Tìm theo
Dexmedetomidine
Các tên gọi khác (8 ) :
  • (+)-4-((S)-alpha,2,3-Trimethylbenzyl)imidazole
  • (+)-medetomidine
  • (S)-medetomidine
  • Dexmedetomidin
  • Dexmedetomidina
  • Dexmédétomidine
  • Dexmedetomidinum
  • MPV 1440
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 113775-47-6
ATC: N05CM18
ĐG : Hospira Inc. , http://www.hospira.com
CTHH: C13H16N2
PTK: 200.2795
An agonist of receptors, adrenergic alpha-2 that is used in veterinary medicine for its analgesic and sedative properties. It is the racemate of dexmedetomidine. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H16N2
Phân tử khối
200.2795
Monoisotopic mass
200.131348522
InChI
InChI=1S/C13H16N2/c1-9-5-4-6-12(10(9)2)11(3)13-7-14-8-15-13/h4-8,11H,1-3H3,(H,14,15)/t11-/m0/s1
InChI Key
InChIKey=CUHVIMMYOGQXCV-NSHDSACASA-N
IUPAC Name
4-[(1S)-1-(2,3-dimethylphenyl)ethyl]-1H-imidazole
Traditional IUPAC Name
dexmedetomidine
SMILES
C[C@H](C1=CNC=N1)C1=C(C)C(C)=CC=C1
Độ hòa tan
Freely soluble in water
logP
2.8
logS
-3.1
pKa (strongest acidic)
14.09
pKa (Strongest Basic)
6.54
PSA
28.68 Å2
Refractivity
62.98 m3·mol-1
Polarizability
23.32 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
1
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
7.1
Dược Lực Học : Dexmedetomidine activates 2-adrenoceptors, and causes the decrease of sympathetic tone, with attenuation of the neuroendocrine and hemodynamic responses to anesthesia and surgery; it reduces anesthetic and opioid requirements; and causes sedation and analgesia.
Cơ Chế Tác Dụng : An agonist of receptors, adrenergic alpha-2 that is used in veterinary medicine for its analgesic and sedative properties. It is the racemate of dexmedetomidine. [PubChem] Dexmedetomidine is a specific and selective alpha-2 adrenoceptor agonist. By binding to the presynaptic alpha-2 adrenoceptors, it inhibits the release if norepinephrine, therefore, terminate the propagation of pain signals. Activation of the postsynaptic alpha-2 adrenoceptors inhibits the sympathetic activity decreases blood pressure and heart rate.
Dược Động Học :

▧ Volume of Distribution :
* 118 L
▧ Protein binding :
94%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
A mass balance study demonstrated that after nine days an average of 95% of the radioactivity, following intravenous administration of radiolabeled dexmedetomidine, was recovered in the urine and 4% in the feces. Fractionation of the radioactivity excreted in urine demonstrated that products of N-glucuronidation accounted for approximately 34% of the cumulative urinary excretion. The majority of metabolites are excreted in the urine.
▧ Half Life :
2 hours
▧ Clearance :
* 39 L/h [Healthy volunteers receiving IV infusion (0.2-0.7 mcg/kg/hr)]
Chỉ Định : For sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting, also used in pain relief; anxiety reduction and analgesia
Tương Tác Thuốc :
  • Tranylcypromine Tranylcypromine, a strong CYP2A6 inhibitor, may decrease the metabolism and clearance of Dexmedetomidine.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Trimipramine Trimipramine may reduce the antihypertensive effect of the alpha2-agonist, Dexmedetomidine. Trimipramine may also increase the rebound hypertensive effect of Clonidine. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Clonidine if Trimipramine is initiated, discontinued or dose changed. Dexmedetomidine should be withdrawn very gradually to reduce the risk of hypertensive crisis.
Liều Lượng & Cách Dùng : Injection, solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Orion
    Sản phẩm biệt dược : Dexdor
  • Công ty : Themis Medicare
    Sản phẩm biệt dược : Dexem
  • Công ty : Abbott
    Sản phẩm biệt dược : Precedex
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00633
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07450
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00514
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0409-1638-02
PharmGKB
http://www.pharmgkb.org/drug/PA449256
Wikipedia
http://en.wikipedia.org/wiki/Dexmedetomidine
RxList
http://www.rxlist.com/cgi/generic/precedex.htm
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