Brands, Medical Use, Clinical Data
- Serotonin reuptake inhibitor
- Antiobesity Agents
- Appetite Depressants
Brands / Synonyms
Adifax; D-Fenfluramine; Dea No. 1670; Dexafenfluramine; Dexfenfluramina [Spanish]; DEXFENFLURAMINE HYDROCHLORIDE; Dexfenfluraminum [Latin]; Dextrofenfluramine; Fenfluramine L-Form; L-Fenfluramine; Levofenfluramina [Spanish]; Levofenfluramine; Levofenfluramine [Inn]; Levofenfluraminum [Latin]; Redux
For the management of obesity including weight loss and maintenance of weight loss in patients on a reduced calorie diet
Used to treat diabetes and obesity, Dexfenfluramine decreases caloric intake by increasing serotonin levels in the brain’s synapses. Dexfenfluramine acts as a serotonin reuptake inhibitor. It also causes release of serotonin from the synaptosomes.
Mechanism of Action
Dexfenfluramine binds to the serotonin reuptake pump. This causes inhbition of serotonin uptake and release of serotonin. The increased levels of serotonin lead to greater serotonin receptor activation which in turn lead to enhancement of serotoninergic transmission in the centres of feeding behavior located in the hypothalamus. This suppresses the appetite for carbohydrates.
Biotrnasformation / Drug Metabolism
Dexfenfluramine is contraindicated in patients with diagnosed pulmonary hypertension. Dexfenfluramine is
contraindicated in patients receiving monoamine oxidase inhibitors (see DRUG
INTERACTIONS). Dexfenfluramine is contraindicated in patients with hypersensitivity to dexfenfluramine,
fenfluramine, or related compounds.
In patients receiving nonselective monoamine oxidase inhibitors (MAOIs) (e.g., selegiline hydrochloride) in
combination with serotoninergic agents (e.g., fluoxetine, fluvoxamine, paroxetine, sertraline, venlafaxine),
there have been reports of serious, sometimes fatal, reactions. Because dexfenfluramine is a serotonin releaser and
reuptake inhibitor, dexfenfluramine should not be used concomitantly with a MAO inhibitor.
At least 14 days should elapse between discontinuation of a MAO inhibitor and initiation of treatment with
dexfenfluramine. At least 3 weeks should elapse between discontinuation of dexfenfluramine and initiation of
treatment with a MAO inhibitor.
A rare, but serious, constellation of symptoms, termed "serotonin syndrome," has been reported with the
concomitant use of selective serotonin reuptake inhibitors (SSRIs) and agents for migraine therapy, such as Imitrex
(sumatriptan succinate) and dihydroergotamine. The syndrome requires immediate medical attention and may include one
or more of the following symptoms: excitement, hypomania, restlessness, loss of consciousness, confusion,
disorientation, anxiety, agitation, motor weakness, myoclonus, tremor, hemiballismus, hyperreflexia, ataxia,
dysarthria, incoordination, hyperthermia, shivering, pupillary dilation, diaphoresis, emesis, and tachycardia.
Dexfenfluramine should not be administered with other serotoninergic agents. The appropriate interval between
administration of these agents and dexfenfluramine has not been established. The use of dexfenfluramine with other
CNS-active drugs has not been systematically evaluated; consequently, caution is advised if dexfenfluramine and such
drugs are prescribed concurrently.