Schedule H

Oral

• Tablet 0.5 mg

• Tablet 1 mg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

▶ Parkinson's Disease (Idiopathic) — Monotherapy (Early Disease)

Parameter Recommendation

Starting dose 1 mg once daily

Titration Not required

Usual maintenance dose 1 mg once daily

Maximum dose 1 mg/day

Clinical Notes:

• Suitable as initial symptomatic treatment in early Parkinson's disease

• May delay initiation of levodopa therapy

• Administer at the same time each day; can be taken with or without food

▶ Parkinson's Disease (Idiopathic) — Adjunct to Levodopa (Moderate-Advanced Disease)

Parameter Recommendation

Starting dose 0.5–1 mg once daily

Titration Not typically required

Usual maintenance dose 1 mg once daily

Maximum dose 1 mg/day

Clinical Notes:

• Use in combination with levodopa ± other antiparkinsonian agents

• Reduces daily "off" time by approximately 1 hour in patients with motor fluctuations

• Assess for increased dyskinesias; levodopa dose reduction may be needed

• Higher doses do not provide additional benefit and increase adverse effect risk

Secondary Indications — Adults (Off-label, if any)

Indication Dose Notes

Parkinson's disease with refractory motor fluctuations (OFF-LABEL) 1 mg once daily Specialist only; used when other adjuncts inadequate

Evidence basis: International RCTs (TEMPO, PRESTO trials); Indian movement disorder specialist practice consensus

Age Group Recommendation

< 18 years Not recommended

Notes:

• Safety and efficacy not established in children or adolescents

• No off-label paediatric indications supported by Indian/WHO/IAP guidance

• Not included in current Indian paediatric neurology protocols

Secondary Indications — Paediatrics (Off-label)

Not applicable.

Severe impairment (eGFR < 30) Use with caution; limited data

End-stage renal disease / Dialysis Avoid; insufficient evidence

• Severe hepatic impairment

• Concurrent use with other MAO inhibitors (including selegiline, linezolid, methylene blue)

• Concurrent use with meperidine, tramadol, propoxyphene, or dextromethorphan

• Known hypersensitivity to rasagiline or any excipient

• Concomitant use with serotonergic antidepressants (SSRIs, SNRIs, TCAs) — risk of serotonin syndrome

• Sympathomimetic agents (nasal/oral decongestants) — potential for hypertensive episodes

• Tyramine-rich foods — theoretical risk of hypertensive crisis; rare at therapeutic doses

• May exacerbate dyskinesias when combined with levodopa

• Orthostatic hypotension, particularly in combination therapy

• Patients with history of psychosis or impulse control disorders

Parameter Details

Overall Safety Limited human data; avoid if alternatives exist

Risk Category No formal Indian classification; use only if benefit clearly outweighs risk

Teratogenicity No teratogenic effects in animal studies; insufficient human data

Preferred Alternative Levodopa-carbidopa if treatment essential

Monitoring Fetal growth, maternal blood pressure; neurologist consultation advised

Parameter Details

Compatibility Not recommended during breastfeeding

Milk Excretion Excreted in animal milk; no human data available

Preferred Alternative Levodopa-carbidopa if treatment essential

Infant Monitoring Feeding difficulty, somnolence, poor weight gain

Parameter Recommendation

Starting dose 1 mg once daily (same as adults)

Titration Not required

Dose reduction Not needed based on age alone

Special Considerations:

• Increased susceptibility to orthostatic hypotension and falls

• Monitor for neuropsychiatric effects (hallucinations, confusion)

• Review polypharmacy for drug interactions

• Assess cognitive status at baseline and periodically

Interacting Drug Effect Management

MAO inhibitors (selegiline, linezolid, methylene blue) Additive MAO inhibition; hypertensive crisis risk Contraindicated

Meperidine, tramadol, methadone, propoxyphene Severe CNS toxicity; serotonin syndrome Contraindicated

Dextromethorphan CNS toxicity; psychosis/bizarre behaviour Contraindicated

SSRIs, SNRIs, TCAs Serotonin syndrome risk Avoid; if essential, use lowest dose under specialist supervision

St. John's Wort Additive serotonergic effect Avoid combination

Interacting Drug Effect Management

Levodopa Increased dyskinesia risk May require levodopa dose reduction

CYP1A2 inhibitors (ciprofloxacin, fluvoxamine) Increased rasagiline plasma levels Monitor for adverse effects; consider dose adjustment

Sympathomimetics (pseudoephedrine, phenylephrine) Risk of hypertension Monitor blood pressure; avoid if possible

Tobacco smoking CYP1A2 induction reduces rasagiline levels May reduce efficacy; advise smoking cessation

Antihypertensives Additive hypotensive effect Monitor for orthostatic hypotension

• Headache

• Arthralgia

• Dyspepsia / Nausea

• Insomnia

• Peripheral oedema

• Orthostatic hypotension (particularly with levodopa)

• Depression

• Dizziness

• Flu-like symptoms

Adverse Effect Notes

Serotonin syndrome Especially with concurrent serotonergic agents; discontinue immediately

Hallucinations / Psychosis More common in combination therapy; may require dose reduction

Severe dyskinesias Dose-dependent; typically with levodopa co-administration

Impulse control disorders Pathological gambling, hypersexuality, compulsive behaviours

Melanoma Theoretical class risk; regular dermatological surveillance advised

Hypertensive crisis Rare at 1 mg/day; mainly with MAO inhibitor/tyramine interactions

Phase Parameters

Baseline Blood pressure (supine and standing); neuropsychiatric assessment; skin examination

After initiation / dose change Dyskinesia assessment (if on levodopa); orthostatic hypotension; confusion/hallucinations

Long-term Periodic liver function tests; mood and impulse control assessment; annual skin examination for melanoma

• Reselient® (Sun Pharma)

• Rasipar® (Intas)

• Rasalect® (Cipla)

• Rasinex® (Lupin)

• AgiOne® (Dr. Reddy's)

Notes:

• Not currently under NLEM price control

• Prices reflect private retail market (may vary by region and brand)

1. Monotherapy vs adjunct: Rasagiline is effective both as initial monotherapy in early disease and as adjunct to levodopa for motor fluctuations.

1. Serotonin syndrome risk: Though rare at 1 mg/day, avoid concurrent serotonergic agents; if essential, use lowest effective doses with close monitoring.

1. Levodopa dose adjustment: When adding rasagiline to levodopa, anticipate dyskinesias and consider reducing levodopa dose by 10–30%.

1. Tyramine restriction: Strict dietary restrictions unnecessary at 1 mg/day; however, advise patients to avoid large quantities of aged cheese, fermented foods, or draft beer.

1. Elderly patients: Exercise caution due to increased risk of orthostatic hypotension and neuropsychiatric effects; review concurrent antihypertensives.

1. Switching from selegiline: Allow at least 14-day washout before starting rasagiline to prevent MAO inhibitor overlap.

Rasagiline; Parkinson's disease; MAO-B inhibitor; levodopa-adjunct; motor fluctuations; elderly-safe; serotonin-syndrome-risk; neuropsychiatric-effects; Schedule H

RxIndia v0.4 — 25 Jan 2025

• CDSCO approved product information

• Indian Pharmacopoeia / National Formulary of India

• API Textbook of Medicine

• AIIMS Neurology Treatment Protocols

• Goodman & Gilman's The Pharmacological Basis of Therapeutics

• International RCTs: TEMPO and PRESTO trials (for off-label evidence context)