Cisatracurium Besylate (cisatracurium besylate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Cisatracurium besylate, a benzylisoquinolone nondepolarizing neuromuscular blocking agent, is an isomer of atracurium.
Cisatracurium besylate is a nondepolarizing neuromuscular blocking agent. Cisatracurium produces skeletal muscle relaxation by binding competitively to cholinergic receptors on the motor end-plate, causing a decreased response to acetylcholine (ACh) and blockade of neuromuscular transmission. The neuromuscular blocking potency of cisatracurium is approximately 3-fold that of atracurium.
Cisatracurium exhibits little histamine-releasing activity at usual therapeutic doses.
Cisatracurium has an intermediate onset and duration of action. Cisatracurium is rapidly metabolized via Hofmann elimination (independent of the liver) to form a monoquaternary acrylate metabolite (which undergoes nonspecific plasma esterase hydrolysis and subsequent Hofmann elimination) and laudanosine (which is demethylated and glucuronidated). Both metabolites lack neuromuscular blocking activity; laudanosine may have CNS excitatory activity when present in large amounts.
Cisatracurium is eliminated principally by Hofmann elimination (77-80%) and to a lesser extent by renal and hepatic elimination (20%). Metabolites of the drug are eliminated principally by renal and hepatic elimination. The elimination half-life of cisatracurium is approximately 22-30 minutes.
Following administration of a radiolabeled dose of cisatracurium to healthy individuals, 95% of the administered dose is recovered in urine and 4% in feces; <10% of the dose is recovered as unchanged drug.
Generic name: cisatracurium besylate
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Cisatracurium Besylate
Indications
The following indications are listed for Cisatracurium Besylate:
- General Anesthesia Adjunct
- Muscle Relaxation
- Skeletal Muscle Relaxation For Endotracheal Intubation
Also known as: Adjunct General Anesthesia, Muscle Flaccidity, Skeletal Muscle Relaxation For Endotracheal Tube Insertion, Skeletal Muscle Relaxation For Intratracheal Intubation, Skeletal Muscle Relaxation For Intubation Of Trachea.
Dosing
Dosage of cisatracurium besylate is expressed in terms of cisatracurium.
Dosage of cisatracurium 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.
Cisatracurium is administered IV only.
Commercially available 20-mL single-dose vials of cisatracurium besylate containing 10 mg/mL are intended for intensive care unit (ICU) use only.
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 cisatracurium or any of its components.
*Multiple-dose vials of cisatracurium containing benzyl alcohol are contraindicated in pediatric patients <1 month of age and low birth-weight infants.
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
The most common adverse reactions (occurring in 0.1-0.4% of patients receiving cisatracurium besylate in clinical trials) were bradycardia, hypotension, flushing, bronchospasm, and rash.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of cisatracurium have not been established in neonates (younger than 1 month of age).
Safety and efficacy of cisatracurium as an adjunct to general anesthesia to facilitate tracheal intubation and to provide skeletal muscle relaxation during surgery in pediatric patients 1 month to 12 years of age were established in 3 pediatric studies.
The 10-mL multiple-dose vials of cisatracurium besylate contain benzyl alcohol as a preservative. Serious and fatal adverse reactions, including ''gasping syndrome,'' can occur in neonates and infants treated with benzyl alcohol-preserved drugs. In reported cases of ''gasping syndrome,'' benzyl alcohol dosages of 99-234 mg/kg/day produced high levels of benzyl alcohol and its metabolites in the blood and urine; adverse reactions included gradual neurological deterioration, seizures, intracranial hemorrhage, hematologic abnormalities, skin breakdown, hepatic and renal failure, hypotension, bradycardia, and cardiovascular collapse. Preterm, low birth-weight infants are more likely to develop these reactions because they are less able to metabolize benzyl alcohol.
Use of the 10-mL multiple-dose vials is contraindicated in pediatric patients <1 month of age and in low birth-weight infants. When prescribing the 10 mL multiple-dose vials, consider the combined daily metabolic load of benzyl alcohol from all sources (multiple-dose vials of cisatracurium besylate contain 9 mg of benzyl alcohol per mL). The minimum amount of benzyl alcohol at which serious adverse reactions may occur is not known. The 20 mL and 5 mL single-dose vials of cisatracurium besylate do not contain benzyl alcohol.
Pediatric patients may exhibit faster clearance of cisatracurium than adults. Onset of the drug is faster and duration is shorter in pediatric patients compared with adults.
There are no clinical trial data available to evaluate the risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes with cisatracurium besylate during pregnancy. No evidence of fetal harm was observed when cisatracurium was administered to pregnant rats during the period of organogenesis at 0.8 times the human exposure with a starting IV bolus dose of 0.2 mg/kg.
The 10-mL multiple-dose vial of cisatracurium besylate contains benzyl alcohol. If cisatracurium besylate is needed during pregnancy, consider using the 5-mL or 20-mL single-dose vials, which do not contain a preservative. Because benzyl alcohol is rapidly metabolized in pregnant women, benzyl alcohol exposure in the fetus is unlikely. However, adverse reactions have occurred in premature neonates and low birth-weight infants who received IV benzyl alcohol-containing drugs.
The action of neuromuscular blocking agents may be enhanced by magnesium salts administered for the management of preeclampsia or eclampsia.
It is not known whether cisatracurium is distributed into human milk. The effects on the breast-fed child and on milk production are also unknown. Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for the drug and any potential adverse effects on the breast-fed child from the drug or from the underlying maternal condition.
The 10-mL multiple-dose vial of cisatracurium besylate contains benzyl alcohol. If cisatracurium besylate is needed during lactation, consider using the 5-mL or 20-mL single-dose vials, which do not contain a preservative. Because benzyl alcohol is rapidly metabolized in lactating women, benzyl alcohol exposure in the breast-fed infant is unlikely. However, adverse reactions have occurred in premature neonates and low birth-weight infants who received IV benzyl alcohol-containing drugs.
Since onset of complete neuromuscular blockade may be slower in geriatric patients, it may be necessary to extend the interval between administration of cisatracurium and the intubation attempt in such patients.
Of the 135 patients in clinical studies of cisatracurium besylate, 57, 63, and 15 patients were 65-70 years of age, 70-80 years of age, and >80 years of age, respectively. The geriatric population included a subset of patients with significant cardiovascular disease. No overall differences in safety and efficacy have been observed in geriatric patients relative to younger adults, but increased sensitivity of some older patients cannot be ruled out.
Because the time to maximum neuromuscular blockade is approximately 1 minute slower in geriatric patients compared to younger patients, consider extending the interval between cisatracurium administration and attempting intubation by at least 1 minute to achieve adequate intubation conditions. Minor alterations in cisatracurium pharmacokinetics have been observed in geriatric patients compared with younger individuals; however, these changes were not associated with substantial differences in recovery profile.
Cisatracurium half-life may be slightly prolonged in geriatric patients.
ICD codes
No ICD codes are available for this drug.
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Last reviewed · Source: First Databank (FDB) drug data
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