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11
Q

Bethanechol and Pilocarpine: Use with caution in patients with…

A

Athsma and COPD
Urinary or GI obstruction and peptic ulcer
Cardiovascular diseases involving bradycardia or hypotension

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12
Q

Acetylcholinesterase Inhibitors

A

Enhance the effects of endogenously released acetycholine by blocking its natural breakdown by acetylcholinesterase

  • Effective at any site where acetycholine is the neurotransmitter
  • Also termed anticholinesterase agents
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13
Q

Acetylcholinesterase Sites of action

A
  • Post-ganglionic parasympathetic neuroeffector junction
  • Ganglia (Sympathetic and Parasympathetic)
  • Neuromuscular junction
  • CNS (if able to penetrate)
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14
Q

Reversible acetycholinesterase inhibitors

A

Edrophonium
Physostigmine
Neostigmine

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15
Q

Edrophonium - Therapeutic Use

A
  • Diagnosis of myasthenia gravis
  • Distinguish cholinergic from myasthenic crisis
  • Reverse paralysis by competitive neuromuscular blocking agents
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16
Q

Administration of Edrophonium

A

Rapid onset and short duration of action
Does not penetrate into CNS
Not orally active (IV administration)

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17
Q

Physostigmine - Therapeutic Use:

A

Treatment of chronic wide-angle glaucoma

Toxicity by antimuscarinic drug poisoning

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18
Q

Physostigmine: Structure

A

Tertiary Amine (lipophilic) - CNS effects

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19
Q

Neostigmine: Structure

A

Synthetic: Quarternary amine so no CNS penetration

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20
Q

Neostigmine - Therapeutic Use:

A

Treatment of myasthenia gravis (oral)
Prevention and treatment of post-operative atony of gut and bladder (oral)
Reversal of paralysis by neuromuscular junction blocking agents

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21
Q

Reversible Acetycholinesterase Inhibitors - Side Effects

A

SLUDGE

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22
Q

Irreversible Acetycholinesterase Inhibitors are all….

A

Lipophilic and can pass through mucosal membranes and skin

23
Q

Nerve gas used in attacks in Japan and Syria

A

Sarin

24
Q

Malathion

A

Insecticide - greater safety than Sarin because it is detoxified in higher organisms

25
Q

Toxicity of Irreversible Acetycholinesterase Inhibitors (Organophosphate)

A
  • SLUDGE
  • Hypotension; Bradycardia; Bronchoconstriction; Blurred vision
  • Death due to respiratory failure
  • Medullary respiratory center depression
  • Symptom onset depends on method of exposure
26
Q

Treatment for Organophosphate

A
  • Remove poisoning
  • Maintain open airway; artificial respiration
  • Treat convulsions and shock
    Antidotes
  • Atropine
  • Pralidoxime
27
Q

Pralidoxime

A

Reactivates Acetycholine esterase peripherally

Must treat quickly (2-3 hours)

28
Q

Muscarinic Receptor Antagonists

A

Competitively block muscarinic receptors (Parasympatholytics)

29
Q

Effects of Muscarinic antagonists

A
  • Relax iris sphincter and ciliary muscles
  • Relax non-vascular smooth muscle
  • Inhibit exocrine gland secretion
  • Increase heart rate
  • CNS effects (Sedation (low doses); Excitement, delirium, psycohsis (high hoses))
30
Q

Atropine - Therapeutic Uses

A
  • Bradyarrhythmias
  • Opthalmic uses - mydriasis and cycloplegia
  • Block vagal reflexes and reduce secretions during anesthesia
  • Acetylcholinesterase and muscarinic toxicity
31
Q

Scopolamine - Therapeutic Use

A

Motion sickness and vestibular diseases

32
Q

Muscarinic Receptor Antagonists: Alkaloids

A

Atropine; Scopolamine

33
Q

Muscarinic Receptor Antagonists: semi-synthetic derivative

A

Ipratropium

34
Q

Ipratropium - Therapeutic Use

A

COPD

Less effective for athsma

35
Q

Ipratropium administration and actions

A

Administered by inhalation
No CNS penetration and poor systemic absorption when inhaled
Reduces bronchial secretions and reduces bronchoconstriction

36
Q

Muscarinic Receptor Antagonists: Synthetics

A

Tropicamide
Oxybutynin
Darifenacin
Glycopyrrolate

37
Q

Tropicamide - Therapeutic Use

A 
Mydriatic and Cycloplegic
Fast onset (20-40 min) and short duration of action (4-6 hours)
38
Q

Oxybutynin
Therapeutic Use:
Side-effects

A

Therapeutic use: Overactive bladder, incontinence

SE: xerostomia, blurred vision, constipation

39
Q

Darifenacin (Has some M3 selectivity)

Therapeutic use:

A

Overactive bladder, incontinence

Less CNS side effects

40
Q

Glycopyrrolate - Therapeutic Use:

A

Used to block parasympathomimetic effects when neostigmine is used to reverse+ skeletal muscle paralysis by neuromuscular blocking agents
No CNS penetration

41
Q

Muscarinic Receptor Antagonists: Side Effects

A 
Hot as a hare (no sweating)
Dry as a bone (Dry mouth)
Red as a beet (Due to excess heat)
Blind as a bat (Mydriasis, cycloplegia)
Drowsiness (CNS actions)
Mad as Hatter (at high concentrations)
42
Q

Muscarinic Receptor Antagonists: Use with caution

A

Glaucoma
Benign Prostatic hyperplasia
Any disease where tachycardia is a problem (angina)

43
Q

Neuromuscular blocking agents

A

Block neurotransmission at the neuromuscular junction producing paralysis of skeletal muscle - Used as adjuvant in surgical anesthesia

44
Q

All competitive neuromuscular blocking agents are…

A

Quartenary amines, so no CNS effects, not absorbed

45
Q

Competitive Neuromuscular blocking agents differ in:

A 
Duration of action (Short, medium, long)
Side Effects (Cardiovascular, histamine)
Elimination route (Metabolism, renal excretion)
46
Q 
Rocuronium
Duration of action:
Elimination:
CV effects:
Histamine Release:
A

Duration of action: Intermediate (30-60 min)
Elimination: Liver metabolism
CV effects: Minimal
Histamine Release: None

47
Q 
Atracurium
Duration of action:
Elimination:
CV effects:
Histamine Release:
A

Duration of action: Intermediate (30-60 minutes)
Elimination: Spontaneously degrades in plasma
CV effects: Minimal
Histamine Release: Slight

48
Q 
Vercuronium
Duration of action:
Elimination:
CV effects:
Histamine Release:
A

Duration of action: Intermediate (60-90 minutes)
Elimination: Liver metabolism
CV effects: Minimal
Histamine Release: None

49
Q 
Pancuronium
Duration of action:
Elimination:
CV effects:
Histamine Release:
A

Duration of action: Long (120-180 min)
Elimination: Renal excretion
CV effects: Slight increase in HR and BP
Histamine Release: Slight

50
Q

Depolarizing Neuromuscular Blockers

A

Activate nicotinic receptors at the neuromuscular junction maintaining motor end plate depolarization and thus prevents transmission of another action potential

51
Q

Succinylcholine (Depolarizing Neurmuscular Blocker)
Duration of Action:
Metabolized by:

A

Ultra short duration of action (5-8 minutes)
- Rapid onset (1 - 1.5 minutes)
Metabolized by pseudocholinesterase

52
Q

Competitive Neuromuscular blockers - Adverse Effects and Toxicity

A
  • Prolonged apnea
  • Toxicity or overdose with competitive antagonists can be reversed by administering an acetylcholinesterase inhibitor
  • If treat with an acetylcholinesterase inhibitor, treat with glycopyrrolate to minimize muscarinic actions
53
Q

Depolarizing Neuromuscular blockers - Adverse Effects and Toxicity

A
  • Prolonged apnea
  • Malignant hyperthermia
  • Post operative muscle pain due to muscle fasciculation
  • Hyperkalemia

PDA Block 1 (13 decks)

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