Med Agents Exam 2

Front 1

Potential Targets of Cholinergic Drugs

Back 1

1) Release of ACh -- Botulinum toxin inhibits
2) Breakdown of ACH by AChE
3) Interaction with cholinergic receptors

Front 2

Mechanism of Action of Botulinum Toxin A

Back 2

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

Front 3

Uses of BOTOX--Strabismus

Back 3

Eyes turn in different directions

Front 4

Uses of BOTOX--Blepharospasm

Back 4

Spasms of the muscles that control the eyelids -- increased blinking

Front 5

Uses of BOTOX--Axillary hyperhidrosis

Back 5

excessive sweating

Front 6

Uses of BOTOX -- Cervival Dystonia

Back 6

Involuntary spasms or tonic contractions of neck muscles

Front 7

Methacholine

Back 7

Cholinomimetic; Synthetic Choline Ester; Mecholyl brand name;

MUSCARINIC RECEPTOR SELECTIVE

Front 8

Carbachol

Back 8

Cholinomimetic; Synthetic Choline Ester; Carbecel brand name;

NONSELECTIVE CHOLINOMIMETIC

Front 9

Bethanechol

Back 9

Cholinomimetic; Synthetic Choline Ester; Urecholine brand name;

M3 muscarinic receptor selective

Front 10

Cevimeline

Back 10

Cholinomimetic; Synthetic Non-choline Derivative; Evoxac brand name;

Muscarinic receptor agonist used to treat Xerostomia in Sjogren's syndrome

Front 11

Edrophonium (AChE Competitive Inhibitor)

Back 11

Mono quarternary Derivative;
Hydrogen bonds @ Serine esteric site;
Associates very well at cation-pi site;

SHORT DURATION of ACTION;
TX of Myasthenia gravis

Front 12

Ambenonium (AChE Competitive Inhibitor)

Back 12

Bis-quarternary derivative;
Therapeutic use: Diagnosis and Tx of myasthenia gravis

Front 13

Myasthenia gravis

Back 13

Disorder of muscular transmission; muscle weakness not associated with fatigue;

Autoimmune disorder; damages receptors @ NMJ causing fewer receptors

Front 14

The Mono and Bis-quarternary derivatives used as AChE Inhibitors to treat Myasthenia Gravis

Back 14

Edrophonium and Ambenonium

Front 15

The Free Amine Derivatives used as AChE Inhibitors to treat Alzheimer's Disease

Back 15

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.

Front 16

Huperzine A (Cerebra)

Back 16

An OTC herbal that increases ACh concentration and cholinergic activity;
AChE competitive inhibitor;
Improves cognition/memory