Term
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Definition
Class: acetylcholinesterase inhibitor, noncovalent
Mechanism: blocks anionic site from binding Ach (prevent best binding for enzymatic action), centrally acting
Indication: Alzheimer's dz (improve cognition and global clinical fx, delay symptomatic progression for up to 1yr)
Adverse Effects: relatively mild, nausea, diarrhea, |
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Term
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Definition
Class: acetylcholinesterase inhibitor, noncovalent
Mechanism: blocks active site from binding Ach, does not enter CNS, 2-10min duration
Indication: diagnosis test of myasthenia gravis (Tensilon test)
Adverse Effects: relatively mild, nausea, diarrhea |
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Term
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Definition
Class: alzheimer drug
Mechanism: NMDA receptor antagonist, may be neuroprotective
Indication: Alzheimer disease (small effect on cognition and global clinical fx)
Adverse Effects: dizziness, increase agitation, delusion behaviors |
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Term
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Definition
Class: AChE inhibitor, reverisble carbamate inhibitor
Mechanism: occupy the enzymatic site of AChE, hydrolyzed from enzyme more slowly --> fewer sties available for ACh cleavage; DOES NOT CROSS BBB
Indication:
1. increase transmission at NMJ (myasthenia gravis, eaton-lambert sydnroe, tubocurare poisoning)
2. increase PSNS tone (PARALYTIC ILEUS, post-up urinary retention or bladder distention)
Contraindication: bronchial asthma, urinary or GI obstruction
Adverse Effects: nausea and diarrhea esp, other excess muscarinic activity |
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Term
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Definition
Class: AChE inhibitor, reverisble carbamate inhibitor
Mechanism: occupy the enzymatic site of AChE, hydrolyzed from enzyme more slowly --> fewer sties available for ACh cleavage; ENTERS CNS
Indication:
1. increase transmission at NMJ (myasthenia gravis, eaton-lambert sydnroe, tubocurare poisoning)
2. increase PSNS tone (post-up urinary retention or bladder distention)
3. ANTIDOTE for CENTRAL ANTIMUSCARINIC POISONING
4. glaucoma - not first line
Contraindication: bronchial asthma, urinary or GI obstruction
Adverse Effects: nausea and diarrhea esp, other excess muscarinic activity |
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Term
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Definition
Class: AChE inhibitor, reverisble carbamate inhibitor
Mechanism: occupy the enzymatic site of AChE, hydrolyzed from enzyme more slowly --> fewer sties available for ACh cleavage; DOES NOT CROSS BBB
Indication:
1. increase transmission at NMJ (myasthenia gravis, eaton-lambert sydnroe, tubocurare poisoning)
2. increase PSNS tone (post-up urinary retention or bladder distention)
Contraindication: bronchial asthma, urinary or GI obstruction
Adverse Effects: nausea and diarrhea esp, other excess muscarinic activity |
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Term
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Definition
Class: AChE inhibitor, organophosphorous compound, therapeutic
Mechanism: substrate of AChE that forms stable practically permanent enzyme-substrate complex, leaves phosphorylate group on enzyme
Indication: topical only for glaucome (not first-line)
Adverse Effects: fixed pupils, blurred vision (can't accomodate) |
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Term
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Definition
Class: AChE inhibitor, organophosphorous compound, pesticide
Mechanism: substrate of AChE that forms stable practically permanent enzyme-substrate complex, leaves phosphorylate group on enzyme
Indication: insecticide
Adverse Effects:
1. depolarizing blockade (nicotinic): NMJ blockade --> muscle weak --> respiratory failure --> death
2. hyperactivity (muscarinic): peripheral PSNS --> bradycardia --> arrhythmias/arerest --> death
3. hyperactivity (muscarinic): excessive airway secretion and constriction --> asphyxiation --> death
4. hyperactivity (muscarinic): CNS --> decreased respiratory drive --> respiratory failure --> death
5. hyperacitivty (muscarinic): CNS --> generalized seizures --> convulsions --> death |
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Term
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Definition
Class: AChE inhibitor, organophosphorous compound, pesticide
Mechanism: substrate of AChE that forms stable practically permanent enzyme-substrate complex, leaves phosphorylate group on enzyme
Indication: insecticide
Adverse Effects:
1. depolarizing blockade (nicotinic): NMJ blockade --> muscle weak --> respiratory failure --> death
2. hyperactivity (muscarinic): peripheral PSNS --> bradycardia --> arrhythmias/arerest --> death
3. hyperactivity (muscarinic): excessive airway secretion and constriction --> asphyxiation --> death
4. hyperactivity (muscarinic): CNS --> decreased respiratory drive --> respiratory failure --> death
5. hyperacitivty (muscarinic): CNS --> generalized seizures --> convulsions --> death |
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Term
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Definition
Class: AChE inhibitor, organophosphorous compound, weapon
Mechanism: substrate of AChE that forms stable practically permanent enzyme-substrate complex, leaves phosphorylate group on enzyme
Indication: nerve gas
Adverse Effects:
1. depolarizing blockade (nicotinic): NMJ blockade --> muscle weak --> respiratory failure --> death
2. hyperactivity (muscarinic): peripheral PSNS --> bradycardia --> arrhythmias/arerest --> death
3. hyperactivity (muscarinic): excessive airway secretion and constriction --> asphyxiation --> death
4. hyperactivity (muscarinic): CNS --> decreased respiratory drive --> respiratory failure --> death
5. hyperacitivty (muscarinic): CNS --> generalized seizures --> convulsions --> death |
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Term
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Definition
Class: AChE inhibitor, organophosphorous compound, weapon
Mechanism: substrate of AChE that forms stable practically permanent enzyme-substrate complex, leaves phosphorylate group on enzyme
Indication: nerve gas
Adverse Effects:
1. depolarizing blockade (nicotinic): NMJ blockade --> muscle weak --> respiratory failure --> death
2. hyperactivity (muscarinic): peripheral PSNS --> bradycardia --> arrhythmias/arerest --> death
3. hyperactivity (muscarinic): excessive airway secretion and constriction --> asphyxiation --> death
4. hyperactivity (muscarinic): CNS --> decreased respiratory drive --> respiratory failure --> death
5. hyperacitivty (muscarinic): CNS --> generalized seizures --> convulsions --> death |
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Term
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Definition
Class: antimuscarinic
Mechanism: muscarinic antagonist; CAN ACCESS CNS
Indication: blocks the effects of organophosphorus compounds at muscarinic receptors (decreases death via their hyperactivity) |
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Term
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Definition
Class: cholinergic
Mechanism: strong nucleophile, yanks organophosphates off of AChE --> frees it up to degrade the excessive AC; no access to CNS
Indication: use to treat peripheral affects of organophosphate poisoning |
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Term
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Definition
misosis
bronchocontriction
GI stimulation
micturition
bradycardia
sweating
depolarizing NMJ blockade - paralysis
convulsions |
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Term
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Definition
excessive ACH side effects
Diarrhea
Urination
Miosis
Bronchospasm/Bradycardia
Emesis
Lacrimation
Salivation/Sweating |
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