Nicotinic antagonist
Encyclopedia
A nicotinic antagonist is a type of anticholinergic
that inhibits the action at nicotinic acetylcholine receptor
s. These compounds are mainly used for peripheral muscle paralysis in surgery, but some centrally acting compounds such as bupropion
, mecamylamine
, and 18-methoxycoronaridine
block nicotinic acetylcholine receptors in the brain and can be used for treating drug addiction.
Anticholinergic
An anticholinergic agent is a substance that blocks the neurotransmitter acetylcholine in the central and the peripheral nervous system. An example of an anticholinergic is dicycloverine, and the classic example is atropine....
that inhibits the action at nicotinic acetylcholine receptor
Nicotinic acetylcholine receptor
Nicotinic acetylcholine receptors, or nAChRs, are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons and on the postsynaptic side of the neuromuscular junction...
s. These compounds are mainly used for peripheral muscle paralysis in surgery, but some centrally acting compounds such as bupropion
Bupropion
Bupropion is an atypical antidepressant and smoking cessation aid. The drug is a non-tricyclic antidepressant and differs from most commonly prescribed antidepressants such as SSRIs, as its primary pharmacological action is thought to be norepinephrine-dopamine reuptake inhibition...
, mecamylamine
Mecamylamine
Mecamylamine is a nonselective and noncompetitive antagonist of the nicotinic acetylcholine receptors that was introduced in the 1950s as an antihypertensive agent.- Uses :...
, and 18-methoxycoronaridine
18-Methoxycoronaridine
-18-Methoxycoronaridine is a derivative of ibogaine invented in 1996 by the research team around the pharmacologist Stanley D. Glick from the Albany Medical College and the chemist Martin E. Kuehne from the University of Vermont...
block nicotinic acetylcholine receptors in the brain and can be used for treating drug addiction.
| Mechanism | Antagonist | Preferred receptor | Clinical use |
|---|---|---|---|
| Ganglionic blocking agents | Hexamethonium Hexamethonium Hexamethonium is a ganglionic blocker, a nicotinic nACh receptor antagonist that acts in autonomic ganglia by binding mostly in or on the NN receptor, and not the acetylcholine binding site itself... |
Ganglion type Ganglion type nicotinic receptor The ganglion type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 23.It is located in the autonomic ganglia, where activation yields EPSP, mainly by increased Na+ and K+ permeability.... |
none |
| Mecamylamine Mecamylamine Mecamylamine is a nonselective and noncompetitive antagonist of the nicotinic acetylcholine receptors that was introduced in the 1950s as an antihypertensive agent.- Uses :... |
Ganglion type Ganglion type nicotinic receptor The ganglion type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 23.It is located in the autonomic ganglia, where activation yields EPSP, mainly by increased Na+ and K+ permeability.... |
||
| Trimethaphan Trimethaphan Trimetaphan camsilate or trimethaphan camsylate , trade name Arfonad, is a drug that counteracts cholinergic transmission at the ganglion type of nicotinic receptors of the autonomic ganglia and therefore blocks both the sympathetic nervous system and the parasympathetic nervous system... |
Ganglion type Ganglion type nicotinic receptor The ganglion type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 23.It is located in the autonomic ganglia, where activation yields EPSP, mainly by increased Na+ and K+ permeability.... |
Rarely used for blood pressure Blood pressure Blood pressure is the pressure exerted by circulating blood upon the walls of blood vessels, and is one of the principal vital signs. When used without further specification, "blood pressure" usually refers to the arterial pressure of the systemic circulation. During each heartbeat, BP varies... decrease during surgery |
|
| Nondepolarizing neuromuscular blocking agents | Atracurium Atracurium Atracurium besylate is a neuromuscular-blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical... |
Muscle type Muscle type nicotinic receptor The muscle-type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 2β1δε or 2β1δγ.... |
muscle relaxant Muscle relaxant A muscle relaxant is a drug which affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therapeutic groups: neuromuscular blockers and spasmolytics... in anaesthesia |
| Doxacurium | Muscle type Muscle type nicotinic receptor The muscle-type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 2β1δε or 2β1δγ.... |
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| Mivacurium Mivacurium Mivacurium chloride is a short-duration non-depolarizing neuromuscular-blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during... |
Muscle type Muscle type nicotinic receptor The muscle-type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 2β1δε or 2β1δγ.... |
||
| Pancuronium Pancuronium Pancuronium is a muscle relaxant with various purposes. It is the second of three drugs administered during most lethal injections in the United States.- Mode of action :... |
Muscle type Muscle type nicotinic receptor The muscle-type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 2β1δε or 2β1δγ.... |
muscle relaxant Muscle relaxant A muscle relaxant is a drug which affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therapeutic groups: neuromuscular blockers and spasmolytics... in anaesthesia |
|
| Tubocurarine Tubocurarine Tubocurarine is a neuromuscular-blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in anesthesia to provide skeletal muscle relaxation during surgery or mechanical ventilation... |
Muscle type Muscle type nicotinic receptor The muscle-type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 2β1δε or 2β1δγ.... |
Rarely used | |
| Vecuronium Vecuronium Vecuronium is a muscle relaxant in the category of non-depolarizing blocking agents. Vecuronium bromide is indicated as an adjunct to general anesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation... |
Muscle type Muscle type nicotinic receptor The muscle-type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 2β1δε or 2β1δγ.... |
muscle relaxant Muscle relaxant A muscle relaxant is a drug which affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therapeutic groups: neuromuscular blockers and spasmolytics... in anaesthesia |
|
| Depolarizing neuromuscular blocking agents | Succinylcholine Suxamethonium chloride Suxamethonium chloride , also known as suxamethonium or succinylcholine, is a paralytic drug used to induce muscle relaxation and short-term paralysis, usually to facilitate tracheal intubation. Suxamethonium is sold under the trade names Anectine, Quelicin, and Scoline. It is used as a paralytic... |
Muscle type Muscle type nicotinic receptor The muscle-type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 2β1δε or 2β1δγ.... |
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| Centrally acting nicotinic antagonists | 18-Methoxycoronaridine 18-Methoxycoronaridine -18-Methoxycoronaridine is a derivative of ibogaine invented in 1996 by the research team around the pharmacologist Stanley D. Glick from the Albany Medical College and the chemist Martin E. Kuehne from the University of Vermont... |
α3β4 | |