| Generic name |
Phenmetrazine
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| Brand Names/Synonyms |
A 66; Bromadryl; Cafilon; Dexphenmetrazine; Fenmetrazin; Hydrochloride; Marsin; Mefolin; Neo-Zine; Oxazimedrine; Phenmetrazin; Phenmetrazine; Phenmetrazinum [Inn-Latin]; Preludin; Preludin Hydrochloride; Probese-P; Psychamine a 66; [Inn-Spanish] |
| Indication |
Used as an anorectic in the treatment of obesity |
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Description |
Not Available |
| Pharmacology |
Phenmetrazine is an amphetamine-like drug. 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. Also acts as a monoamine oxidase inhibitor. |
Phenmetrazine News
(When available) |
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| Dosage Forms |
Not Available |
| Drug_Category |
Appetite Depressants; Central Nervous System Agents; |
| Absorption |
Readily absorbed from gastro-intestinal tract, complete absorption after 4-6 hours |
| Interactions |
Not Available |
| Toxicity |
Highly addictive; fatalities have been reported with doeses as low as 1.3 mg/kg. |
| Organisms Affected |
Humans and other mammals |
| Chemical IUPAC Name |
3-methyl-2-phenyl-morpholine |
| Chemical Formula |
C11H15NO |
| Molecular Weight |
177.243 g/mol |
| Smiles String |
CC1C(OCCN1)C2=CC=CC=C2 |
| Melting Point |
139 oC |
| Water Solubility |
>5 mg/L |
| State |
Solid |
| LogP/Hphobicity |
1.796 |
| Isoelectric Point |
Not Available |
| Biotransformation |
Primarily hepatic via CYP3A and CYP2D6. 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. |
| Half Life |
16-31 hours |
| Protein Binding [%] |
Not Available |
| RxList Link |
Not Available>RXlist |
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| Drug Reference |
Not Available |
| Drug Type |
Approved Drug – recently withdrawn |
| Accession No |
APRD00262 |
| CAS Registry Number |
134-49-6 |
| KEGG Compound ID |
C07432 |
| PubChem ID |
SID:9636 |
| PharmGKB ID |
Not Available |
| SwissProt ID |
Not Available |
| GenBank ID |
Not Available |
| Drug ID Number [DIN] |
Not Available
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