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27 Cards in this Set

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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)
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)
Mechanism of:

Bethanecol
Direct-Acting Agonist

Rx- ileus (postop/neurogenic), urinary retention

Muscarinic at High and Low Dose M3 (Ca2+)

No Nicotinic action!
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
Mechanism of:

Varenicline
Direct-Acting Agonist

Muscarinic: NONE

Nicotinic: alpha4beta2 to depol ↑AP ↑DA
Smoking cessation
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
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.
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
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
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
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
Mechanism of:

Botox
Acetylcholine Release Inhibitor

Blocks release of ACh from terminals by cleaving SNAP-25 (req'd for synaptic vesicle release)
Mechanism of:

Atropine
Muscarinic Antagonists

Block Muscarinic Activation
(heart, eye, glands, GI and urinary, CNS)
Pre-anesthetic medication (reduce secretions, relax, bronchi, antispasmodic, antidiarrheal)
Mechanism of:

Ipratropium
Muscarinic Antagonists

Block Muscarinic Activation

Bronchodilation in COPD and Asthma

Suspended inhalation aerosol
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.
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
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
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.
Mechanism of:

Pralidoxine
Cholinesterase Reactivator
2-PAM

Regeneration of acetylcholinesterase
Sarin treatment
Nicotinic Receptor Subtypes
MUSCLE:
Alpha1

NEURONAL:
Autonomic Ganglia:
Alpha3

CNS:
Alpha4
Alpha7
Mechanism of:
Methacholine
Cholinergic Activator
(M and N)
Mechanism of:
Echothiopate
AChE inhibitor
Irreversible
Mechanism of:
Malathione
AChE inhibitor
Irreversible
Mechanism of:
Parathion
AChE inhibitor
Irreversible
Mechanism of:
Benztropine
Cholinergic Antagonist
Muscarinic blocker
Mechanism of:
Scopolamine
Cholinergic Antagonist
Muscarinic blocker
Mechanism of:
Mecamylamine
Cholinergic Antagonist
Ganglionic blocker