Tìm theo
Mivacurium
Các tên gọi khác (2) :
  • Mivacurium
  • SID50112723
Thuốc Gốc
Small Molecule
CAS: 106791-40-6
ATC: M03AC10
CTHH: C58H80N2O14
PTK: 1029.2608
Mivacurium is a bisbenzylisoquinolinium based neuromuscular blocker or muscle relaxant. It binds competitively to cholinergic receptors on the motor end-plate to antagonize the action of acetylcholine, resulting in a block of neuromuscular transmission.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C58H80N2O14
Phân tử khối
1029.2608
Monoisotopic mass
1028.560955278
InChI
InChI=1S/C58H80N2O14/c1-59(25-21-41-35-47(63-3)49(65-5)37-43(41)45(59)29-39-31-51(67-7)57(71-11)52(32-39)68-8)23-17-27-73-55(61)19-15-13-14-16-20-56(62)74-28-18-24-60(2)26-22-42-36-48(64-4)50(66-6)38-44(42)46(60)30-40-33-53(69-9)58(72-12)54(34-40)70-10/h13-14,31-38,45-46H,15-30H2,1-12H3/q+2/b14-13+/t45-,46-,59?,60?/m1/s1
InChI Key
InChIKey=ILVYCEVXHALBSC-OTBYEXOQSA-N
IUPAC Name
(1R)-2-(3-{[(4E)-8-{3-[(1R)-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinolin-2-ium-2-yl]propoxy}-8-oxooct-4-enoyl]oxy}propyl)-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinolin-2-ium
Traditional IUPAC Name
(1R)-2-(3-{[(4E)-8-{3-[(1R)-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]-3,4-dihydro-1H-isoquinolin-2-ium-2-yl]propoxy}-8-oxooct-4-enoyl]oxy}propyl)-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]-3,4-dihydro-1H-isoquinolin-2-ium
SMILES
COC1=CC(C[C@@H]2C3=CC(OC)=C(OC)C=C3CC[N+]2(C)CCCOC(=O)CC\C=C\CCC(=O)OCCC[N+]2(C)CCC3=CC(OC)=C(OC)C=C3[C@H]2CC2=CC(OC)=C(OC)C(OC)=C2)=CC(OC)=C1OC
Độ hòa tan
3.26e-05 g/l
logP
-0.76
logS
-7.5
pKa (strongest acidic)
18.59
pKa (Strongest Basic)
-4.1
PSA
144.9 Å2
Refractivity
308.74 m3·mol-1
Polarizability
116.68 Å3
Rotatable Bond Count
30
H Bond Acceptor Count
12
H Bond Donor Count
0
Physiological Charge
2
Number of Rings
6
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Mivacurium is a short-acting, nondepolarizing skeletal neuromuscular blocking agent which is hydrolyzed by plasma cholinesterase. Mivacurium results in a blockade of neuromuscular transmission by binding competitively with cholinergic receptors on the motor end-plate to antagonize the action of acetylcholine. The neuromuscular block produced by mivacurium is readily antagonized by anticholinesterase agents. The deeper the level of neuromuscular block at reversal, the longer the time required for recovery of neuromuscular function and the greater the dose of anticholinesterase agent required. Because spontaneous recovery after mivacurium is rapid, routine reversal may not always result in a clinical benefit.
Cơ Chế Tác Dụng : Mivacurium is a bisbenzylisoquinolinium based neuromuscular blocker or muscle relaxant. It binds competitively to cholinergic receptors on the motor end-plate to antagonize the action of acetylcholine, resulting in a block of neuromuscular transmission. Mivacurium binds competitively to cholinergic receptors on the motor end-plate to antagonize the action of acetylcholine, resulting in a block of neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine.
Dược Động Học :

▧ Protein binding :
The protein binding of mivacurium has not been determined due to its rapid hydrolysis by plasma cholinesterase.
▧ Metabolism :
Extensive and rapid via enzymatic hydrolysis catalyzed by plasma cholinesterase. Biotransformation may be significantly slowed in patients with abnormal or decreased plasma cholinesterase activity, especially individuals with a homozygous atypical cholinesterase gene abnormality.
▧ Half Life :
The mean elimination half-life ranges from 1.7 to 2.6 minutes in healthy, young adults administered 0.1 to 0.25 mg/kg mivacurium. In 9 patients with end-stage liver disease undergoing liver transplant surgery, plasma clearance was approximately 50% lower than that in 8 control patients with normal hepatic function, while the elimination half-life increased to 4.4 minutes from the 1.8 minute control value.
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.
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 Decrease 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 : Mivacron
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01226
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5281042
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505071
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07550
ChemSpider
http://www.chemspider.com/Chemical-Structure.4444509.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0409-4375-20
PharmGKB
http://www.pharmgkb.org/drug/PA450528
Wikipedia
http://en.wikipedia.org/wiki/Mivacurium
RxList
http://www.rxlist.com/cgi/generic3/mivacur.htm
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