Term
| How is the action of acetylcholine terminated? |
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Definition
|
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Term
| Where is acetylcholinesterase located? |
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Definition
| Pre- and post-synaptic membranes |
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Term
|
Definition
| Inhibits transport of acetylcholine down axon |
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Term
|
Definition
| Blocks the release of acetylcholine |
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Term
|
Definition
| Promotes the release of acetylcholine |
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Term
| What happens to choline after acetylcholinesterase acts? |
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Definition
| Choline is taken up by the neuron - Recycled |
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Term
| What are the two products of acetylcholinesterase? |
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Definition
|
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Term
| Do somatic neurons have ganglia? |
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Definition
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Term
| What type of receptors are located at the NMJ? What does the neuron release onto them? |
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Definition
| Nicotinic - receive acetylcholine |
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Term
| What type of receptor is present at all autonomic ganglia? What type of neurotransmitter do they receive |
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Definition
| Nicotinic - Acetylcholine |
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Term
What type of receptors are found on the adrenal medulla?
What does it release? |
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Definition
|
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Term
| What do most sympathetic neurons release at the effector organ? |
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Definition
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Term
| Name the 3 neurotransmitters that bind to muscarinic receptors in order of affinity. |
|
Definition
1. Muscarine
2. Acetylcholine
3. Nicotine |
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Term
| Name the 3 neurotransmitters that bind to nicotinic receptors in order of affinity (highest first). |
|
Definition
1. Nicotine
2. Acetylcholine
3. Muscarine |
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Term
| Describe the nicotinic receptor. |
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Definition
Pentamer
Ligand (Ach) Gated Ion channel (Na goes through) |
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|
Term
| Describe the muscarinic receptor. |
|
Definition
7 transmembrane regions
G-Protein Coupled |
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Term
| 2 Types of Neuromuscular Nicotinic Receptors |
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Definition
|
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Term
| 2 Types of Nicotinic Neuronal Receptors |
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Definition
|
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Term
| Stimulatory Muscarinic Receptors |
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Definition
|
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Term
| Inhibitory Muscarinic Receptors |
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Definition
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Term
| Muscarinic Effects on the Heart |
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Definition
Decrease Rate
Decrease conduction velocity
No effect on contraction force |
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Term
| Muscarinic Effects on the Eye |
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Definition
| Miosis (pupil constriction) |
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Term
| Muscarinic Effects on Respiration |
|
Definition
Bronchoconstriction
Increased Secretions |
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Term
|
Definition
Increased Motility, Relax sphincters
N/V/D/Cramps |
|
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Term
|
Definition
| Relax Sphincters, Bladder Wall Contraction |
|
|
Term
| Muscarinic Effects on Glands |
|
Definition
|
|
Term
|
Definition
Muscle contraction
Fasciculations and tremors |
|
|
Term
| Nicotine Effect on Ganglia |
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Definition
|
|
Term
| Nicontine Effect on Adrenal Medulla |
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Definition
|
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Term
|
Definition
Direct Acting Agonist
Not Clinically Useful
Acts at both Muscarinic and Nicotinic Receptors
5 Minute Duration
Quaternary Amine |
|
|
Term
|
Definition
Direct Acting Agonist
1 hour duration
Subcutaneous, Topical
Quaternary Amine
Binds preferentially at muscarinic receptors
Treats Urinary Retention (relax sphincters, bladder wall contraction) |
|
|
Term
|
Definition
Direct Acting Agonist
1-2 Hour Duration
Only Topical - Eye
Quaternary Amine
Miosis during ocular surgery
Reduces intraocular pressure in open-angle or narrow-angle glaucoma (especially if you are tolerant to pilocarpine) |
|
|
Term
|
Definition
|
|
Term
|
Definition
Direct Acting Agonist
24 Hour duration - not a substrate for Ach esterase
Topical - Eye
Treats Glaucoma (Narrow or Wide Angle)
Immediately lowers Intraocular Pressure
Increases Aqueous Humor Drainage
M3 - Contracts Ciliary Muscle & Pupil
Tertiary Amine = Can penetrate CNS (uncharged) |
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|
Term
|
Definition
Ach Esterase Inhibitor (Indirect agonist)
Indirect Muscarinic Agonist - Increased Ach Conc.
Half Life: 4-6 hours (longest)
Does NOT enter CNS
Treatment: MG, open-angle glaucoma, reverses non-depolarizing NM blockade after surgery
Adverse Effects: general cholinergic side effects |
|
|
Term
|
Definition
Reversible Cholinesterase Inhibitor
Indirect Muscarinic Agonist - Increased Ach Conc.
Half Life: 2-4 hours (intermediate)
Does NOT enter CNS
Prevent post-operative abdominal distention and urinary retention
Treat myasthenia gravis
Antidote for turbocurarine |
|
|
Term
|
Definition
Reversible Cholinesterase Inhibitor
Indirect Muscarinic Agonist - Increased Ach Conc.
Half Life: 5-10 MINUTES (short!)
Good for evaluating myasthenia gravis patients
Antidote for turbocurarine |
|
|
Term
| What are the 2 mechanisms for lowering eye pressure? |
|
Definition
1. Decrease production of aqueous humor (b1)
2. Increase outflow of aqueous humor (M3) |
|
|
Term
|
Definition
Dilates the pupil (mydriasis)
Muscarinic Antagonist
Can reverse the effects of irreversible Cholinesterase inhibitors (nerve gas)
Works better at peripheral muscarinic sites |
|
|
Term
| Side effects of Muscarinic Agonists |
|
Definition
Diarrhea
Urination
Miosis
Bronchoconstriction
Bradycardia
Excitation of skeletal muscle and CNS
Lacrimation
Salivation
Sweating |
|
|
Term
| Quaternary Amines & Carbamates - Reversible Cholinesterase Inhibitors |
|
Definition
Do Not Enter CNS or Ganglia
Less Effect at Muscarinic (PNS) sites
Show Preference for Neuromuscular Junctions - Nicotinic Receptors |
|
|
Term
|
Definition
Reversible Cholinesterase Inhibitor
Half Life: 15-40 minutes (intermediate)
Enters CNS (tertiary amine) - not for peripheral use
Increased intestinal & bladder motility
Reduced intraocular pressure in glaucoma
Reverse CNS & cardiac effects of tricyclic antidepressants
Reverse CNS effects of atropine |
|
|
Term
| Major Disorder Treated With Reversible Cholinesterase Inhibitors |
|
Definition
| Myasthenia Gravis (destruction of NMJ) |
|
|
Term
| Can Rivastigmine help with Alzheimers? |
|
Definition
|
|
Term
| What do reversible Ach esterase inhibitors do in normal people? |
|
Definition
| Cause fasciculations (involuntary muscle twitch) and weakness |
|
|
Term
|
Definition
| Irreversible Cholinesterase Inhibitors |
|
|
Term
Isofluorophate
Echothiophate |
|
Definition
Irreversible Cholinesterase Inhibitors
Topical - Eye (effective for 1 week)
Treatment: Chronic Glaucoma
Mechanism: inhibit cholinesterase by phosphorylation, contracts ciliary body, allows aqueous humor drainage |
|
|
Term
|
Definition
Can reactivate deactivated Cholinesterase
Treatment for irreversible cholinesterase inhibitors
Must give before the aging process has occurred (giving off CH2OH)
Works best in tissues with nicotinic receptors |
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Term
| A person comes to emergency room with constricted pupils, sweating, hypotension and the spouse says that the patient was spraying in the garden, the likely drug responsible is |
|
Definition
| Acetylcholinesterase Inhibitor |
|
|
Term
| Name 2 Cholinergic Agonists that are Tertiary Amines |
|
Definition
|
|
Term
| What is special about tertiary amines? |
|
Definition
| They can penetrate the CNS |
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