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药品详细

Metixene (Metixene )

化学结构式图
中文名
Metixene
英文名
Metixene
分子式
Not Available
化学名
1-methyl-3-(9H-thioxanthen-9-ylmethyl)piperidine
分子量
Average: 309.468
Monoisotopic: 309.155120431
CAS号
4969-02-2
ATC分类
N04A 未知
药物类型
small molecule
阶段
商品名
Atosil;Contalyl;Methixart;Tremaril;Tremaril hydrochloride;Tremonil;Trest;
同义名
Methixen [German];Methixene;Methixene hydrochloride;Metisene [DCIT];Metixene hydrochloride;Metixeno [INN-Spanish];Metixenum [INN-Latin];
基本介绍

Metixene (or methixene) is a anticholinergic used as an anti-parkinson drug. [Wikipedia]

生产厂家
  • Novartis pharmaceuticals corp
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Link
剂型
规格
化合物类型
Type small molecule
Classes
  • Thioxanthenes
Substructures
  • Ethers
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Heterocyclic compounds
  • Aromatic compounds
  • Thioxanthenes
  • Piperidines
适应症
PARKINSON 帕金森氏症;
药理
Indication Used for the symptomatic treatment of parkinsonism.
Pharmacodynamics Metixene is a tertiary antimuscarinic with actions similar to those of atropine; it also has antihistaminic and direct antispasmodic properties. It is used for the symptomatic treatment of parkinsonism, including the alleviation of the extrapyramidal syndrome induced by other drugs such as phenothiazines, but, like other antimuscarinics, it is of no value against tardive dyskinesias. Metixene has been discontinued.
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 metixene is considered to relate to competitive antagonism of acetylcholine at muscarinic receptors in the corpus striatum, which then restores the balance.
Absorption Absorbed in the gastrointestinal tract following oral administration, however the extent of absorption is not known.
Volume of distribution Not Available
Protein binding Not Available
Metabolism

Hepatic. Metabolism occurs via sulfoxydation and N-demethylation.

Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity 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 liquid
Melting point < 25 oC
Experimental Properties
Property Value Source
water solubility Soluble as HCl salt PhysProp
logP 4.7 PhysProp
Predicted Properties
Property Value Source
water solubility 1.02e-04 g/l ALOGPS
logP 5.51 ALOGPS
logP 5.06 ChemAxon Molconvert
logS -6.48 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 1 ChemAxon Molconvert
hydrogen donor count 0 ChemAxon Molconvert
polar surface area 3.24 ChemAxon Molconvert
rotatable bond count 2 ChemAxon Molconvert
refractivity 97.17 ChemAxon Molconvert
polarizability 35.67 ChemAxon Molconvert
药物相互作用
食物相互作用
Not Available

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