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Active ingredient: Dexfenfluramine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Serotonin reuptake inhibitor
  • Antiobesity Agents
  • Appetite Depressants

Dosage Forms

  • Not Available

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

Indications

For the management of obesity including weight loss and maintenance of weight loss in patients on a reduced calorie diet

Pharmacology

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.

Absorption

Not Available

Toxicity

Not Available

Biotrnasformation / Drug Metabolism

Not Available

Contraindications

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.

Drug Interactions

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.

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