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MAO-B Inhibitor — Parkinson's Disease Pregnancy: Avoid — insufficient safety data

Selegiline

Brand names: Eldepryl, Zelapar (buccal)

Adult dose

Dose: Standard tablet: 5 mg twice daily (morning and midday); Zelapar buccal: 1.25 mg once daily
Route: Oral (tablet) or oromucosal (Zelapar)
Frequency: Twice daily (tablet — take with breakfast and lunch to avoid insomnia); Once daily (Zelapar)
Max: 10 mg/day (tablet); 2.5 mg/day (Zelapar)
Avoid evening doses — metabolised to amphetamine derivatives causing insomnia. Zelapar buccal avoids first-pass metabolism — lower doses required, higher bioavailability. Take tablets with food. Irreversible MAO-B inhibition — 2-week washout before serotonergic agents.

Paediatric dose

Route:
Seek specialist opinion — not licensed in paediatrics

Dose adjustments

Renal

Use with caution in renal impairment — no specific dose adjustment

Hepatic

Use with caution — hepatic metabolism

Clinical pearls

  • Older MAO-B inhibitor than rasagiline — both irreversible, but rasagiline has cleaner metabolite profile (no amphetamine derivatives)
  • At standard doses, selegiline is MAO-B selective; at high doses, MAO-A selectivity lost — tyramine restriction ('cheese effect') not usually required at therapeutic doses
  • Still widely used, particularly in patients already established on it — rasagiline generally preferred for de novo initiation
  • 2-week washout mandatory before starting any serotonergic drug — MAO-B inhibition is irreversible

Contraindications

  • Concurrent meperidine (pethidine) — fatal serotonin syndrome risk
  • Concurrent SSRIs or SNRIs — serotonin syndrome
  • Concurrent tramadol or dextromethorphan
  • Pheochromocytoma

Side effects

  • Insomnia (if dosed in evening)
  • Nausea
  • Dry mouth
  • Confusion and hallucinations (especially elderly)
  • Hypotension
  • Dyskinesias (when combined with levodopa)
  • Amphetamine-type effects (metabolites: amphetamine, methamphetamine)

Interactions

  • Meperidine/pethidine — absolute contraindication (hyperpyrexia, serotonin syndrome, death)
  • SSRIs/SNRIs — serotonin syndrome
  • Tramadol, dextromethorphan, linezolid — serotonin syndrome
  • Levodopa — enhanced effects, may require levodopa dose reduction
  • Sympathomimetics — exaggerated pressor response

Monitoring

  • BP (especially orthostatic)
  • Neuropsychiatric assessment
  • Sleep assessment
  • LFTs baseline

Reference: BNFc; BNF 90; NICE NG71 (Parkinson's Disease); DATATOP Trial. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.

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