||Duloxetine (brand names Cymbalta, Yentreve, and in parts of Europe, Xeristar or Ariclaim) is a drug which primarily targets major depressive disorder (MDD), generalized anxiety disorder (GAD), pain related to diabetic peripheral neuropathy and in some countries stress urinary incontinence (SUI). It is manufactured and marketed by Eli Lilly and Company.
Duloxetine has not yet been FDA approved for stress urinary incontinence or for fibromyalgia.
Duloxetine is a selective SNRI (selective serotonin-norepinephrine reuptake inhibitor). Duloxetine is a systemic drug therapy which affects the body as a whole. Known also under the code name LY248686, it is a potent dual reuptake inhibitor of serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE), possessing comparable affinities in binding to NE- and 5-HT transporter sites. It is a less potent inhibitor of dopamine reuptake.
||The major biotransformation pathways for duloxetine involve oxidation of the naphthyl ring followed by conjugation and further oxidation. Both CYP2D6 and CYP1A2 catalyze the oxidation of the naphthyl ring in vitro. Metabolites found in plasma include 4-hydroxy duloxetine glucuronide and 5-hydroxy, 6-methoxy duloxetine sulfate. The major circulating metabolites have not been shown to contribute significantly to the pharmacologic activity of duloxetine.
||Humans and other mammals
||Orally administered duloxetine hydrochloride is well absorbed.
||Oral, rat LD<sub>50</sub>: 491 mg/kg for males and 279 mg/kg for females. Symptoms of overdose include tremors, convulsions, reduced activity, slow pupillary response, intermittent tremors, and rigidity.
||Food does not affect maximum levels reached, but delays it (from 6 to 10 hours) and total product exposure appears to be reduced by only 10%. People taking this product who drink large amounts of alcohol are exposed to a higher risk of liver toxicity. Take without regard to meals.
||Amitriptyline: Possible increase in the levels of this agent when used with duloxetine. Ciprofloxacin: Ciprofloxacin increases the effect/toxicity of duloxetine. Desipramine: Possible increase in the levels of this agent when used with duloxetine. Flecainide: Possible increase in the levels of this agent when used with duloxetine. Fluvoxamine: Fluvoxamine increases the effect and toxicity of duloxetine. Imipramine: Possible increase in the levels of this agent when used with duloxetine. Isocarboxazid: Possible severe adverse reaction with this combination. Nortriptyline: Possible increase in the levels of this agent when used with duloxetine. Phenelzine: Possible severe adverse reaction with this combination. Propafenone: Possible increase in the levels of this agent when used with duloxetine. Rasagiline: Possible severe adverse reaction with this combination. Thioridazine: Increased risk of cardiotoxicity and arrhythmias. Tranylcypromine: Possible severe adverse reaction with this combination
||http://dbpedia.org/page/Duloxetine, http://en.wikipedia.org/wiki/Duloxetine, http://www.drugbank.ca/drugs/DB00476
||Duloxetine (Cymbalta, and generics) is a serotonin-norepinephrine reuptake inhibitor (SNRI) created by Eli Lilly. It is mostly prescribed for major depressive disorder, generalized anxiety disorder, fibromyalgia and neuropathic pain.Duloxetine failed to receive US approval for stress urinary incontinence amid concerns over liver toxicity and suicidal events; however, it was approved for this indication in the UK, where it is recommended as an add-on medication in stress urinary incontinence instead of surgery.
||Duloxetine (Cymbalta, and generics) is a serotonin-norepinephrine reuptake inhibitor (SNRI) created by Eli Lilly.