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Non-depolarizing blocking agents: These agents constitute the majority of the clinically relevant neuromuscular blockers. They act by competitively blocking the binding of ACh to its receptors, and in some cases, they also directly block the ionotropic activity of the ACh receptors.
Non-depolarizing NMBAs are classified based on their duration of action (short, intermediate, or long-acting agents. The two most commonly used non-depolarizing NMBDs in the operating room are rocuronium and vecuronium. Both are intermediate-acting, steroidal NMBAs.
Consequently, depolarizing and muscle-contracting effects are decreased. Non-depolarizing neuromuscular blockers are generally reversible, and hence have no permanent effects on acetylcholine receptors. [1] [4] Unlike depolarizing neuromuscular blockers, non-depolarizing drugs do not produce conformational changes to the receptor. [1]
Rocuronium bromide is a competitive antagonist for the nicotinic acetylcholine receptors at the neuromuscular junction. Of the neuromuscular-blocking drugs it is considered to be a non-depolarizing neuromuscular junction blocker, because it acts by dampening the receptor action causing muscle relaxation, instead of continual depolarisation which is the mechanism of action of the depolarizing ...
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.
Pancuronium is a typical non-depolarizing curare-mimetic muscle relaxant. It competitively inhibits the nicotinic acetylcholine receptor at the neuromuscular junction by blocking the binding of acetylcholine. It has slight vagolytic activity, causing an increase in heart rate, but no ganglioplegic (i.e., blocking ganglions) activity.
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.
In this sense, tubocurarine is the prototypical adjunctive neuromuscular non-depolarizing agent. However, others before Griffith and Johnson had attempted use of tubocurarine in several situations: [6] [7] [8] some under controlled study conditions [9] [10] while others not quite controlled and remained unpublished. [11]