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Cholinergic blocking drugs are a group of drugs that block the action of acetylcholine (ACh), a neurotransmitter, in synapses of the cholinergic nervous system. [1] They block acetylcholine from binding to cholinergic receptors, namely the nicotinic and muscarinic receptors.
An acetylcholine receptor (abbreviated AChR) or a cholinergic receptor is an integral membrane protein that responds to the binding of acetylcholine, a neurotransmitter. Classification [ edit ]
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)
Muscle relaxants inhibit neuron transmission to muscle by blocking the nicotinic acetylcholine receptor. What they have in common, and is necessary for their effect, is the structural presence of quaternary ammonium groups, usually two. Some of them are found in nature and others are synthesized molecules. [9] [5]
A muscarinic acetylcholine receptor antagonist, also simply known as a muscarinic antagonist or as an antimuscarinic agent, is a type of anticholinergic drug that blocks the activity of the muscarinic acetylcholine receptors (mAChRs). The muscarinic receptors are proteins involved in the transmission of signals through certain parts of the ...
Most neuromuscular blockers function by blocking transmission at the end plate of the neuromuscular junction. Normally, a nerve impulse arrives at the motor nerve terminal, initiating an influx of calcium ions, which causes the exocytosis of synaptic vesicles containing acetylcholine. Acetylcholine then diffuses across the synaptic cleft.
Benzatropine is an anticholinergic which works by blocking the activity of muscarinic acetylcholine receptors. [4] Benzatropine was approved for medical use in the United States in 1954. [4] It is available as a generic medication. [4]
Acetylcholine Acetylcholinesterase Acetylcholinesterase inhibition. Acetylcholinesterase inhibitors (AChEIs) also often called cholinesterase inhibitors, [1] inhibit the enzyme acetylcholinesterase from breaking down the neurotransmitter acetylcholine into choline and acetate, [2] thereby increasing both the level and duration of action of acetylcholine in the central nervous system, autonomic ...