药品详细
Phenmetrazine(苯甲吗啉)
化学结构式图
中文名
苯甲吗啉
英文名
Phenmetrazine
分子式
C11H15NO
化学名
3-methyl-2-phenylmorpholine
分子量
Average: 177.2429
Monoisotopic: 177.115364107
Monoisotopic: 177.115364107
CAS号
134-49-6
ATC分类
药物类型
small molecule
阶段
illicit, approved
商品名
同义名
基本介绍
A sympathomimetic drug used primarily as an appetite depressant. Its actions and mechanisms are similar to dextroamphetamine. [PubChem]
生产厂家
- Boehringer ingelheim pharmaceuticals 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 |
|
| Substructures |
|
适应症
药理
| Indication | Used as an anorectic in the treatment of obesity. |
| Pharmacodynamics | Phenmetrazine is a sympathomimetic drug used primarily as an appetite depressant. Its actions and mechanisms are similar to dextroamphetamine. Amphetamines are non-catecholamine sympathomimetic amines with CNS stimulant activity. Phenmetrazine was originally sold under the tradename Preludin as an anorectic. It has since been removed from the market. It is by some considered to have a greater potential for addiction than the amphetamines, and has been abused in many countries, for example Sweden. |
| Mechanism of action | Phenmetrazine is thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron leading to an increase in the release of these monoamines into the extraneuronal space. Dopamine integrates incoming sensory stimuli, initiates and controls fine movement (nigro-neostriatal pathway), controls emotional behavior (midbrain mesolimbic-forebrain system) and controls hypothalamic-pituitary endocrine system (tubero-infundibular system). It is this latter effect on the tubero-infundibular systm that seems to lead to reduced food intake. Phenmetrazine also acts as a monoamine oxidase inhibitor. |
| Absorption | Readily absorbed from the gastro-intestinal tract and buccal mucosa. |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism |
Primarily hepatic (via CYP3A and CYP2D6). Resistant to metabolism by monoamine oxidase. Metabolism involves deamination to para-hydroxyamphetamine and phenylacetone; this latter compound is subsequently oxidize to benzoic acid and excreted as glucuronide or glycine (hippuric acid) conjugate. Smaller amounts of amphetamine are converted to norephedrine by oxidation.
|
| Route of elimination | Not Available |
| Half life | 16 to 31 hours |
| Clearance | Not Available |
| Toxicity | Adult monkeys have an LD50 of 15 to 20 mg/kg, whereas for young monkeys the LD50 is only 5 mg/kg. Symptoms of overdose include acute central nervous system stimulation, cardiotoxicity causing tachycardia, arrhythmias, hypertension, and cardiovascular collapse. Whilst some patients show signs of toxicity at blood concentrations of 20 µg/L, chronic abusers of amphetamine have been known to have blood concentration of up to 3000 µg/L. |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | ||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
|
|||||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
|||||||||||||||||||||||||||||||||||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Chlorpromazine | Decreased anorexic effect, may increase psychotic symptoms |
| Fluphenazine | Decreased anorexic effect, may increase psychotic symptoms |
| Guanethidine | Phenmetrazine 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 |
| Perphenazine | Decreased anorexic effect, may increase psychotic symptoms |
| 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
收藏