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The effect of non-depolarizing neuromuscular-blocking drugs may be reversed with acetylcholinesterase inhibitors, neostigmine, and edrophonium, as commonly used examples. Of these, edrophonium has a faster onset of action than neostigmine, but it is unreliable when used to antagonize deep neuromuscular block. [ 29 ]
A muscle relaxant is a drug that 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.
Depolarizing neuromuscular blockers: Depolarizing neuromuscular blockers directly bind to postsynaptic cholinergic receptors of the neuromuscular junction to generate a sustained action potential. This causes prolonged stimulation and desensitization of neuroreceptors, causing skeletal muscle relaxation effects such as paralysis. [ 1 ]
Anticholinergics (anticholinergic agents) are substances that block the action of the acetylcholine (ACh) neurotransmitter at synapses in the central and peripheral nervous system. [ 1 ] [ 2 ] These agents inhibit the parasympathetic nervous system by selectively blocking the binding of ACh to its receptor in nerve cells .
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Suxamethonium is in the neuromuscular blocker family of medications and is of the depolarizing type. [7] It works by blocking the action of acetylcholine on skeletal muscles. [7] Suxamethonium was described as early as 1906 and came into medical use in 1951. [5] It is on the World Health Organization's List of Essential Medicines. [11]
A neuromuscular junction. Curare blocks ACh receptors (bottom left). Curare is an example of a non-depolarizing muscle relaxant that blocks the nicotinic acetylcholine receptor (nAChR), [24] one of the two types of acetylcholine (ACh) receptors, at the neuromuscular junction.
A nicotinic agonist is a drug that mimics the action of acetylcholine (ACh) at nicotinic acetylcholine receptors (nAChRs). The nAChR is named for its affinity for nicotine. Examples include nicotine (by definition), acetylcholine (the endogenous agonist of nAChRs), choline, epibatidine, lobeline, varenicline and cytisine. [1]