药品详细

Trimethaphan(Trimethaphan)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

Trimethaphan

英文名

Trimethaphan

分子式

C₂₂H₂₅N₂OS

化学名

3,5-dibenzyl-4-oxo-8$l^{4}-thia-3,5-diazatricyclo[6.3.0.0^{2,6}]undecan-8-ylium

分子量

Average: 365.512
Monoisotopic: 365.168759122

CAS号

7187-66-8

ATC分类

C02B 未知

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

A nicotinic antagonist that has been used as a ganglionic blocker in hypertension, as an adjunct to anesthesia, and to induce hypotension during surgery. [PubChem]

生产厂家

Hoffmann la roche inc

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

Thienoimidazoles

Substructures

Benzene and Derivatives
Ureas and Derivatives
Heterocyclic compounds
Aromatic compounds
Thienoimidazoles
Imidazolidines
Cations

适应症

药理

Indication	For the controlled reduction of blood pressure during surgery and in the treatment of hypertensive emergencies.
Pharmacodynamics	Trimethaphan is indicated for production of controlled hypotension during surgery to reduce bleeding into the surgical field and also for rapid reduction of blood pressure in the treatment of hypertensive emergencies, especially in patients with acute dissecting aneurysm, and in the emergency treatment of pulmonary edema in patients with pulmonary hypertension associated with systemic hypertension.
Mechanism of action	Trimethaphan is a ganglionic blocking agent prevents stimulation of postsynaptic receptors by competing with acetylcholine for these receptor sites. Additional effects may include direct peripheral vasodilation and release of histamine. Trimethaphan's hypotensive effect is due to reduction in sympathetic tone and vasodilation, and is primarily postural.
Absorption	Not Available
Volume of distribution	Not Available
Protein binding	Not Available
Metabolism	Not Available
Route of elimination	Not Available
Half life	Not Available
Clearance	Not Available
Toxicity	Not Available
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
logP	3.473	Not Available

Predicted Properties

Property	Value	Source
water solubility	6.65e-03 g/l	ALOGPS
logP	4.4	ALOGPS
logP	2.32	ChemAxon
logS	-4.8	ALOGPS
pKa (strongest basic)	-2	ChemAxon
physiological charge	1	ChemAxon
hydrogen acceptor count	1	ChemAxon
hydrogen donor count	0	ChemAxon
polar surface area	23.55	ChemAxon
rotatable bond count	4	ChemAxon
refractivity	105.43	ChemAxon
polarizability	40.13	ChemAxon

药物相互作用

食物相互作用

Not Available

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