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Aminosteroid
Aminosteroids are a group of steroids with a similar structure based on an amino- substituted steroid nucleus. They are neuromuscular blocking agents, acting as competitive antagonists of the nicotinic acetylcholine receptor (nAChR), and block the signaling of acetylcholine in the nervous system. These drugs include candocuronium iodide (chandonium iodide), dacuronium bromide, dihydrochandonium, dipyrandium, malouetine, pancuronium bromide, pipecuronium bromide, rapacuronium bromide, rocuronium bromide, stercuronium iodide, and vecuronium bromide. See also * Benzylisoquinolines, such as atracurium and tubocurarine Tubocurarine (also known as ''d''-tubocurarine or DTC) is a toxic alkaloid historically known for its use as an arrow poison. In the mid-1900s, it was used in conjunction with an anesthetic to provide skeletal muscle relaxation during surgery or ..., the other major group of neuromuscular blocking agents References Muscle relaxants Nicotinic antagonists ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuromuscular Blocking Agent
Neuromuscular-blocking drugs block neuromuscular 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 intubation of the trachea, 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. Patients are still aware of pain even after full conduction block has occurred; hence, general anesthetics and/or analgesics must also be given to prevent anesthesia awareness. Nomenclature Neuromuscular blocking drugs are often classified into two broad ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vecuronium Bromide
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pancuronium Bromide
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 abo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Candocuronium Iodide
Candocuronium iodide (INN, formerly chandonium, HS-310) is an aminosteroid neuromuscular-blocking drug. Its use in anesthesia for endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation was briefly evaluated in clinical studies in India. However, further development was discontinued due to attendant cardiovascular effects, primarily tachycardia that was about the same as the clinically established pancuronium bromide. Candocuronium demonstrated a short duration and a rapid onset of action, with little or no ganglion blocking activity, with a greater potency than pancuronium. Background As with other neuromuscular blocking agents, candocuronium preferentially antagonizes competitively the nicotinic subtype of acetylcholine receptors. The agent was developed by the laboratory of Harkishan Singh, Panjab University, Chandigarh, India, as part of the search for a non-depolarizing replacement for the most popular clinically used depola ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rocuronium Bromide
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, most commonly required 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 acetyl-choline 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 monoquaternar ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pipecuronium Bromide
Pipecuronium (Arduan) is a bisquaternary aminosteroid muscle relaxant which blocks nicotinic acetylcholine receptors at the neuromuscular junction. It is also an antagonist of M2 and M3 muscarinic receptors The muscarinic acetylcholine receptor, also known as cholinergic/acetylcholine receptor M3, or the muscarinic 3, is a muscarinic acetylcholine receptor encoded by the human gene CHRM3. The M3 muscarinic receptors are located at many places in t ... 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Malouetine
Malouetine is an aminosteroid neuromuscular blocking agent and antinicotinic A nicotinic antagonist is a type of anticholinergic drug that inhibits the action of acetylcholine (ACh) at nicotinic acetylcholine receptors. These compounds are mainly used for peripheral muscle paralysis in surgery, the classical agent of this t ... 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. References Nicotinic antagonists Steroidal alkaloids Alkaloids found in Apocynaceae Neuromuscular blockers Quaternary ammonium compounds {{musculoskeletal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stercuronium Iodide
Stercuronium iodide (INN, USAN) (developmental code names MYC-1080, MYSC-1080) is an aminosteroid neuromuscular blocking agent which was never marketed. It acts as a competitive antagonist of the nicotinic acetylcholine receptor (nAChR), and is also reported to be an acetylcholinesterase inhibitor Acetylcholinesterase inhibitors (AChEIs) also often called cholinesterase inhibitors, inhibit the enzyme acetylcholinesterase from breaking down the neurotransmitter acetylcholine into choline and acetate, thereby increasing both the level and .... References Acetylcholinesterase inhibitors Muscle relaxants Nicotinic antagonists Quaternary ammonium compounds Neuromuscular blockers {{musculoskeletal-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rapacuronium Bromide
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'' ( grc, Ὄργανον, 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. The six ... 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dacuronium Bromide
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 polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral ne ... (nAChR). References Muscle relaxants Nicotinic antagonists Quaternary ammonium compounds Abandoned drugs Neuromuscular blockers Cyclopentanols Piperidines Acetate esters Bromides {{musculoskeletal-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
