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Lesson 1: ANS
ANS (Classes and drugs)
19
Pharmacology
Graduate
06/07/2014

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Term
Muscarainic Agonists (Indirect acting)
Cholinesterase inhibitors/AChE inhibitors

MOA
Therapeutic uses
ADRs
Definition
MOA:
-AChE inhibitor
-Act primarily on CNS AChE enzyme

Therapeutic uses:
-Treatment of myasthenia gravis
-Treat AD
-Do not expect dramatic improvements (on meds -> require 1 hr/day less and delays NH placement by 2 yrs)
-Do not slow progression of disease or repair damage

Adverse Effects
-SLUD-related:
salivation, larimation, diarrhea, abdominal cramps, heartburn, loss of bladder control, bradycardia, weak pulse, pin-point pupils, blurry vision, bronchoconstrition, sweating
-CNS-related:
N/V, loss of appetite, seizures, dizziness, headache
Term
Cholinesterase inhibitors (Muscarainic Agonists)

Drugs
Definition
Donepezil (Aricept®)
Galantamine (Razadyne®)
Rivastigmine (Exelon®)

Treat AD
Term
Muscarinic Agonists (Direct Acting)

MOA
Therapeutic uses
ADRs
Definition
MOA:
-bind directly to muscarinic receptors and mimic ACh
-stimulates muscarinic recptors
-No effect on nicotinic receptors (CNS)

Therapeutic uses:
-Atonic bladder (detrussor muscle weakened, help strengthen)
-Urinary retention in postpartum and postoperative
-GI paralysis/slowness

ADRs
-Salivation = drooling
-Lacrimation = tearing
-Urinary incontinence
-Defecation = diarrhea
-GI = stomach acid, heartburn, cramping
-Bronchoconstriction = hypotension
-Bradycardia = low pulse, weak pulse
Term
Muscarinic Agonists (Direct Acting)

Drugs
Definition
bethanecol (Urecholine®)
Term
Muscarinic Antagonists

MOA
Definition
MOA:
-Compete w/ ACh for muscarinic receptors
-Bind and block muscarinic receptors
-By blocking the PNS, they leave the SNS opposed

ADRs
-Anticholinergic SE (Anti-SLUD)
-Dry mouth
-Blurred vision
-Constipation
-Urinary retention
-Tachycardia
-CNS: memory loss, confusion, restlessness, agitation, hallucination, and delirium
Term
Muscarinic Antagonists

Drugs
Definition
-Atropine
-Scopolamine
-Hyoscyamine
-darifenacin (Enablex)
-oxybutynin (Ditropan®)
-propantheline (Pro-Banthine®)
-solifencacin (VESIcare®)
-tolterodine (Detrol®)
-trospium (Sanctura)
Term
atropine (muscarinic antagonist)
Definition
Therapeutic uses:
-Antidote for overdoses of cholinergic agonists (insecticides, nerve gas)
-Cardiac arrest/"code blue" - treats severe bradycardia and asytole
-Antispasmodic and antidiarrheal - relaxes GI tract and bladder
-Opthalmic - mydriatic (eye exams and surgeries)
Term
scopolamine (muscarinic antagonist)
Definition
Therapeutic uses:
-Similar to atropine
-Anti-motion sickness drug - block ACh and reduce feeling of nausea
Term
hyoscyamine (muscarinic antagonist)
Definition
Therapeutic uses:
-GI spasms
-Irritable bowel
-Spastic bladder
Term
darifenacin (Enablex)
oxybutynin (Ditropan®)
propantheline (Pro-Banthine®)
solifencacin (VESIcare®)
tolterodine (Detrol®)
trospium (Sanctura)

muscarinic antagonists
Definition
Therapeutic uses:
-Urinary incontinence
-Overactive bladder
-Urge incontinence
-Minimally effective and significant ADRs
Term
Adrenergic Agonists
Drugs
MOA
Therapeutic uses
ADRs
Definition
-mirabegron (Myrbetriq®)
-midodrine (ProAmantine®)
-epinephrine (Adrenaline®)
Term
mirabegron (Myrbetriq®) Adrenergic Agonists

MOA
Therapeutic uses
ADRs
Definition
MOA:
-B3 agonist
-relaxes bladder (able to fill easier)

Therapeutic uses:
-alternatives to antimuscarinics in treatment of overactive bladder

ADRs
-slight increase in BP
-Increased risk of UTI
-long term safety unknown
Term
midodrine (ProAmantine®) Adrenergic Agonists

MOA
Therapeutic uses
ADRs
Definition
MOA:
-A1 agonist

Therapeutic uses:
-Dysautonomia
-Orthostatic hypotension (vasocontricts vessels to prevent)

ADRs:
-HTN
-urinary incontinence
-HA
-dry mouth
-nervousness/anxiety
Term
epinephrine (Adrenaline®) Adrenergic Agonists
Vascular effects
Definition
A1 receptors:
-Location -> skin and mucous membrane
-Stimulation causes -> vasoconstriction (BP increases)
B2 receptors:
-Location -> vasculature of liver, heart, and skeletal muscle
-Stimulation causes -> vasodilation (BP decreases)
Overall change in BP:
-BP increases (skin largest organ)
Term
epinephrine (Adrenaline®) Adrenergic Agonists
Cardiac effects
Definition
B1 receptors: (Heart)
-HR: Increases (Positive Chronotrope)
-Force of contraction: Increases (Positive inotrope)
Term
epinephrine (Adrenaline®) Adrenergic Agonists
Pulmonary effects
Definition
B2 receptors: (lungs)
-Stimulation causes: bronchodilation
A1 receptors (mucous membranes)
-respiratory secretions: decreased (drying effect)
Term
epinephrine (Adrenaline®) Adrenergic Agonists
other effects B2
Definition
B2 receptors: (liver)
-Hyperglycemia
-Anxiety, restlessness, tremor
Term
epinephrine (Adrenaline®) Adrenergic Agonists
Therapeutic uses
Definition
-OTC bronchodilator (B2 agonist)
-Anaphylactic shock (EpiPen®)
-Stops small bleeding
-local anesthetics (lidocaine) prolong effectiveness
-cardiac arrest, code blue, ACLS (epi and atropine
->stimulate heart)
Term
Other Arenergic Agonists drugs
Definition
-B2 agonist bronchodilator
-Phenylephrine - decongestant
-Pseudoephedrine - decongestant
-Oxymetolazone (Visine®) - blood shot eyes -> vessels vasodilator due to A1 effect, will help to vasoconstrict
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