Selegiline (selegiline hydrochloride)
OTHER BRAND NAMES
Monoamine oxidase inhibitor (MAOI) (type B)
Adjunct in the management of parkinsonian patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy.
Adjunct in the Management of Patients Being Treated w/ Levodopa/Carbidopa Who Exhibit Deterioration in the Quality of Response to this Therapy:
Usual: 10mg/day as divided doses of 5mg each taken at breakfast and lunch
After 2-3 days of therapy, may attempt to reduce levodopa/carbidopa dose; during continued therapy, further reductions of levodopa/carbidopa may be possible
Take in divided doses at breakfast and lunch
Tab: 5mg; (Eldepryl) Cap: 5mg
Concomitant use with meperidine or other opioids.
Do not use at doses >10mg/day due to risks associated with nonselective inhibition of MAO. Exacerbation of levodopa-associated side effects may occur; may mitigate effects by reducing levodopa/carbidopa dose by 10-30%. Observe closely for atypical responses. Patients with Parkinson's disease have a higher risk of developing melanoma; monitor for melanomas frequently and on a regular basis.
Nausea, dizziness/lightheadedness/fainting, abdominal pain, confusion, hallucinations, dry mouth.
See Contraindications. Avoid with SSRIs (eg, fluoxetine, sertraline, paroxetine) and TCAs (eg, amitriptyline, protriptyline); severe toxicity reported. At least 14 days should elapse between discontinuation of selegiline and initiation of TCAs or SSRIs. At least 5 weeks (longer with chronic/high-dose fluoxetine) should elapse between discontinuation of fluoxetine and initiation of selegiline due to long T1/2 of fluoxetine and its active metabolite. Hypertensive crises/reactions reported with ephedrine or tyramine-containing foods.
PREGNANCY AND LACTATION
Category C, caution in nursing.
MECHANISM OF ACTION
MAOI (Type B); not established. Irreversibly inhibits MAO type B (selectivity is dose-dependent), blocking the catabolism of dopamine. May also act through other mechanisms to increase dopaminergic activity.
Absorption: Cmax=1ng/mL. Metabolism: Extensive (presumably attributable to presystemic clearance in gut and liver); N-desmethylselegiline (active major metabolite), L-amphetamine and L-methamphetamine (major metabolites). Elimination: T1/2=2 hrs (single dose), 10 hrs (steady state).
Assess for drug hypersensitivity, pregnancy/nursing status, and possible drug interactions.
Monitor for exacerbation of levodopa-associated side effects, atypical responses, and other adverse reactions. Monitor for melanomas frequently and on a regular basis.
Advise of the possible need to reduce levodopa dosage after initiation of therapy. Instruct not to exceed 10mg/day and explain the risk of using higher daily doses; provide a brief description of the 'cheese reaction.' Inform about the signs and symptoms associated with MAOI-induced hypertensive reactions; instruct to immediately report to physician any severe headache or other atypical/unusual symptoms not previously experienced. Instruct to inform physician if new or increased gambling urges, increased sexual urges, or other intense urges develop.
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