Nicotinic antagonist

Short description: Drug that inhibits the action of acetylcholine at nicotinic acetylcholine receptors

A nicotinic antagonist is a type of anticholinergic drug that inhibits the action of acetylcholine (ACh) at nicotinic acetylcholine receptors. These compounds are mainly used for peripheral muscle paralysis in surgery, the classical agent of this type being tubocurarine,[1] but some centrally acting compounds such as bupropion, mecamylamine, and 18-methoxycoronaridine block nicotinic acetylcholine receptors in the brain and have been proposed for treating nicotine addiction.

Comparison  Mechanism  | Antagonist  | Preferred receptor  | Clinical use

|
|
|

Ganglionic blocking agents  | Hexamethonium | Ganglion type  | None[2]
Mecamylamine | Ganglion type  |
Trimethaphan  | Ganglion type  | Rarely used for blood pressure decrease during surgery[2]
Nondepolarizing neuromuscular blocking agents | Atracurium  | Muscle type  | Muscle relaxant in anaesthesia[2]
Doxacurium  | Muscle type  |
Mivacurium  | Muscle type  |
Pancuronium  | Muscle type  | Muscle relaxant in anaesthesia[2]
Tubocurarine  | Muscle type  | Discovered in arrow poison it was the first pheripheral muscle relaxant. Rarely used since 1980s.[2]
Vecuronium  | Muscle type  | Muscle relaxant in anaesthesia[2]
Depolarizing neuromuscular blocking agents | Succinylcholine*  | Muscle type  |
Centrally acting nicotinic antagonists  | 18-Methoxycoronaridine | α3β4  |
Bupropion | α3β4. α4β2, α1β1γδ | Antidepressant (NDRI)  |
Hydroxybupropion | α3β4. α4β2, α1β1γδ | Antidepressant (NDRI). Metabolite of bupropion.  |
Threohydrobupropion | α3β4.  | Antidepressant (NDRI). Metabolite of bupropion.  |
Dextromethorphan | α3β4. α4β2, α7 | Common over the counter antitussive.
Dextrorphan | α3β4. α4β2, α7 | Metabolite of dextromethorphan; no accepted medical uses.
3-Methoxymorphinan | α3β4  | Secondary metabolite of dextromethorphan; not used in medical practice. Unknown medical efficacy.

* Note: Succinylcholine is a nicotinic agonist. See neuromuscular blocking agents page for details on the mechanism of action.

## See also

* Nicotinic acetylcholine receptor
* Nicotinic agonist
* Muscarinic acetylcholine receptor
* Muscarinic agonist
* Muscarinic antagonist

## References

1. ↑ P. Taylor (1990). In Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th Ed., (A. G. Gilman et al., Eds.), pp. 166-186, New York: Pergamon Press.
2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 149

## External links

* Nicotinic+antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)

* v
* t
* e

Pharmacomodulation

Types|

* ♦ Enzyme: Inducer
* Inhibitor

* ♦ Ion channel: Opener
* Blocker

* ♦ Receptor: Agonist
* Partial agonist
* Antagonist
* Inverse agonist
* Positive allosteric modulator (PAM)
* Negative allosteric modulator (NAM)

* ♦ Transporter [Reuptake vs Efflux]: Enhancer (RE)
* Inhibitor (RI)
* Releaser (RA)

* ♦ Miscellaneous: Precursor
* Cofactor

Classes|

| Enzyme|

see Enzyme inhibition

|

Ion channel|

See Ion channel modulators

Receptor &
transporter|

| BA/M|

| Adrenergic|

* Adrenergic receptor agonist (α
* β (1
* 2))
* Adrenergic receptor antagonist (α (1
* 2)
* β)
* Norepinephrine reuptake inhibitor (NRI)

|

Dopaminergic|

* Dopamine receptor agonist
* Dopamine receptor antagonist
* Dopamine reuptake inhibitor (DRI)

Histaminergic|

* Histamine receptor agonist
* Histamine receptor antagonist (H1
* H2
* H3)

Serotonergic|

* Serotonin receptor agonist
* Serotonin receptor antagonist (5-HT3)
* Serotonin reuptake inhibitor (SRI)

AA|

| GABAergic|

* GABA receptor agonist
* GABA receptor antagonist
* GABA reuptake inhibitor (GRI)

|

Glutamatergic|

* Glutamate receptor agonist (AMPA)
* Glutamate receptor antagonist (NMDA)
* Glutamate reuptake inhibitor

Cholinergic|

* Acetylcholine receptor agonist (Muscarinic
* Nicotinic)
* Acetylcholine receptor antagonist (Muscarinic
* Nicotinic (Ganglionic
* Muscular))

Cannabinoidergic|

* Cannabinoid receptor agonist
* Cannabinoid receptor antagonist
* Endocannabinoid enhancer (eCBE)
* Endocannabinoid reuptake inhibitor (eCBRI)

Opioidergic|

* Opioid modulator
* Opioid receptor agonist
* Opioid receptor antagonist
* Enkephalinase inhibitor

Other|

* Adenosine reuptake inhibitor (AdoRI)
* Angiotensin II receptor antagonist
* Endothelin receptor antagonist
* NK1 receptor antagonist
* Vasopressin receptor antagonist

Miscellaneous|

* Cofactor (see Enzyme cofactors)
* Precursor (see Amino acids)

Medical uses

* v
* t
* e

Treatment of drug dependence (N07B)

Nicotine dependence|

* Bupropion
* Cytisine
* Lobeline
* Mecamylamine
* Varenicline
* AA (Clonidine)

Alcohol dependence|

* AD inhibitor (Disulfiram
* Calcium carbimide
* Hydrogen cyanamide)
* Acamprosate
* Opioid antagonists
* Naltrexone
* Nalmefene)
* κ-Opioid receptor antagonists
* Aticaprant
* Topiramate
* AA (Clonidine)
* Baclofen
* Metadoxine
* Phenibut

Opioid dependence|

* AA (Clonidine
* Lofexidine)
* Ibogaine
* Opioids
* Buprenorphine (+naloxone)
* Levacetylmethadol
* Methadone
* Dihydrocodeine
* Dihydroetorphine
* Hydromorphone (extended-release)
* Morphine (extended-release)
* Opioid antagonists (Naltrexone
* Nalmefene)

Benzodiazepine dependence|

* AA (Clonidine)
* Benzodiazepines (Diazepam
* Lorazepam
* Chlordiazepoxide
* Oxazepam)
* Barbiturates (Phenobarbital)

Research|

Salvia divinorum

* v
* t
* e

Sympatholytic (and closely related) antihypertensives (C02)

Sympatholytics
(antagonize α-adrenergic
vasoconstriction)|

| Central|

| α2 agonist|

* Clonidine
* Guanabenz
* Guanfacine
* Methyldopa#
* Tiamenidine‡

|

Adrenergic release inhibitors|

* Bethanidine
* Bretylium
* Debrisoquine
* Guanadrel
* Guanazodine
* Guanethidine
* Guanoclor
* Guanoxabenz
* Guanoxan

Imidazoline receptor agonist|

* Moxonidine
* Rilmenidine
* Tolonidine

Ganglion-blocking/nicotinic antagonist|

* Hexamethonium‡
* Mecamylamine
* Pentolinium
* Trimethaphan

Peripheral|

| Indirect|

| MAOI|

* Pargyline‡

|

Adrenergic uptake inhibitor|

* Bietaserpine
* Deserpidine
* Methoserpidine
* Rescinnamine
* Reserpine
* Syrosingopine

Tyrosine hydroxylase inhibitor|

* Metirosine

Direct|

| α1 blockers|

* Prazosin
* Indoramin
* Trimazosin
* Doxazosin
* Urapidil

|

Non-selective α blocker|

* Phentolamine

Other antagonists|

| Serotonin antagonist|

* Ketanserin
* Lidanserin

|

Endothelin antagonist (for PH)|

* dual (Bosentan, Macitentan)
* selective (Ambrisentan, Sitaxentan)

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

* v
* t
* e

Skeletal muscle relaxants (M03)

Peripherally acting
(primarily antinicotinic,
NMJ block)|

| Non-depolarizing|

| Curare alkaloids|

* Alcuronium
* Dimethyltubocurarine
* Tubocurarine

|

4° ammonium agents|

* ultra-short duration: Gantacurium

* short duration: Mivacurium
* Chandonium

* intermediate duration: Atracurium
* Cisatracurium
* Fazadinium
* Rocuronium
* Vecuronium

* long duration: Doxacurium
* Dimethyltubocurarine
* Pancuronium
* Pipecuronium
* Laudexium
* Gallamine

* unsorted: Hexafluronium (Hexafluorenium)

Depolarizing|

* Choline derivatives: Suxamethonium (Succinylcholine)

* Polyalkylene derivatives: Hexamethonium

ACh release inhibitors|

* Botulinum toxin

Centrally acting|

| Carbamic acid esters|

* Carisoprodol
* Cyclarbamate
* Difebarbamate
* Febarbamate
* Meprobamate
* Phenprobamate
* Styramate
* Tybamate

|

Benzodiazepines|

* Bromazepam
* Diazepam
* Clonazepam
* Flunitrazepam
* Lorazepam
* Nitrazepam
* Temazepam
* Tetrazepam

Nonbenzodiazepines|

* Eszopiclone

Thienodiazepines|

* Etizolam

Quinazolines|

* Methaqualone

Anticholinergics
(Antimuscarinics)|

* Cyclobenzaprine
* Orphenadrine

Other|

* Arbaclofen placarbil
* Baclofen
* Chlormezanone
* Chlorphenesin
* Chlorzoxazone
* Donepezil
* Eperisone
* Fenyramidol
* Flopropione
* Gabapentin
* GHB
* Inaperisone
* Lanperisone
* Mephenesin
* Mephenoxalone
* Metaxalone
* Methocarbamol
* Phenibut
* Pregabalin
* Pridinol
* Promoxolane
* Quinine
* Silperisone
* Thiocolchicoside
* Tizanidine
* Tolperisone
* Zoxazolamine

Directly acting|

* Dantrolene

Acetylcholine receptor modulators

* v
* t
* e

Muscarinic acetylcholine receptor modulators

mAChRs|

| Agonists|

* 77-LH-28-1
* AC-42
* AC-260,584
* Aceclidine
* Acetylcholine
* AF30
* AF150(S)
* AF267B
* Alvameline
* AQRA-741
* Arecoline
* Bethanechol
* Bevonium
* Butyrylcholine
* Carbachol
* CDD-0034
* CDD-0078
* CDD-0097
* CDD-0098
* CDD-0102
* Cevimeline
* Choline
* cis-Dioxolane
* Clozapine
* Desmethylclozapine (norclozapine)
* Ethoxysebacylcholine
* Itameline
* 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
* Suberyldicholine
* 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 (+formoterol)
* Abediterol
* AF-DX 250
* AF-DX 384
* Ambutonium bromide
* Anisodamine
* Anisodine
* Antihistamines (first-generation) (e.g., brompheniramine, buclizine, captodiame, chlorphenamine (chlorpheniramine), cinnarizine, clemastine, cyproheptadine, dimenhydrinate, [[Chemistry:Dimetdimetindene, Diphenhydramine|diphenhydramine]], doxylamine, meclizine, mepyramine (pyrilamine), mequitazine, perlapine, phenindamine, pheniramine, Phenyltoloxamine|Phenyltoloxamine]]]], promethazine, propiomazine, triprolidine)
* AQ-RA 741
* Atropine
* Atropine methonitrate
* Atypical antipsychotics (e.g., clozapine, Chemistry:Fluperlapine

Precursors
(and prodrugs)|

* Acetyl-coA
* Adafenoxate
* Choline (lecithin)
* Citicoline
* Cyprodenate
* Dimethylethanolamine
* Glycerophosphocholine
* Meclofenoxate (centrophenoxine)
* Phosphatidylcholine
* Phosphatidylethanolamine
* Phosphorylcholine
* Pirisudanol

See also: Receptor/signaling modulators • Nicotinic acetylcholine receptor modulators • Acetylcholine metabolism/transport modulators

* v
* t
* e

Nicotinic acetylcholine receptor modulators

nAChRs|

| Agonists
(and PAMs)|

* 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
* Bephenium hydroxynaphthoate
* Butinoline
* Butyrylcholine
* Carbachol
* Choline
* Cotinine
* Cytisine
* Decamethonium
* Desformylflustrabromine
* Dianicline
* Dimethylphenylpiperazinium
* Epibatidine
* Epiboxidine
* Ethanol (alcohol)
* Ethoxysebacylcholine
* EVP-4473
* EVP-6124
* Galantamine
* GTS-21
* Ispronicline
* Ivermectin
* JNJ-39393406
* Levamisole
* Lobeline
* MEM-63,908 (RG-3487)
* Morantel
* Nicotine (tobacco)
* NS-1738
* PHA-543,613
* PHA-709,829
* PNU-120,596
* PNU-282,987
* Pozanicline
* Pyrantel
* Rivanicline
* RJR-2429
* Sazetidine A
* SB-206553
* Sebacylcholine
* SIB-1508Y
* SIB-1553A
* SSR-180,711
* Suberyldicholine
* Suxamethonium (succinylcholine)
* Suxethonium (succinyldicholine)
* TC-1698
* TC-1734
* TC-1827
* TC-2216
* TC-5214
* TC-5619
* TC-6683
* Tebanicline
* Tribendimidine
* Tropisetron
* UB-165
* Varenicline
* WAY-317,538
* XY-4083

|

Antagonists
(and NAMs)|

* 18-MAC
* 18-MC
* α-Neurotoxins (e.g., α-bungarotoxin, α-cobratoxin, α-conotoxin, many others)
* ABT-126
* Alcuronium
* Allopregnanolone
* Amantadine
* Anatruxonium
* AQW051
* Atracurium
* Barbiturates (e.g., pentobarbital, sodium thiopental)
* BNC-210
* Bungarotoxins (e.g., α-bungarotoxin, κ-bungarotoxin)
* Bupropion
* BW284C51
* BW-A444
* Candocuronium iodide (chandonium iodide)
* Chlorisondamine
* Cisatracurium
* Coclaurine
* Coronaridine
* Curare
* Cyclopropane
* Dacuronium bromide
* Decamethonium
* Dehydronorketamine
* Desflurane
* Dextromethorphan
* Dextropropoxyphene
* Dextrorphan
* Diadonium
* DHβE
* Dihydrochandonium
* Dimethyltubocurarine (metocurine)
* Dioscorine
* Dipyrandium
* Dizocilpine (MK-801)
* Doxacurium
* Encenicline
* Enflurane
* Erythravine
* Esketamine
* Fazadinium
* Gallamine
* Gantacurium chloride
* Halothane
* Hexafluronium
* Hexamethonium (benzohexonium)
* Hydroxybupropion
* Hydroxynorketamine
* Ibogaine
* Isoflurane
* Ketamine
* Kynurenic acid
* Laudanosine
* Laudexium (laudolissin)
* Levacetylmethadol
* Levomethadone
* Malouetine
* ME-18-MC
* Mecamylamine
* Memantine
* Methadone
* Methorphan (racemethorphan)
* Methyllycaconitine
* Metocurine
* Mivacurium
* Morphanol (racemorphan)
* Neramexane
* Nitrous oxide
* Norketamine
* Pancuronium bromide
* Pempidine
* Pentamine
* Pentolinium
* Phencyclidine
* Pipecuronium bromide
* Progesterone
* Promegestone
* Radafaxine
* Rapacuronium bromide
* Reboxetine
* Rocuronium bromide
* Sevoflurane
* Stercuronium iodide
* Surugatoxin
* Thiocolchicoside
* Toxiferine
* Tramadol
* Trimetaphan camsilate (trimethaphan camsylate)
* Tropeinium
* Tubocurarine
* Vanoxerine
* Vecuronium bromide
* Xenon

Precursors
(and prodrugs)|

* Acetyl-coA
* Adafenoxate
* Choline (lecithin)
* Citicoline
* Cyprodenate
* Dimethylethanolamine
* Glycerophosphocholine
* Meclofenoxate (centrophenoxine)
* Phosphatidylcholine
* Phosphatidylethanolamine
* Phosphorylcholine
* Pirisudanol

See also: Receptor/signaling modulators • Muscarinic acetylcholine receptor modulators • Acetylcholine metabolism/transport modulators

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*[AA]: Adrenergic agonist
*[AD]: Acetaldehyde dehydrogenase
*[mAChRs]: Muscarinic acetylcholine receptors
*[nAChRs]: Nicotinic acetylcholine receptors
*[PAMs]: positive allosteric modulators
*[NAMs]: negative allosteric modulators