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Psychopharmacology
(Index , Outline )
Hexamethonium is a ganglionic blocker ,[1] nAch (NN ) receptor antagonist which acts in autonomic ganglia by binding mostly in or on the NN receptor, and not the acetylcholine binding site itself. It has no effect on the muscarinic acetylcholine receptors (mAChR ) located on target organs of the parasympathetic nervous system , nor the nicotinic acetylcholine receptors at the neuromuscular junction (NM ) that are responsible for skeletal muscle motor response.
Pharmacology It can act on receptors at pre-ganglionic sites in both the sympathetic and parasympathetic nervous system, which are both regulated (again, only pre-ganglionically) by nicotinic acetylcholine receptors. Postganglionic sympathetic systems are usually regulated by norepinephrine or adrenaline (adrenergic receptors), while parasympathetic systems are still acetylcholine based, but instead rely on muscarinic receptors (some post-ganglionic sympathetic neurons, such as those stimulating sweating, release acetylcholine).
The organ system and adverse effects of ganglion blockers are because both the parasympathetic and sympathetic stimuli are blocked at the preganglionic sites. Side effects include combined sympatholytic (e.g. orthostatic hypotension and sexual dysfunction ) and parasympatholytic effects (e.g. constipation, urinary retention , glaucoma , blurry vision, decreased lacrymal secretion, dry mouth (xerostomia ) effects.
Uses It was formerly used to treat disorders of the peripheral nervous system , such as chronic hypertension , which is innervated only by the sympathetic nervous system . The non-specificity of this treatment led to discontinuing its use.[2]
The use of hexamethonium, an unapproved drug, in a normal volunteer during a medical study is believed to have caused her death.[3] [4]
References See also
Cholinergics
Receptor ligands
Agonists : 77-LH-28-1 • AC-42 • AC-260,584 • Aceclidine • Acetylcholine • AF30 • AF150(S) • AF267B • AFDX-384 • Alvameline • AQRA-741 • Arecoline • Bethanechol • Butyrylcholine • Carbachol • CDD-0034 • CDD-0078 • CDD-0097 • CDD-0098 • CDD-0102 • Cevimeline • cis-Dioxolane • Ethoxysebacylcholine • LY-593,039 • L-689,660 • LY-2,033,298 • McNA343 • Methacholine • Milameline • Muscarine • NGX-267 • Ocvimeline • Oxotremorine • PD-151,832 • Pilocarpine • RS86 • Sabcomeline • SDZ 210-086 • Sebacylcholine • Suberylcholine • Talsaclidine • Tazomeline • Thiopilocarpine • Vedaclidine • VU-0029767 • VU-0090157 • VU-0152099 • VU-0152100 • VU-0238429 • WAY-132,983 • Xanomeline • YM-796 Antagonists : 3-Quinuclidinyl Benzilate • 4-DAMP • Aclidinium Bromide • Anisodamine • Anisodine • Atropine • Atropine Methonitrate • Benactyzine • Benzatropine (Benztropine) • Benzydamine • BIBN 99 • Biperiden • Bornaprine • CAR-226,086 • CAR-301,060 • CAR-302,196 • CAR-302,282 • CAR-302,368 • CAR-302,537 • CAR-302,668 • CS-27349 • Cyclobenzaprine • Cyclopentolate • Darifenacin • DAU-5884 • Dimethindene • Dexetimide • DIBD • Dicyclomine (Dicycloverine) • Ditran • EA-3167 • EA-3443 • EA-3580 • EA-3834 • Elemicin • Etanautine • Etybenzatropine (Ethylbenztropine) • Flavoxate • Himbacine • HL-031,120 • Ipratropium bromide • J-104,129 • Hyoscyamine • Mamba Toxin 3 • Mamba Toxin 7 • Mazaticol • Mebeverine • Methoctramine • Metixene • Myristicin • N -Ethyl-3-Piperidyl BenzilateN -Methyl-3-Piperidyl BenzilateOrphenadrine • Otenzepad • Oxybutynin • PBID • PD-102,807 • Penehyclidine • Phenglutarimide • Phenyltoloxamine • Pirenzepine • Piroheptine • Procyclidine • Profenamine • RU-47,213 • SCH-57,790 • SCH-72,788 • SCH-217,443 • Scopolamine (Hyoscine) • Solifenacin • Telenzepine • Tiotropium bromide • Tolterodine • Trihexyphenidyl • Tripitamine • Tropatepine • Tropicamide • WIN-2299 • Xanomeline • Zamifenacin ; Others : 1st Generation Antihistamines (Brompheniramine , chlorphenamine , cyproheptadine , dimenhydrinate , diphenhydramine , doxylamine , mepyramine /pyrilamine , phenindamine , pheniramine , tripelennamine , triprolidine , etc) • Tricyclic Antidepressants (Amitriptyline , doxepin , trimipramine , etc) • Tetracyclic Antidepressants (Amoxapine , maprotiline , etc) • Typical Antipsychotics (Chlorpromazine , thioridazine , etc) • Atypical Antipsychotics (Clozapine , olanzapine , quetiapine , etc)
Agonists : 5-HIAA • A-84,543 • A-366,833 • A-582,941 • A-867,744 • ABT-202 • ABT-418 • ABT-560 • ABT-894 • Acetylcholine • Altinicline • Anabasine • Anatoxin-a • AR-R17779 • Butyrylcholine • Carbachol • Cotinine • Cytisine • Decamethonium • Desformylflustrabromine • Dianicline • Dimethylphenylpiperazinium • Epibatidine • Epiboxidine • Ethanol • Ethoxysebacylcholine • EVP-4473 • EVP-6124 • Galantamine • GTS-21 • Ispronicline • Lobeline • MEM-63,908 (RG-3487) • Nicotine • NS-1738 • PHA-543,613 • PHA-709,829 • PNU-120,596 • PNU-282,987 • Pozanicline • Rivanicline • Sazetidine A • Sebacylcholine • SIB-1508Y • SIB-1553A • SSR-180,711 • Suberylcholine • TC-1698 • TC-1734 • TC-1827 • TC-2216 • TC-5214 • TC-5619 • TC-6683 • Tebanicline • Tropisetron • UB-165 • Varenicline • WAY-317,538 • XY-4083 Antagonists : 18-Methoxycoronaridine • α-Bungarotoxin • α-Conotoxin • Alcuronium • Amantadine • Anatruxonium • Atracurium • Bupropion (Amfebutamone) • Chandonium • Chlorisondamine • Cisatracurium • Coclaurine • Coronaridine • Dacuronium • Decamethonium • Dextromethorphan • Dextropropoxyphene • Dextrorphan • Diadonium • DHβE • Dimethyltubocurarine (Metocurine) • Dipyrandium • Dizocilpine (MK-801) • Doxacurium • Duador • Esketamine • Fazadinium • Gallamine • Hexafluronium • Hexamethonium (Benzohexonium) • Ibogaine • Isoflurane • Ketamine • Kynurenic acid • Laudexium (Laudolissin) • Levacetylmethadol • Malouetine • Mecamylamine • Memantine • Methadone • Methorphan (Racemethorphan) • Methyllycaconitine • Metocurine • Mivacurium • Morphanol (Racemorphanol) • Neramexane • Nitrous Oxide • Pancuronium • Pempidine • Pentamine • Pentolinium • Phencyclidine • Pipecuronium • Radafaxine • Rapacuronium • Rocuronium • Surugatoxin • Suxamethonium (Succinylcholine) • Thiocolchicoside • Toxiferine • Trimethaphan • Tropeinium • Tubocurarine • Vecuronium • Xenon
Reuptake inhibitors
Plasmalemmal
CHT Inhibitors
Hemicholinium-3 (Hemicholine; HC3) • Triethylcholine
Enzyme inhibitors
1-(-Benzoylethyl)pyridinium • 2-(α-Naphthoyl)ethyltrimethylammonium • 3-Chloro-4-stillbazole • 4-(1-Naphthylvinyl)pyridine • Acetylseco hemicholinium-3 • Acryloylcholine • AF64A • B115 • BETA • CM-54,903 • N ,N -DimethylaminoethylacrylateN ,N -Dimethylaminoethylchloroacetate
Reversible : Carbamates Aldicarb • Bendiocarb • Bufencarb • Carbaryl • Carbendazim • Carbetamide • Carbofuran • Chlorbufam • Chloropropham • Ethienocarb • Ethiofencarb • Fenobucarb • Fenoxycarb • Formetanate • Furadan • Ladostigil • Methiocarb • Methomyl • Miotine • Oxamyl • Phenmedipham • Pinmicarb • Pirimicarb • Propamocarb • Propham • Propoxur ; Stigmines Ganstigmine • Neostigmine • Phenserine • Physostigmine • Pyridostigmine • Rivastigmine ; Others : Acotiamide • Ambenonium • Donepezil • Edrophonium • Galantamine • Huperzine A • Minaprine • Tacrine • Zanapezil Irreversible : Organophosphates Acephate • Azinphos-methyl • Bensulide • Cadusafos • Chlorethoxyfos • Chlorfenvinphos • Chlorpyrifos • Chlorpyrifos-Methyl • Coumaphos • Cyclosarin (GF) • Demeton • Demeton-S-Methyl • Diazinon • Dichlorvos • Dicrotophos • Diisopropyl fluorophosphate (Guthion) • Diisopropylphosphate • Dimethoate • Dioxathion • Disulfoton • EA-3148 • Echothiophate • Ethion • Ethoprop • Fenamiphos • Fenitrothion • Fenthion • Fosthiazate • GV • Isofluorophate • Isoxathion • Malaoxon • Malathion • Methamidophos • Methidathion • Metrifonate • Mevinphos • Monocrotophos • Naled • Novichok agent • Omethoate • Oxydemeton-Methyl • Paraoxon • Parathion • Parathion-Methyl • Phorate • Phosalone • Phosmet • Phostebupirim • Phoxim • Pirimiphos-Methyl • Sarin (GB) • Soman (GD) • Tabun (GA) • Temefos • Terbufos • Tetrachlorvinphos • Tribufos • Trichlorfon • VE • VG • VM • VR • VX ; Others : Demecarium • Onchidal (Onchidella binneyi
Cymserine * Many of the acetylcholinesterase inhibitors listed above act as butyrylcholinesterase inhibitors.
Others
Choline (Lecithin ) • Citicoline • Cyprodenate • Dimethylethanolamine (DMAE, deanol) • Glycerophosphocholine • Meclofenoxate (Centrophenoxine) • Phosphatidylcholine • Phosphatidylethanolamine • Phosphorylcholine • Pirisudanol
Acetic acid • Acetylcarnitine • Acetyl-coA • Vitamin B5 (Pantethine , Pantetheine , Panthenol )
Others
Acetylcholine releasing agents : α-Latrotoxin • β-Bungarotoxin ; Acetylcholine release inhibitors : Botulinum toxin (Botox); Acetylcholinesterase reactivators : Asoxime • Obidoxime • Pralidoxime
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