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药品详细

Biperiden(比哌立登)

化学结构式图
中文名
比哌立登
英文名
Biperiden
分子式
C21H29NO
化学名
1-{bicyclo[2.2.1]hept-5-en-2-yl}-1-phenyl-3-(piperidin-1-yl)propan-1-ol
分子量
Average: 311.4611
Monoisotopic: 311.224914555
CAS号
514-65-8
ATC分类
N04A 未知
药物类型
small molecule
阶段
approved
商品名
Akineton;Akinophyl;
同义名
Beperiden;Biperiden [Usan:Ban:Inn:Jan];Biperiden Hydrochloride;Biperidene [INN-French];Biperidene Hydrochloride;Biperideno [INN-Spanish];Biperidenum [INN-Latin];Biperidine;Biperidine Hydrochloride;
基本介绍

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]

生产厂家
  • Abbott laboratories
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Nishiyama K, Mizuno T, Sakuta M, Kurisaki H: Chronic dementia in Parkinson’s disease treated by anticholinergic agents. Neuropsychological and neuroradiological examination. Adv Neurol. 1993;60:479-83. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Cumenes and Derivatives
  • Phenylpropylamines
Substructures
  • Hydroxy Compounds
  • Alkanes and Alkenes
  • Benzyl Alcohols and Derivatives
  • Benzene and Derivatives
  • Cumenes and Derivatives
  • Aliphatic and Aryl Amines
  • Alcohols and Polyols
  • Heterocyclic compounds
  • Aromatic compounds
  • Phenylpropylamines
  • Cyclohexenes and Derivatives
  • Piperidines
适应症
PARKINSON 帕金森氏症;
药理
Indication For use as an adjunct in the therapy of all forms of parkinsonism and control of extrapyramidal disorders secondary to neuroleptic drug therapy.
Pharmacodynamics 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.
Mechanism of action 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.
Absorption 87% bioavailability
Volume of distribution Not Available
Protein binding 60%
Metabolism
The metabolism of biperiden is not completely understood, but does involve hydroxylation.
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity 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.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 114 °C PhysProp
water solubility 25.1 mg/L Not Available
logP 4.25 SANGSTER (1993)
Predicted Properties
Property Value Source
water solubility 4.26e-03 g/l ALOGPS
logP 4.28 ALOGPS
logP 3.54 ChemAxon
logS -4.9 ALOGPS
pKa (strongest acidic) 13.82 ChemAxon
pKa (strongest basic) 9.3 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 23.47 ChemAxon
rotatable bond count 5 ChemAxon
refractivity 97.02 ChemAxon
polarizability 36.74 ChemAxon
药物相互作用
Drug Interaction
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.
食物相互作用
  • Avoid alcohol.
  • Take with food.

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