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16 Cards in this Set

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Potential Targets of Cholinergic Drugs
1) Release of ACh -- Botulinum toxin inhibits
2) Breakdown of ACH by AChE
3) Interaction with cholinergic receptors
Mechanism of Action of Botulinum Toxin A
BTA binds to cholinergic nerve terminals --> Internalization via endosome formation --> Translocation of Zn-dependent endopeptidase domain into the cytosol --> Proteolytic cleavage of SNARE proteins (which are responsible for fusion of vesicles to membrane) --> Inhibition of ACh release
Uses of BOTOX--Strabismus
Eyes turn in different directions
Uses of BOTOX--Blepharospasm
Spasms of the muscles that control the eyelids -- increased blinking
Uses of BOTOX--Axillary hyperhidrosis
excessive sweating
Uses of BOTOX -- Cervival Dystonia
Involuntary spasms or tonic contractions of neck muscles
Methacholine
Cholinomimetic; Synthetic Choline Ester; Mecholyl brand name;

MUSCARINIC RECEPTOR SELECTIVE
Carbachol
Cholinomimetic; Synthetic Choline Ester; Carbecel brand name;

NONSELECTIVE CHOLINOMIMETIC
Bethanechol
Cholinomimetic; Synthetic Choline Ester; Urecholine brand name;

M3 muscarinic receptor selective
Cevimeline
Cholinomimetic; Synthetic Non-choline Derivative; Evoxac brand name;

Muscarinic receptor agonist used to treat Xerostomia in Sjogren's syndrome
Edrophonium (AChE Competitive Inhibitor)
Mono quarternary Derivative;
Hydrogen bonds @ Serine esteric site;
Associates very well at cation-pi site;

SHORT DURATION of ACTION;
TX of Myasthenia gravis
Ambenonium (AChE Competitive Inhibitor)
Bis-quarternary derivative;
Therapeutic use: Diagnosis and Tx of myasthenia gravis
Myasthenia gravis
Disorder of muscular transmission; muscle weakness not associated with fatigue;

Autoimmune disorder; damages receptors @ NMJ causing fewer receptors
The Mono and Bis-quarternary derivatives used as AChE Inhibitors to treat Myasthenia Gravis
Edrophonium and Ambenonium
The Free Amine Derivatives used as AChE Inhibitors to treat Alzheimer's Disease
Tacrine (cognex), Galantamine (Reminyl), and Donepezil (Aricept)

All Lipophilic and can enter the brain to increase cholinergic activity in brain;

Cholinergic systemic side effects -- salivation, cramping, diarrhea, and urinary freq.
Huperzine A (Cerebra)
An OTC herbal that increases ACh concentration and cholinergic activity;
AChE competitive inhibitor;
Improves cognition/memory