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药品详细

Amphetamine(安非他明)

化学结构式图
中文名
安非他明
英文名
Amphetamine
分子式
C9H13N
化学名
1-phenylpropan-2-amine
分子量
Average: 135.2062
Monoisotopic: 135.104799421
CAS号
300-62-9
ATC分类
N06B 未知;N06B 未知
药物类型
small molecule
阶段
illicit, approved
商品名
同义名
基本介绍

Amphetamine is a chiral compound. The racemic mixture can be divided into its optical antipodes: levo- and dextro-amphetamine. Amphetamine is the parent compound of its own structural class, comprising a broad range of psychoactive derivatives, e.g., MDMA (Ecstasy) and the N-methylated form, methamphetamine. Amphetamine is a homologue of phenethylamine.

生产厂家
  • Akorn inc
  • Lannett co inc
  • Teva pharmaceuticals usa inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Leith NJ, Kuczenski R: Chronic amphetamine: tolerance and reverse tolerance reflect different behavioral actions of the drug. Pharmacol Biochem Behav. 1981 Sep;15(3):399-404. Pubmed
  2. Chaudhry IA, Turkanis SA, Karler R: Characteristics of “reverse tolerance” to amphetamine-induced locomotor stimulation in mice. Neuropharmacology. 1988 Aug;27(8):777-81. Pubmed
  3. Sax KW, Strakowski SM: Behavioral sensitization in humans. J Addict Dis. 2001;20(3):55-65. Pubmed
  4. Sulzer D, Sonders MS, Poulsen NW, Galli A: Mechanisms of neurotransmitter release by amphetamines: a review. Prog Neurobiol. 2005 Apr;75(6):406-33. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes Not Available
Substructures Not Available
适应症
药理
Indication For treatment of Attention Deficit Disorder with Hyperactivity (ADDH) and narcolepsy in children.
Pharmacodynamics Amphetamine and dextroamphetamine, non-catechloamine sypathomimetic agents, are used in combination to treat attention-deficit hyperactivity disorder (ADHD) or narcolepsy. Adderall consists of equivalent amounts of amphetamine aspartate, amphetamine sulfate, dextroamphetamine saccharate, and dextroamphetamine sulfate.
Mechanism of action Amphetamines stimulate the release of norepinephrine from central adrenergic receptors. At higher dosages, they cause release of dopamine from the mesocorticolimbic system and the nigrostriatal dopamine systems. Amphetamine may also act as a direct agonist on central 5-HT receptors and may inhibit monoamine oxidase (MAO). In the periphery, amphetamines are believed to cause the release of noradrenaline by acting on the adrenergic nerve terminals and alpha- and beta-receptors. Modulation of serotonergic pathways may contribute to the calming affect. The drug interacts with VMAT enzymes to enhance release of DA and 5-HT from vesicles. It may also directly cause the reversal of DAT and SERT.
Absorption Amphetamine forms easily absorbed molecules that are highly lipid soluble
Volume of distribution Not Available
Protein binding 15-40%
Metabolism
Hepatic
Route of elimination Not Available
Half life 10 hours
Clearance Not Available
Toxicity LD50=180 mg/kg(subcutaneous injection in rat). The most common presenting symptoms seen are agitation, hallucinations, suicidal behaviour, and chest pain.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point Volatizes slowly at room temperature Not Available
water solubility Slightly Not Available
logP 1.76 HANSCH,C ET AL. (1995)
pKa 10.1 (at 20 °C) PERRIN,DD (1965)
Predicted Properties
Property Value Source
water solubility 1.74e+00 g/l ALOGPS
logP 1.85 ALOGPS
logP 1.8 ChemAxon
logS -1.9 ALOGPS
pKa (strongest basic) 10.01 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 43.71 ChemAxon
polarizability 16.17 ChemAxon
药物相互作用
Drug Interaction
Chlorpromazine Decreased anorexic effect, may increase psychotic symptoms
Dihydrocodeine Amphetamines may enhance analgesic effects of dihydrocodeine. Monitor for enhanced analgesia. Dose reductions of dihydrocodeine may be appropriate.
Fluoxetine Risk of serotoninergic syndrome
Fluphenazine Decreased anorexic effect, may increase psychotic symptoms
Fluvoxamine Risk of serotoninergic syndrome
Guanethidine Amphetamine may decrease the effect of guanethidine.
Isocarboxazid Possible hypertensive crisis
Mesoridazine 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 pyschotic symptoms
Promethazine Decreased anorexic effect, may increase pyschotic symptoms
Propericiazine Decreased anorexic effect, may increase pyschotic symptoms
Rasagiline Possible hypertensive crisis
Thioridazine Decreased anorexic effect, may increase psychotic symptoms
Trifluoperazine Decreased anorexic effect, may increase psychotic symptoms
食物相互作用
Not Available

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