Tìm theo
Rocuronium
Các tên gọi khác (2) :
  • Rocuronium
  • SID50112687
Thuốc giãn cơ và tăng trương lực cơ
Thuốc Gốc
Small Molecule
CAS: 143558-00-3
ATC: M03AC09
ĐG : Baxter International Inc. , http://www.baxter.com
CTHH: C32H53N2O4
PTK: 529.7742
Rocuronium (rapid onset-curonium) is a desacetoxy analogue of vecuronium with a more rapid onset of action. It is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Introduced in 1994, rocuronium has rapid onset, and intermediate duration of action. It is marketed under the trade name of Zemuron in the United States and Esmeron in most other countries. There is considered to be a risk of allergic reaction to the drug in some patients (particularly those with asthma), but a similar incidence of allergic reactions has been observed by using other members of the same drug class (non-depolarizing neuromuscular blocking drugs). The γ-cyclodextrin derivative sugammadex (trade name Bridion) has been recently introduced as a novel agent to reverse the action of rocuronium.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C32H53N2O4
Phân tử khối
529.7742
Monoisotopic mass
529.400533194
InChI
InChI=1S/C32H53N2O4/c1-5-14-34(15-6-7-16-34)28-20-26-24-9-8-23-19-29(36)27(33-12-17-37-18-13-33)21-32(23,4)25(24)10-11-31(26,3)30(28)38-22(2)35/h5,23-30,36H,1,6-21H2,2-4H3/q+1/t23-,24+,25-,26-,27-,28-,29-,30-,31-,32-/m0/s1
InChI Key
InChIKey=YXRDKMPIGHSVRX-OOJCLDBCSA-N
IUPAC Name
1-[(1S,2S,4S,5S,7S,10R,11S,13S,14R,15S)-14-(acetyloxy)-5-hydroxy-2,15-dimethyl-4-(morpholin-4-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-13-yl]-1-(prop-2-en-1-yl)pyrrolidin-1-ium
Traditional IUPAC Name
rocuronium
SMILES
[H][C@@]12C[C@@H]([C@H](OC(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC[C@@]2([H])C[C@H](O)[C@H](C[C@]12C)N1CCOCC1)[N+]1(CC=C)CCCC1
Độ hòa tan
Complete
logP
-0.33
logS
-7.3
pKa (strongest acidic)
14.59
pKa (Strongest Basic)
7.96
PSA
59 Å2
Refractivity
161.65 m3·mol-1
Polarizability
62.87 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
2
Number of Rings
6
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Neuromuscular blocking agents are drugs that cause skeletal muscle relaxation primarily by causing a decreased response to the neurotransmitter acetylcholine (ACh) at the myoneural (neuromuscular) junction of skeletal muscle. At that site, ACh normally produces electrical depolarization of the postjunctional membrane of motor end-plate, which leads to conduction of muscle action potential and subsequently induces skeletal muscle contraction. Neuromuscular agents are classified as depolarizing or nondepolarizing. Rocuronium is a nondepolarizing neuromuscular blocking agent with a rapid to intermediate onset depending on dose and intermediate duration. Rocuronium, like vecuronium is longer acting in infants than in children. However, unlike vecuronium, rocuronium retains the characteristics of an intermediate-acting NMBD in infants.
Cơ Chế Tác Dụng : Rocuronium (rapid onset-curonium) is a desacetoxy analogue of vecuronium with a more rapid onset of action. It is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Introduced in 1994, rocuronium has rapid onset, and intermediate duration of action. It is marketed under the trade name of Zemuron in the United States and Esmeron in most other countries. There is considered to be a risk of allergic reaction to the drug in some patients (particularly those with asthma), but a similar incidence of allergic reactions has been observed by using other members of the same drug class (non-depolarizing neuromuscular blocking drugs). The γ-cyclodextrin derivative sugammadex (trade name Bridion) has been recently introduced as a novel agent to reverse the action of rocuronium. Rocuronium acts by competing for cholinergic receptors at the motor end-plate. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine and edrophonium. Rocuronium acts by competitively binding to nicotinic cholinergic receptors. The binding of vecuronium decreases the opportunity for acetylcholine to bind to the nicotinic receptor at the postjunctional membrane of the myoneural junction. As a result, depolarization is prevented, calcium ions are not released and muscle contraction does not occur. Evidence also suggests that nondepolarizing agents can affect ACh release. It has been hypothesized that nondepolarzing agents bind to postjunctional ("curare") receptors and may therefore interfere with the sodium and potassium flux, which is responsible for depolarization and repolarization of the membranes involved in muscle contraction.
Dược Động Học :
▧ Absorption :
Poorly absorbed from the GI tract.
▧ Volume of Distribution :
* 0.3 L/kg [3 to <12 mos] * 0.26 L/kg [1 to <3 yrs] * 0.21 L/kg [3 to <8 yrs]
▧ Protein binding :
Approximately 30% bound to human plasma proteins.
▧ Metabolism :
Rocuronium is metabolized to a less active metabolite, 17-desacetyl-rocuronium, and is eliminated primarily by the liver.
▧ Route of Elimination :
Studies of distribution, metabolism, and excretion in cats and dogs indicate that rocuronium is eliminated primarily by the liver.
▧ Half Life :
The rapid distribution half-life is 1-2 minutes and the slower distribution half-life is 14-18 minutes. Renal impairment has no net effect on half-life, however, half-life is almost doubled in patients with impaired liver function.
▧ Clearance :
* 0.25 L/kg/hr [Adults (Ages 27 to 58 years)] * 0.21 L/kg/hr [Geriatrics (>=65 yrs)] * 0.16 L/kg/hr [Normal ewnal and hepatice function] * 0.13 L/kg/hr [Renal transplant patients] * 0.13 L/kg/hr [Hepatic dysfunction patients] * 0.35 +/- 0.08 L/kg/hr [Pediatric Patients 3 to <12 mos] * 0.32 +/- 0.07 L/kg/hr [Pediatric Patients 1 to 3 yrs] * 0.44 +/- 0.16 L/kg/hr [Pediatric Patients 3 to 8 yrs]
Độc Tính : No cases of significant accidental or intentional overdose have been reported. 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 both rapid sequence and routine 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
  • Clindamycin The agent increases the effect of muscle relaxant
  • 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).
  • Gentamicin The agent increases the effect of muscle relaxant
  • Lincomycin The agent increases the effect of muscle relaxant
  • Netilmicin The agent increases the effect of muscle relaxant
  • Piperacillin The agent increases 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
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Esmeron
  • Công ty :
    Sản phẩm biệt dược : Zemuron
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00728
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=441290
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506855
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00765
ChemSpider
http://www.chemspider.com/Chemical-Structure.390053.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0781-3220-75
PharmGKB
http://www.pharmgkb.org/drug/PA164754992
Wikipedia
http://en.wikipedia.org/wiki/Rocuronium
RxList
http://www.rxlist.com/cgi/generic2/rocuronium.htm
Drugs.com
http://www.drugs.com/cdi/rocuronium.html
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