Neuromuscular Blockers
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Neuromuscular Blockers
Neuromuscular-blocking drugs, or Neuromuscular blocking agents (NMBAs), block transmission at the neuromuscular junction, causing paralysis of the affected skeletal muscles. This is accomplished via their action on the post-synaptic acetylcholine (Nm) receptors. In clinical use, neuromuscular block is used adjunctively to anesthesia to produce paralysis, firstly to paralyze the vocal cords, and permit endotracheal intubation, and secondly to optimize the surgical field by inhibiting spontaneous ventilation, and causing relaxation of skeletal muscles. Because the appropriate dose of neuromuscular-blocking drug may paralyze muscles required for breathing (i.e., the diaphragm), mechanical ventilation should be available to maintain adequate Respiration (physiology), respiration. This class of medications helps to reduce patient movement, breathing, or ventilator dyssynchrony and allows lower insufflation pressures during laparoscopy. It has several indication ...
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Synapse Diag3
In the nervous system, a synapse is a structure that allows a neuron (or nerve cell) to pass an electrical or chemical signal to another neuron or a target effector cell. Synapses can be classified as either chemical or electrical, depending on the mechanism of signal transmission between neurons. In the case of electrical synapses, neurons are coupled bidirectionally with each other through gap junctions and have a connected cytoplasmic milieu. These types of synapses are known to produce synchronous network activity in the brain, but can also result in complicated, chaotic network level dynamics. Therefore, signal directionality cannot always be defined across electrical synapses. Chemical synapses, on the other hand, communicate through neurotransmitters released from the presynaptic neuron into the synaptic cleft. Upon release, these neurotransmitters bind to specific receptors on the postsynaptic membrane, inducing an electrical or chemical response in the target neuro ...
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Decamethonium
Decamethonium (Syncurine) is a depolarizing muscle relaxant or neuromuscular blocking agent, and is used in anesthesia to induce paralytic, paralysis. Pharmacology Decamethonium, which has a short action time, is similar to acetylcholine and acts as a partial agonist of the nicotinic acetylcholine receptor. In the motor endplate, it causes depolarization, preventing further effects to the normal release of acetylcholine from the presynaptic terminal, and therefore preventing the neural stimulus from affecting the muscle. In the process of binding, decamethonium activates (depolarizes) the motor endplate - but since the decamethonium itself is not degraded, the membrane remains depolarized and unresponsive to normal acetylcholine release. Contraindications/limitations Decamethonium does not produce unconsciousness or anesthesia, and its effects may cause considerable psychological distress while simultaneously making it impossible for a patient to communicate. For these re ...
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Chandonium
Candocuronium iodide ( INN, formerly chandonium, HS-310) is an aminosteroid neuromuscular-blocking drug. It was clinically evaluated in India for use in anesthesia for endotracheal intubation, and for providing skeletal muscle relaxation and assistance mechanical ventilation during surgery. Its development was discontinued due to cardiovascular side effects, primarily tachycardia, the severity of which is similar to the clinically established pancuronium bromide. Candocuronium has a short duration in the body, but a rapid onset of action, with little to no ganglion-blocking activity and greater potency than pancuronium bromide. Background Candocuronium iodide, like other neuromuscular-blocking agents, is a preferential competitive antagonist of nicotinic acetylcholine receptors. It was developed by the laboratory of Harkishan Singh at Panjab University Panjab University (PU) is an Indian collegiate public state university located in Chandigarh. Funded through both State ...
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Pipecuronium
Pipecuronium (Arduan) is a bisquaternary aminosteroid muscle relaxant which blocks nicotinic acetylcholine receptors at the neuromuscular junction A neuromuscular junction (or myoneural junction) is a chemical synapse between a motor neuron and a muscle fiber. It allows the motor neuron to transmit a signal to the muscle fiber, causing muscle contraction. Muscles require innervation to .... It is also an antagonist of M2 and M3 muscarinic receptors and is the most potent neuromuscular blocking agent of the aminosteroid class. It is sold under the trade names Arduan and Pycuron. See also * Pancuronium bromide References Muscle relaxants Quaternary ammonium compounds Piperazines Acetate esters Bromides Nicotinic antagonists Androstanes {{musculoskeletal-drug-stub ...
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Dihydrochandonium
Dihydrochandonium is an aminosteroid non-depolarizing neuromuscular blocking agent. References Muscle relaxants Nicotinic antagonists Quaternary ammonium compounds Steroids Neuromuscular blockers {{musculoskeletal-drug-stub ...
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Malouètine
Malouetine is an aminosteroid neuromuscular blocking agent and antinicotinic alkaloid isolated from '' Malouetia'' spp. The structure of malouetine inspired the development of modern aminosteroid muscle relaxants such as pancuronium bromide and vecuronium bromide by workers at Organon The ''Organon'' (, meaning "instrument, tool, organ") is the standard collection of Aristotle's six works on logical analysis and dialectic. The name ''Organon'' was given by Aristotle's followers, the Peripatetics, who maintained against the .... References Nicotinic antagonists Steroidal alkaloids Alkaloids found in Apocynaceae Neuromuscular blockers Quaternary ammonium compounds {{musculoskeletal-drug-stub ...
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Dacuronium
Dacuronium bromide ( INN, BAN) (developmental code name NB-68) is an aminosteroid neuromuscular blocking agent which was never marketed. It acts as a competitive antagonist of the nicotinic acetylcholine receptor Nicotinic acetylcholine receptors, or nAChRs, are Receptor (biochemistry), receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the c ... (nAChR). References Muscle relaxants Nicotinic antagonists Quaternary ammonium compounds Abandoned drugs Neuromuscular blockers Cyclopentanols Piperidines Acetate esters Bromides {{musculoskeletal-system-drug-stub ...
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Rapacuronium
Rapacuronium bromide (brand name Raplon) is a rapidly acting, non-depolarizing aminosteroid neuromuscular blocker formerly used in modern anaesthesia, to aid and enable endotracheal intubation, which is often necessary to assist in the controlled ventilation of unconscious patients during surgery and sometimes in intensive care. As a non-depolarizing agent it did not cause initial stimulation of muscles before weakening them. Due to risk of fatal bronchospasm it was withdrawn from the United States market by Organon The ''Organon'' (, meaning "instrument, tool, organ") is the standard collection of Aristotle's six works on logical analysis and dialectic. The name ''Organon'' was given by Aristotle's followers, the Peripatetics, who maintained against the ... on March 27, 2001, less than 2 years after its FDA approval in 1999. References Muscle relaxants Nicotinic antagonists Withdrawn drugs Quaternary ammonium compounds 1-Piperidinyl compounds Acetate esters ...
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Rocuronium
Rocuronium bromide (brand names Zemuron, Esmeron) is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia to facilitate tracheal intubation by providing skeletal muscle relaxation for surgery or mechanical ventilation. It is used for standard endotracheal intubation, as well as for rapid sequence induction (RSI). Pharmacology Mechanism of action 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 neuromuscular junction blockers, like succinylcholine. It was designed to be a weaker antagonist at the neuromuscular junction than pancuronium; hence its monoquaternary structure and its hav ...
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Vecuronium
Vecuronium bromide, sold under the brand name Norcuron among others, is a medication used as part of general anesthesia to provide skeletal muscle relaxation during surgery or mechanical ventilation. It is also used to help with endotracheal intubation; however, agents such as suxamethonium (succinylcholine) or rocuronium are generally preferred if this needs to be done quickly. It is given by injection into a vein. Effects are greatest at about 4 minutes and last for up to an hour. Side effects may include low blood pressure and prolonged paralysis. Allergic reactions are rare. It is unclear if use in pregnancy is safe for the baby. Vecuronium is in the aminosteroid neuromuscular-blocker family of medications and is of the non-depolarizing type. It works by competitively blocking the action of acetylcholine on skeletal muscles. The effects may be reversed with sugammadex or a combination of neostigmine and glycopyrrolate. To minimize residual blockade, reversal ...
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Pancuronium
Pancuronium (trademarked as Pavulon) is an aminosteroid muscle relaxant with various medical uses. It is used in euthanasia and is used in some states as the second of three drugs administered during lethal injections in the United States. Mechanism of action 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. It is a very potent muscle relaxant drug, with an ED95 (i.e., the dose that causes 95% depression of muscle twitch response) of only 60 μg/kg body weight. Onset of action is relatively slow compared to other similar drugs, in part due to its low dose: an intubating dose takes 3–6 minutes for full effect. Clinical effects (muscle activity lower than 25% of physiological) last for ab ...
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