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 a medically induced loss of consciousness that renders the patient unarousable even with painful stimuli. This effect is achieved by administering either intravenous or inhalational general ...

to provide skeletal muscle relaxation during surgery or

mechanical ventilation Mechanical ventilation, assisted ventilation or intermittent mandatory ventilation (IMV), is the medical term for using a machine called a ventilator to fully or partially provide artificial ventilation. Mechanical ventilation helps move a ...

. It is also used to help with

endotracheal intubation Tracheal intubation, usually simply referred to as intubation, is the placement of a flexible plastic tube into the trachea (windpipe) to maintain an open airway or to serve as a conduit through which to administer certain drugs. It is frequently ...

; however, agents such as

suxamethonium Suxamethonium chloride, also known as suxamethonium or succinylcholine, or simply sux by medical abbreviation, is a medication used to cause short-term paralysis as part of general anesthesia. This is done to help with tracheal intubation or ele ...

(succinylcholine) or rocuronium are generally preferred if this needs to be done quickly. It is given by

injection into a vein Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutri ...

. Effects are greatest at about 4 minutes and last for up to an hour. Side effects may include

low blood pressure Hypotension is low blood pressure. Blood pressure is the force of blood pushing against the walls of the arteries as the heart pumps out blood. Blood pressure is indicated by two numbers, the systolic blood pressure (the top number) and the di ...

and prolonged paralysis.

Allergic reactions Allergies, also known as allergic diseases, refer a number of conditions caused by the hypersensitivity of the immune system to typically harmless substances in the environment. These diseases include hay fever, food allergies, atopic derm ...

are rare. It is unclear if use in

pregnancy Pregnancy is the time during which one or more offspring develops (gestation, gestates) inside a woman, woman's uterus (womb). A multiple birth, multiple pregnancy involves more than one offspring, such as with twins. Pregnancy usually occur ...

is safe for the baby. Vecuronium is in the

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 th ...

neuromuscular-blocker 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 clin ...

family of medications and is of the

non-depolarizing 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 clin ...

type. It works by competitively blocking the action of acetylcholine on

skeletal muscles Skeletal muscles (commonly referred to as muscles) are organs of the vertebrate muscular system and typically are attached by tendons to bones of a skeleton. The muscle cells of skeletal muscles are much longer than in the other types of muscle ...

. The effects may be reversed with

sugammadex Sugammadex, sold under the brand name Bridion, is a medication for the reversal of neuromuscular blockade induced by rocuronium and vecuronium in general anaesthesia. It is the first selective relaxant binding agent (SRBA). It is marketed by Mer ...

or a combination of

neostigmine Neostigmine, sold under the brand name Bloxiverz, among others, is a medication used to treat myasthenia gravis, Ogilvie syndrome, and urinary retention without the presence of a blockage. It is also used in anaesthesia to end the effects of n ...

and

glycopyrrolate Glycopyrronium bromide is a medication of the muscarinic anticholinergic group. It does not cross the blood–brain barrier and consequently has few to no central effects. It is available in oral, intravenous, topical, and inhaled forms. It is a ...

. To minimize residual blockade, reversal should only be attempted if some degree of spontaneous recovery have been achieved. Vecuronium was approved for medical use in the United States in 1984 and is available as a generic medication. It is on the

World Health Organization's List of Essential Medicines The WHO Model List of Essential Medicines (aka Essential Medicines List or EML), published by the World Health Organization (WHO), contains the medications considered to be most effective and safe to meet the most important needs in a health s ...

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, or when a

steady state In systems theory, a system or a process is in a steady state if the variables (called state variables) which define the behavior of the system or the process are unchanging in time. In continuous time, this means that for those properties ''p' ...

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 end-stage kidney disease, 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 failure is classified as eit ...

. Reversal of vecuronium can be accomplished by administration of

which is a γ-

cyclodextrin Cyclodextrins are a family of cyclic oligosaccharides, consisting of a macrocyclic ring of glucose subunits joined by α-1,4 glycosidic bonds. Cyclodextrins are produced from starch by enzymatic conversion. They are used in food, pharmaceutical ...

which encapsulates vecuronium preventing it from binding to receptors. Reversal can also be accomplished with

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 South American 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 both ar ...

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 Members of ...

'') is found in both

South America South America is a continent entirely in the Western Hemisphere and mostly in the Southern Hemisphere, with a relatively small portion in the Northern Hemisphere at the northern tip of the continent. It can also be described as the sout ...

and

Africa Africa is the world's second-largest and second-most populous continent, after Asia in both cases. At about 30.3 million km2 (11.7 million square miles) including adjacent islands, it covers 6% of Earth's total surface area ...

. 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 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. Mecha ...

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

muscle relaxants, including the mono-quaternary analogue of pancuronium, later called vecuronium.

Society and culture

It is commercially available as ampoules containing 4 or 10 mg of the drug in powder form which needs to be dissolved in distilled water prior to being given.

Non-medical use

Vecuronium bromide has been used as part of a drug cocktail that prisons in the

United States The United States of America (U.S.A. or USA), commonly known as the United States (U.S. or US) or America, is a country primarily located in North America. It consists of 50 states, a federal district, five major unincorporated territori ...

use for execution by lethal injection. Vecuronium is used to paralyze the prisoner and stop his or her breathing, in conjunction with a sedative and potassium chloride 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.

References

External links

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