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Pharmacology Autonomic Drugs
Autonomic Drugs
27
Health Care
Professional
05/06/2012

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Term
Urge Incontinence
Definition
Trospium
Oxybutynin
Tolterodine
Solifenacin
Darifenacin

"TOTS"
Term
Acetylcholine synthesis
Definition
Acetyl Coa + Choline --> ACh (choline acetyl transferase)

ACh enters vesicle
Ca helps vesicle degranulate

4 fates:
ACh receptor
ACh degredation
ACh reuptake with autoreceptor
Diffuse away
Term
Vesamicol
Definition
Inhibits ACh entering the vesicle
Term
Hemicholinium
Definition
Inhibits entry of choline into the neuron. Doesn't form with Acetyl CoA
Term
Norepinephrine synthesis
Definition
Phe --> Tyrosine (Phe Hydroxylase)
Tyrosine --> DOPA (Tyr Hydroxylase)
DOPA --> Dopamine (DOPA Decarboxylase)
Dopamine --> NE (Dopamine B Hydroxylase)
NE --> Epi (PNMT)

NE released from vesicle via Ca

4 Fates:
alpha1, alpha2, beta1, beta2 Receptors
Reuptake via autoreceptor
Metabolism via MAO/COMT
Term
Metyrosine
Definition
Inhibits tyrosine hydroxylase in formation of NE
Term
Inhibits NE Autoreceptors on noradrenergic nerves
Definition
Cocaine and TCA
Term
Stimulates release of NE in noradrenergic pathway
Definition
Amphatamines
Ephedrine
Tyramine
Term
Blocks NE from exiting noradrenergic nerve
Definition
Guanethidine
Bretylium
Term
Effect of Alpha 2, Muscarinic M2, and Angiotensin II on Noradrenergic NE release
Definition
Decreased
Decreased
Increased (vasoconstriction)
Term
Inhibits Dopamine to enter Vesicle to convert to NE
Definition
Reserpine
Term
G protein pathway (Gs)
Definition
7 membrane subunit
Gs protein subunits
Activates Adenylyl Cyclase
Creates cAMP from ATP
Stimulates Protein Kinase A
Term
G Protein Pathway (Gq)
Definition
7 transmembrane receptor
Gq Protein subunit
Activates Phospholipase C

Cleaves PIP3 (from membrane) into:
DiacylGlycerol (DAG) to make Protein Kinase C
IP3 to stimulate Ca release from SR
Term
Tyrosine Kinase Receptor pathway
Definition
Insulin binds to 2 transmembrane receptor
Autophosphorylation of its own Tyr
Eventual activation of p21Ras

Ras signal molecule to effect growth
Term
Gs proteins stimulated by what receptors
Definition
Beta 1
Beta 2
D1
H2
V2
Term
Gq proteins stimulated by what receptors
Definition
H1
A1
V1
M1
M3

"GQ's have 1 M&M"
Term
Gi proteins stimulated by what receptors
Definition
M2
A2
D2

"MAD 2"
Term
Sympathomimetics (direct)
Definition
Epinephrine a1,a2,b1,b2 (for anaphylaxis, asthma)
NE a1,a2>b1 (Hypotension)
Isoproterenol B1=B2 (AV block)
Dopamine D1=D2>B>a (Shock with inc renal)
Dobutamine B1>B2 (for heart failure, stress test, cardio shock)
Phenylephrine a1>a2 (pupil dil., nasal decongestion)

B2 Agonists
Metaproterenol
albuterol/levalbuterol
salmeterol
terbutaline
Term
Indirect Sympathomimetics
Definition
Amphetamine - release stored (narcolepsy, obesity, ADD)
Ephedrine - release stored (nasal decongestion)
Cocaine - uptake inhibitor (vasoconstriction)
Term
Sympathoplegics
Definition
Clonidine - centrally acting A2 agonist (for hypertension)
Term
Alpha Blockers
Definition
Nonselective
Phenoxybenzamine (pheochromocytoma)
Phentolamine

Alpha1 selective
Prazosin, terazosin, doxazosin (HTN and BPH - will get first dose orthostatic Hypotension)

Alpha 2 selective
Mirtazapine (depression)
Term
Beta Blockers
Definition
Beta 1 selective
Acebutolol
Betaxolol
Esmolol
Atenolol
Metoprolol
"A BEAM"

Nonselective
Propranolol
Term
Nicotinic Antagonist
Definition
Hexamethonium
Term
Cholinomimetic Agents
Definition
"Chol"
Bethanechol (post op ileus and urinary retention)
Carbachol (glaucoma)
Pilocarpine (glaucoma emergency, simulates sweat/tears)
Methacholine (Challenge test for asthma)
Term
Indirect Cholinergic agonists
Definition
Anticholinesterases

Neostigmine (myasthenia gravis)
Pyridostigmine (myasthenia gravis)
Edrophonium (MG diagnostic test)
Physostigmine (glaucoma)
Echothiophate (glaucoma)
Term
Drug to regenerate active cholinesterase
Definition
Pralidoxime
Term
Muscarinic Antagonists
Definition
"-trop"

Atropine (Tx for Organophosphate poison, ACLS drug, otometry drug)
Benztropine (Parkinsons Disease)
Scoplamine (motion sickness)
Ipratropium (asthma)
Oxybutynin (urinary urge)
Methscoploamine (PUD)
Propantheline (PUD
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