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Vecuronium bromide, sold under the brand name Norcuron among others, is a medication used as part of
general anesthesia General anaesthesia (UK) or general anesthesia (US) is medically induced loss of consciousness that renders a patient unarousable even by painful stimuli. It is achieved through medications, which can be injected or inhaled, often with an analgesi ...
to provide skeletal muscle relaxation during
surgery Surgery is a medical specialty that uses manual and instrumental techniques to diagnose or treat pathological conditions (e.g., trauma, disease, injury, malignancy), to alter bodily functions (e.g., malabsorption created by bariatric surgery s ...
or
mechanical ventilation Mechanical ventilation or assisted ventilation is the Medicine, medical term for using a ventilator, ventilator machine to fully or partially provide artificial ventilation. Mechanical ventilation helps move air into and out of the lungs, wit ...
. 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 Paralysis (: paralyses; also known as plegia) is a loss of Motor skill, motor function in one or more Skeletal muscle, muscles. Paralysis can also be accompanied by a loss of feeling (sensory loss) in the affected area if there is sensory d ...
.
Allergic reactions Allergies, also known as allergic diseases, are various conditions caused by hypersensitivity of the immune system to typically harmless substances in the environment. These diseases include hay fever, food allergies, atopic dermatitis, alle ...
are rare. It is unclear if use in
pregnancy Pregnancy is the time during which one or more offspring gestation, gestates inside a woman's uterus. A multiple birth, multiple pregnancy involves more than one offspring, such as with twins. Conception (biology), Conception usually occurs ...
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 Acetylcholine (ACh) is an organic compound that functions in the brain and body of many types of animals (including humans) as a neurotransmitter. Its name is derived from its chemical structure: it is an ester of acetic acid and choline. Par ...
on skeletal muscles. The effects may be reversed with sugammadex or a combination of neostigmine and glycopyrrolate. To minimize residual blockade, reversal should only be attempted if some degree of spontaneous recovery has been achieved. Vecuronium was approved for medical use in the United States in 1984 and is available as a
generic medication A generic drug is a pharmaceutical drug that contains the same chemical substance as a drug that was originally protected by chemical patents. Generic drugs are allowed for sale after the patents on the original drugs expire. Because the active ch ...
. It is on the World Health Organization's List of Essential Medicines.


Mechanism of action

Vecuronium operates by competing for the cholinoceptors at the motor end plate, thereby exerting its muscle-relaxing properties, which are used adjunctively to general anesthesia. Under balanced anesthesia, the time to recovery to 25% of control (clinical duration) is approximately 25 to 40 minutes after injection and recovery is usually 95% complete approximately 45 to 65 minutes after injection of an intubating dose. The neuromuscular blocking action of vecuronium is slightly enhanced in the presence of potent inhalation anesthetics. If vecuronium is first administered more than 5 minutes after the start of the inhalation of enflurane, isoflurane, or
halothane Halothane, sold under the brand name Fluothane among others, is a general anaesthetic. It can be used to induce or maintain anaesthesia. One of its benefits is that it does not increase the production of saliva, which can be particularly useful ...
, or when a steady state has been achieved, the intubating dose of vecuronium may be decreased by approximately 15%. Vecuronium has an active metabolite, 3-desacetyl-vecuronium, that has 80% of the effect of vecuronium. Accumulation of this metabolite, which is cleared by the kidneys, can prolong the duration of action of the drug, particularly when an infusion is used in a person with
kidney failure Kidney failure, also known as renal failure or end-stage renal disease (ESRD), is a medical condition in which the kidneys can no longer adequately filter waste products from the blood, functioning at less than 15% of normal levels. Kidney fa ...
. Reversal of vecuronium can be accomplished by administration of sugammadex which is a γ-
cyclodextrin Cyclodextrins are a family of cyclic oligosaccharides, consisting of a macrocycle, macrocyclic ring of glucose subunits joined by α-1,4 glycosidic bonds. Cyclodextrins are produced from starch by enzyme, enzymatic conversion. They are used in ...
which encapsulates vecuronium preventing it from binding to receptors. Reversal can also be accomplished with neostigmine or other cholinesterase inhibitors, but their efficacy is lower than that of sugammadex.


History

As long ago as 1862, adventurer Don Ramon Paez described a Venezuelan poison, guachamaca, which the indigenous peoples used to lace sardines as bait for herons and cranes. If the head and neck of a bird so killed was cut off, the remainder of the flesh could be eaten safely. Paez also described the attempt of a
Llanero A (, 'plainsman') is a Venezuelan and Colombian herder. The name is taken from the Llanos grasslands occupying eastern Colombia and western-central Venezuela. During the Spanish American wars of independence, lancers and cavalry served in b ...
woman to murder a rival to her lover's affections with guachamaca and unintentionally killed 10 other people when her husband shared his food with their guests. It is probable that the plant was '' Malouetia nitida'' or ''Malouetia schomburgki''. The genus ''Malouetia'' (family ''
Apocynaceae Apocynaceae (, from '' Apocynum'', Greek for "dog-away") is a family of flowering plants that includes trees, shrubs, herbs, stem succulents, and vines, commonly known as the dogbane family, because some taxa were used as dog poison. Notable mem ...
'') is found in both
South America South America is a continent entirely in the Western Hemisphere and mostly in the Southern Hemisphere, with a considerably smaller portion in the Northern Hemisphere. It can also be described as the southern Subregion#Americas, subregion o ...
and
Africa Africa is the world's second-largest and second-most populous continent after Asia. At about 30.3 million km2 (11.7 million square miles) including adjacent islands, it covers 20% of Earth's land area and 6% of its total surfac ...
. The botanist Robert E. Woodson Jr comprehensively classified the American species of ''Malouetia'' in 1935. At that time, only one African species of ''Malouetia'' was recognized, but the following year Woodson described a second: ''Malouetia bequaertiana'', from the Belgian Congo. In 1960, scientists reported the isolation of malouetine from the roots and bark of ''Malouetia bequaertiana'' Woodson by means of an ion exchange technique. Optimization of the aminosteroid nucleus led to a sequence of synthesized derivatives, ultimately leading to pancuronium bromide in 1964. The name was derived from p(iperidino)an(drostane)cur(arising)-onium. A paper published in 1973 discussed the structure-activity relationships of a series of aminosteroid muscle relaxants, including the mono-quaternary analogue of pancuronium, later called vecuronium.


Society and culture

Vecuronium bromide has been used as part of a drug cocktail that prisons in the
United States The United States of America (USA), also known as the United States (U.S.) or America, is a country primarily located in North America. It is a federal republic of 50 U.S. state, states and a federal capital district, Washington, D.C. The 48 ...
use for execution by
lethal injection Lethal injection is the practice of injecting one or more drugs into a person (typically a barbiturate, paralytic, and potassium) for the express purpose of causing death. The main application for this procedure is capital punishment, but t ...
. Vecuronium is used to paralyze the prisoner and stop his or her breathing, in conjunction with a sedative and
potassium chloride Potassium chloride (KCl, or potassium salt) is a metal halide salt composed of potassium and chlorine. It is odorless and has a white or colorless vitreous crystal appearance. The solid dissolves readily in water, and its solutions have a sa ...
to stop the prisoner's heart. Injections of vecuronium bromide without proper sedation allow the person to be fully awake but unable to move in response to pain. In 2001, Japanese nurse Daisuke Mori was reported to have murdered 10 patients using vecuronium bromide. He was convicted of murder and was sentenced to
life imprisonment Life imprisonment is any sentence (law), sentence of imprisonment under which the convicted individual is to remain incarcerated for the rest of their natural life (or until pardoned or commuted to a fixed term). Crimes that result in life impr ...
. In 2022, Vanderbilt University Medical Center nurse RaDonda Vaught was convicted of two felony charges in the death of a patient who was mistakenly administered vecuronium bromide, rather than the
sedative A sedative or tranquilliser is a substance that induces sedation by reducing irritability or Psychomotor agitation, excitement. They are central nervous system (CNS) Depressant, depressants and interact with brain activity, causing its decelera ...
midazolam Midazolam, sold under the brand name Versed among others, is a benzodiazepine medication used for anesthesia, premedication before surgical anesthesia, and procedural sedation, and to treat psychomotor agitation, severe agitation. It induces ...
, also known as Versed.


References


External links

* {{Portal bar, Medicine Acetate esters Androstanes Muscle relaxants Drugs developed by Schering-Plough Neuromuscular blockers Nicotinic antagonists Piperidines Quaternary ammonium compounds Wikipedia medicine articles ready to translate World Health Organization essential medicines