Peringatan Keamanan

Overdosage with neuromuscular blocking agents such as cisatracurium may result in neuromuscular block beyond the time needed for surgery and anesthesia. Maintenance of a patent airway and controlled ventilation until recovery of normal neuromuscular function is the primary treatment for overdose cases. To facilitate further recovery, a cholinesterase inhibitor in conjunction with an appropriate cholinergic inhibitor may be administered once recovery from the neuromuscular block begins. If complete neuromuscular blockade is evident or suspected, cholinesterase inhibitors should not be administered. The reversal of paralysis may not be sufficient to maintain a patent airway and an appropriate level of spontaneous ventilation.L43577

The long-term carcinogenicity of cisatracurium has not been evaluated. In an in vitro mouse lymphoma forward gene mutation assay, cisatracurium besylate led to mutations in the presence and absence of exogenous metabolic activation. Other assays did not show evidence of mutagenicity or clastogenicity.L43577

Cisatracurium

DB00565

small molecule approved investigational

Deskripsi

Cisatracurium is a non-depolarising neuromuscular blocking agent of the benzylisoquinolinium class, available in its salt form, cisatracurium besylate.A243416,A253592 Cisatracurium has an intermediate duration of action and is one of the most commonly used neuromuscular blocking agents in intensive care.A253592,A253597. Cisatracurium acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine.A243416,A253592 Cisatracurium is an R-cis-R-cis isomer of atracurium and has approximately 3 times its neuromuscular blocking potency.A243416 Compared to atracurium, cisatracurium produces a lower degree of histamine release.A253597

Struktur Molekul 2D

Berat 929.16
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Cisatracurium has an elimination half-life of 22 minutes.[L43577]
Volume Distribusi Cisatracurium has a volume of distribution at steady state of 145 mL/kg.[L43577] The volume of distribution of cisatracurium besylate is small due to its relatively large molecular weight and high polarity.[A253602]
Klirens (Clearance) Cisatracurium has a plasma clearance of 4.57 mL/min/kg.[L43577]

Absorpsi

The pharmacokinetics of cisatracurium follow a two-compartment open model.A253602,L43577 Cisatracurium is metabolized into laudanosine and monoquaternary alcohol metabolite (MQA). Following the IV infusion of cisatracurium, the Cmax of laudanosine and MQA were 6% and 11% of the parent compound, respectively.L43577 Compared to young patients, the volume of distribution of cisatracurium is slightly larger in elderly patients, which also leads to longer half-life values. The plasma clearance of cisatracurium was not affected by age. Patients with hepatic impairment have a slightly higher volume of distribution and plasma clearance values; however, these minor pharmacokinetic differences are not considered clinically significant. Additionally, the pharmacokinetic parameters of cisatracurium in patients with end-stage renal disease were similar to those detected in healthy adult patients.L43577

Metabolisme

The degradation of cisatracurium is largely independent of liver metabolism. Cisatracurium undergoes Hofmann elimination (a pH and temperature-dependent chemical process) to form laudanosine and the monoquaternary acrylate metabolite. Non-specific plasma esterases hydrolyze the monoquaternary acrylate metabolite to form the monoquaternary alcohol metabolite (MQA). The MQA can also undergo Hofmann elimination, but the rate of this process is slower than the one detected for cisatracurium. Laudanosine is further metabolized to desmethyl metabolites that are conjugated with glucuronic acid and excreted in the urine. Laudanosine may cause transient hypotension and, in higher doses, cerebral excitatory effects when administered to several animal species; however, the effects of laudanosine in humans have not been established.L43577

Rute Eliminasi

The predominant elimination mechanism of cisatracurium is Hofmann elimination, a chemical process dependent on pH and temperature (approximately 80% in healthy surgical patients). The liver and kidney play a minor role in the elimination of cisatracurium (about 20%); however, they have a significant role in the metabolism of cisatracurium metabolites.L43577 In healthy male patients (n=6) given 14C-cisatracurium, 4% of the recovered dose was found in feces, and 95% was found in urine, mostly as conjugated metabolites. Less than 10% of the cisatracurium dose was excreted as the unchanged patent drug. In another group of patients with Foley catheters for surgical management given non-radiolabeled cisatracurium (n=12), 15% of the cisatracurium dose was excreted unchanged in urine.L43577

Interaksi Obat

1376 Data
Buprenorphine Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Cisatracurium.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Cisatracurium.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Cisatracurium.
Hydrocodone Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Cisatracurium.
Magnesium sulfate The therapeutic efficacy of Cisatracurium can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Cisatracurium may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the neuromuscular blocking activities of Cisatracurium.
Mirtazapine Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Cisatracurium.
Orphenadrine Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Cisatracurium.
Pramipexole Cisatracurium may increase the sedative activities of Pramipexole.
Ropinirole Cisatracurium may increase the sedative activities of Ropinirole.
Rotigotine Cisatracurium may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Cisatracurium.
Sodium oxybate The risk or severity of CNS depression can be increased when Cisatracurium is combined with Sodium oxybate.
Suvorexant Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Cisatracurium.
Thalidomide Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Capreomycin Capreomycin may increase the neuromuscular blocking activities of Cisatracurium.
Cyclosporine The therapeutic efficacy of Cisatracurium can be increased when used in combination with Cyclosporine.
Doxycycline Doxycycline may increase the neuromuscular blocking activities of Cisatracurium.
Lymecycline Lymecycline may increase the neuromuscular blocking activities of Cisatracurium.
Framycetin Framycetin may increase the neuromuscular blocking activities of Cisatracurium.
Clomocycline Clomocycline may increase the neuromuscular blocking activities of Cisatracurium.
Quinine The therapeutic efficacy of Cisatracurium can be increased when used in combination with Quinine.
Vancomycin Vancomycin may increase the neuromuscular blocking activities of Cisatracurium.
Tigecycline Tigecycline may increase the neuromuscular blocking activities of Cisatracurium.
Oxytetracycline Oxytetracycline may increase the neuromuscular blocking activities of Cisatracurium.
Chloroquine The therapeutic efficacy of Cisatracurium can be increased when used in combination with Chloroquine.
Demeclocycline Demeclocycline may increase the neuromuscular blocking activities of Cisatracurium.
Mecamylamine The therapeutic efficacy of Cisatracurium can be increased when used in combination with Mecamylamine.
Tobramycin Tobramycin may increase the neuromuscular blocking activities of Cisatracurium.
Tetracycline Tetracycline may increase the neuromuscular blocking activities of Cisatracurium.
Gentamicin Gentamicin may increase the neuromuscular blocking activities of Cisatracurium.
Etacrynic acid The therapeutic efficacy of Cisatracurium can be increased when used in combination with Etacrynic acid.
Quinidine Quinidine may increase the neuromuscular blocking activities of Cisatracurium.
Metacycline Metacycline may increase the neuromuscular blocking activities of Cisatracurium.
Netilmicin Netilmicin may increase the neuromuscular blocking activities of Cisatracurium.
Neomycin Neomycin may increase the neuromuscular blocking activities of Cisatracurium.
Streptomycin Streptomycin may increase the neuromuscular blocking activities of Cisatracurium.
Colistimethate The therapeutic efficacy of Cisatracurium can be increased when used in combination with Colistimethate.
Kanamycin Kanamycin may increase the neuromuscular blocking activities of Cisatracurium.
Rolitetracycline Rolitetracycline may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium oxide Magnesium oxide may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium cation The therapeutic efficacy of Cisatracurium can be increased when used in combination with Magnesium cation.
Paromomycin Paromomycin may increase the neuromuscular blocking activities of Cisatracurium.
Lincomycin Lincomycin may increase the neuromuscular blocking activities of Cisatracurium.
Ribostamycin Ribostamycin may increase the neuromuscular blocking activities of Cisatracurium.
Geneticin Geneticin may increase the neuromuscular blocking activities of Cisatracurium.
Apramycin Apramycin may increase the neuromuscular blocking activities of Cisatracurium.
Gentamicin C1a Gentamicin C1a may increase the neuromuscular blocking activities of Cisatracurium.
Neamine Neamine may increase the neuromuscular blocking activities of Cisatracurium.
Arbekacin Arbekacin may increase the neuromuscular blocking activities of Cisatracurium.
Viomycin Viomycin may increase the neuromuscular blocking activities of Cisatracurium.
Puromycin Puromycin may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium hydroxide Magnesium hydroxide may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium trisilicate The therapeutic efficacy of Cisatracurium can be increased when used in combination with Magnesium trisilicate.
Magnesium chloride Magnesium chloride may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium acetate tetrahydrate The therapeutic efficacy of Cisatracurium can be increased when used in combination with Magnesium acetate tetrahydrate.
Magnesium carbonate Magnesium carbonate may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium citrate Magnesium citrate may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium glycinate The therapeutic efficacy of Cisatracurium can be increased when used in combination with Magnesium glycinate.
Magnesium Aluminum Silicate The therapeutic efficacy of Cisatracurium can be increased when used in combination with Magnesium Aluminum Silicate.
Dihydrostreptomycin Dihydrostreptomycin may increase the neuromuscular blocking activities of Cisatracurium.
Hygromycin B Hygromycin B may increase the neuromuscular blocking activities of Cisatracurium.
Sisomicin Sisomicin may increase the neuromuscular blocking activities of Cisatracurium.
Plazomicin Plazomicin may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium silicate The therapeutic efficacy of Cisatracurium can be increased when used in combination with Magnesium silicate.
Penimepicycline Penimepicycline may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium aspartate Magnesium aspartate may increase the neuromuscular blocking activities of Cisatracurium.
Isepamicin Isepamicin may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium gluconate Magnesium gluconate may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium orotate Magnesium orotate may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium phosphate The therapeutic efficacy of Cisatracurium can be increased when used in combination with Magnesium phosphate.
Magnesium acetate The therapeutic efficacy of Cisatracurium can be increased when used in combination with Magnesium acetate.
Procainamide Procainamide may increase the neuromuscular blocking activities of Cisatracurium.
Dantrolene The therapeutic efficacy of Cisatracurium can be increased when used in combination with Dantrolene.
Piperacillin Piperacillin may increase the neuromuscular blocking activities of Cisatracurium.
Magnesium stearate The therapeutic efficacy of Cisatracurium can be increased when used in combination with Magnesium stearate.
Colistin Colistin may increase the neuromuscular blocking activities of Cisatracurium.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Cisatracurium.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Cisatracurium.
Spironolactone Spironolactone may increase the neuromuscular blocking activities of Cisatracurium.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Cisatracurium is combined with Botulinum toxin type A.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Cisatracurium is combined with Botulinum toxin type B.
Ethanol Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Cisatracurium.
Fluvoxamine The risk or severity of adverse effects can be increased when Cisatracurium is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Cisatracurium is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Cisatracurium is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Cisatracurium is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Cisatracurium is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Cisatracurium is combined with Sertraline.

Target Protein

Neuronal acetylcholine receptor subunit alpha-2 CHRNA2
Neuronal Acetylcholine (nACh) Receptor Subunits CHRNA10
Acetylcholine receptor subunit alpha CHRNA1
Muscarinic acetylcholine receptor M2 CHRM2

Referensi & Sumber

Synthesis reference: Arad O., et al. (2013). Process for producing cisatracurium and associated intermediates (U.S. Patent No. 2013/0041154 A1). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/c3/a4/c7/67ee80a0faa6dc/US20130041154A1.pdf
Artikel (PubMed)
  • PMID: 30969664
    Strawbridge AD, Khanna NR, Hauser JM: Cisatracurium .
  • PMID: 24721895
    Szakmany T, Woodhouse T: Use of cisatracurium in critical care: a review of the literature. Minerva Anestesiol. 2015 Apr;81(4):450-60. Epub 2014 Apr 10.
  • PMID: 9129870
    Bryson HM, Faulds D: Cisatracurium besilate. A review of its pharmacology and clinical potential in anaesthetic practice. Drugs. 1997 May;53(5):848-66. doi: 10.2165/00003495-199753050-00012.
  • PMID: 9989341
    Kisor DF, Schmith VD: Clinical pharmacokinetics of cisatracurium besilate. Clin Pharmacokinet. 1999 Jan;36(1):27-40. doi: 10.2165/00003088-199936010-00003.

Contoh Produk & Brand

Produk: 72 • International brands: 3
Produk
  • Aj-cisatracurium
    Solution • 2 mg / mL • Intravenous • Canada • Generic • Approved
  • Aj-cisatracurium
    Solution • 2 mg / mL • Intravenous • Canada • Generic • Approved
  • Cisatracurium
    Injection, solution • 2 mg/1mL • Intravenous • US • Generic • Approved
  • Cisatracurium
    Injection, solution • 2 mg/1mL • Intravenous • US • Generic • Approved
  • Cisatracurium
    Injection, solution • 10 mg/1mL • Intravenous • US • Generic • Approved
  • Cisatracurium Besylate
    Injection • 2 mg/1mL • Intravenous • US • Generic • Approved
  • Cisatracurium Besylate
    Injection • 10 mg/1mL • Intravenous • US • Generic • Approved
  • Cisatracurium Besylate
    Injection • 2 mg/1mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 72 produk.
International Brands
  • Nimbex — AbbVie
  • Nimbex Preservative Free — AbbVie
  • Nimbium — GlaxoSmithKline

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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