Tìm theo
Sufentanil
Các tên gọi khác (6 ) :
  • N-(4-(Methoxymethyl)-1-(2-(2-thienyl)ethyl)-4-piperidinyl)-N-phenylpropanamide
  • N-(4-(Methoxymethyl)-1-(2-(2-thienyl)ethyl)-4-piperidyl)propionanilide
  • Sufentanil
  • Sufentanilo
  • Sufentanilum
  • Sufentanyl
Thuốc gây mê
Thuốc Gốc
Small Molecule
CAS: 56030-54-7
ATC: N01AH03
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C22H30N2O2S
PTK: 386.551
An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H30N2O2S
Phân tử khối
386.551
Monoisotopic mass
386.202798904
InChI
InChI=1S/C22H30N2O2S/c1-3-21(25)24(19-8-5-4-6-9-19)22(18-26-2)12-15-23(16-13-22)14-11-20-10-7-17-27-20/h4-10,17H,3,11-16,18H2,1-2H3
InChI Key
InChIKey=GGCSSNBKKAUURC-UHFFFAOYSA-N
IUPAC Name
N-[4-(methoxymethyl)-1-[2-(thiophen-2-yl)ethyl]piperidin-4-yl]-N-phenylpropanamide
Traditional IUPAC Name
sufentanil
SMILES
CCC(=O)N(C1=CC=CC=C1)C1(COC)CCN(CCC2=CC=CS2)CC1
Độ tan chảy
97 °C
Độ hòa tan
76 mg/L (at 25 °C)
logP
3.95
logS
-3.71
pKa (Strongest Basic)
8.86
PSA
32.78 Å2
Refractivity
111.42 m3·mol-1
Polarizability
43.85 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Sufentanil is a synthetic opioid analgesic. Sufentanil interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissues. In clinical settings, sufentanil exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Sufentanil may increase the patient's tolerance for pain and decrease the perception of suffering, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Sufentanil depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
Cơ Chế Tác Dụng : An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent. [PubChem] Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Sufentanil's analgesic activity is, most likely, due to its conversion to morphine. Opioids open calcium-dependent inwardly rectifying potassium channels (OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Dược Động Học :

▧ Half Life :
265 minutes
Độc Tính : LD50: 18.7 mg/kg (IV in mice)
Chỉ Định : Used as an analgesic adjunct in anesthesia and as a primary anesthetic drug in procedures requiring assisted ventilation and in the relief of pain.
Tương Tác Thuốc :
  • Alvimopan Increases levels by receptor binding competition. Discontinue opioid administration at least 7 days prior to administrating Alvimopan.
  • Cimetidine Increases the effect of the narcotic
  • Telithromycin Telithromycin may reduce clearance of Sufentanil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Sufentanil if Telithromycin is initiated, discontinued or dose changed.
  • Tranylcypromine Possible increased risk of serotonin syndrome.
  • Triprolidine The CNS depressants, Triprolidine and Sufentanil, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of sufentanil by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of sufentanil if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Liquid - Intravenous
Solution - Epidural
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : DURECT
    Sản phẩm biệt dược : Chronogesic
  • Công ty : Angenerico
    Sản phẩm biệt dược : Disufen
  • Công ty : Cristália
    Sản phẩm biệt dược : Fastfen
  • Công ty : Janssen
    Sản phẩm biệt dược : Sufenta
  • Công ty : Janssen
    Sản phẩm biệt dược : Sufenta Forte
  • Công ty : Janssen
    Sản phẩm biệt dược : Sufenta mite
  • Sản phẩm biệt dược : Sufentil
  • Công ty : Pisa
    Sản phẩm biệt dược : Zuftil
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00708
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=41693
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504737
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08022
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05938
ChemSpider
http://www.chemspider.com/Chemical-Structure.38043.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50012490
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/11098-050-01
PharmGKB
http://www.pharmgkb.org/drug/PA451527
Wikipedia
http://en.wikipedia.org/wiki/Sufentanil
Drugs.com
http://www.drugs.com/cdi/sufentanil.html
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