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MAO-B Inhibitor — Parkinson's Disease Pregnancy: There are no data from use in pregnant women; animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure it is preferable to avoid the use of rasagiline during pregnancy. Breast-feeding: non-clinical data indicate that rasagiline inhibits prolactin secretion and may therefore inhibit lactation; it is not known whether rasagiline is excreted in human milk — caution should be exercised in breast-feeding mothers (section 4.6).

Rasagiline

Brand names: Azilect

Rasagiline is an irreversible, selective monoamine oxidase-B (MAO-B) inhibitor used in Parkinson's disease, both as monotherapy in early disease and as an adjunct to levodopa in more advanced disease.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 1 mg once daily (one 1 mg tablet), taken with or without levodopa
Route: Oral (may be taken with or without food)
Frequency: Once daily
The UK SPC states a single recommended dose of 1 mg once daily for Parkinson's disease, as monotherapy or as adjunct to levodopa; no titration schedule and no separate maximum dose are given. Elderly: no change in dose is required. Hepatic impairment: contraindicated in severe impairment; use should be avoided in moderate impairment; caution when initiating in mild impairment, and rasagiline should be stopped if a patient progresses from mild to moderate impairment. Paediatric: safety and efficacy in children and adolescents have not been established and there is no relevant use in the paediatric population for Parkinson's disease. US labelling differs — as adjunct to levodopa the recommended initial dose is 0.5 mg once daily, increased to 1 mg once daily if tolerated but the clinical response is insufficient, and a maximum of 0.5 mg once daily is recommended in patients taking ciprofloxacin or other CYP1A2 inhibitors and in mild hepatic impairment (openFDA) — verify against the UK SPC before applying. US labelling also warns that recommended doses should not be exceeded because of the risk of hypertension.

Dose adjustments

Renal

No special precautions are required in patients with renal impairment (section 4.2).

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • Hypersensitivity to the active substance or to any of the excipients
  • Concomitant treatment with other monoamine oxidase (MAO) inhibitors, including medicinal and natural products available without prescription such as St John's wort
  • Concomitant pethidine (meperidine) — at least 14 days must elapse between discontinuing rasagiline and starting an MAO inhibitor or pethidine
  • Severe hepatic impairment
  • US labelling additionally contraindicates tramadol, methadone, propoxyphene, cyclobenzaprine and dextromethorphan (risk of serotonin syndrome, or of psychosis/bizarre behaviour with dextromethorphan) — openFDA

Side effects

  • Monotherapy: headache (very common), depression, vertigo, influenza and rhinitis, arthritis, musculoskeletal and neck pain (common)
  • Adjunct to levodopa: dyskinesia (very common), orthostatic hypotension, falls, abdominal pain, constipation, nausea and vomiting, dry mouth (common)
  • Hallucinations and abnormal dreams (common); impulse control disorders including compulsions, obsessive thoughts, pathological gambling, hypersexuality and compulsive spending (frequency not known)
  • Excessive daytime sleepiness and sudden sleep onset episodes (frequency not known); serotonin syndrome (frequency not known)
  • Skin melanoma and skin carcinoma (uncommon) — evaluate any suspicious or changing skin lesion; hypertension (frequency not known); decreased appetite, fever, malaise

Interactions

  • Other MAO inhibitors (including over-the-counter and herbal products such as St John's wort) and pethidine — contraindicated; allow at least 14 days after stopping rasagiline before starting them
  • Fluoxetine and fluvoxamine — concomitant use should be avoided; allow at least 5 weeks between stopping fluoxetine and starting rasagiline, and at least 14 days between stopping rasagiline and starting fluoxetine or fluvoxamine
  • Dextromethorphan and sympathomimetics (e.g. nasal and oral decongestants or cold remedies containing ephedrine or pseudoephedrine) — concomitant use is not recommended
  • Levodopa — rasagiline potentiates its effects: levodopa adverse reactions may be increased and pre-existing dyskinesia exacerbated (reducing the levodopa dose may help); hypotensive effects have been reported with concomitant use
  • CYP1A2 inhibitors such as ciprofloxacin — US labelling limits the rasagiline dose to 0.5 mg once daily (openFDA)

Clinical monograph

How it works

By selectively and irreversibly inhibiting MAO-B, it reduces the breakdown of dopamine in the brain, thereby enhancing dopaminergic transmission.

Prescribing in practice

  • It should not be combined with pethidine, and concurrent use with other MAO inhibitors or sympathomimetics carries a risk of serotonin syndrome or hypertensive reactions, so combinations must be reviewed carefully.
  • When used as an adjunct to levodopa it can increase dopaminergic adverse effects such as dyskinesia, which may require a reduction in the levodopa dose.
  • Caution is needed in hepatic impairment, as systemic exposure is increased.

Monitoring

Monitor for dopaminergic effects, dyskinesia, impulse-control behaviours and any features suggestive of serotonin toxicity when combined with serotonergic drugs.

Counselling the patient

  • Report any new gambling, compulsive shopping, hypersexuality or binge-eating behaviour, as impulse-control disorders can occur with dopaminergic therapy.
  • Tell any prescriber you take rasagiline before starting new medicines, particularly antidepressants and certain painkillers.
  • Daytime sleepiness and sudden onset of sleep can occur, which may affect driving.

Evidence & guidelines

Rasagiline's efficacy in early and adjunctive Parkinson's disease was demonstrated in randomised trials including the TEMPO and PRESTO studies, and it is recommended as a treatment option by NICE.

Reference: NICE NG71; TEMPO Trial; ADAGIO Trial; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.