cymbalta
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Duloxetine
|
| Systematic (IUPAC) name |
| (+)-(S)-N-methyl-3-(1-naphthyloxy)- 3-(thiophen-2-yl)-propan-1-amine |
| Identifiers |
| CAS number |
136434-34-9 |
| ATC code |
N06AX21 |
| PubChem |
60835 |
| DrugBank |
APRD00060 |
| Chemical data |
| Formula |
C18H19NOS |
| Mol. weight |
297.416 g/mol |
| Pharmacokinetic data |
| Bioavailability |
? |
| Protein binding |
>90% |
| Metabolism |
Liver, two P450 isozymes, CYP2D6 and CYP1A2. |
| Half life |
8-17 hours |
| Excretion |
70% in urine, 20% in feces |
| Therapeutic considerations |
| Pregnancy cat. |
C (USA)
|
| Legal status |
Prescription only (USA)
|
| Routes |
Oral |
Duloxetine hydrochloride (brand names: Cymbalta/Yentreve and in Europe known as Xeristar) 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 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. 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.[1] Long-term side-effects seen in these trials did not vary from the original approval studies.
Duloxetine is approved by the FDA for the treatment of diabetic neuropathy. Approved dosages for treatment of diabetic peripheral neuropathic pain are 60 mg and 120 mg once daily.
When used for the treatment of depression, the approved dosage is 40 mg to 60 mg once daily. Duloxetine is available in capsules of 20 mg, 30 mg, and 60 mg.
Duloxetine is also being used to treat pain symptoms in patients with fibromyalgia.
References
- ^ www.lillytrials.com
External links
- Manufacturer website
- Duloxetine and Duloxetine (Systemic) - medlineplus.org
- Prescribing Guide
- FDA Alert for Healthcare Professionals
- FDA Patient Information Sheet
| Antidepressants (ATC N06A) edit |
| Monoamine oxidase inhibitors (MAOI) |
Harmaline, Iproclozide, Iproniazid, Isocarboxazid, Nialamide, Phenelzine, Selegiline, Toloxatone, Tranylcypromine |
| Reversible inhibitor of monoamine oxidase A (RIMA) |
Brofaromine, Moclobemide |
| Dopamine reuptake inhibitor (DARI) |
Amineptine, Phenmetrazine, Vanoxerine |
| Norepinephrine-dopamine reuptake inhibitors |
Bupropion |
| Norepinephrine reuptake inhibitor (NRI) or (NARI) |
Atomoxetine, Maprotiline, Reboxetine, Viloxazine |
| Serotonin-norepinephrine reuptake inhibitor (SNRI) |
Duloxetine, Milnacipran, Venlafaxine |
| Selective serotonin reuptake inhibitor (SSRI) |
Alaproclate, Etoperidone, Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Zimelidine |
| Selective serotonin reuptake enhancer (SSRE) |
Tianeptine |
| Tricyclic antidepressants (TCA) |
Amitriptyline, Amoxapine, Butriptyline, Clomipramine, Desipramine, Dibenzepin, Dothiepin, Doxepin, Imipramine, Iprindole, Lofepramine, Melitracen, Nortriptyline, Opipramol, Protriptyline, Trimipramine |
| Tetracyclic antidepressants |
Maprotiline, Mianserin, Nefazodone, Trazodone |
| Noradrenergic and specific serotonergic antidepressant (NaSSA) Mirtazapine |
Categories: Articles lacking sources | NPOV disputes | Serotonin-norepinephrine reuptake inhibitors | Pharmacology stubs |
