DRUG LISTING

Drug Listing: Autonomic Pharmacology

* Direct Muscarinic Agonists
o Choline Esters
o Alkaloids
* Direct Nicotinic Agonist
* Acetylcholinesterase Inhibitor (Reversible)
* Acetylcholinesterase Inhibitor (Irreversible)
* Muscarinic Antagonist
* 2-PAM
* Ganglionic Blockers



* Catecholamines
* Direct Adrenoceptor Agonists
* Indirect-Acting Sympathomimetics
* Alpha adrenoceptor Antagonists
* Beta-adrenoceptor Antagonists
* Adrenergic Neuron Blocking Drugs



Direct Muscarinic Agonists

Choline Esters

* Acetylcholine
* Bethanechol (Urecholine)
* Carbachol
* Methacholine (Provocholine)



Alkaloids

* Muscarine
* Pilocarpine (Pilocar)




Direct Nicotinic Agonist

Nicotine


Acetylcholinesterase Inhibitors

Acetylcholinesterase Inhibitors ("Reversible")

* Neostigmine (Prostigmin)
* Physostigmine (Antilirium)
* Edrophonium (Tensilon)



Acetylcholinesterase Inhibitors ("Irreversible")

* Soman
* Parathion
* Malathion
* Isoflurophate (Floropryl)
* (Diisopropylflurorphosphate DFP)
* Echothiophate (Phospholine)



Muscarinic Antagonists

* Atropine
* Scopolamine
* Ipratropium (Atrovent)
* Pirenzepine (M1 selective)



2-PAM: Acetylcholinesterase Reactivator

* Pralidoxime (Protopam) {2-PAM}:peripheral acetylcholinesterase reactivator for certain phosphoryl-enzyme complexes



Ganglionic Blockers

* Mecamylamine (Inversine)
* Hexamethonium
* Trimethaphan



Catecholamines

DRUG

Epinephrine

Norepinephrine (Levophed)

Isoproterenol (Isuprel)

Dobutamine (Dobutrex)

Dopamine (Intropin)




Receptor Classification

alpha-1, alpha-2, beta-1, beta-2

alpha-1, alpha-2, beta-1

beta-1, beta-2

beta-1 (alpha-1)

D-1 (alpha-1 and beta-1 at high doses)


Direct Adrenoceptor Agonists

Drug

Phenylephrine (Neo-Synephrine)

Methoxamine (Vasoxyl)

Oxymetazoline (Afrin)

Clonidine (Catapres)

Ritodrine (Yutopar)

Terbutaline (Brethine)

Albuterol (Ventolin,Proventil)

Salmeterol (Serevent)




Receptor Classification

alpha-1

alpha-1

alpha-1, alpha-2

alpha-2

beta-2

beta-2

beta-2

beta-2


Indirect-Acting Sympathomimetics

Drug

Ephedrine, Pseudoephedrine

Cocaine

Tyramine

Amphetamine




Mechanism of Action

Release & direct receptor activation

Uptake I inhibitor

Release

similar to ephedrine, but greater CNS actions


Alpha-Adrenoceptor Antagonists

Drug

Prazosin (Minipress)

Terazosin (Hytrin)

Trimazosin

Doxazosin (Cardura)

Phentolamine (Regitine)

Phenoxybenzamine (Dibenzyline)

Tolazoline (Priscoline)

Labetalol (Trandate, Normodyne)

Yohimbine (Yocon)




Receptor Selectivity(alpha1 vs. alpha2)

alpha-1

alpha-1

alpha-1

alpha-1

non-selective

only slightly selective for alpha-1 (non-competitive)

non-selective

alpha-1 (also non-selective beta-antagonist)

alpha-2


ß-Adrenoceptor antagonists

Drug

Propranolol (Inderal)

Metoprolol (Lopressor)

Esmolol (Brevibloc)

Atenolol (Tenormin)

Nadolol (Corgard)

Timolol (Blocadren)

Pindolol (Visken)

Labetalol (Trandate, Normodyne)

Butoxamine




Receptor Selectivity

non-selective

beta-1

beta-1

beta-1

non-selective

non-selective

non-selective (partial agonist)

non-selective (selective alpha-1-antagonist)

beta-2 (no clinical applications)


Adrenergic Neuron Blocking Drugs
Reserpine

Guanethidine (Ismelin)




* non-selective blockade of vesicular uptake and storage of biogenic amines

* similar to reserpine: Uptake I dependent

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