Schedule H

Oral

Formulation Type Strengths Available

Tablets 5 mg

Orally Disintegrating Tablets 5 mg

Note: Selegiline is also available in some fixed-dose combinations with Levodopa-Carbidopa. Transdermal patch formulations are NOT AVAILABLE in India.

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Idiopathic Parkinson's Disease (Adjunct to Levodopa-Carbidopa)

Used to reduce motor fluctuations ("wearing-off" phenomenon) in patients already receiving Levodopa therapy.

Parameter Dosing

Starting dose 5 mg orally once daily in the morning

Titration May increase to 5 mg twice daily (morning and midday) after 2–4 weeks if tolerated

Usual maintenance dose 5–10 mg/day in 1–2 divided doses

Maximum dose 10 mg/day

Clinical Notes:

• Administer with breakfast and lunch; avoid evening dosing to prevent insomnia

• Doses exceeding 10 mg/day lose MAO-B selectivity and increase risk of hypertensive crisis

• When adding to established Levodopa therapy, consider reducing Levodopa dose by 10–30% to minimise dyskinesias

• Not recommended as monotherapy for Parkinson's disease in Indian practice due to limited efficacy

1. Early Parkinson's Disease (Monotherapy — Limited Use)

Parameter Dosing

Starting dose 5 mg once daily in the morning

Titration May increase to 5 mg twice daily after 4 weeks

Usual maintenance dose 10 mg/day

Maximum dose 10 mg/day

Clinical Notes:

• Modest symptomatic benefit as monotherapy

• May delay need for Levodopa initiation in early disease

• Transition to Levodopa-based therapy typically required as disease progresses

Secondary Indications — Adults (Off-label)

Indication Dose Duration Notes Evidence Basis

Treatment-Resistant Depression 5–10 mg/day in divided doses (morning and midday) Minimum 6–8 weeks trial OFF-LABEL; Specialist psychiatrist only; Contraindicated with serotonergic antidepressants Limited RCT data; not standard practice in India

PAEDIATRIC DOSING (Specialist Only)

Primary Indications

Not applicable. Selegiline is NOT RECOMMENDED for use in children and adolescents below 18 years of age due to absence of safety and efficacy data.

Secondary Indications — Paediatric (Off-label)

Not applicable.

Clear Statement: Use in paediatric population is not established. Any use in rare paediatric movement disorders is strictly OFF-LABEL and must be under specialist paediatric neurologist supervision only.

• Concurrent use with meperidine (pethidine) — risk of severe serotonin syndrome or opioid toxicity reaction

• Concurrent use with serotonergic drugs: SSRIs, SNRIs, tricyclic antidepressants, St. John's Wort — contraindicated or require minimum 14-day washout period before initiating Selegiline (5 weeks for fluoxetine)

• Concurrent use with non-selective MAO inhibitors

• Concurrent use with tramadol or dextromethorphan

• Pheochromocytoma

• Known hypersensitivity to Selegiline or any excipient

• Severe hepatic insufficiency

• Cardiovascular disease including uncontrolled hypertension — monitor blood pressure

• History of psychosis, hallucinations, or impulse control disorders — may exacerbate

• Peptic ulcer disease — potential for GI adverse effects

• Concomitant tyramine-rich diet at doses exceeding 10 mg/day — risk of hypertensive crisis

• History of melanoma or suspicious skin lesions — theoretical concern with dopaminergic therapy

• Elderly patients — increased susceptibility to orthostatic hypotension, falls, confusion

• Abrupt discontinuation — avoid; taper gradually to prevent rebound motor symptoms

• Concomitant Levodopa therapy — may require Levodopa dose reduction

Parameter Details

Risk category Limited human data; animal studies inconclusive; not formally classified in India

Preferred alternatives Levodopa-Carbidopa alone under neurologist supervision if antiparkinsonian therapy essential

When it may be used Only if maternal benefit clearly outweighs potential fetal risk; specialist supervision mandatory

Monitoring Fetal growth parameters, maternal blood pressure, uterine activity

Parameter Details

Compatibility Not recommended; excretion in human milk unknown

Drug levels in milk Unknown

Preferred alternatives Consider alternative antiparkinsonian therapy or avoid breastfeeding

Monitoring in infant If inadvertent exposure: sleep disturbances, feeding difficulties, irritability, excessive sedation

Parameter Recommendation

Starting dose 2.5–5 mg once daily in the morning

Titration Slower than younger adults; increase after 1–2 weeks if tolerated

Extra risks Orthostatic hypotension and falls, confusion, hallucinations, vivid dreams, insomnia

Special considerations Monitor blood pressure (lying and standing); assess cognitive and psychiatric status regularly; polypharmacy increases interaction risk

Interacting Drug Effect Recommendation

SSRIs (Fluoxetine, Sertraline, Paroxetine, Escitalopram) Serotonin syndrome — potentially fatal Contraindicated; washout 14 days before Selegiline (5 weeks for Fluoxetine)

SNRIs (Venlafaxine, Duloxetine) Serotonin syndrome risk Contraindicated; washout 14 days

Tricyclic antidepressants (Amitriptyline, Imipramine) Serotonin syndrome, hypertensive crisis Contraindicated; washout 14 days

Meperidine (Pethidine) Severe reaction — agitation, rigidity, hyperthermia, cardiovascular collapse Contraindicated

Tramadol Serotonin syndrome risk Contraindicated

Dextromethorphan CNS toxicity, serotonin syndrome Contraindicated

Non-selective MAO inhibitors Hypertensive crisis Contraindicated

Linezolid MAO inhibition — serotonin syndrome risk Avoid; if life-threatening infection, specialist supervision only

Sympathomimetic amines (Pseudoephedrine, Phenylephrine) Hypertensive reaction Avoid combination

Interacting Drug Effect Recommendation

Levodopa-Carbidopa Enhanced dopaminergic effects; increased dyskinesias May require 10–30% reduction in Levodopa dose

Antihypertensives Additive hypotensive effect Monitor blood pressure closely

Rasagiline, Safinamide Overlapping MAO-B inhibition Avoid combination — no additional benefit, increased risk

Dopamine agonists (Pramipexole, Ropinirole) Additive dopaminergic effects Monitor for dyskinesias, hallucinations, impulse control disorders

Ciprofloxacin (CYP1A2 inhibitor) May increase Selegiline levels Monitor for adverse effects

Tyramine-rich foods (aged cheese, fermented foods, red wine) Hypertensive crisis at doses >10 mg/day Counsel patients; maintain dietary restrictions if using higher doses

Opioids (other than meperidine/tramadol) Potential for enhanced CNS effects Use with caution; monitor

• Nausea, dry mouth

• Dizziness, lightheadedness

• Insomnia, sleep disturbances

• Headache

• Orthostatic hypotension

• Dyskinesias (when combined with Levodopa)

• Vivid dreams

• Constipation

• Abdominal discomfort

• Serotonin syndrome (with serotonergic drugs) — requires immediate discontinuation and supportive care

• Hallucinations, psychosis, confusion — particularly in elderly

• Hypertensive crisis (with tyramine-rich foods at doses >10 mg/day or with sympathomimetics)

• Severe dyskinesias

• Impulse control disorders (pathological gambling, hypersexuality, compulsive behaviours)

• Melanoma — theoretical association with dopaminergic therapy; skin surveillance recommended

• Suicidal ideation (rare; primarily in depression use)

Phase Parameters to Monitor

Baseline Blood pressure (lying and standing), liver function tests (if hepatic comorbidity), cognitive and psychiatric status, skin examination for suspicious lesions, complete medication review for interactions

After initiation / dose change Blood pressure at 1–2 weeks, motor symptom response, emergence of dyskinesias, sleep quality, psychiatric symptoms

Long-term Motor fluctuations, dyskinesias, psychiatric status (hallucinations, impulse control), annual skin examination, blood pressure periodically

Note: Eldepryl (originator brand) has limited availability in India. Some fixed-dose combinations with Levodopa-Carbidopa may be available.

Note: Selegiline is NOT included in NLEM India 2022; prices are not NPPA-controlled. Availability may vary across regions.

• Timing is critical: Always dose in the morning (and midday if twice daily) — never in the evening to avoid insomnia.

• Respect the 10 mg ceiling: Doses exceeding 10 mg/day lose MAO-B selectivity and significantly increase risk of hypertensive crisis and serotonin syndrome.

• Reduce Levodopa when adding Selegiline: A 10–30% reduction in Levodopa dose may be needed to prevent worsening dyskinesias.

• Avoid serotonergic drugs: Cross-check all medications — SSRIs, SNRIs, TCAs, tramadol, meperidine, and dextromethorphan are contraindicated.

• Washout periods matter: At least 14 days (5 weeks for fluoxetine) washout required before starting Selegiline after discontinuing serotonergic antidepressants; similarly, wait 14 days after stopping Selegiline before initiating serotonergic drugs.

• Not ideal as monotherapy: In Indian practice, Selegiline is primarily used as adjunct to Levodopa; monotherapy provides only modest symptomatic benefit.

Selegiline; MAO-B inhibitor; Parkinson's disease; adjunct therapy; motor fluctuations; wearing-off; serotonin syndrome risk; Schedule H; elderly-caution; pregnancy-avoid; Neurology

RxIndia v1.0 — 11 Jun 2025

• CDSCO approved product inserts

• Indian Pharmacopoeia

• API Textbook of Medicine

• AIIMS Neurology Drug Protocols

• Goodman & Gilman's The Pharmacological Basis of Therapeutics

• Harrison's Principles of Internal Medicine, 21st edition

• Parkinson's Disease Society of India clinical protocols

• International RCTs (for off-label depression indication — clearly marked)