Tìm theo
Edrophonium
Các tên gọi khác (8 ) :
  • (3-Hydroxyphenyl)dimethylethylammonium
  • 3-hydroxy-N,N-dimethyl-N-ethylanilinium
  • EDR
  • Edrophonium
  • Edrophonium Ion
  • Ethyl-(3-hydroxy-phenyl)-dimethyl-ammonium
  • N-ethyl-3-hydroxy-N,N-dimethylanilinium
  • N-ethyl-3-hydroxy-N,N-dimethylbenzenaminium
cholinesterase inhibitors, antidotes
Thuốc Gốc
Small Molecule
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C10H16NO
PTK: 166.2401
A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H16NO
Phân tử khối
166.2401
Monoisotopic mass
166.123189139
InChI
InChI=1S/C10H15NO/c1-4-11(2,3)9-6-5-7-10(12)8-9/h5-8H,4H2,1-3H3/p+1
InChI Key
InChIKey=VWLHWLSRQJQWRG-UHFFFAOYSA-O
IUPAC Name
N-ethyl-3-hydroxy-N,N-dimethylanilinium
Traditional IUPAC Name
edrophonium
SMILES
CC[N+](C)(C)C1=CC(O)=CC=C1
Độ tan chảy
162-163
Độ hòa tan
Appreciable as liquid hydrochloride salt
logP
-2.95
logS
-3.6
pKa (strongest acidic)
8.59
pKa (Strongest Basic)
-6.1
PSA
20.23 Å2
Refractivity
62.41 m3·mol-1
Polarizability
19.15 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
1
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Edrophonium is a short and rapid-acting anticholinesterase drug. Its effect is manifest within 30 to 60 seconds after injection and lasts an average of 10 minutes. Edrophonium's pharmacologic action is due primarily to the inhibition or inactivation of acetylcholinesterase at sites of cholinergic transmission. Nicotinic acetylcholine (nAChR)receptors are found throughout the body, especially on muscle. Stimulation of these receptors causes to muscle contraction. In myasthenia gravis the body's immune system destroys many of the nicotinic acetylcholine receptors, so that the muscle becomes less responsive to nervous stimulation. Edrophonium chloride increases the amount of acetylcholine at the nerve endings. Increased levels of acetylcholine allow the remaining receptors to function more efficiently.
Cơ Chế Tác Dụng : A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles. [PubChem] Edrophonium works by prolonging the action acetylcholine, which is found naturally in the body. It does this by inhibiting the action of the enzyme acetylcholinesterase. Acetylcholine stimulates nicotinic and muscarinic receptors. When stimulated, these receptors have a range of effects.
Dược Động Học :
▧ Absorption :
Rapidly absorbed.
▧ Volume of Distribution :
* 1.6±0.4 L/kg [Adults] * 2.2±1.5 L/kg [Children (0.08-10 yrs)] * 1.8±1.2 L/kg [Elderly (65-75 yrs)]
▧ Route of Elimination :
Edrophonium is primarily renally excreted with 67% of the dose appearing in the urine. Hepatic metabolism and biliary excretion have also been demonstrated in animals
▧ Half Life :
Distribution half-life is 7 to 12 minutes. Elimination half-life is 33 to 110 minutes.
▧ Clearance :
* 6.8 +/- 2. mL/kg/min [Adults] * 6.4 +/- 3.9 mL/kg/min [Children (0.08-10 yrs)] * 2.9 +/- 1.9 mL/kg/min [Elderly (65-75 yrs)]
Độc Tính : With drugs of this type, muscarine-like symptoms (nausea, vomiting, diarrhea, sweating, increased bronchial and salivary secretions and bradycardia) often appear with overdosage (cholinergic crisis).
Chỉ Định : For the differential diagnosis of myasthenia gravis and as an adjunct in the evaluation of treatment requirements in this disease. It may also be used for evaluating emergency treatment in myasthenic crises.
Tương Tác Thuốc :
  • Betamethasone The corticosteroid, betamethasone, may decrease the effect of the anticholinesterase, edrophonium.
  • Dexamethasone The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, edrophonium.
  • Fludrocortisone The corticosteroid, fludrocortisone, may decrease the effect of the anticholinesterase, edrophonium.
  • Hydrocortisone The corticosteroid, hydrocortisone, may decrease the effect of the anticholinesterase, edrophonium.
  • Prednisolone The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, edrophonium.
  • Prednisone The corticosteroid, prednisone, may decrease the effect of the anticholinesterase, edrophonium.
  • Tacrine The acetylcholinesterase inhibitor, Tacrine, may increase the adverse/toxic effects of Edrophonium, a cholinergic agonist. Monitor for increased cholinergic effects and toxicity.
  • Triamcinolone The corticosteroid, triamcinolone, may decrease the effect of the anticholinesterase, edrophonium.
Liều Lượng & Cách Dùng : Liquid - Intramuscular
Liquid - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Enlon-plus ampul
    Giá bán buôn : USD >1.87
    Đơn vị tính : ml
  • Biệt dược thương mại : Enlon-plus multi-dose vial
    Giá bán buôn : USD >1.92
    Đơn vị tính : ml
  • Biệt dược thương mại : Enlon 10 mg/ml vial
    Giá bán buôn : USD >0.69
    Đơn vị tính : ml
Nhà Sản Xuất
  • Công ty : Kyorin
    Sản phẩm biệt dược : Antirex
  • Công ty :
    Sản phẩm biệt dược : Enlon
  • Công ty :
    Sản phẩm biệt dược : Enlon Plus
  • Công ty :
    Sản phẩm biệt dược : Reversol
  • Công ty : Roche
    Sản phẩm biệt dược : Tensilon
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01010
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3202
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507530
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06976
ChemSpider
http://www.chemspider.com/Chemical-Structure.3090.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/10019-873-15
PharmGKB
http://www.pharmgkb.org/drug/PA449437
Wikipedia
http://en.wikipedia.org/wiki/Edrophonium
RxList
http://www.rxlist.com/cgi/generic3/edrophonium.htm
Drugs.com
http://www.drugs.com/mtm/edrophonium.html
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