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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 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. | '''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. Most common side effects in clinical trials were nausea, somnolence, and dry mouth. In clinical trials weight gain was neutral compared to placebo. Ongoing studies including a 52 week safety and efficacy trial are available at . Long-term side-effects seen in these trials did not vary from the original approval studies. | 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 side effects in clinical trials were nausea, somnolence, and dry mouth. In clinical trials weight gain was neutral compared to placebo. Ongoing studies including a 52 week safety and efficacy trial are available at . 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 ] are 60mg and 120mg once daily. | Duloxetine is also approved by the FDA for the treatment of ] neuropathy. Approved dosages for treatment ] are 60mg and 120mg once daily. | ||
| When used for the treatment of depression, the approved dosage is 40mg-60 mg once daily. Duloxetine is available in capsules of 20mg, 30mg, and 60mg. | When used for the treatment of depression, the approved dosage is 40mg-60 mg once daily. Duloxetine is available in capsules of 20mg, 30mg, and 60mg. | ||
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| ==External links== | ==External links== | ||
| * | * | ||
| * and - medlineplus.org | * and - medlineplus.org | ||
| * | * | ||
Revision as of 12:22, 18 January 2006
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| 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 side effects in clinical trials were nausea, somnolence, and dry mouth. In clinical trials weight gain was neutral compared to placebo. Ongoing studies including a 52 week safety and efficacy trial are available 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 available in capsules of 20mg, 30mg, and 60mg.
External links
- Manufacturer website
- Duloxetine and Duloxetine (Systemic) - medlineplus.org
- Prescribing Guide
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