Tìm theo
Doxacurium chloride
Các tên gọi khác (1) :
  • Doxacurium
Thuốc Gốc
Small Molecule
CAS: 106819-53-8
ATC: M03AC07
CTHH: C56H78N2O16
PTK: 1035.2223
Doxacurium chloride is a long-acting, nondepolarizing skeletal muscle relaxant for intravenous administration.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C56H78N2O16
Phân tử khối
1035.2223
Monoisotopic mass
1034.535134458
InChI
InChI=1S/C56H78N2O16/c1-57(23-19-37-33-45(65-7)53(69-11)55(71-13)49(37)39(57)27-35-29-41(61-3)51(67-9)42(30-35)62-4)21-15-25-73-47(59)17-18-48(60)74-26-16-22-58(2)24-20-38-34-46(66-8)54(70-12)56(72-14)50(38)40(58)28-36-31-43(63-5)52(68-10)44(32-36)64-6/h29-34,39-40H,15-28H2,1-14H3/q+2
InChI Key
InChIKey=GBLRQXKSCRCLBZ-UHFFFAOYSA-N
IUPAC Name
6,7,8-trimethoxy-2-methyl-2-(3-{[4-oxo-4-(3-{6,7,8-trimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinolin-2-ium-2-yl}propoxy)butanoyl]oxy}propyl)-1-[(3,4,5-trimethoxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinolin-2-ium
Traditional IUPAC Name
6,7,8-trimethoxy-2-methyl-2-(3-{[4-oxo-4-(3-{6,7,8-trimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]-3,4-dihydro-1H-isoquinolin-2-ium-2-yl}propoxy)butanoyl]oxy}propyl)-1-[(3,4,5-trimethoxyphenyl)methyl]-3,4-dihydro-1H-isoquinolin-2-ium
SMILES
COC1=CC(CC2C3=C(CC[N+]2(C)CCCOC(=O)CCC(=O)OCCC[N+]2(C)CCC4=C(C2CC2=CC(OC)=C(OC)C(OC)=C2)C(OC)=C(OC)C(OC)=C4)C=C(OC)C(OC)=C3OC)=CC(OC)=C1OC
Độ hòa tan
9.02e-05 g/l
logP
-2.5
logS
-7.1
pKa (strongest acidic)
18.41
pKa (Strongest Basic)
-4.1
PSA
163.36 Å2
Refractivity
302.15 m3·mol-1
Polarizability
113.06 Å3
Rotatable Bond Count
29
H Bond Acceptor Count
14
H Bond Donor Count
0
Physiological Charge
2
Number of Rings
6
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Doxacurium chloride is a long-acting, nondepolarizing skeletal muscle relaxant. The neuromuscular block produced by doxacurium chloride may be antagonized by anticholinesterase agents. As with other nondepolarizing neuromuscular blocking agents, the more profound the neuromuscular block at reversal, the longer the time and the greater the dose of anticholinesterase required for recovery of neuromuscular function. Doxacurium chloride is approximately 2.5 to 3 times more potent than pancuronium and 10 to 12 times more potent than metocurine.
Cơ Chế Tác Dụng : Doxacurium chloride is a long-acting, nondepolarizing skeletal muscle relaxant for intravenous administration. Doxacurium chloride binds competitively to cholinergic receptors on the motor end-plate to antagonize the action of acetylcholine, resulting in a block of neuromuscular transmission (non-depolarizing). This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine.
Dược Động Học :

▧ Volume of Distribution :
* 0.11-0.43 L/kg [Healthy Young Adult Patients] * 0.17-0.55 L/kg [Kidney Transplant Patients] * 0.17-0.35 L/kg [Liver Transplant Patients]
▧ Protein binding :
Approximately 30%.
▧ Metabolism :
In vivo data from humans suggest that doxacurium chloride is not metabolized and that the major elimination pathway is excretion of unchanged drug in urine and bile.
▧ Route of Elimination :
In vivo data from humans suggest that NUROMAX is not metabolized and that the major elimination pathway is excretion of unchanged drug in urine and bile.
▧ Half Life :
99 minutes in normal healthy adults.
▧ Clearance :
* 2.66 mL/min/kg [Healthy Young Adult Patients] * 1.23 mL/min/kg [Kidney Transplant Patients] * 2.3 mL/min/kg [Liver Transplant Patients] * 1.75 +/- 0.16 mL/min/kg [Elderly patients (70-83 yrs)] * 2.54 +/- 0.24 mL/min/kg [younger patients (19-39 yrs)]
Độc Tính : Overdosage with neuromuscular blocking agents may result in neuromuscular block beyond the time needed for surgery and anesthesia.
Chỉ Định : Used to provide skeletal muscle relaxation as an adjunct to general anesthesia, for endotracheal intubation or to facilitate mechanical ventilation.
Tương Tác Thuốc :
  • Amikacin The agent increases the effect of muscle relaxant
  • Aminophylline Theophylline decreases the effect of muscle relaxant
  • Azathioprine The agent decreases the effect of the muscle relaxant
  • Carbamazepine Decreases the effect of muscle relaxant
  • Clindamycin The agent increases the effect of muscle relaxant
  • Fosphenytoin Phenytoin decreases the effect of muscle relaxant
  • Gentamicin The agent increases the effect of muscle relaxant
  • Lincomycin The agent increases the effect of muscle relaxant
  • Mercaptopurine The agent dereases the effect of the muscle relaxant
  • Netilmicin The agent increases the effect of muscle relaxant
  • Oxtriphylline Theophylline decreases the effect of muscle relaxant
  • Phenytoin Phenytoin decreases the effect of the muscle relaxant
  • Piperacillin The agent increases the effect of the muscle relaxant
  • Theophylline Theophylline decreases the effect of the muscle relaxant
  • Tobramycin The agent increases the effect of the muscle relaxant
Liều Lượng & Cách Dùng : Liquid - Intravenous
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Nuromax
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01135
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60169
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506733
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07549
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00760
ChemSpider
http://www.chemspider.com/Chemical-Structure.54249.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0074-4437-05
PharmGKB
http://www.pharmgkb.org/drug/PA164744927
Wikipedia
http://en.wikipedia.org/wiki/Doxacurium_chloride
RxList
http://www.rxlist.com/cgi/generic3/doxacur.htm
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