Tìm theo
Remifentanil
Các tên gọi khác (2) :
  • REMIFENTANIL
  • Remifentanyl
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 132875-61-7
ATC: N01AH06
ĐG : Abbott Laboratories Ltd. , http://www.abbott.com
CTHH: C20H28N2O5
PTK: 376.4467
Remifentanil (marketed by Abbott as Ultiva) is a potent ultra short-acting synthetic opioid analgesic drug. It is given to patients during surgery to relieve pain and as an adjunct to an anaesthetic. Remifentanil is a specific mu-type-opioid receptor agonist. Hence, it causes a reduction in sympathetic nervous system tone, respiratory depression and analgesia.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H28N2O5
Phân tử khối
376.4467
Monoisotopic mass
376.199822016
InChI
InChI=1S/C20H28N2O5/c1-4-17(23)22(16-8-6-5-7-9-16)20(19(25)27-3)11-14-21(15-12-20)13-10-18(24)26-2/h5-9H,4,10-15H2,1-3H3
InChI Key
InChIKey=ZTVQQQVZCWLTDF-UHFFFAOYSA-N
IUPAC Name
methyl 1-(3-methoxy-3-oxopropyl)-4-(N-phenylpropanamido)piperidine-4-carboxylate
Traditional IUPAC Name
remifentanil
SMILES
CCC(=O)N(C1=CC=CC=C1)C1(CCN(CCC(=O)OC)CC1)C(=O)OC
Độ hòa tan
5.91e-01 g/l
logP
1.4
logS
-2.8
pKa (Strongest Basic)
7.51
PSA
76.15 Å2
Refractivity
100.56 m3·mol-1
Polarizability
40.82 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Remifentanil is an opioid agonist with rapid onset and peak effect and ultra-short duration of action. The opioid activity of remifentanil is antagonized by opioid antagonists such as naloxone. The analgesic effects of remifentanil are rapid in onset and offset. Its effects and side effects are dose dependent and similar to other opioids. Remifentanil in humans has a rapid blood-brain equilibration half-time of 1 ± 1 minutes (mean ± SD) and a rapid onset of action.
Cơ Chế Tác Dụng : Remifentanil (marketed by Abbott as Ultiva) is a potent ultra short-acting synthetic opioid analgesic drug. It is given to patients during surgery to relieve pain and as an adjunct to an anaesthetic. Remifentanil is a specific mu-type-opioid receptor agonist. Hence, it causes a reduction in sympathetic nervous system tone, respiratory depression and analgesia. Remifentanil is a µ-opioid agonist with rapid onset and peak effect, and short duration of action. The µ-opioid activity of remifentanil is antagonized by opioid antagonists such as naloxone.
Dược Động Học :

▧ Volume of Distribution :
* 350 mL/kg * 452 ± 144 mL/kg [neonates] * 223 ± 30.6 mL/kg [adolescents]
▧ Protein binding :
70% (bound to plasma proteins)
▧ Metabolism :
By hydrolysis of the propanoic acid-methyl ester linkage by nonspecific blood and tissue esterases.
▧ Route of Elimination :
Remifentanil is an esterase-metabolized opioid. The carboxylic acid metabolite is essentially inactive (1/4600 as potent as remifentanil in dogs) and is excreted by the kidneys with an elimination half-life of approximately 90 minutes.
▧ Half Life :
1-20 minutes
▧ Clearance :
* 40 mL/min/kg [young, healthy adults]
Chỉ Định : For use during the induction and maintenance of general anesthesia.
Tương Tác Thuốc :
  • Tranylcypromine Possible increased risk of serotonin syndrome.
  • Triprolidine The CNS depressants, Triprolidine and Remifentanil, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Powder, for solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Ultiva 1 mg vial
    Giá bán buôn : USD >30.19
    Đơn vị tính : vial
  • Biệt dược thương mại : Ultiva 2 mg vial
    Giá bán buôn : USD >57.2
    Đơn vị tính : vial
  • Biệt dược thương mại : Ultiva 5 mg vial
    Giá bán buôn : USD >118.15
    Đơn vị tính : vial
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00899
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60815
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504538
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08021
ChemSpider
http://www.chemspider.com/Chemical-Structure.54803.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50012491
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/67457-198-03
PharmGKB
http://www.pharmgkb.org/drug/PA451232
Wikipedia
http://en.wikipedia.org/wiki/Remifentanil
RxList
http://www.rxlist.com/cgi/generic2/ultiva.htm
Drugs.com
http://www.drugs.com/cdi/remifentanil.html
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