Products
Duloxetine is commercially available in the form of capsules (Cymbalta, generic). It has been approved in many countries since 2005.
Structure and properties
Duloxetine (C18H19NOS, Mr = 297.4 g/mol) is present in drugs as pure -duloxetine hydrochloride, a white to light brown powder that is sparingly soluble in water.
Effects
Duloxetine (ATC N06AX21) has antidepressant properties. The effects are due to selective and simultaneous inhibition of reuptake of serotonin and norepinephrine into presynaptic neurons.
Indications
For the treatment of depression, relapse prevention of unipolar depression, treatment of pain caused by diabetic neuropathy, and treatment of generalized anxiety disorder. In the EU, duloxetine is additionally approved for the treatment of women with moderate to severe stress incontinence (Yentreve). It is also registered in the United States for the treatment of fibromyalgia and chronic musculoskeletal pain.
Dosage
According to the SmPC. Duloxetine is usually taken once daily, independent of meals (urinary incontinence: twice daily). Discontinuation must be gradual.
Contraindications
- Hypersensitivity
- Therapy with MAO inhibitors such as selegiline
- Liver disease with hepatic dysfunction
- Severe renal dysfunction
- Duloxetine must not be combined with CYP1A2 inhibitors.
Full details of precautions and interactions can be found in the drug label.
Interactions
Duloxetine is biotransformed to inactive metabolites by CYP2D6 and CYP1A2. Combination with CYP1A2 inhibitors such as fluvoxamine, ciprofloxacin, or enoxacin is contraindicated because relevant increases in plasma levels may occur. Serotonin syndrome may develop with concomitant use of MAO inhibitors.
Adverse effects
The most common possible adverse effects include headache, nausea, dry mouth, drowsiness, and dizziness. These may disappear during the course of treatment. Other common side effects include decreased appetite, central disturbances, tremor, formication, tinnitus, palpitations, flushing, yawning, digestive disturbances such as diarrhea and vomiting, sweating, skin rash, muscle discomfort, erectile dysfunction, fatigue, and abdominal pain. Rarely, severe side effects are possible (including serotonin syndrome, seizures, suicide, hypertensive crisis, liver failure, Stevens-Johnson syndrome).
In popular culture.
In the TV series, the protagonist Clay Jensen has been treated with duloxetine in the past.
