Alcuronium chloride (formerly marketed as Alloferin) is a
neuromuscular blocking (NMB) agent, alternatively referred to as a skeletal
muscle relaxant
A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therap ...
. It is a semi-synthetic substance prepared from C-
toxiferine
Toxiferine (C-toxiferine I) is a curare toxin. It is a bisindole alkaloid derived from ''Strychnos toxifera'' and a nicotinic acetylcholine receptor antagonist. This alkaloid is the main toxic component of Calabash curare, and one of the most t ...
I, a ''bis''-quaternary alkaloid obtained from ''
Strychnos toxifera
''Strychnos toxifera'', called bush rope and devil doer, is a species of flowering plant in the genus ''Strychnos'', native to Costa Rica, Panama, Colombia, Ecuador, Venezuela, the Guianas, Brazil, Peru and Bolivia. It is the principal source of ...
''. C-
toxiferine
Toxiferine (C-toxiferine I) is a curare toxin. It is a bisindole alkaloid derived from ''Strychnos toxifera'' and a nicotinic acetylcholine receptor antagonist. This alkaloid is the main toxic component of Calabash curare, and one of the most t ...
I itself has been tested for its pharmacological action and noted to be a very long acting neuromuscular blocking agent For a formal definition of the durations of actions associated with NMB agents, see page for
gantacurium. The replacement of both the ''N''-methyl groups with ''N-allyl'' moieties yielded ''N,N''-diallyl-''bis''-nortoxiferine, now recognized as alcuronium.
Inclusion of the allylic functions presented an enhanced potential area of biotransformation, and thus alcuronium is observed to have a much shorter duration of neuromuscular blocking action than its parent C-toxiferine I. It also has a more rapid onset of action, and is ~1.5 times as potent as
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 pharmacological action of alcuronium is readily reversed by
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 it produces little
histamine
Histamine is an organic nitrogenous compound involved in local immune responses, as well as regulating physiological functions in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. Since histamine was discovered ...
release. The major disadvantage of alcuronium is that it elicits a vagolytic effect produced by a selective
atropine-like blockade of cardiac
muscarinic receptors
Muscarinic acetylcholine receptors, or mAChRs, are acetylcholine receptors that form G protein-coupled receptor complexes in the cell membranes of certain neurons and other cells. They play several roles, including acting as the main end-rec ...
.
Effects
* Cardiovascular system: histamine release and blockage of the sympathetic ganglia
The sympathetic ganglia, or paravertebral ganglia are autonomic ganglia, of the sympathetic nervous system. Ganglia are 20,000 to 30,000 Afferent nerve fiber, afferent and Efferent nerve fiber, efferent nerve cell bodies that run along on either s ...
including adrenal medulla could cause hypotension
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 dia ...
* Respiratory system
The respiratory system (also respiratory apparatus, ventilatory system) is a biological system consisting of specific organs and structures used for gas exchange in animals and plants. The anatomy and physiology that make this happen varies ...
: apnea due to phrenic blockage but bronchoconstriction
Bronchoconstriction is the constriction of the airways in the lungs due to the tightening of surrounding smooth muscle, with consequent coughing, wheezing, and shortness of breath.
Causes
The condition has a number of causes, the most common be ...
can occur from the histamine release
* Central nervous system
The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain and spinal cord. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all p ...
: no effect on intraocular pressure
Intraocular pressure (IOP) is the fluid pressure inside the eye. Tonometry is the method eye care professionals use to determine this. IOP is an important aspect in the evaluation of patients at risk of glaucoma. Most tonometers are calibrated t ...
* Autonomic ganglion
An autonomic ganglion is a cluster of nerve cell
A neuron, neurone, or nerve cell is an electrically excitable cell that communicates with other cells via specialized connections called synapses. The neuron is the main component of nervous tis ...
blockade can cause a decrease in gut motility
Peristalsis ( , ) is a radially symmetrical contraction and relaxation of muscles that propagate in a wave down a tube, in an anterograde direction. Peristalsis is progression of coordinated contraction of involuntary circular muscles, which ...
Special points
* Duration of action prolonged in states of low potassium
Hypokalemia is a low level of potassium (K+) in the blood serum. Mild low potassium does not typically cause symptoms. Symptoms may include feeling tired, leg cramps, weakness, and constipation. Low potassium also increases the risk of an abno ...
, calcium
Calcium is a chemical element with the symbol Ca and atomic number 20. As an alkaline earth metal, calcium is a reactive metal that forms a dark oxide-nitride layer when exposed to air. Its physical and chemical properties are most similar t ...
and protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residues. Proteins perform a vast array of functions within organisms, including catalysing metabolic reactions, DNA replication, res ...
, also in states of high magnesium and acidosis
Acidosis is a process causing increased acidity in the blood and other body tissues (i.e., an increase in hydrogen ion concentration). If not further qualified, it usually refers to acidity of the blood plasma.
The term ''acidemia'' describes ...
.
* Pharmaceutically incompatible with thiopentone
Sodium thiopental, also known as Sodium Pentothal (a trademark of Abbott Laboratories), thiopental, thiopentone, or Trapanal (also a trademark), is a rapid-onset short-acting barbiturate general anesthetic. It is the thiobarbiturate analog of p ...
* Infusion
Infusion is the process of extracting chemical compounds or flavors from plant material in a solvent such as water, oil or alcohol, by allowing the material to remain suspended in the solvent over time (a process often called steeping). An in ...
can cause fixed dilated pupils
Mydriasis is the dilation of the pupil, usually having a non-physiological cause, or sometimes a physiological pupillary response. Non-physiological causes of mydriasis include disease, trauma, or the use of certain types of drugs.
Normally, as ...
See also
* The International Pharmacopoeia
''The International Pharmacopoeia'' (''Pharmacopoeia Internationalis'', ''Ph. Int.'') is a pharmacopoeia issued by the World Health Organization as a recommendation, with the aim to provide international quality specifications for pharmaceutical s ...
References
Further reading
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{{portal bar, Medicine
Allyl compounds
Muscle relaxants
Neuromuscular blockers
Nicotinic antagonists
Hoffmann-La Roche brands