Acetylcholinesterase Inhibitors Flashcards
What is MOA of Physostigmine?
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.
What are the Indications of Physostigmine?
"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)"
What is the Onset, DOA, E1/2 life, Vd, and metabolism of action of physostigmine?
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
What are the adverse effects of physostigmine?
“Bradycardia
Increased secretions, bronchoconstriction,
N/V
Cholinergic crisis when given to MG with NDMB
Hypotension
Pupillary constriction
EEG arousal – crosses BBB”
What are the contraindications of Physostigmine?
“Urinary or GI obstruction
Concomitant use with succs
CV disease”
What is the drug class of Edrophonium?
Acetylcholinesterase Inhibitor with quaternary ammonium structure
What is the MOA of Edrophonium?
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.
What are the indications of Edrophonium?
“Reversal of Non depolarizing NMB
Diagnosis and management of cardiac dysrhythymias (SVT), and MG”
What is the onset, DOA, Vd, PB, and Metabolism of Edrophonium?
1) Onset = 1 min
2) DOA = 45-60mins
3) Vd = 1.4L/kg
4) 0% PB
5) Hepatic metabolism 25% and 75% via kidneys
What are the adverse effects of Edrophonium?
"Bradycardia, cardiac arrest Salivation, Bronchospasm, laryngospasm Hypotension or hypertension Diarrhea, vomiting Seizure Diaphoresis Resp depression"
What are the contraindications of Edrophonium?
“Caution without co-administration of antiAch
hypotension
Bradycardia
Hypotension
Intestinal obstruction, urinary obstruction
Asthma
Drug interactions with aminoglycosides”
What are the dosage of Edrophonium?
“0.5-1.0mg/kg IV (Atropine 0.01mg/kg)
1/10th potency of neostigmine”
What is the drug class of Neostigmine?
Acetylcholinesterase Inhibitor with quaternary ammonium structure
What is the MAO of Neostigmine?
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.
What are the indications of Neostigmine?
“Reversal of Non depolarizing NMB
Treatment of MG, glaucoma, urinary retention, paralytic ileus”
What is the Onset, Peak, DOA, Vd, E1/2t, and Metabolism of Neostigmine?
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
What are the adverse effects of Neostigmine?
"Bronchospasm Salivation Bradycardia Abdominal cramps, nausea, vomiting Loss of bladder and rectal control"
What are the contraindications of Neostigmine?
"Without co-administration of antiAch Severe CAD Asthma GI obstruction Previous AchE Caution in renal disease"
What are the dosage of Neostigmine?
0.05-0.1mg/kg (glycopyrrolate 0.01 mg/kg)
What is the drug class of Pyridostigmine?
“Acetylcholinesterase Inhibitor
Quaternary ammonium structure”
What is the MAO of Pyridostigmine?
“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.”
What are indications of Pyridostigmine?
"Antagonize nondepolarizing NMB Urinary and GI motility agent Treat glaucoma MG treatment Pretreatment for Soman nerve gas"
What is the Onset, dOA, E1/2t, Vd, PB, and metabolism of Pyridostigmine?
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%
What are the adverse effects of Pyridostigmine?
"Bradycardia Hypotension Bronchospasm Intestinal spasm dysrhythmias"
What are the contraindications of Pyridostigmine?
“Hypersensitivity
Bromide allergy
Gi-GU obstruction
Caution in renal disease”
What are the dosage of Pyridostigmine?
“100-300mcg/kg (max 350mcg/kg)
(with atropine 0.02mg/kg or glycol 0.01mg/kg)”
What is the class of Physostigmine?
“Acetylcholinesterase Inhibitor: Tertiary amine crosses BBB”
