Tìm theo
Pralidoxime
Các tên gọi khác (5 ) :
  • 2-PAM
  • Pralidoxim
  • Pralidoxima
  • Pralidoxime
  • Pralidoximum
cholinesterase reactivators
Thuốc Gốc
Small Molecule
CAS: 6735-59-7
ATC: V03AB04
ĐG : Baxter International Inc. , http://www.baxter.com
CTHH: C7H9N2O
PTK: 137.1592
Pralidoxime is an antidote to organophosphate pesticides and chemicals. Organophosphates bind to the esteratic site of acetylcholinesterase, which results initially in reversible inactivation of the enzyme. If given within 24 hours,after organophosphate exposure, pralidoxime reactivates the enzyme cholinesterase by cleaving the phosphate-ester bond formed between the organophosphate and acetylcholinesterase.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C7H9N2O
Phân tử khối
137.1592
Monoisotopic mass
137.07148792
InChI
InChI=1S/C7H8N2O/c1-9-5-3-2-4-7(9)6-8-10/h2-6H,1H3/p+1
InChI Key
InChIKey=JBKPUQTUERUYQE-UHFFFAOYSA-O
IUPAC Name
2-[(1E)-(hydroxyimino)methyl]-1-methylpyridin-1-ium
Traditional IUPAC Name
pralidoxime
SMILES
C[N+]1=C(\C=N\O)C=CC=C1
Độ tan chảy
215-225 °C
Độ hòa tan
1.49e-01 g/l
logP
1.564
logS
-3.1
pKa (strongest acidic)
5.78
pKa (Strongest Basic)
-1.1
PSA
36.47 Å2
Refractivity
40.33 m3·mol-1
Polarizability
14.44 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Pralidoxime is to reactivate cholinesterase (mainly outside of the central nervous system) which has been inactivated by phosphorylation due to an organophosphate pesticide or related compound. The destruction of accumulated acetylcholine can then proceed, and neuromuscular junctions will again function normally. Pralidoxime also slows the process of "aging" of phosphorylated cholinesterase to a nonreactivatable form, and detoxifies certain organophosphates by direct chemical reaction. The drug has its most critical effect in relieving paralysis of the muscles of respiration. Because pralidoxime is less effective in relieving depression of the respiratory center, atropine is always required concomitantly to block the effect of accumulated acetylcholine at this site. Pralidoxime relieves muscarinic signs and symptoms, salivation, bronchospasm, etc., but this action is relatively unimportant since atropine is adequate for this purpose.
Cơ Chế Tác Dụng : Pralidoxime is an antidote to organophosphate pesticides and chemicals. Organophosphates bind to the esteratic site of acetylcholinesterase, which results initially in reversible inactivation of the enzyme. If given within 24 hours,after organophosphate exposure, pralidoxime reactivates the enzyme cholinesterase by cleaving the phosphate-ester bond formed between the organophosphate and acetylcholinesterase. Pralidoxime is an antidote to organophosphate pesticides and chemicals. Organophosphates bind to the esteratic site of acetylcholinesterase, which results initially in reversible inactivation of the enzyme. Acetylcholinesterase inhibition causes acetylcholine to accumulate in synapses, producing continuous stimulation of cholinergic fibers throughout the nervous systems. If given within 24 hours after organophosphate exposure, pralidoxime reactivates the acetylcholinesterase by cleaving the phosphate-ester bond formed between the organophosphate and acetylcholinesterase.
Dược Động Học :

▧ Protein binding :
No binding to plasma proteins
▧ Metabolism :
Hepatic
▧ Route of Elimination :
The drug is rapidly excreted in the urine partly unchanged, and partly as a metabolite produced by the liver.
▧ Half Life :
74-77 minutes
Chỉ Định : For the treatment of poisoning due to those pesticides and chemicals of the organophosphate class which have anticholinesterase activity and in the control of overdosage by anticholinesterase drugs used in the treatment of myasthenia gravis.
Liều Lượng & Cách Dùng : Powder, for solution - Intramuscular
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : ComboPen
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Contrathion
  • Công ty : Neiss
    Sản phẩm biệt dược : Nispam
  • Công ty : Oriental
    Sản phẩm biệt dược : Pamcl
  • Công ty : Siu Guan
    Sản phẩm biệt dược : Pampara
  • Công ty : Choong Wae
    Sản phẩm biệt dược : Pamu
  • Công ty : Meridian
    Sản phẩm biệt dược : Pralidoxime Chloride
  • Sản phẩm biệt dược : Protopam
  • Công ty : Baxter
    Sản phẩm biệt dược : Protopam Chloride
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00733
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07400
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50241085
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/60977-141-01
PharmGKB
http://www.pharmgkb.org/drug/PA164744926
Wikipedia
http://en.wikipedia.org/wiki/Pralidoxime
RxList
http://www.rxlist.com/cgi/generic2/pralidoxime.htm
Drugs.com
http://www.drugs.com/mtm/pralidoxime-injection.html
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