Tìm theo
Cisatracurium Besylate
Các tên gọi khác (9 ) :
  • (1R-cis,1'R-cis)-2,2'-{pentane-1,5-diylbis[oxy(3-oxopropane-3,1-diyl)]}bis[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolinium] bisbenzenesulfonate
  • (1R-cis,1'R-cis)-atracurium besylate
  • (1R,1'R,2R,2'r)-atracurium besylate
  • Besilate de cisatracurium
  • Besilato de cisatracurio
  • Cisatracurii besilas
  • Cisatracurium besilate
  • Cisatracurium dibenzenesulfonate
  • Cisatracurium-Kation
neuromuscular blocking agents
Thuốc Gốc
Small Molecule
CAS: 96946-42-8
ATC: M03AC11
ĐG : Abbott Laboratories Ltd. , http://www.abbott.com
CTHH: C65H82N2O18S2
PTK: 1243.479
Cisatracurium Besylate is a nondepolarizing skeletal muscle relaxant for intravenous administration. Cisatracurium Besylate acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine. The neuromuscular block produced by cisatracurium besylate is readily antagonized by anticholinesterase agents once recovery has started. As with other nondepolarizing neuromuscular blocking agents, the more profound the neuromuscular block at the time of reversal, the longer the time required for recovery of neuromuscular function. Compared to other neuromuscular blocking agents, it is intermediate in its onset and duration of action.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C65H82N2O18S2
Phân tử khối
1243.479
Monoisotopic mass
1242.50040521
InChI
InChI=1S/C53H72N2O12.2C6H6O3S/c1-54(22-18-38-32-48(62-7)50(64-9)34-40(38)42(54)28-36-14-16-44(58-3)46(30-36)60-5)24-20-52(56)66-26-12-11-13-27-67-53(57)21-25-55(2)23-19-39-33-49(63-8)51(65-10)35-41(39)43(55)29-37-15-17-45(59-4)47(31-37)61-6;2*7-10(8,9)6-4-2-1-3-5-6/h14-17,30-35,42-43H,11-13,18-29H2,1-10H3;2*1-5H,(H,7,8,9)/q+2;;/p-2/t42-,43-,54-,55-;;/m1../s1
InChI Key
InChIKey=XXZSQOVSEBAPGS-DONVQRBFSA-L
IUPAC Name
(1R,2R)-1-[(3,4-dimethoxyphenyl)methyl]-2-(3-{[5-({3-[(1R,2R)-1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-2-ium-2-yl]propanoyl}oxy)pentyl]oxy}-3-oxopropyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-2-ium dibenzenesulfonate
Traditional IUPAC Name
(1R,2R)-1-[(3,4-dimethoxyphenyl)methyl]-2-(3-{[5-({3-[(1R,2R)-1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-2-ium-2-yl]propanoyl}oxy)pentyl]oxy}-3-oxopropyl)-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-2-ium dibenzenesulfonate
SMILES
[O-]S(=O)(=O)C1=CC=CC=C1.[O-]S(=O)(=O)C1=CC=CC=C1.COC1=C(OC)C=C(C[C@@H]2C3=CC(OC)=C(OC)C=C3CC[N@+]2(C)CCC(=O)OCCCCCOC(=O)CC[N@@+]2(C)CCC3=CC(OC)=C(OC)C=C3[C@H]2CC2=CC(OC)=C(OC)C=C2)C=C1
Độ hòa tan
4.17e-05 g/l
logP
-0.96
logS
-7.5
pKa (strongest acidic)
19.02
pKa (Strongest Basic)
-4.1
PSA
126.44 Å2
Refractivity
280.68 m3·mol-1
Polarizability
105.55 Å3
Rotatable Bond Count
28
H Bond Acceptor Count
10
H Bond Donor Count
0
Physiological Charge
2
Number of Rings
8
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Cisatracurium Besylate is a nondepolarizing skeletal muscle relaxant for intravenous administration. Cisatracurium Besylate acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine. The neuromuscular block produced by cisatracurium besylate is readily antagonized by anticholinesterase agents once recovery has started. As with other nondepolarizing neuromuscular blocking agents, the more profound the neuromuscular block at the time of reversal, the longer the time required for recovery of neuromuscular function. Compared to other neuromuscular blocking agents, it is intermediate in its onset and duration of action.
Cơ Chế Tác Dụng : Cisatracurium Besylate is a nondepolarizing skeletal muscle relaxant for intravenous administration. Cisatracurium Besylate acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine. The neuromuscular block produced by cisatracurium besylate is readily antagonized by anticholinesterase agents once recovery has started. As with other nondepolarizing neuromuscular blocking agents, the more profound the neuromuscular block at the time of reversal, the longer the time required for recovery of neuromuscular function. Compared to other neuromuscular blocking agents, it is intermediate in its onset and duration of action. Cisatracurium Besylate binds to the nicotinic acetycholine (cholinergic) receptors in the motor endplate and blocks access to the receptors. In the process of binding, the receptor is actually activated - causing a process known as depolarization. Since it is not degraded in the neuromuscular junction, the depolarized membrane remains depolarized and unresponsive to any other impulse, causing muscle paralysis.
Dược Động Học :

▧ Protein binding :
The binding of cisatracurium to plasma proteins has not been successfully studied due to its rapid degradation at physiologic pH.
▧ Metabolism :
The degradation of cisatracurium is largely independent of liver metabolism. Results from in vitro experiments suggest that cisatracurium undergoes Hofmann elimination (a pH and temperature-dependent chemical process) to form laudanosine and the monoquaternary acrylate metabolite. The monoquaternary acrylate undergoes hydrolysis by non-specific plasma esterases to form the monoquaternary alcohol metabolite. The monoquaternary alcohol metabolite can also undergo Hofmann elimination but at a much slower rate than cisatracurium. Laudanosine is further metabolized to desmethyl metabolites which are conjugated with glucuronic acid and excreted in the urine.
▧ Route of Elimination :
Biliary and urinary excretion were the major routes of excretion of radioactivity (totaling >90% of the labeled dose within 7 hours of dosing), of which atracurium represented only a minor fraction.
▧ Half Life :
Elimination half-life of 22 minutes.
Độc Tính : Overdosage with neuromuscular blocking agents may result in neuromuscular block beyond the time needed for surgery and anesthesia.
Chỉ Định : For inpatients and outpatients as an adjunct to general anesthesia, to facilitate tracheal intubation, and to provide skeletal muscle relaxation during surgery or mechanical ventilation in the ICU.
Tương Tác Thuốc :
  • Colistimethate Colistimethate may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. If possible, avoid concomitant use of these products. Monitor for deeper, prolonged neuromuscular-blocking effects (respiratory paralysis) in patients receiving concomitant neuromuscular-blocking agents and polymyxin antibiotics (e.g., colistimethate, polymyxin B).
Liều Lượng & Cách Dùng : Liquid - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Nimbex 2 mg/ml vial
    Giá bán buôn : USD >2.91
    Đơn vị tính : ml
  • Biệt dược thương mại : Nimbex 10 mg/ml vial
    Giá bán buôn : USD >13.8
    Đơn vị tính : ml
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00565
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=62886
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506666
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00759
ChemSpider
http://www.chemspider.com/Chemical-Structure.56614.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0074-4378-05
PharmGKB
http://www.pharmgkb.org/drug/PA164744925
RxList
http://www.rxlist.com/cgi/generic2/nimbex.htm
Drugs.com
http://www.drugs.com/cdi/cisatracurium.html
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