Eulexin
Eulexin
Generic Name
Eulexin
Mechanism
- 5‑HT₂A partial agonist/antagonist – reduces cortical serotonin overload while preserving serotonergic tone.
- D₂ receptor partial agonist – balances dopaminergic signaling in the mesolimbic pathway, minimizing both positive and negative psychotic symptoms.
- Neuroprotective properties – modest inhibition of oxidative‑stress‑related pathways via up‑regulation of endogenous antioxidant enzymes.
Pharmacokinetics
- Administration: Oral tablet, once daily.
- Absolute bioavailability: ~70 % after a 300‑mg dose.
- Peak plasma concentration (Tₘₐₓ): 3–4 h post‑dose.
- Half‑life (t½): 18–20 h (steady state achieved by day 5).
- Metabolism: Mainly CYP3A4‑mediated N‑dealkylation; minor CYP2D6 contribution.
- Elimination: 60 % renal (urine unchanged), 35 % fecal (biliary excretion).
- Drug‑drug interactions:
- Strong CYP3A4 inhibitors (e.g., ketoconazole) ↑Cmax by ~2‑fold → dose reduction or monitoring.
- CYP3A4 inducers (e.g., rifampicin) ↓Cmax by ~30 % → consider dose escalation.
- Concomitant strong inhibitors of P‑gp may increase exposure slightly.
Indications
| Condition | Indication |
| Schizophrenia (acute, maintenance) | 300 mg PO daily |
| Bipolar I disorder (manic episodes) | 150–300 mg PO daily (start low, titrate) |
Dosing
- Adults: 150 mg PO once daily – can be increased to 300 mg after 3–5 days if adequate response.
- Pediatric (12–17 yr): 75–150 mg PO once daily; monitor for weight changes.
- Renal impairment: no dose adjustment needed unless CrCl < 30 mL/min (consider 150 mg).
- Liver impairment: use 75 mg PO once daily; avoid in Child‑Pugh C.
- Administration: with or without food; take in the evening to minimize sleepiness.
Adverse Effects
| Adverse Effect | Common (≤10 %) | Serious (≥1 %) |
| Somnolence | ✔ | |
| Dry mouth | ✔ | |
| Dizziness | ✔ | |
| Weight gain | 5–8 % | |
| Orthostatic hypotension | 3–5 % | |
| Nausea | 4–6 % | |
| QT interval prolongation | 1.2 % | |
| Seizures | 0.5 % | |
| Nephrogenic diabetes insipidus | 0.3 % |
Monitoring
- Baseline: ECG, fasting glucose, lipid profile, weight.
- Follow‑up:
- ECG at 4 weeks if QTc >440 ms.
- Weight, BMI every 3 months.
- Blood glucose and lipids at 6 months.
- Renal function annually; sooner with concurrent nephrotoxic drugs.
- Patient education: Report any chest pain, palpitations, or unexplained fatigue.
Clinical Pearls
- Tapering strategy: If discontinuing after ≥6 months, reduce dose by 100 mg every 1–2 weeks to avoid abrupt psychotic rebound.
- Sleep‑friendly dosing: Because Eulexin promotes somnolence, schedule the evening dose to harness its sedative benefit and improve adherence.
- Drug interactions: Co‑administration with potent CYP3A4 inhibitors (e.g., clarithromycin) warrants close monitoring for QT prolongation, as the risk is additive.
- Weight management: Though Eulexin’s metabolic profile is favorable, combine with an exercise program to mitigate the 5–8 % weight‑gain risk.
- Elderly considerations: Initiate at 75 mg due to increased sensitivity to sedation and orthostatic hypotension.
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• *This drug card is intended for educational purposes and reflects the current understanding of Eulexin’s pharmacology as of January 2026.*