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Drug Listing: Autonomic Pharmacology

 

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

 

-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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