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QuickView for Duloxetine (compound)

Name: duloxetine
PubChem Compound ID: 10086118
Molecular formula: C18H19NOS
Molecular weight: 299.408 g/mol
Name: duloxetine
Name (isomeric): DB00476
Drug Type: small molecule
Duloxetine HCl; (+-)-duloxetine; Duloxetine Hydrochloride
Brand: Cymbalta, Yentreve
Category: Dopamine Uptake Inhibitors, Adrenergic Uptake Inhibitors, Serotonin Uptake Inhibitors, Antidepressive Agents
CAS number: 136434-34-9
Indication: For the acute and maintenance treatment of major depressive disorder (MDD), as well as acute management of generalized anxiety disorder. Also used for the management of neuropathic pain associated with diabetic peripheral neuropathy, and fibromyalgia. Has been used in the management of moderate to severe stress urinary incontinence (SUI) in women.
Duloxetine is in a class of medications called selective serotonin and norepinephrine reuptake inhibitors (SSNRIs) and primarily targets major depressive disorders (MDD) and stress urinary incontinence (SUI). Duloxetine is also used to treat pain and tingling caused by diabetic neuropathy (damage to nerves that can develop in people who have diabet...
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Mechanism of Action:
Duloxetine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake and a less potent inhibitor of dopamine reuptake. Duloxetine has no significant affinity for dopaminergic, adrenergic, cholinergic, histaminergic, opioid, glutamate, and GABA receptors. The antidepressant and pain inhibitory actions of duloxetine are believed to be r...
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Absorption: Orally administered duloxetine hydrochloride is well absorbed.
Protein binding: Protein binding is greater than 90%.
Biotransformation: 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.
Route of elimination: Many additional metabolites have been identified in urine, some representing only minor pathways of elimination. Most (about 70%) of the duloxetine dose appears in the urine as metabolites of duloxetine; about 20% is excreted in the feces.
Half Life: 12 hours (range 8-17 hours)
Toxicity: Oral, rat LD50: 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.
Affected organisms: Humans and other mammals
Food interaction:
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%.
Take without regard to meals.
People taking this product who drink large amounts of alcohol are exposed to a higher risk of liver toxicity.
Drug interaction:
TriprolidineThe CNS depressants, Triprolidine and Duloxetine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
FlecainidePossible increase in the levels of this agent when used with duloxetine
NortriptylinePossible increase in the levels of this agent when used with duloxetine
PhenelzinePossible severe adverse reaction with this combination
ThioridazineIncreased risk of cardiotoxicity and arrhythmias
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