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药品详细

Trihexyphenidyl(苯海索)

化学结构式图
中文名
苯海索
英文名
Trihexyphenidyl
分子式
C20H31NO
化学名
1-cyclohexyl-1-phenyl-3-(piperidin-1-yl)propan-1-ol
分子量
Average: 301.4662
Monoisotopic: 301.240564619
CAS号
144-11-6
ATC分类
N04A 未知
药物类型
small molecule
阶段
approved
商品名
Apo-Trihex;Artane;Artane Sequels;Benzhexol;Benzhexolum;Parkinane Retard;PMS Trihexyphenidyl;Tremin;Trihexane;Trihexy;
同义名
Trihexifenidilo [INN-Spanish];Trihexylphenidyl;Trihexylphenidyle;Trihexylphenizyl;Trihexyphenidyl HCl;Trihexyphenidyle;Trihexyphenidyle [INN-French];Trihexyphenidylum [INN-Latin];Triphenidyl;
基本介绍

One of the centrally acting muscarinic antagonists used for treatment of parkinsonian disorders and drug-induced extrapyramidal movement disorders and as an antispasmodic. [PubChem]

生产厂家
  • Lederle laboratories div american cyanamid co
  • Mikart inc
  • Nylos trading co inc
  • Pharmaceutical assoc inc div beach products
  • Pharmaceutical ventures ltd
  • Schering corp sub schering plough corp
  • Vangard laboratories inc div midway medical co
  • Vintage pharmaceuticals inc
  • Watson laboratories inc
  • West ward pharmaceutical corp
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Cumenes and Derivatives
  • Phenylpropylamines
Substructures
  • Hydroxy Compounds
  • Benzyl Alcohols and Derivatives
  • Benzene and Derivatives
  • Cumenes and Derivatives
  • Aliphatic and Aryl Amines
  • Alcohols and Polyols
  • Heterocyclic compounds
  • Aromatic compounds
  • Phenylpropylamines
  • Piperidines
适应症
PARKINSON 帕金森氏症;
药理
Indication Indicated for the treatment of parkinson's disease and extrapyramidal reactions caused by drugs.
Pharmacodynamics Trihexyphenidyl is an anticholinergic used in the symptomatic treatment of all etiologic groups of parkinsonism and drug induced extrapyramidal reactions (except tardive dyskinesia). Trihexyphenidyl possesses both anticholinergic and antihistaminic effects, although only the former has been established as therapeutically significant in the management of parkinsonism.
Mechanism of action Trihexyphenidyl is a selective M1 muscarinic acetylcholine receptor antagonist. It is able to discriminate between the M1 (cortical or neuronal) and the peripheral muscarinic subtypes (cardiac and glandular). Trihexyphenidyl partially blocks cholinergic activity in the CNS, which is responsible for the symptoms of Parkinson's disease. It is also thought to increase the availability of dopamine, a brain chemical that is critical in the initiation and smooth control of voluntary muscle movement.
Absorption Trihexyphenidyl is rapidly absorbed from the gastrointestinal tract.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination Not Available
Half life 3.3-4.1 hours
Clearance Not Available
Toxicity Symptoms of overdose include mydriasis, dryness of mucous membranes, red face, atonic states of bowels and bladder, and hyperthermia in high doses. Central consequences are agitation, confusion, and hallucinations. An untreated overdose may be fatal, particular in children. Premortal signs are respiratory depression and cardiac arrest.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 258.5 °C Not Available
logP 4.49 SANGSTER (1993)
Predicted Properties
Property Value Source
water solubility 3.14e-03 g/l ALOGPS
logP 4.93 ALOGPS
logP 4.23 ChemAxon
logS -5 ALOGPS
pKa (strongest acidic) 13.84 ChemAxon
pKa (strongest basic) 9.32 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 93.21 ChemAxon
polarizability 36.73 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
Potassium Chloride The ulcerative effects of solid oral dosage forms of KCl may be enhanced by Trihexyphenidyl, an anticholinergic. Anticholinergics slow gastric emptying, increasing the contact time between the gastrointestinal mucosa and KCl. Prolonged exposure to KCl increases the risk of gastric and intestinal irritation and ulceration. Solid oral dosage forms of KCl should be avoided; alternatives include liquid or effervescent potassium preparations.
Pramlintide The anticholinergic effects of Trihexyphenidyl may be enhanced by Pramlintide. Additive effects of reduced GI motility may occur. Pramlintide slows gastic emptying and should not be used with drugs that alter GI motility (e.g. anticholinergics). Consider alternative treatments or use caution during concomitant therapy.
Rivastigmine Possible antagonism of action
Secretin The stimulatory effect of Secretin may be reduced by anticholinergics such as Trihexyphenidyl. Concomitant use of Secretin and drugs with substantial anticholinergic effects should be avoided. If combination therapy must be used, Secretin efficacy should be closely monitored.
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Trihexyphenidyl, 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 Trihexyphenidyl, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Triprolidine and Trihexyphenidyl, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trospium Trospium and Trihexyphenidyl, 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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