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'''Duloxetine hydrochloride''' (brand names: '''Cymbalta'''/'''Yentreve''') is a medically used drug that primarily targets major ] disorders (MDD), pain related to ] ] and stress ] (SUI). Known also as LY248686, chemically (+)-(''S'')-''N''-methyl-3-(1-naphthyloxy)-<br>2-thiophenepropanamine, it is a potent dual inhibitor of ] (5-hydroxytryptamine, 5-HT) and ] (NE) reuptake, possessing comparable affinities in binding to NE and 5-HT transport sites. Its behavior contrasts to most other dual-reuptake inhibitors. '''Duloxetine hydrochloride''' (brand names: '''Cymbalta'''/'''Yentreve''') is a medically used drug that primarily targets major ] disorders (MDD), pain related to ] ] and stress ] (SUI). Known also as LY248686, chemically (+)-(''S'')-''N''-methyl-3-(1-naphthyloxy)-<br>2-thiophenepropanamine, it is a potent dual reuptake inhibitor of ] (5-hydroxytryptamine, 5-HT) and ] (NE), possessing comparable affinities in binding to NE and 5-HT transport sites. Its behavior contrasts to most other dual-reuptake inhibitors in that Ki values are nearly 1:1.


Furthermore, duloxetine lacks affinity for ] ] within the ]. While there is limited data available regarding the ] profile of duloxetine in humans, its ] is reported to be 10 to 15 hours. Furthermore, duloxetine lacks affinity for ] ] within the ]. While there is limited data available regarding the ] profile of duloxetine in humans, its ] is reported to be 10 to 15 hours. Most common sideeffects in clinical trials were nausea, somnolence, and dry mouth. In clinical trials weight gain was neutral compared to placebo. On going studies including a 52 week safety and efficacy trial are availaable at ]. Long-term side-effects seen in these trials did not vary from the original approval studies.


Duloxentine is also approved by the FDA for the treatment of diabetic neuropathy. Duloxetine is also approved by the FDA for the treatment of diabetic neuropathy. Approved dosages for treatment ] are 60mg and 120mg once daily.


When used for the treatment of depression, it is commonly prescribed in doses of either 20 mg, 30 mg, or 60 mg. The long-term side-effects are unknown at this time. When used for the treatment of depression, the approved dosage is 40mg-60 mg once daily. Duloxetine is availble in capsules of 20mg, 30mg, and 60mg.


==External links== ==External links==

Revision as of 23:08, 15 January 2006

Duloxetine chemical structure of duloxetine
Duloxetine

IUPAC chemical name
CAS number
 ?
ATC code
 ?
Chemical formula C18H19NOS, HCl
Molecular weight 333.38
Bioavailability ?
Metabolism Hepatic Oxidation
Elimination half-life 8-17 hours
Excretion 70% in urine, 20% in feces
Pregnancy category C (USA)
Legal status Prescription only (USA)
Routes of administration Oral

Duloxetine hydrochloride (brand names: Cymbalta/Yentreve) is a medically used drug that primarily targets major depressive disorders (MDD), pain related to diabetic peripheral neuropathy and stress urinary incontinence (SUI). Known also as LY248686, chemically (+)-(S)-N-methyl-3-(1-naphthyloxy)-
2-thiophenepropanamine, 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 transport sites. Its behavior contrasts to most other dual-reuptake inhibitors in that Ki values are nearly 1:1.

Furthermore, duloxetine lacks affinity for monoamine receptors within the central nervous system. While there is limited data available regarding the pharmacokinetic profile of duloxetine in humans, its half-life is reported to be 10 to 15 hours. Most common sideeffects in clinical trials were nausea, somnolence, and dry mouth. In clinical trials weight gain was neutral compared to placebo. On going studies including a 52 week safety and efficacy trial are availaable at www.lillytrials.com. Long-term side-effects seen in these trials did not vary from the original approval studies.

Duloxetine is also approved by the FDA for the treatment of diabetic neuropathy. Approved dosages for treatment diabetic peripheral neuropathic pain are 60mg and 120mg once daily.

When used for the treatment of depression, the approved dosage is 40mg-60 mg once daily. Duloxetine is availble in capsules of 20mg, 30mg, and 60mg.

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Antidepressants (N06A)
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