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Pharmacology > Acetylcholinesterase Inhibitors > Flashcards

Acetylcholinesterase Inhibitors Flashcards

1
Q

What is MOA of Physostigmine?

A

REVERSIBLY binds through electrostatic attachment to anionic site on AchE to inhibit rapid hydrolysis of Ach by Ache = ↑concentration of Ach in synaptic cleft at muscarinic and nicotinic receptors.

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2
Q

What are the Indications of Physostigmine?

A 
"Treat atropine and scopolamine toxicity (reverse effects – crosses BBB)
Treat MG
Treat Glaucoma via gtts
To improve alzheimers
Not used to reverse NMB (bc big dose)"
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3
Q

What is the Onset, DOA, E1/2 life, Vd, and metabolism of action of physostigmine?

A

1) Onset = 5 mins
2) DOA = 0.5-5hrs
3) E1/2 life = 15-40mins
4) Vd = 0.1L/kg
5) Hydrolyzed at its ester linkage by cholinesterase and renal excretion is minimal

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4
Q

What are the adverse effects of physostigmine?

A

“Bradycardia
Increased secretions, bronchoconstriction,
N/V
Cholinergic crisis when given to MG with NDMB
Hypotension
Pupillary constriction
EEG arousal – crosses BBB”

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5
Q

What are the contraindications of Physostigmine?

A

“Urinary or GI obstruction
Concomitant use with succs
CV disease”

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6
Q

What is the drug class of Edrophonium?

A

Acetylcholinesterase Inhibitor with quaternary ammonium structure

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7
Q

What is the MOA of Edrophonium?

A

Binds REVERSIBLY through electrostatic attachment to anionic site on AchE to inhibit rapid hydrolyisis of Ach by AchE = ↑concentration of Ach in synaptic cleft at muscarinic and nicotinic receptors. Antagonizing Nondepolarizing NMB at muscarinic receptors.

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8
Q

What are the indications of Edrophonium?

A

“Reversal of Non depolarizing NMB

Diagnosis and management of cardiac dysrhythymias (SVT), and MG”

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9
Q

What is the onset, DOA, Vd, PB, and Metabolism of Edrophonium?

A

1) Onset = 1 min
2) DOA = 45-60mins
3) Vd = 1.4L/kg
4) 0% PB
5) Hepatic metabolism 25% and 75% via kidneys

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10
Q

What are the adverse effects of Edrophonium?

A 
"Bradycardia, cardiac arrest
Salivation, Bronchospasm, laryngospasm
Hypotension or hypertension
Diarrhea, vomiting
Seizure
Diaphoresis
Resp depression"
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11
Q

What are the contraindications of Edrophonium?

A

“Caution without co-administration of antiAch
hypotension
Bradycardia
Hypotension
Intestinal obstruction, urinary obstruction
Asthma
Drug interactions with aminoglycosides”

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12
Q

What are the dosage of Edrophonium?

A

“0.5-1.0mg/kg IV (Atropine 0.01mg/kg)

1/10th potency of neostigmine”

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13
Q

What is the drug class of Neostigmine?

A

Acetylcholinesterase Inhibitor with quaternary ammonium structure

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14
Q

What is the MAO of Neostigmine?

A

Binds IRREVERSIBLY through electrostatic attachment to anionic site on AchE to inhibit rapid hydrolyisis of Ach by AchE = ↑concentration of Ach in synaptic cleft at muscarinic and nicotinic receptors. Antagonizing Nondepolarizing NMB at muscarinic receptors.

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15
Q

What are the indications of Neostigmine?

A

“Reversal of Non depolarizing NMB

Treatment of MG, glaucoma, urinary retention, paralytic ileus”

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16
Q

What is the Onset, Peak, DOA, Vd, E1/2t, and Metabolism of Neostigmine?

A

1) Onset 5-15mins
2) Peak = 7mins
3) DOA = 45-90mins (1)
4) Vd = 0.8L/kg (1)
5) E1/2t = 80mins
6) 25% Liver, 25% plasma esterases, 50% renal

17
Q

What are the adverse effects of Neostigmine?

A 
"Bronchospasm
Salivation
Bradycardia
Abdominal cramps, nausea, vomiting
Loss of bladder and rectal control"
18
Q

What are the contraindications of Neostigmine?

A 
"Without co-administration of antiAch
Severe CAD
Asthma
GI obstruction
Previous AchE
Caution in renal disease"
19
Q

What are the dosage of Neostigmine?

A

0.05-0.1mg/kg (glycopyrrolate 0.01 mg/kg)

20
Q

What is the drug class of Pyridostigmine?

A

“Acetylcholinesterase Inhibitor

Quaternary ammonium structure”

21
Q

What is the MAO of Pyridostigmine?

A

“Bind REVERSIBILY through electrostatic attachment to anionic site on AchE to inhibit rapid hydrolysis of Ach by AchE =
↑concentration of Ach in synaptic cleft at muscarinic and nicotinic receptors.”

22
Q

What are indications of Pyridostigmine?

A 
"Antagonize nondepolarizing NMB
Urinary and GI motility agent
Treat glaucoma
MG treatment
Pretreatment for Soman nerve gas"
23
Q

What is the Onset, dOA, E1/2t, Vd, PB, and metabolism of Pyridostigmine?

A

1) Onset = 16 mins
2) DOA 2 hrs
3) E1/2t = 2 hrs
4) Vd 1L/kg
5) 0% PB
6) Hepatic 25%, renal 75%

24
Q

What are the adverse effects of Pyridostigmine?

A 
"Bradycardia
Hypotension
Bronchospasm
Intestinal spasm
dysrhythmias"
25
Q

What are the contraindications of Pyridostigmine?

A

“Hypersensitivity
Bromide allergy
Gi-GU obstruction
Caution in renal disease”

26
Q

What are the dosage of Pyridostigmine?

A

“100-300mcg/kg (max 350mcg/kg)

(with atropine 0.02mg/kg or glycol 0.01mg/kg)”

27
Q

What is the class of Physostigmine?

A

“Acetylcholinesterase Inhibitor: Tertiary amine crosses BBB”

Pharmacology (17 decks)

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