Tìm theo
Alfentanil
Các tên gọi khác (3) :
  • Alfentanilum
  • Alfentanyl
  • N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide
anesthetics intravenous, analgesics opioid, narcotics
Thuốc Gốc
Small Molecule
CAS: 71195-58-9
ATC: N01AH02
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C21H32N6O3
PTK: 416.5172
A short-acting opioid anesthetic and analgesic derivative of fentanyl. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H32N6O3
Phân tử khối
416.5172
Monoisotopic mass
416.25358892
InChI
InChI=1S/C21H32N6O3/c1-4-19(28)27(18-9-7-6-8-10-18)21(17-30-3)11-13-24(14-12-21)15-16-26-20(29)25(5-2)22-23-26/h6-10H,4-5,11-17H2,1-3H3
InChI Key
InChIKey=IDBPHNDTYPBSNI-UHFFFAOYSA-N
IUPAC Name
N-{1-[2-(4-ethyl-5-oxo-4,5-dihydro-1H-1,2,3,4-tetrazol-1-yl)ethyl]-4-(methoxymethyl)piperidin-4-yl}-N-phenylpropanamide
Traditional IUPAC Name
alfentanil
SMILES
CCN1N=NN(CCN2CCC(COC)(CC2)N(C(=O)CC)C2=CC=CC=C2)C1=O
Độ tan chảy
140.8
Độ hòa tan
34.6 mg/L
logP
2.16
logS
-3.2
pKa (Strongest Basic)
7.5
PSA
81.05 Å2
Refractivity
118.59 m3·mol-1
Polarizability
45.57 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
6
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 : Alfentanil is a synthetic opioid analgesic. Alfentanil 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, alfentanil exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Alfentanil 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. Alfentanil depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
Cơ Chế Tác Dụng : A short-acting opioid anesthetic and analgesic derivative of fentanyl. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients. [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. Alfentanil's analgesic activity is, most likely, due to its conversion to morphine. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Dược Động Học :
▧ Absorption :
For intravenous injection or infusion only.
▧ Volume of Distribution :
* 0.4 to 1 L/kg
▧ Protein binding :
92%
▧ Metabolism :
The liver is the major site of biotransformation.
▧ Route of Elimination :
Only 1.0% of the dose is excreted as unchanged drug; urinary excretion is the major route of elimination of metabolites.
▧ Half Life :
90-111 minutes
▧ Clearance :
* 5 mL/kg/min
Độc Tính : Symptoms of overexposure include characteristic rigidity of the skeletal muscles, cardiac and respiratory depression, and narrowing of the pupils.
Chỉ Định : For the management of postoperative pain and the maintenance of general anesthesia.
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
  • Erythromycin The macrolide, erythromycin, may increase the effect and toxicity of alfentanil.
  • Fluconazole Increases the effect and toxicity of alfentanil
  • Itraconazole Itraconazole may increase the effect and toxicity of alfentanil.
  • Ketoconazole Ketoconazole may increase the effect and toxicity of alfentanil.
  • Rifampicin Rifampin reduces levels and efficacy of alfentanil
  • Telithromycin Telithromycin may reduce clearance of Alfentanil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Alfentanil if Telithromycin is initiated, discontinued or dose changed.
  • Tranylcypromine Possible increased risk of serotonin syndrome.
  • Triprolidine The CNS depressants, Triprolidine and Alfentanil, 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 alfentanil by decreasing its metabolism. Monitor for increased anesthetic and respiratory depressant effects and consider using lower alfentanil doses or alternate anesthetic.
Liều Lượng & Cách Dùng : Injection, solution - Intravenous - 0.5 mg/ml
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00802
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=51263
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505618
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08005
ChemSpider
http://www.chemspider.com/Chemical-Structure.46451.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50008979
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/17478-067-02
PharmGKB
http://www.pharmgkb.org/drug/PA448084
Wikipedia
http://en.wikipedia.org/wiki/Alfentanil
RxList
http://www.rxlist.com/cgi/generic2/alfent.htm
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