Tìm theo
Biperiden
Các tên gọi khác (7 ) :
  • 1-Bicyclo[2.2.1]hept-5-en-2-yl-1-phenyl-3-piperidin-1-yl-propan-1-ol
  • alpha-5-Norbornen-2-yl-alpha-phenyl-1-piperidinepropanol
  • alpha-Bicyclo[2.2.1]hept-5-en-2-yl-alpha-phenyl-1-piperidinepropanol
  • Beperiden
  • Biperidene
  • Biperideno
  • Biperidenum
Thuốc chống Parkinson
Thuốc Gốc
Small Molecule
CAS: 514-65-8
ATC: N04AA02
ĐG : Abbott Laboratories Ltd. , http://www.abbott.com
CTHH: C21H29NO
PTK: 311.4611
A muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H29NO
Phân tử khối
311.4611
Monoisotopic mass
311.224914555
InChI
InChI=1S/C21H29NO/c23-21(19-7-3-1-4-8-19,11-14-22-12-5-2-6-13-22)20-16-17-9-10-18(20)15-17/h1,3-4,7-10,17-18,20,23H,2,5-6,11-16H2
InChI Key
InChIKey=YSXKPIUOCJLQIE-UHFFFAOYSA-N
IUPAC Name
1-{bicyclo[2.2.1]hept-5-en-2-yl}-1-phenyl-3-(piperidin-1-yl)propan-1-ol
Traditional IUPAC Name
biperiden
SMILES
OC(CCN1CCCCC1)(C1CC2CC1C=C2)C1=CC=CC=C1
Độ tan chảy
114 °C
Độ hòa tan
25.1 mg/L
logP
4.25
logS
-4.9
pKa (strongest acidic)
13.82
pKa (Strongest Basic)
9.3
PSA
23.47 Å2
Refractivity
97.02 m3·mol-1
Polarizability
36.74 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Biperiden is a weak peripheral anticholinergic agent. It has, therefore, some antisecretory, antispasmodic and mydriatic effects. In addition, biperiden possesses nicotinolytic activity. The parenteral form of biperiden is an effective and reliable agent for the treatment of acute episodes of extrapyramidal disturbances sometimes seen during treatment with neuroleptic agents. Akathisia, akinesia, dyskinetic tremors, rigor, oculogyric crisis, spasmodic torticollis, and profuse sweating are markedly reduced or eliminated. With parenteral biperiden, these drug-induced disturbances are rapidly brought under control.
Cơ Chế Tác Dụng : A muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine. [PubChem] Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as biperiden is considered to relate to competitive antagonism of acetylcholine at cholinergic receptors in the corpus striatum, which then restores the balance.
Dược Động Học :
▧ Absorption :
87% bioavailability
▧ Protein binding :
60%
▧ Metabolism :
The metabolism of biperiden is not completely understood, but does involve hydroxylation.
Độc Tính : LD50=760 mg/kg (Orally in rats). Signs of overdose include dilated and sluggish pupils, warm, dry skin, facial flushing, decreased secretions of the mouth, pharynx, nose, and bronchi, foul-smelling breath, elevated temperature, tachycardia, cardiac arrhythmias, decreased bowel sounds, urinary retention, delirium, disorientation, anxiety, hallucinations, illusions, confusion, incoherence, agitation, hyperactivity, ataxia, loss of memory, paranoia, combativeness, and seizures.
Chỉ Định : For use as an adjunct in the therapy of all forms of parkinsonism and control of extrapyramidal disorders secondary to neuroleptic drug therapy.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia
  • Rivastigmine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Biperidin, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
  • Trimethobenzamide Trimethobenzamide and Biperiden, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Biperiden, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trospium Trospium and Biperiden, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Abbott
    Sản phẩm biệt dược : Akineton
  • Công ty : Winston
    Sản phẩm biệt dược : Bilino
  • Công ty : Orion
    Sản phẩm biệt dược : Ipsatol
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00810
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2381
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508325
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07941
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00779
ChemSpider
http://www.chemspider.com/Chemical-Structure.2289.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50240680
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/49884-693-01
PharmGKB
http://www.pharmgkb.org/drug/PA448626
Wikipedia
http://en.wikipedia.org/wiki/Biperiden
RxList
http://www.rxlist.com/cgi/generic2/biperiden.htm
Drugs.com
http://www.drugs.com/cdi/biperiden.html
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