药品详细

Phentermine(芬特明)

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

芬特明

英文名

Phentermine

分子式

C₁₀H₁₅N

化学名

2-methyl-1-phenylpropan-2-amine

分子量

Average: 149.2328
Monoisotopic: 149.120449485

CAS号

122-09-8

ATC分类

A08A 未知

药物类型

small molecule

阶段

illicit, approved

商品名

同义名

基本介绍

A central nervous system stimulant and sympathomimetic with actions and uses similar to those of dextroamphetamine. It has been used most frequently in the treatment of obesity. [PubChem]. Some common brand names for phentermine are Adipex-P® and Suprenza™. Phentermine is also available in combination medications such as Qsymia®.

生产厂家

Abc holding corp
Able laboratories inc
Actavis elizabeth llc
Actavis totowa llc
Barr laboratories inc
Baxter healthcare corp anesthesia critical care
Camall co inc
Caraco pharmaceutical laboratories ltd
Duramed pharmaceuticals inc sub barr laboratories inc
Ferndale laboratories inc
Glaxosmithkline
Ivax pharmaceuticals inc
Kvk tech inc
Lannett co inc
Lannett holdings inc
Mm mast and co
Mutual pharmaceutical co inc
Quantum pharmics ltd
Sandoz inc
Shire richwood inc
Solvay pharmaceuticals
Teva pharmaceuticals usa inc
Tg united inc
Tg united labs llc
Ucb inc
Usl pharma inc
Vintage pharmaceuticals inc
Vitarine pharmaceuticals inc
Watson laboratories inc

封装厂家

参考

Synthesis Reference	Not Available
General Reference	Bray GA: A concise review on the therapeutics of obesity. Nutrition. 2000 Oct;16(10):953-60. Pubmed Nelson DL, Gehlert DR: Central nervous system biogenic amine targets for control of appetite and energy expenditure. Endocrine. 2006 Feb;29(1):49-60. Pubmed

剂型

规格

化合物类型

Type	small molecule

Classes

Phenethylamines
Amphetamines

Substructures

Aliphatic and Aryl Amines
Benzene and Derivatives
Phenethylamines
Aromatic compounds
Amphetamines

适应症

药理

Indication	For the treatment and management of obesity.
Pharmacodynamics	Phentermine is indicated in the management of exogenous obesity as a short term (a few weeks) adjunct in a regimen of weight reduction based on caloric restriction. Phentermine hydrochloride is a sympathomimetic amine with pharmacologic activity similar to the prototype drugs of this class used in obesity, the amphetamines. Actions include central nervous system stimulation and elevation of blood pressure. Tachyphylaxis and tolerance have been demonstrated with all drugs of this class in which these phenomena have been looked for.
Mechanism of action	Phentermine is an amphetamine that stimulates neurons to release or maintain high levels of a particular group of neurotransmitters known as catecholamines; these include dopamine and norepinephrine. High levels of these catecholamines tend to suppress hunger signals and appetite. The drug seems to inhibit reuptake of noradrenaline, dopamine, and seratonin through inhibition or reversal of the reuptake transporters. It may also inhibit MAO enzymes leaving more neurotransmitter available at the synapse.Phentermine (through catecholamine elevation) may also indirectly affect leptin levels in the brain. It is theorized that phentermine can raise levels of leptin which signal satiety. It is also theorized that increased levels of the catecholamines are partially responsible for halting another chemical messenger known as neuropeptide Y. This peptide initiates eating, decreases energy expenditure, and increases fat storage.
Absorption	Phentermine is rapidly absorbed after oral ingestion.
Volume of distribution	Not Available
Protein binding	Approximately 96.3%
Metabolism	Hepatic.
Route of elimination	Not Available
Half life	16 to 31 hours
Clearance	Not Available
Toxicity	LD₅₀ is adult monkeys is 15 to 20 mg/kg. Symptoms of overdose include delirium, mania, self-injury, marked hypertension, tachycardia, arrhythmia, hyperpyrexia, convulsion, coma, and circulatory collapse.
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	205 °C	Not Available
water solubility	18.6 g/L	Not Available
logP	1.90	HANSCH,C ET AL. (1995)

Predicted Properties

Property	Value	Source
water solubility	7.57e-01 g/l	ALOGPS
logP	2.32	ALOGPS
logP	2.08	ChemAxon
logS	-2.3	ALOGPS
pKa (strongest basic)	10.25	ChemAxon
physiological charge	1	ChemAxon
hydrogen acceptor count	1	ChemAxon
hydrogen donor count	1	ChemAxon
polar surface area	26.02	ChemAxon
rotatable bond count	2	ChemAxon
refractivity	48.34	ChemAxon
polarizability	17.87	ChemAxon

药物相互作用

Drug	Interaction
Acetophenazine	Decreased anorexic effect, may increase psychotic symptoms
Chlorpromazine	Decreased anorexic effect, may increase psychotic symptoms
Ethopropazine	Decreased anorexic effect, may increase psychotic symptoms
Fluoxetine	Risk of serotoninergic syndrome
Fluphenazine	Decreased anorexic effect, may increase psychotic symptoms
Fluvoxamine	Risk of serotoninergic syndrome
Guanethidine	Phentermine may decrease the effect of guanethidine.
Isocarboxazid	Possible hypertensive crisis
Mesoridazine	Decreased anorexic effect, may increase psychotic symptoms
Methdilazine	Decreased anorexic effect, may increase psychotic symptoms
Methotrimeprazine	Decreased anorexic effect, may increase psychotic symptoms
Paroxetine	Risk of serotoninergic syndrome
Perphenazine	Decreased anorexic effect, may increase psychotic symptoms
Phenelzine	Possible hypertensive crisis
Prochlorperazine	Decreased anorexic effect, may increase psychotic symptoms.
Promazine	Decreased anorexic effect, may increase psychotic symptoms
Promethazine	Decreased anorexic effect, may increase psychotic symptoms.
Propericiazine	Decreased anorexic effect, may increase psychotic symptoms.
Propiomazine	Decreased anorexic effect, may increase psychotic symptoms
Rasagiline	Possible hypertensive crisis
Thiethylperazine	Decreased anorexic effect, may increase psychotic symptoms
Thioridazine	Decreased anorexic effect, may increase psychotic symptoms
Tramadol	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Trandolapril	Phentermine may reduce the efficacy of Trandolapril.
Tranylcypromine	The MAO inhibitor, tranylcypromine, may increase the vasopressor effect of the amphetamine, phentermine. Concomitant therapy should be avoided.
Trifluoperazine	Decreased anorexic effect, may increase psychotic symptoms
Triflupromazine	Decreased anorexic effect, may increase psychotic symptoms
Trimeprazine	Decreased anorexic effect, may increase psychotic symptoms
Triprolidine	Triprolidine may reduce the sedative effect of the antihistamine, Phentermine.
Venlafaxine	Risk of serotoninergic syndrome

食物相互作用

Limit caffeine intake.
Take without regard to meals.

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