Tìm theo
Ephedrine
Các tên gọi khác (6 ) :
  • (-)-Ephedrine
  • (1R,2S)-1-Phenyl-1-hydroxy-2-methylaminopropane
  • Ephedrine
  • L-Ephedrine
  • L-erythro-2-(Methylamino)-1-phenylpropan-1-ol
  • L(-)-Ephedrine
Thuốc tác dụng trên đường hô hấp
Thuốc Gốc
Small Molecule
CAS: 299-42-3
ATC: C01CA26, S01FB02, R03CA02, R01AB05, R01AA03
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C10H15NO
PTK: 165.2322
An alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used in the treatment of several disorders including asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H15NO
Phân tử khối
165.2322
Monoisotopic mass
165.115364107
InChI
InChI=1S/C10H15NO/c1-8(11-2)10(12)9-6-4-3-5-7-9/h3-8,10-12H,1-2H3/t8-,10-/m0/s1
InChI Key
InChIKey=KWGRBVOPPLSCSI-WPRPVWTQSA-N
IUPAC Name
(1R,2S)-2-(methylamino)-1-phenylpropan-1-ol
Traditional IUPAC Name
ephedrine
SMILES
CN[C@@H](C)[C@H](O)C1=CC=CC=C1
Độ tan chảy
34 °C
Độ sôi
255 °C
Độ hòa tan
6.36E+004 mg/L (at 30 °C)
logP
1.13
logS
-1.3
pKa (strongest acidic)
13.89
pKa (Strongest Basic)
9.52
PSA
32.26 Å2
Refractivity
49.69 m3·mol-1
Polarizability
18.8 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
10.3 (at 0 °C)
Dược Lực Học : Ephedrine is similar in structure to the derivatives amphetamine and methamphetamine. Chemically, it is an alkaloid derived from various plants in the genus Ephedra (family Ephedraceae). It works mainly by increasing the activity of noradrenaline on adrenergic receptors.
Cơ Chế Tác Dụng : An alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used in the treatment of several disorders including asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists. [PubChem] Ephedrine is a sympathomimetic amine - that is, its principal mechanism of action relies on its direct and indirect actions on the adrenergic receptor system, which is part of the sympathetic nervous system. Ephedrine increases post-synaptic noradrenergic receptor activity by (weakly) directly activating post-synaptic α-receptors and β-receptors, but the bulk of its effect comes from the pre-synaptic neuron being unable to distinguish between real adrenaline or noradrenaline from ephedrine. The ephedrine, mixed with noradrenaline, is transported through the noradrenaline reuptake complex and packaged (along with real noradrenaline) into vesicles that reside at the terminal button of a nerve cell. Ephedrine's action as an agonist at most major noradrenaline receptors and its ability to increase the release of both dopamine and to a lesser extent, serotonin by the same mechanism is presumed to have a major role in its mechanism of action.
Dược Động Học :
▧ Absorption :
85%
▧ Route of Elimination :
mainly renal
▧ Half Life :
3-6 hours
Độc Tính : Cardiovascular: tachycardia, cardiac arrhythmias, angina pectoris, vasoconstriction with hypertension
Chỉ Định : Ephedrine commonly used as a stimulant, appetite suppressant, concentration aid, decongestant, and to treat hypotension associated with anaesthesia.
Tương Tác Thuốc :
  • Amitriptyline The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of ephedrine.
  • Amoxapine The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of ephedrine.
  • Clomipramine The tricyclic antidepressant, clomipramine, increases the sympathomimetic effect of ephedrine.
  • Desipramine The tricyclic antidepressant, desipramine, increases the sympathomimetic effect of ephedrine.
  • Desvenlafaxine Desvenlafaxine may increase the tachycardic and vasopressor effects of ephedrine. Consider alternate therapy or monitor for increased sympathomimetic effects, such as increased blood pressure, chest pain and headache.
  • Doxepin The tricyclic antidepressant, doxepin, increases the sympathomimetic effect of ephedrine.
  • Guanethidine Ephedrine may decrease the effect of guanethidine.
  • Imipramine The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of ephedrine.
  • Iobenguane Sympathomimetic that increase chances of producing a false negative imaging result
  • Isocarboxazid Increased arterial pressure
  • Linezolid Possible increase of arterial pressure
  • Methyldopa Increased arterial pressure
  • Midodrine Increased arterial pressure
  • Moclobemide Moclobemide increases the sympathomimetic effect of ephedrine.
  • Nortriptyline The tricyclic antidepressant, nortriptyline, increases the sympathomimetic effect of ephedrine.
  • Phenelzine Increased arterial pressure
  • Rasagiline Increased arterial pressure
  • Reserpine Increased arterial pressure
  • Rotigotine Risk of sedation may decrease with concomitant therapy. Monitor therapy closely.
  • Tranylcypromine The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of Ephedrine. Concomitant therapy should be avoided.
  • Venlafaxine Venlafaxine may increase the tachycardic and vasopressor effects of ephedrine. Consider alternate therapy or monitor for increased sympathomimetic effects, such as increased blood pressure, chest pain and headache.
Liều Lượng & Cách Dùng : Capsule - Oral
Liquid - Intramuscular
Liquid - Intravenous
Powder - Oral
Solution - Intramuscular
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01364
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=9294
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507538
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C01575
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00124
ChemSpider
http://www.chemspider.com/Chemical-Structure.8935.html
PharmGKB
http://www.pharmgkb.org/drug/PA449466
Wikipedia
http://en.wikipedia.org/wiki/Ephedrine
RxList
http://www.rxlist.com/cgi/generic/ephedrine.htm
Drugs.com
http://www.drugs.com/ephedrine.html
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