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Acetylcholine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Mixed receptor Agonist (direct acting)
- Receptors: Nn, Nm, M1-5
- T.U.: Opthalmic solution for surgery (M3)
- Other: Quaternary Amine, Short duration
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Nicotine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Nicotinic agonist (direct acting)
- Receptors: Nn, Nm
- T.U.: treat nicotine dependence, insecticide
- Other: Tertiary amine, metabolized in liver
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Varenicline (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Nicotinic partial agonist
- Receptors: α4β2
- T.U.: Treat nicotine dependence
- Other: crosses BBB, decreases effect of nicotine
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Muscarine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Muscarinic Agonist (Direct acting)
- Receptors: M1-5
- T.U.: N/A
- Other: quaternary amine
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Pilocarpine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Muscarinic agonist (Direct acting)
- Receptors: M1-5
- T.U.: Wide angle glaucoma, Xerostomia
- Other: Tertiary amine
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Methacholine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Muscarinic Agonist (Direct acting)
- Receptors: M1-5 (weak Nn)
- T.U.: Diagnose bronchial hyperractivity (s.c.)
- Other: slower metabolism by AChE
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Carbachol (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Mixed receptor Agonist (direct acting)
- Receptors: Nn, M1-5
- T.U.: Miosis for surgery, Wide angle Glaucoma
- Other: Long duration of action
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Bethanecol (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Muscarinic Agonist (Direct acting)
- Receptors: M1-5
- T.U.: GI atony, Urinary retention
- Other: Long duration, Contraindicated with obstruction, Orally effective
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Edrophonium (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Reversible Anticholinesterase (Indirect acting)
- Receptors: All ACh receptors
- T.U.: Diagnose Myasthenia Gravis, evaluate myasthenic/cholinergic crisis, Paroxysmal atrial tachycardia
- Other: Quaternary amine, short duration ~10min
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Neostigmine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Reversible Anticholinesterase (Indirect acting)
- Receptors: All ACh receptors
- T.U.: Myasthenia Gravis, Glaucoma, GI/U atony, Reversal NMJ block
- Other: Quaternary amine, long duration (4-6hr)
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Pyridostigmine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Reversible Anticholinesterase (Indirect acting)
- Receptors: All Ach receptors
- T.U.: Myasthenia Gravis, Nerve Gas Prophylaxis
- Other: Quaternary amine, 6-8 hrs
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Physostigmine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Reversible Anticholinesterase (Indirect acting)
- Receptors: All Ach receptors
- T.U.: Glaucoma, Muscarinic antagonist OD (severe),
- Other: Tertiary amine
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Donepezil (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Reversible Anticholinesterase (Indirect acting)
- Receptors: All Ach receptors
- T.U.: Alzheimer disease
- Other: tertiary amine, Does NOT prevent degeneration
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Echothiophate (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Irreversible Anticholinesterase (Indirect acting) Organophosphate
- Receptors: Binds to AChE/BuChE
- T.U.: Glaucoma
- Other: Quaternary Amine
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Methylparathion (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Irreversible Anticholinesterase (Indirect acting) Organophosphate
- Receptors: Binds to AChE/BuChE
- T.U.: Insecticide
- Other: activated in liver, fairly safe
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Malathion (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Irreversible Anticholinesterase (Indirect acting) Organophosphate
- Receptors: Binds to AChE/BuChE
- T.U.: Insecticide
- Other: activated in liver, fairly safe
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Sarin (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Irreversible Anticholinesterase (Indirect acting) Organophosphate
- Receptors: Binds to AChE/BuChE
- T.U.: Nerve Gas
- Other: Treat exposure with 2-PAM
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Soman (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Irreversible Anticholinesterase (Indirect acting) Organophosphate
- Receptors: Binds to AChE/BuChE
- T.U.: Nerve Gas
- Other: Treat exposure with 2-PAM
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Pralidoxime (2-PAM) (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Cholinesterase regenerator
- Receptors: Binds to AChE/BuChE
- T.U.: Nerve gas exposure
- Other: Highly nucleophilic, have to treat before “aging” occurs
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Sildenafil (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Parasympathomimetic (Indirect)
- Receptors: cGMP PDE
- T.U.: ED (Viagra), Pulmonary hypertension (Revatio)
- Other: ~1hr onset, 4-5hr duration
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Tadalafil (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Parasympathomimetic (Indirect)
- Receptors: cGMP PDE
- T.U.: ED
- Other: 1-2hr Onset, 36 hr duration “the weekender”
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Vardenafil (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Parasympathomimetic (Indirect)
- Receptors: cGMP PDE
- T.U.: ED
- Other: ~1hr onset, 4-5hr duration
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Trimethaphan (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Nicotinic Receptor Antagonist (Ganglionic Blocker)
- Receptors: Nn (α3β4)
- T.U.: Rapidly decrease BP to decrease blood loss during surgery/dissecting AA
- Other: Acute IV treatment only
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Mecamylamine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Nicotinic Receptor Antagonist (Ganglionic Blocker)
- Receptors: Nn (α3β4)
- T.U.: Tourette’s Syndrome
- Other: Oral
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Tubocurarine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Neuromuscular Blocker
- Receptors: Nm antagonist
- T.U.: Adjunct to general anesthesia, surgery, artificial respiration, intubation, seizure control
- Other: IV only, No CNS, slow onset ~4-6 min, Long duration ~80-120min, histamine release
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Pancuronium (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Neuromuscular Blocker
- Receptors: Nm antagonist
- T.U.: Adjunct to general anesthesia, surgery, artificial respiration, intubation, seizure control
- Other: slow onset ~4-6 min, Long duration ~120-180min, “vagolytic” action
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Cisatracurium (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Neuromuscular Blocker
- Receptors: Nm antagonist
- T.U.: Brief procedures
- Other: Onset ~2-4 mins, Duration ~ 30-40min, spontaneous hydrolysis
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Mivacurium (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Neuromuscular Blocker
- Receptors: Nm antagonist
- T.U.: Aid tracheal intubation
- Other: Onset ~ 2-4min Duration ~ 12-18min, Inactivated by hydrolysis
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Rocuronium (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Neuromuscular Blocker
- Receptors: Nm antagonist
- T.U.: Rapid tracheal intubation
- Other: 1-2min onset, 30-40min duration
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Succinylcholine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Neuromuscular Blocker (depolarizing blockade)
- Receptors: Nm agonist
- T.U.: Rapid paralysis
- Other: onset 1-2min, 5 min duration, Metabolized by BuChE, not AchE
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Dantroline (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Skeletal Muscle Relaxant
- Receptors: Sarcoplasmic Reticulum Ca^2+ channels
- T.U.: Treatment of malignant hyperthermia brought about by anesthetics
- Other: Blocks Ca^2+ release from sarcoplasmic reticulum
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Botulism Toxin A (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Neuromuscular Blocker
- Receptors: Cholinergic Nerve Terminals, then L chain targets SNARE proteins
- T.U.: Skeletal muscle disorders, Skin disorders, Esophagus/LES spasms
- Other: Duration is variable (Nm upregulation, antibodies, nerve sprouting), no response in 2-5% patients
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Propantheline (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Muscarinic Receptor Antagonist
- Receptors: M1-5
- T.U.: Diarrhea
- Other: quaternary amine, Blocks receptors on GI muscle
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Ipratropium (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Muscarinic Receptor Antagonist
- Receptors: M1-5
- T.U.: Asthma, COPD
- Other: Inhaled
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Atropine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Muscarinic Receptor Antagonist
- Receptors: M1-5
- T.U.: Cholinergic antagonist OD, mydriasis, cycloplegia
- Other: tertiary amine (CNS effects)
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Scopolamine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Muscarinic Receptor Antagonist
- Receptors: M1-5
- T.U.: Motion Sickness
- Other: significant sedation, tertiary amine
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Tolterodine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Muscarinic Receptor Antagonist
- Receptors: M3
- T.U.: Overactive bladder, incontinence
- Other: M3 selective so less side effects, tertiary amine
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Tropicamide (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Muscarinic Receptor Antagonist
- Receptors: M1-5
- T.U.: Brief mydriasis, cycloplegia
- Other: 4-6hr duration, tertiary amine
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Benzotropine (Class, Receptors, Therapeutic Use, Other Comments)
- Class: Muscarinic Receptor Antagonist
- Receptors: M1-5
- T.U.: Parkinsons disease
- Other: tertiary amine, adjunct to L-DOPA therapy
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