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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 ]
By 1943, neuromuscular blocking drugs became established as muscle relaxants in the practice of anesthesia and surgery. [ 6 ] The U.S. Food and Drug Administration (FDA) approved the use of carisoprodol in 1959, metaxalone in August 1962, and cyclobenzaprine in August 1977.
Effective neuromuscular block by non-depolarizing neuromuscular drugs occurs only when 70-80% of acetylcholine receptors are occupied by the drug. [11] This is because at this occupancy rate, junctional potential cannot reach the threshold value required for muscle contraction. Diagram of nicotinic receptor (Acetylcholine receptor)
Examples of alpha 2 blockers include yohimbine and idazoxan. [2] Apart from being used as antidotes to reverse the overdose effects of alpha 2 agonists, they only have a limited number of indications. [3] For instance, Yohimbine has been used to treat sexual dysfunction in males. [3]
Atracurium is in the neuromuscular-blocker family of medications and is of the non-depolarizing type. [1] It works by blocking the action of acetylcholine on skeletal muscles. [1] Atracurium was approved for medical use in the United States in 1983. [1] It is on the World Health Organization's List of Essential Medicines. [3]
Gantacurium chloride (formerly recognized as GW280430A and as AV430A) is a new experimental neuromuscular blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in surgical anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation.
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