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Pharm 1 > Anti-cholinesterase Drugs > Flashcards

Anti-cholinesterase Drugs Flashcards

1
Q

Which drug is a tertiary amine (NH3) and what makes it unique?

A

Physostigmine

- lipophillic and small enough to cross the BBB

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2
Q

Which drugs are quaternary ammoniums (NH4)?

A

Edrophonium
Neostigmine
Pyrostigmine

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3
Q

Which organs can Ach go to?

A

Heart
Gut
Lungs

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4
Q

How do anti-AchE drugs work?

A
  • inhibit acetylcholinesterase

—> result in increased availability of Ach at neuromuscular junction, muscarinic receptors, and autonomic ganglia

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5
Q

What happens if anti-AchE meds are given when NMB not there?

A

Will cause fasiculations/overstimulation- in large doses

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6
Q

How do neostigmine and pyridostigmine reverse NMBs?

A
  • hydrolyzed by AchE (enzyme)
  • carbamalates the enzyme is the process
  • blocks enzymes ability to hydrolyze Ach

(Interferes with the breakdown of Ach, neostigmine
Indirectly stimulates nicotinic and muscarinic receptors)

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7
Q

How does Edrophonium work?

A

Forms a reversible elecrostatic attachment

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8
Q

What are the different classifications for AchE inhibiting drugs?

A

Reversible inhibition:
- electrostatic attachment at anionic site

Formation of carbamylesters (reversible)
- done at esteratic site
(Neo, pyrido, physostigmine)

Irreversible inhibition:
- organophosphates combine with the esteratic site to form a stable inactive complex—> lasts for months
(Pesticides, chemical warfare)

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9
Q

T/F At doses greater than usual clinical doses, anticholinesterase drugs have been reported to produce some form of neuromuscular blockade.

A

True

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10
Q

T/F dementia meds other than Namenda might interact with NMBs.

A

True

Dementia meds are P.O. AchE inhibitors

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11
Q

______________ is the most important determinant of relative potency.

A

Affinity

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12
Q

Clinically all AchE inhibitors have the same duration, which is:

A

T 1/2= 60-120 min

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13
Q

What is the onset of action for edrophonium, neostigmine, and pyridostigmine?

A
  • edrophonium: 1-2 min
  • neostigmine: 7-11 min
  • pyridostigmine: up to 16 min
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14
Q

What influence does age have with AchE inhibitors?

A

Neostigmine dose: adult > child > infant

- Edrophonium doses all the same across age

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15
Q

What are muscarinic effects?

A

More Ach= more rest and digest

  • bradycardia
  • salivation (risk of aspiration)
  • bronchoconstriction
  • miosis (delirium since they can’t see)
  • hyperperistalsis—> increased risk of PONV- pretty significant
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16
Q

What are nicotinic effects?

A

Act on neuromuscular junction and autonomic ganglia

17
Q

___________ and ___________ (but not Edrophonium) produce a marked and prolonged inhibition of plasma cholinesterase.

A

Neostigmine and pyridostigmine

18
Q

What are anticholinesterase effects on CV, GI, GU, lungs and eyes?

A

(All from increasing PSNS)
CV
- bradycardia/bradyarhythmia, AV block, decreased SVR and BP
GI/GU
Increased fluid secretion, increased motility, post op NV (neo)
Lung
- bronchoconstriction, increased airway resistance
Eye
- miosis, inability to focus on near vision, increased IOP

19
Q

What are clinical uses for anticholinesterase drugs?

A
  • antagonist assisted reversal of NMB
  • treatment of CNS effects of certain drugs
    • tertiary amines cross the BBB
  • treatment of myasthenia gravis
    • increase Ach at neuromuscular junction
  • treatment of glaucoma
    • causes miosis
  • post op analgesia
  • post op shivering
20
Q

With antagonist-assisted reversal of NMB, when should the anticholinesterase drug be administered?

A

During time of spontaneous recovery—> increases availability of Ach at NMJ
- acts pre and post synaptic

21
Q

What is the onset and duration like for anticholinesterase drugs?

A 
Onset:
- Edrophonium = rapid
- neostigmine= intermediate
- pyridostigmine = delayed
Duration:
- similar for all—> 55-75 min
22
Q

Potency depends on:

A
  • NMB being antagonized
  • speed of spontaneous recovery
  • depth of NMB when reversal is initiated
  • end point selected
23
Q

Why area anticholinesterase drugs mixed with anti cholinergic drugs?

A

To block muscarinic effects (reversal requires only nicotinic effects)
- administer anti cholinergic with a faster onset than anticholinesterase drug to minimize bradycardia

Pharm 1 (9 decks)

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