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Published online by Cambridge University Press: 06 October 2020
THERAPEUTICS
Brands
• Cymbalta, Xeristar, Yentreve, Ariclaim
Generic?
• Yes
Class
• Serotonin and norepinephrine reuptake inhibitor (SNRI)
Commonly Prescribed for
(FDA approved in bold)
• Major depressive disorder
• Diabetic peripheral neuropathic pain
• Generalized anxiety disorder (GAD)
• Fibromyalgia
• Chronic musculoskeletal pain
• Stress urinary incontinence
• Migraine or tension-type headache prophylaxis
• Other painful peripheral neuropathies
• Depression secondary to stroke
• Binge-eating disorder
• Post-traumatic stress disorder
• Attention deficit hyperactivity disorder
• Perimenopausal/menopausal hot flushes
• Cataplexy
How the Drug Works
• It blocks serotonin and norepinephrine reuptake transporters (SERT, NET), increasing serotonin and norepinephrine levels within hours, but antidepressant effects take weeks. Effect is more likely related to adaptive changes in serotonin and norepinephrine receptor systems over time
• Weakly blocks dopamine reuptake pump (dopamine transporter)
• Interacts with opioid receptors and α2-adrenergic receptor
• Inhibition of serotonin and norepinephrine reuptake in Onuf's nucleus in the sacral spinal cord may increase urethral closure pressure
• Duloxetine has 100-fold or higher affinity for human and rat SERT and at least 300-fold higher affinity for NET in vitro compared to venlafaxine
How Long Until It Works
• Migraines: effective in as little as 2 weeks, but can take up to 10 weeks on a stable dose to see full effect
• Tension-type headache prophylaxis: effective in 4–8 weeks
• Neuropathic pain: usually some effect within 4 weeks
• Diabetic neuropathy: may have significant improvement with high doses within 6 weeks
• Depression: 2 weeks but up to 2 months for full effect
If It Works
• Migraine/tension-type headache: goal is a 50% or greater reduction in headache frequency or severity. Consider tapering or stopping if headaches remit for more than 6 months or if considering pregnancy
• Neuropathic pain: the goal is to reduce pain intensity and symptoms, but usually does not produce remission. Continue to use and monitor for AE
• Diabetic neuropathy: the goal is to reduce pain intensity and reduce use of analgesics, but usually does not produce remission. Continue to use and maintain strict glycemic control and diabetic management
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