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L-deprenyl (Selegiline, Eldepryl, Emsam, Zelapar)

Indications: 1) treatment of the symptoms of Parkinson's disease 2) adjunctive treatment to carbidopa/L-dopa 3) symptomatic treatment of Alzheimer's disease Contraindications: - coadministration of dextromethorphan, meperidine, methadone, propoxyphene Dosage: 1) 5 mg PO BID (breakfast & lunch dosing) 2) after 2-3 days of treatment, try to decreased L-dopa/ carbidopa by 30-30% 3) giving the dose in the evening increases insomnia & nightmares 4) doses > 10 mg/day decreases MAO-B selectivity 5) transdermal patch: 1 patch QD - apply to dry, intact skin on upper torso, upper thigh, or outer surface of upper arm 6) Zelapar 1.25-2.5 mg PO QD Tabs: 5 mg. Transdermal patch: (Emsam) 6, 9, 12 mg [9] (box of 30) Zelapar: 1.25 mg, 2.5 mg Pharmacokinetics: 1) about 75% of oral dose is absorbed from the GI tract 2) metabolized by the liver 3) metabolized to 2 amphetamine derivatives that enhance release & decrease re-uptake of dopamine 4) excreted in the urine Adverse effects: 1) common (> 10%) - mood changes, dyskinesias, dizziness, dry mouth, nausea/vomiting, insomnia, abdominal pain 2) less common (1-10%) - orthostatic hypotension, arrhythmias, hypertension, hallucinations, confusion, depression, insomnia, agitation, increased involuntary movements, bradykinesia, bruxism, muscle twitches 3) other - nightmares - ataxia - tachycardia Drug interactions: 1) meperidine: mechanism unknown; fatal reactions have occurred 2) use in combination with: a) other antidepressants - selective serotonin re-uptake inhibitors (SSRI) - tricyclic antidepressants (TCA) b) buspirone, cyclobenzaprine, dextromethorphan, meperidine, methadone, propoxyphene tramadol, St. John's wort can cause serotonin syndrome [9] 3) amphetamines, pseudoephedrine, phenylephrine in combination may result in excessive sympathetic stimulation... hypertension 4) carbamazepine, oxcarbazepine in combination can increase deprenyl levels [9] Mechanism of action: 1) selective MAO-B inhibitor - MAO-B accounts for 70% of MAO in brain 2) in contrast to nonspecific MAO inhibitors, deprenyl does NOT cause profound & potentially lethal potentiation of catechol- amines when administered concurrently with indirect sympatho- mimetic amines 3) inhibits CNS degradation of dopamine 4) potentiates the effects of L-dopa 5) metabolized to 2 amphetamine derivatives that enhance release & decrease re-uptake of dopamine 6) it has been suggested that MAO-B inhibitors may slow the progression of Parkinson's disease; however, this issue is controversial 7) symptomatic improvement in Alzheimer's disease -> does not alter the course of the disease [8]

Interactions

drug interactions drug adverse effects (more general classes)

Related

Alzheimer's disease (AD) monoamine oxidase [MAO]-B Parkinson's disease (paralysis agitans, PD)

General

alkyne amine aromatic compound monoamine oxidase [MAO] inhibitor pharmacologic agents for treatment of Parkinson's disease

Properties

SIZE: hcl salt = 223.75 G/M MISC-INFO: elimination route LIVER KIDNEY MP 141-142 C {HCL_SALT} C13 H17 N pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. Merck Index 11th ed #2893
  2. Research Biochemicals International 1993-94 catalog
  3. The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill pg 475
  4. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  5. Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 1051-52
  6. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  7. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  8. Alafuzoff et al Eur J Clin Pharmacol 55:815, 2000
  9. Prescriber's Letter 13(4): 2006 New Drug: Emsam (Selegiline) Transdermal Patch Detail-Document#: 220407 (subscription needed) http://www.prescribersletter.com
  10. Prescriber's Letter 13(7): 2006 New treatments for Parkinson's Disease (Azilect and Zelapar) Detail-Document#: 220710 (subscription needed) http://www.prescribersletter.com