agomelatine: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
agomelatine: clinical details
Prescribing considerations
- Assess hepatic risk factors, including obesity, fatty liver disease, diabetes, substantial alcohol intake and concurrent hepatotoxic medicines.
- Use caution with bipolar disorder or a history of mania or hypomania, and discontinue if manic symptoms develop.
- Clinical data are limited in moderate or severe renal impairment.
- Not recommended for people under 18; it should not be used in adults aged 75 years or older.
- Monitor clinical worsening, suicidality and unusual behavioural change, particularly early in treatment and following treatment changes.
Contraindications and cautions
- Hepatic impairment, including cirrhosis or active liver disease.
- Baseline ALT or AST exceeding three times the upper limit of normal.
- Concurrent potent CYP1A2 inhibitors, including fluvoxamine or ciprofloxacin.
- Hypersensitivity to agomelatine or product excipients.
Monitoring
- Obtain baseline liver-function tests.
- Repeat liver-function tests periodically during treatment and whenever clinically indicated.
- Repeat testing promptly if transaminases rise; discontinue if they exceed three times the upper limit of normal.
- Discontinue immediately for clinical features of possible liver injury and monitor until transaminases normalise.
- Monitor mood, suicidality and emergence of mania or hypomania.
Clinical pharmacology
Agomelatine is an MT1/MT2 receptor agonist and 5-HT2C antagonist. It is rapidly absorbed but has low, variable oral bioavailability because of first-pass metabolism, mainly through CYP1A2, with lesser CYP2C9 and CYP2C19 involvement. Inactive metabolites are eliminated mainly in urine.
Formulation and product differences
- Both selected products are film-coated oral tablets.
- The selected Valdoxan formulation contains lactose; the selected Zentiva formulation lists mannitol and does not list lactose.
- Valdoxan requires no special storage conditions; Agomelatine Zentiva should be kept in its original packaging to protect it from moisture.
- Tablet appearance, dimensions, excipients, blister materials and available pack sizes differ between products.
agomelatine preparations and strengths
Tablet
Route: Oral
Strengths: 25 mg
agomelatine interactions
Check all prescribed, over-the-counter and herbal products with a pharmacist or prescriber. Important examples include:
Fluvoxamine
Strongly inhibits agomelatine metabolism and must not be used with it because exposure can rise substantially.
Ciprofloxacin
Strongly inhibits CYP1A2 and is contraindicated with agomelatine.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.