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27 Cards in this Set
- Front
- Back
- 3rd side (hint)
Mechanism of:
Acetylcholine |
Direct-Acting Agonist
Muscarinic at High and Low Dose (cAMP, Ca2+, or K+) Nicotinic at High Dose (depolarization or enhance NT release) |
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Mechanism of:
Carbachol |
Direct-Acting Agonist
Muscarinic M3 (IP3 ^Ca2+) Nicotinic at High Dose (depolarization or enhance NT release) Constricts iris and ciliary muscle to improve drainage. |
Glaucoma (like pilocarpine)
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Mechanism of:
Bethanecol |
Direct-Acting Agonist
Rx- ileus (postop/neurogenic), urinary retention Muscarinic at High and Low Dose M3 (Ca2+) No Nicotinic action! |
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Mechanism of:
Nicotine |
Direct-Acting Agonist
Muscarinic: NONE Nicotinic: alpha4beta2 to depol ↑AP ↑DA Increases Dopamine release in Nucleus Accumbens in Midbrain Reward Pathway, 3 different ways! |
dopamine
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Mechanism of:
Varenicline |
Direct-Acting Agonist
Muscarinic: NONE Nicotinic: alpha4beta2 to depol ↑AP ↑DA |
Smoking cessation
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Mechanism of:
Edrophonium |
Indirect-Acting Agonists (Anticholinesterases): Blocks enzyme to increase ACh levels at synapse. Does not directly activate cholinergic receptors, but increases endogenous ACh. Used to Dx MG. Used to differentiate MG from cholinergic crises.
Muscarinic: low to moderate; enhance action of ACh Nicotinic at High Dose (depolarization or enhance NT release) |
diagnose Myasthenia Gravis
5-15 min |
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Mechanism of:
Neostigmine |
Indirect-Acting Agonists (Anticholinesterases): Increase ACh levels at synapse. Does not directly activate cholinergic receptors.
Muscarinic: low to moderate; enhance action of ACh Nicotinic at High Dose (depolarization or enhance NT release) Treatment of MG. Does not cross BBB (unlike physiostigmine, the glaucoma drug) Combined with Atropine to reduce unwanted Muscarinic Activation. |
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Mechanism of:
Physostigmine |
Indirect-Acting Agonists (Anticholinesterases):
Teriary amine enters CNS. Unlike direct agonists, there is little effect on vascular smooth muscle and blood pressure, because there is no cholinergic innervation. Muscarinic: low to moderate; enhance action of ACh Nicotinic: high dose; enhance action of ACh |
Glaucoma
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Mechanism of:
Donepezil |
Indirect-Acting Agonists (Anticholinesterases): Increase ACh levels at synapse by 40% decreased enzyme activity. Unlike direct agonists, there is little effect on vascular smooth muscle and blood pressure.
Muscarinic: low to moderate Nicotinic: high dose Alzheimer's treatment Once a day pill Crosses BBB |
Alzheimer's Disease
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Mechanism of:
Galantamine |
Indirect-Acting Agonists (Anticholinesterases): Blocks enzyme to increase ACh levels at synapse. Does not directly activate cholinergic receptors, but increases endogenous ACh.
Muscarinic: low to moderate; enhance action of ACh Nicotinic: high dose; enhance action of ACh Also enhances ACh activation of nicotinic receptors by binding to an allosteric site on the nicotinic receptor. Treatment of Alzheimer's Disease Twice a day pill |
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Mechanism of:
Sarin |
Indirect-Acting Agonists (Anticholinesterases): Blocks enzyme to increase ACh levels at synapse. Does not directly activate cholinergic receptors, but increases endogenous ACh.
IRREVERSIBLE Organophosphate Muscarinic: low to moderate; enhance action of ACh Nicotinic: high dose; enhance action of ACh |
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Mechanism of:
Botox |
Acetylcholine Release Inhibitor
Blocks release of ACh from terminals by cleaving SNAP-25 (req'd for synaptic vesicle release) |
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Mechanism of:
Atropine |
Muscarinic Antagonists
Block Muscarinic Activation (heart, eye, glands, GI and urinary, CNS) |
Pre-anesthetic medication (reduce secretions, relax, bronchi, antispasmodic, antidiarrheal)
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Mechanism of:
Ipratropium |
Muscarinic Antagonists
Block Muscarinic Activation Bronchodilation in COPD and Asthma Suspended inhalation aerosol |
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Mechanism of:
Hexamethonium |
Nicotinic Antagonists (ganglionic)
Blocks Nicotinic Activation Sloppy drug! Sympathetic and Parasympathetic action. No longer used! |
No longer used!
Was used to treat decrease BP but had too many undesirable effects, like syncopy. |
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Mechanism of:
Tubocurarine |
Nicotinic Antagonists
Non-Depolarizing Skeletal Muscle Blocker Hypotension due to both direct action on mast cells to release histamine and to some blockade of neuronal nicotinic receptors in autonomic ganglia. Highly charged, does not cross BBB. Reversed by Neostigmine (often with Atropine) to increase ACh at NMJ. |
Surgery
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Mechanism of:
Vecuronium |
Nicotinic Antagonists
Non-Depolarizing Skeletal Muscle Blocker Shorter duration than Tubocurarine and less hypotension/histamine release. Frequently used! |
Frequently used in surgery
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Mechanism of:
Succinylcholine |
Nicotinic Antagonists
Depolarizing Skeletal Muscle Blocker Phase 1: agonist (activator) Phase 2: channel block Metabolized by cholinesterase, so do not use Neostigmine to reverse. In patients with atypical cholinesterase, the effects will be pronounced and prolonged. |
Rapid sequence induction endotracheal intubation.
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Mechanism of:
Pralidoxine |
Cholinesterase Reactivator
2-PAM Regeneration of acetylcholinesterase |
Sarin treatment
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Nicotinic Receptor Subtypes
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MUSCLE:
Alpha1 NEURONAL: Autonomic Ganglia: Alpha3 CNS: Alpha4 Alpha7 |
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Mechanism of:
Methacholine |
Cholinergic Activator
(M and N) |
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Mechanism of:
Echothiopate |
AChE inhibitor
Irreversible |
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Mechanism of:
Malathione |
AChE inhibitor
Irreversible |
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Mechanism of:
Parathion |
AChE inhibitor
Irreversible |
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Mechanism of:
Benztropine |
Cholinergic Antagonist
Muscarinic blocker |
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Mechanism of:
Scopolamine |
Cholinergic Antagonist
Muscarinic blocker |
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Mechanism of:
Mecamylamine |
Cholinergic Antagonist
Ganglionic blocker |
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