Tìm theo
Enflurane
Các tên gọi khác (8 ) :
  • 2-chloro-1,1,2-trifluoroethyl difluoromethyl ether
  • Alyrane
  • Efrane
  • Enflurane
  • Enflurano
  • Enfluranum
  • Ethrane
  • Methylflurether
anesthetics inhalation, anesthetics
Thuốc Gốc
Small Molecule
CAS: 13838-16-9
ATC: N01AB04
ĐG : Apothecon , http://www.apothecon.nl
CTHH: C3H2ClF5O
PTK: 184.492
An extremely stable inhalation anesthetic that allows rapid adjustments of anesthesia depth with little change in pulse or respiratory rate. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C3H2ClF5O
Phân tử khối
184.492
Monoisotopic mass
183.971433418
InChI
InChI=1S/C3H2ClF5O/c4-1(5)3(8,9)10-2(6)7/h1-2H
InChI Key
InChIKey=JPGQOUSTVILISH-UHFFFAOYSA-N
IUPAC Name
2-chloro-1-(difluoromethoxy)-1,1,2-trifluoroethane
Traditional IUPAC Name
enflurane
SMILES
FC(F)OC(F)(F)C(F)Cl
Độ sôi
56.5
Độ hòa tan
5620 mg/L (at 37 °C)
logP
2.10
logS
-1.7
pKa (Strongest Basic)
-5
PSA
9.23 Å2
Refractivity
23.07 m3·mol-1
Polarizability
9.74 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
1
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
0
Bioavailability
1
Rule of Five
true
Dược Lực Học : Enflurane is an extremely stable halogenated ether inhalation anesthetic that allows rapid adjustments of anesthesia depth with little change in pulse or respiratory rate. Enflurane induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. Induction of and recovery from anesthesia with enflurane are rapid. Enflurane may provide a mild stimulus to salivation or tracheobronchial secretions. Pharyngeal and laryngeal reflexes are readily obtunded. In the cardiovascular system, enflurane is a mild negative inotrope, causing a marked decrease in systemic vascular resistance, thus leading to a decrease in mean arterial pressure. This results in a reflex tachycardia. Enflurane also decreases coronary vascular resistance and sensitizes the myocardium to circulating catecholamines. Enflurane is a strong respiratory depressant. It decreases tidal volume but may increase respiratory rate. It also causes bronchodilatationa and inhibits pulmonary macrophage activity and mucociliary activity. Enflurane principle action in the CNS is general anaesthesia with little analgesic effect. It causes increased cerebral blood flow in concentrations and may induce tonic/clonic muscle activity and epileptiform EEG traces. It also causes a marked decrease in skeletal muscle tone. Actions in the genitourinary system include a decreased renal blood flow and glomerular filtration rate and the tone of pregnant uterus is decreased.
Cơ Chế Tác Dụng : An extremely stable inhalation anesthetic that allows rapid adjustments of anesthesia depth with little change in pulse or respiratory rate. [PubChem] Enflurane induces a reduction in junctional conductance by decreasing gap junction channel opening times and increasing gap junction channel closing times. Enflurane also activates calcium dependent ATPase in the sarcoplasmic reticulum by increasing the fluidity of the lipid membrane. It also appears to bind the D subunit of ATP synthase and NADH dehydogenase. Enflurane also binds to and angonizes the GABA receptor, the large conductance Ca2+ activated potassium channel, the glycine receptor, and antagonizes the glutamate receptor receptor. These yield a decreased depolarization and therefore, tissue excitability which results in anesthesia.
Dược Động Học :
▧ Absorption :
Rapidly absorbed into the circulation via the lungs.
▧ Protein binding :
97%
▧ Metabolism :
2.4% of the dose is slowly metabolized hepatically via oxidation and dehalogenation (primarily through the actions of cytochrome P450 2E1). Leads to low levels of serum fluoride (15 µmol/L).
Độc Tính : LD50=5.4 ml/kg (oral, rat). Symptoms of acute overdose include nausea, vomiting, irritation to the eyes, skin and nose/throat, headache, dizziness, and drowsiness. Symptoms of chronic overdose include hypotension, cardiac arrhythmias, respiratory depression, and liver/kidney dysfunction.
Chỉ Định : Used for the induction and maintenance of general anaesthesia during surgery and cesarean section and also used for analgesia during vaginal delivery.
Tương Tác Thuốc :
  • Labetalol Monitor arterial pressure closely
  • Rotigotine Risk of sedation may increase with concomitant therapy. Monitor therapy closely.
Liều Lượng & Cách Dùng : Liquid - Respiratory (inhalation)
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Ethrane inhalation
    Giá bán buôn : USD >0.55
    Đơn vị tính : ml
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00228
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3226
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505314
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07516
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00543
ChemSpider
http://www.chemspider.com/Chemical-Structure.3113.html
PharmGKB
http://www.pharmgkb.org/drug/PA449461
Wikipedia
http://en.wikipedia.org/wiki/Enflurane
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