Ballicules.com

Selegiline

ELDEPRYL

What it isSelective MAO-B inhibitor; Parkinson disease, and transdermally for depression.

Why this oneAt low oral dose it spares MAO-A so no dietary restriction is needed, and the patch bypasses gut MAO-A for depression.

What limits itSelectivity is lost at higher doses, restoring tyramine risk. Amphetamine metabolites cause insomnia; serotonin syndrome with SSRIs.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Parkinson's disease (adjunct to levodopa/carbidopa)Adult1.25 mg QD2.5 mg QD2.5 mg/day

Titration Maintain 1.25 mg once daily for at least 6 weeks before increasing to 2.5 mg once daily

Renal No adjustment for mild–moderate (CLcr 30–89); not recommended if CLcr <30 or ESRD

Hepatic Reduce to 1.25 mg in mild–moderate (Child-Pugh 5–9); not recommended in severe (Child-Pugh >9)

Doses >2.5 mg/day provide no added benefit and should be avoided

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy No adequate human data; animal developmental toxicity (decreased embryofetal/postnatal growth and survival)

Lactation No data; breastfeeding not recommended during treatment and for 7 days after final dose (risk of hypertensive reactions)

NO BOXED WARNINGS

No boxed warning for oral selegiline for Parkinson disease, but EMSAM, the transdermal patch for depression carries a boxed warning for suicidal thoughts and behaviors in patients under 25.

Principal riskSelectivity lost at higher doses, restoring tyramine risk

Cost, est. cash$300–$5,000/month

Generic entryLong generic

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability1 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryC

Defining liabilityOrthostasis, hallucinations, dyskinesia and impulse-control symptoms; abrupt withdrawal can be hazardous.

Mechanism of action: Selegiline ballicule

Selegiline ballicule: receptor binding, kinetics and half-life diagram

Open Selegiline in the interactive console ↗

Memory aids: mascots and interaction avatars

Selegiline ELDEPRYL mascot mnemonic cartoon
“Elderly Seal’s gills”
Mao Zedong → MAO inhibitor
Selegiline CYP2B6 substrate avatar
CYP2B6 substrate

Open Selegiline in the interactive console ↗