Atracurium Besylate (atracurium besylate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Atracurium besylate is a benzylisoquinolone nondepolarizing neuromuscular blocking agent.
Atracurium besylate is a nondepolarizing neuromuscular blocking agent with an intermediate duration of action. Nondepolarizing neuromuscular blocking agents antagonize the neurotransmitter action of acetylcholine by binding competitively with cholinergic receptor sites on the motor end-plate. On a weight basis, atracurium besylate is about 20-25% as potent as vecuronium bromide.
The duration of neuromuscular blockade induced by equipotent doses of atracurium besylate is similar to or slightly longer than that induced by vecuronium bromide.
Atracurium can stimulate histamine release. Histamine release is generally minimal with initial doses of atracurium besylate up to 0.5 mg/kg; however, administration of a 0.6-mg/kg dose of the drug elicited moderate histamine release and a substantial hypotensive effect. The histamine and hemodynamic responses were poorly correlated, and these effects appeared to be transient and easily managed; however, the potential for substantial histamine release in sensitive individuals must be considered.
The manufacturers state that the ED95 (dose required to produce 95% suppression of the control twitch response) of the drug in patients undergoing balanced anesthesia averages 0.23 mg/kg (range: 0.11-0.26 mg/kg). As with other nondepolarizing neuromuscular blocking agents, the time from injection to maximum blockade decreases and the duration of maximum effect increases as the dose of atracurium increases. Following IV administration of a 0.4- to 0.5-mg/kg dose of atracurium besylate, maximum neuromuscular blockade generally occurs within 3-5 minutes, with good or excellent intubation conditions occurring within 2-2.5 minutes.
The duration of neuromuscular blockade under balanced anesthesia is about 20-35 minutes; recovery to 25% of control is achieved approximately 35-45 minutes after injection, and recovery is usually 95% complete approximately 60-70 minutes after injection. Repeated administration of maintenance doses of atracurium does not appear to have a cumulative effect on duration of the neuromuscular blockade, provided recovery from blockade is allowed to begin prior to administering repeated maintenance doses. In addition, since the time necessary to recover from maintenance doses does not change with each additional dose, doses may be administered at relatively regular intervals with predictable neuromuscular blocking results.
After an initial atracurium besylate dose of 0.4-0.5 mg/kg under balanced anesthesia, the first maintenance dose (0.08-0.1 mg/kg) is generally required within 20-45 minutes, and subsequent maintenance doses are usually required at approximately 15-25 minute intervals. Regardless of the dose of atracurium, the time from complete block to complete recovery (95%) is approximately 30 minutes under balanced anesthesia and approximately 40 minutes under anesthesia with isoflurane. Repeated administration of maintenance doses of atracurium does not appear to have a cumulative effect on the rate of recovery from neuromuscular blockade.
The pharmacokinetics of atracurium are essentially linear within the dose range of 0.3-0.6 mg/kg. Atracurium is inactivated by 2 nonoxidative pathways: ester hydrolysis (catalyzed by nonspecific esterases) and Hofmann elimination (a nonenzymatic chemical process that occurs at physiologic pH). Laudanosine, a major biologically active metabolite of atracurium, does not have neuromuscular blocking activity but can produce transient hypotension and, in higher doses, cerebral excitatory effects.
The elimination half-life of atracurium is approximately 20 minutes. Atracurium besylate and its metabolites are excreted principally in urine and bile. The metabolites recovered in urine and bile are similar.
Generic name: atracurium besylate
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Atracurium Besylate
Indications
The following indications are listed for Atracurium Besylate:
- Muscle Relaxation
Also known as: Muscle Flaccidity.
Dosing
Dosage of atracurium besylate is expressed in terms of the salt. The dosage must be carefully adjusted according to individual requirements and response. The use of a peripheral nerve stimulator is recommended to accurately monitor the degree of muscle relaxation, determine the need for additional doses, determine the adequacy of spontaneous recovery or antagonism, and minimize the complications of overdosage if additional doses are administered.
Atracurium besylate is administered IV. The initial intubating dose is administered by rapid IV injection; maintenance doses may be administered by intermittent IV injection or by continuous IV infusion. Atracurium should not be administered by IM injection.
Commercially available atracurium besylate injection should be refrigerated at 2-8degreesC and protected from light; do not freeze. Once removed from refrigeration, the injection should be used within 14 days, even if the product is returned to the refrigerator.
For continuous IV infusion, atracurium besylate injection should be diluted to the desired concentration (usually 0.2 or 0.5 mg/mL) in 5% dextrose, 5% dextrose and 0.9% sodium chloride, or 0.9% sodium chloride injection. Infusion solutions may be stored under refrigeration or at room temperature, and should be used within 24 hours following dilution. Atracurium besylate should not be diluted in Lactated ringer's. Accurate dosing of continuous infusions is best achieved using a precision infusion device.
Atracurium should not be mixed in the same syringe nor administered simultaneously through the same needle as an alkaline solution (e.g., barbiturate solution).
Atracurium besylate injection and diluted solutions of the drug should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to atracurium or any component of the formulation (e.g., benzyl alcohol in multiple dose vials).
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects of atracurium observed in 5% or more of patients in clinical studies included skin flush.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
The safety and effectiveness of atracurium in pediatric patients <1 month of age have not been established.
Multiple dose vials of atracurium besylate contain benzyl alcohol, which has been associated with an increased incidence of neurological and other complications in neonates. In some cases, these complications may be fatal.
There are no adequate and well-controlled studies of atracurium in pregnant women. In animal studies, atracurium has been shown to be potentially teratogenic. When atracurium besylate was administered subcutaneously to nonventilated rabbits on days 6-18 of gestation, an increased incidence of spontaneously-occurring visceral and skeletal abnormalities was observed. Use atracurium during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Atracurium has been used in a limited number of pregnant women undergoing cesarean section. No harmful effects were attributed to atracurium in any of the neonates, although small amounts of atracurium were shown to cross the placental barrier. The potential for respiratory depression in the neonate should always be considered. In patients receiving magnesium sulfate, neuromuscular blocker reversal may be unsatisfactory and the dose of atracurium should be lowered as indicated.
It is not known whether neuromuscular blockers administered during vaginal delivery have immediate or delayed effects on the fetus or increase the likelihood that resuscitation of the newborn will be necessary. The possibility that forceps delivery will be required may increase.
It is not known whether atracurium is excreted in human milk. Use caution when administering atracurium to a breast-feeding woman.
The manufacturer makes no specific dosage recommendations for geriatric patients.
Uncontrolled clinical experience and limited data from controlled trials have not identified differences in effectiveness, safety, or dosage requirements between healthy elderly and younger patients. As with other neuromuscular blocking agents, the use of a peripheral nerve stimulator to monitor neuromuscular function is suggested.
Elderly patients may have slightly altered pharmacokinetic parameters compared to younger patients, with a slightly decreased total plasma clearance; however, this is offset by a corresponding increase in volume of distribution. The net effect of these pharmacokinetic changes is no significant difference in clinical duration and recovery from neuromuscular blockade between elderly and younger patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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