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Atracurium besylate
API |
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Haorui supplies high quality Atracurium besylate API produced by our
GMP facility that has been successfully inspected by the
FDA.
We offer
competitive prices and support our products with reliable technical and
regulatory services. Atracurium besylate API is available from R&D to
commercial quantities. Please contact us for more details. |
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The following
information is provided for general information purposes
ONLY. |
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What is Atracurium besylate?
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Atracurium besylate is a synthetic,
non-depolarizing neuromuscular blocking agent.
Atracurium, is a bisquaternary, non-choline diester
structurally similar to metocurine and tubocurarine. |
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Atracurium besylate is an intermediate-duration,
nondepolarizing, skeletal muscle relaxant for
intravenous administration. Atracurium besylate is
designated as
2,2'-[1,5-pentanediylbis[oxy(3-oxo-3,1-propanediyl)]]bis[1-[(3,4-
dimethoxyphenyl)
methyl]-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methylisoquinolinium]dibenzenesulfonate.
It has a molecular weight of 1243.51, and its
molecular formula is C65H82N2O18S2. |
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What is Atracurium besylate used
for? |
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Atracurium is indicated as an adjunct
to general anesthesia to produce muscle relaxation
during surgical procedures or mechanical ventilation
and also to facilitate endotracheal intubation.
Atracurium can be used in patients with significant
renal or hepatic disease. |
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Atracurium besylate is a complex molecule containing
four sites at which different stereochemical
configurations can occur. The symmetry of the
molecule, however, results in only ten, instead of
sixteen, possible different isomers. The manufacture
of atracurium besylate results in these isomers
being produced in unequal amounts but with a
consistent ratio. Those molecules in which the
methyl group attached to the quaternary nitrogen
projects on the opposite side to the adjacent
substituted-benzyl moiety predominate by
approximately 3:1. |
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Atracurium besylate
Pharmacokinetics |
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After IV injection, maximal
neuromuscular blockade generally occurs within 3-5
minutes. The duration of maximal blockade increases
as the dosage increases. Systemic alkalosis may
diminish the degree and duration of blockade;
acidosis potentiates it. In conjunction with
balanced anesthesia, the duration of blockade
generally persists for 20-35 minutes. Recovery times
do not change after maintenance doses are given, so
predictable blocking effects can be attained when
the drug is administered at regular intervals.
Atracurium is metabolized by ester
hydrolysis and Hofmann elimination which occurs
independently of renal or hepatic function. |
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Atracurium besylate Drug
Interaction |
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The following agents may enhance the
neuromuscular blocking activity of atracurium:
procainamide, quinidine, verapamil, aminoglycoside
antibiotics, lincomycin, clindamycin, bacitracin,
polymyxin B, lithium, magnesium sulfate, thiazide
diuretics, enflurane, isoflurane, and halothane.
Loop diuretics have been reported to both decrease
and increase the effects of nondepolarizing
neuromuscular blockers. Other muscle relaxant drugs
may cause a synergistic or antagonistic effect.
Succinylcholine may speed the onset of action and
enhance the neuromuscular blocking actions of
atracurium. Do not give atracurium until
succinylcholine effects have diminished.
Theophylline or phenytoin may inhibit or reverse the
neuromuscular blocking action of atracurium. |
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Precautions Before Using
Atracurium besylate |
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Atracurium is contraindicated in patients who are
hypersensitive to it. Because it may rarely cause
significant release of histamine it should be used
with caution in patients where this would be
hazardous (severe cardiovascular disease, asthma,
etc.). Atracurium has minimal cardiac effects and
will not counteract the bradycardia or vagal
stimulation induced by other agents. Use of
neuromuscular blocking agents must be done with
extreme caution, or not at all, in patients
suffering from myasthenia gravis. Atracurium has no
analgesic or sedative/anesthetic actions. |
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Atracurium besylate side effects
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Clinically significant adverse effects are
apparently quite rare in patients (<1% in humans)
receiving recommended doses of atracurium and
usually are secondary to histamine release. They
can include: allergic reactions, inadequate or
prolonged block, hypotension vasodilatation,
bradycardia, tachycardia, dyspnea, broncho-,
laryngospasm, rash, urticaria, and a reaction at the
injection site. Patients developing hypotension
usually have preexisting severe cardiovascular
disease. |
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Overdose Atracurium besylate |
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Overdosage possibilities can be minimized by
monitoring muscle twitch response to peripheral
nerve stimulation. Increased risks of hypotension
and histamine release occur with overdoses, as well
as prolonged duration of muscle blockade. |
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Atracurium besylate Storage |
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Atracurium injection should be stored in the
refrigerator and protected against freezing. At room
temperature, approximately 5% potency loss occurs
each month; when refrigerated, a 6% potency loss
occurs over a year time. |
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Disclaimer:
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Information on this page is
provided for general information purposes. You
should not make a clinical treatment decision based
on information contained in this page without
consulting other references including the package
insert of the drug, textbooks and where relevant,
expert opinion. We cannot be held responsible for
any errors you make in administering drugs mentioned
on this page, nor for use of any erroneous
information contained on this page.
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