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药品详细

Procyclidine(丙环定)

化学结构式图
中文名
丙环定
英文名
Procyclidine
分子式
C19H29NO
化学名
1-cyclohexyl-1-phenyl-3-(pyrrolidin-1-yl)propan-1-ol
分子量
Average: 287.4397
Monoisotopic: 287.224914555
CAS号
77-37-2
ATC分类
N04A 未知
药物类型
small molecule
阶段
approved
商品名
Arpicolin;Elorine;Kemadrin;Kemadrine;Lergine;Metanin;Osnervan;Procyclid;Procyklidin;Prosyklidin;Spamol;Triciclidina;Triciloid;Tricoloid;Tricyclamol;Vagosin;
同义名
Prociclidina [INN-Spanish];Procyclidinum [INN-Latin];
基本介绍

A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism. [PubChem]

生产厂家
  • Monarch pharmaceuticals inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Theodoridis GC, Stark L: Central role of solar information flow in pregenetic evolution. J Theor Biol. 1971 Jun;31(3):377-88. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Cumenes and Derivatives
  • Phenylpropylamines
Substructures
  • Hydroxy Compounds
  • Benzyl Alcohols and Derivatives
  • Pyrrolidines
  • Benzene and Derivatives
  • Cumenes and Derivatives
  • Aliphatic and Aryl Amines
  • Alcohols and Polyols
  • Heterocyclic compounds
  • Aromatic compounds
  • Phenylpropylamines
适应症
PARKINSON 帕金森氏症;
药理
Indication For the treatment of all forms of Parkinson's Disease, as well as control of extrapyramidal reactions induced by antipsychotic agents.
Pharmacodynamics Procyclidine has an atropine-like action on parasympathetic-innervated peripheral structures including smooth muscle. It's antispasmodic effects are thought to be related to the blockage of central cholinergic receptors M1, M2 and M4. It is used to treat symptomatic Parkinsonism and extrapyramidal dysfunction caused by antipsychotic agents.
Mechanism of action The mechanism of action is unknown. It is thought that Procyclidine acts by blocking central cholinergic receptors, and thus balancing cholinergic and dopaminergic activity in the basal ganglia. Many of its effects are due to its pharmacologic similarities with atropine. Procyclidine exerts an antispasmodic effect on smooth muscle, and may produce mydriasis and reduction in salivation.
Absorption Not Available
Volume of distribution Not Available
Protein binding Approximately 100% bound to albumin.
Metabolism
Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity LD50=60 mg/kg (IV in mice)
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 86 °C PhysProp
water solubility Moderately soluble in water, ~ 30 mg/ml Not Available
logP 4.2 Not Available
Predicted Properties
Property Value Source
water solubility 9.84e-03 g/l ALOGPS
logP 4.13 ALOGPS
logP 3.79 ChemAxon
logS -4.5 ALOGPS
pKa (strongest acidic) 13.84 ChemAxon
pKa (strongest basic) 9.45 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 88.6 ChemAxon
polarizability 34.43 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
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Procyclidine, 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 Procyclidine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Triprolidine and Procyclidine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trospium Trospium and Procyclidine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
食物相互作用
Not Available

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