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Cholinesterase Inhibitors and Other Pharmacologic Antagonists to NMBA > Cholinergic Pharmacology: The Basics > Flashcards

Cholinergic Pharmacology: The Basics Flashcards

Information from M&M Notecards

1
Q

ACh Synthesis:

A

ACh is synthesized in nerve terminals by the enzyme CHOLINE ACETYLTRANSFERASE from CHOLINE and ACETYLCOENZYME A

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2
Q

ACh Degradation:

A

ACh is hydrolyzed by the enzyme acetylcholinesterase into:

acetate and choline

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3
Q

What are the two receptor types?

A

nicotinic and muscarinic

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4
Q

Nicotinic Receptors

A

stimulate autonomic ganglia and sk. m.

these receptors are also activated by the nicotine alkaloid

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5
Q

Muscarinic Receptors

A

stimulate end organ receptors

these receptors are also activated by the alkaloid muscarine

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6
Q

How does normal muscle action work?

A

NM Transmission depends on the release of ACh from presynaptic neurons and activation of postsynaptic nicotinic cholinergic receptors on the motor end plate

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7
Q

How do non depolarizing muscle relaxants work?

A

NM transmission is blocked by non depolarizing muscle relaxants that bind to POSTSYNAPTIC NICOTINIC cholinergic receptors

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8
Q

Reversal of Nondepolarizing Muscle Relaxants:

Spontaneous Reversal

A

occurs with gradual diffusion
redistribution
metabolism
and excretion of non depolarizing muscle relaxant

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9
Q

Reversal of Nondepolarizing Muscle Relaxants:

Pharmacologic Reversal

A

occurs with the admin of specific reversal agents

Reversal with acetylcholinesterase inhibitors should be monitored with a peripheral nerve stimulator

At least 1 twitch with TOF stim should be present before reversal

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10
Q

What are organophosphates?

A

they are used in ophthalmology and pesticides.

they IRREVERSIBLY bind to cholinesterase inhibitors

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11
Q

Side Effects of Acetylcholinesterase Inhibitors

A

in addition to increasing the availability of acetylcholine at the NMJ, inhibition of acetylcholinesterase can increase CHOLINERGIC receptor activity elsewhere leading to side effects.

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12
Q

Side Effects of Acetylcholinesterase Inhibitors:

Cardiovascular

A

CV System: the predominant muscarinic effect on the heart is vagal like bradycardia that can progress to sinus arrest

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13
Q

Side Effects of Acetylcholinesterase Inhibitors:

Pulmonary

A

Pulmonary Receptors: muscarinic stim can result in bronchospasm and increased respiratory secretions

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14
Q

Side Effects of Acetylcholinesterase Inhibitors:

Cerebral

A

Cerebral receptors: Physostigmine is a cholinesterase inhibitor that can cross the BBB. It can diffuse activation of the EEG by stimulating muscarinic and nicotinic receptors within the CNS

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15
Q

Side Effects of Acetylcholinesterase Inhibitors:

GI

A

GI Receptors:

muscarinic stim increases peristaltic activity - esophageal, gastric, and intestinal;

Glandular secretions - salivary and parietal

Periooperative bowel anastomotic leakage

Nausea and vomiting

Fecal incontinence

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16
Q

Neostigmine: Mechanism of Action

A

acetylcholinesterase inhibitor

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17
Q

Neostigmine: Dosage

A

up to 0.08 mg/kg in children

5 mg in adults

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18
Q

Neostigmine: Onset

A

effects apparent in 5-10 mins

peak at 10 minutes and last more than 1 hour

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19
Q

Neostigmine: Clinical Note

A

typically administered with glycopyrrolate to prevent bradycardia

20
Q

Neostigmine: Structure

A

carbamate moiety - binds to acetylcholinesterase

quaternary ammonium group - prevents passage across BBB

21
Q

Pyridostigmine: Mechanism of Action

A

acetylcholinesterase inhibitor

22
Q

Pyridostigmine: Dosage

A

up to 0.4 mg/kg in children

20 mg in adults

23
Q

Pyridostigmine: Onset

A

effects apparent in 10-15 mins and lasts more than 2 hours

24
Q

Pyridostigmine: Clinical Note

A

typically admin with glycopyrrolate to prevent bradycardia

25
Q

Pyridostigmine: Structure

A

carbamate moiety - binds to actylcholinesterase

quaternary ammonium incorporated into PHENOL ring - prevents passage across BBB

26
Q

Edrophonium: Mechanism of Action

A

acetylcholinesterase inhibitor

27
Q

Edrophonium: Dosage

A

0.5 - 1 mg/kg

28
Q

Edrophonium: Onset

A

most rapid onset and shortest duration for class. effects apparent in 1-2 mins. higher dosages last up to 1 hour.

29
Q

Edrophonium: Clinical Note

A

typically administered with atropine to prevent bradycardia.

If used with glycopyrrolate, should be given several minutes after glycol so that onset time matches

30
Q

Edrophonium: structure

A

noncovalent binding to acetylcholinesterase

Quaternary ammonium group - prevents passage across BBB

31
Q

Physostigmine: Mechanism of Action

A

Acetylcholinesterase inhibitor

32
Q

Physostigmine: Dosage

A

0.01 - 0.03 mg/kg

33
Q

Physostigmine: Clinical Note

A

can be used to treat anticholinergic toxicity from scopolamine or atropine overdose

also reverses some of the CNS depression from benzodiazapines and volatile anesthetics

34
Q

Physostigmine: Structure

A

carbamate moiety.

lack of quaternary ammonium allows passage across the BBB

35
Q

Which cholinesterase inhibitor allows passage across the BBB?

A

Physostigmine - b/c it lacks the quaternary ammonium group

36
Q

Sugammadex: Mechanism of Action

A

hydrophobic structural interactions trap aminosteroid NMBA (rocuronium, vecuronium) within CYCLODEXTRIN cavity, terminating NMB

37
Q

Suggamadex: Dosage

A

4 - 8 mg/kg

38
Q

Suggamadex: onset

A

can reverse shallow and deep NMB within 2 mins

39
Q

Suggamadex: Clinical Note

A

b/c of concerns about hypersensitivity and allergic reactions, not yet approved by US FDA

currently available in Europe

40
Q

Suggamadex: Structure

A

Modified cyclodextrin

41
Q

L-Cysteine: Mechanism of Action

A

combines with gantacurium to form less active degradation products

42
Q

L-Cysteine: Dosage

A

10-50 mg/kg

43
Q

L-Cysteine: Clinical Note

A

Still in investigative stages

44
Q

L-Cysteine: Structure

A

an endogenous amino acid

45
Q

The parasympathetic nervous system uses acetylcholine where?

A

As a PREganglionic and POSTganglionic NT

46
Q

Nicotinic receptors are blocked by_______

Muscarinic receptors are blocked by _________

A

Muscle relaxants (NMBAs)

Anticholinergic drugs (ex: atropine)

47
Q

Nicotine stimulates _______

Muscarine activates _______

A

Autonomic ganglia and skeletal muscle receptors (nicotinic receptors)

End organ effector cells in bronchial smooth muscle, salivary glands and SA node (Muscarinic receptors)

Cholinesterase Inhibitors and Other Pharmacologic Antagonists to NMBA (1 decks)

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