L-deprenyl (Selegiline, Eldepryl, Emsam, Zelapar)
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Indications
- treatment of the symptoms of Parkinson's disease
- adjunctive treatment to carbidopa/L-dopa
- symptomatic treatment of Alzheimer's disease
Contraindications
- coadministration of dextromethorphan, meperidine, methadone, propoxyphene
Dosage
- 5 mg PO BID (breakfast & lunch dosing)
- after 2-3 days of treatment, try to decreased L-dopa/ carbidopa by 30-30%
- giving the dose in the evening increases insomnia & nightmares
- doses > 10 mg/day decreases MAO-B selectivity
- transdermal patch: 1 patch QD
- 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
- about 75% of oral dose is absorbed from the GI tract
- metabolized by the liver
- metabolized to 2 amphetamine derivatives that enhance release & decrease re-uptake of dopamine
- excreted in the urine
elimination via liver
elimination via kidney
Adverse effects
- common (> 10%)
- mood changes, dyskinesias, dizziness, dry mouth, nausea/vomiting, insomnia, abdominal pain
- less common (1-10%)
- orthostatic hypotension, arrhythmias, hypertension, hallucinations, confusion, depression, insomnia, agitation, increased involuntary movements, bradykinesia, bruxism, muscle twitches
- other
- drug adverse effects of MAO inhibitors
- drug adverse effects of antidepressants
- drug adverse effects of psychotropic agents
Drug interactions
- meperidine: mechanism unknown; fatal reactions have occurred
- use in combination with:
- other antidepressants
- selective serotonin re-uptake inhibitors (SSRI)
- tricyclic antidepressants (TCA)
- buspirone, cyclobenzaprine, dextromethorphan, meperidine, methadone, propoxyphene tramadol, St. John's wort can cause serotonin syndrome[9]
- other antidepressants
- amphetamines, pseudoephedrine, phenylephrine in combination may result in excessive sympathetic stimulation... hypertension
- carbamazepine, oxcarbazepine in combination can increase deprenyl levels[9]
- drug interaction(s) of antidepressant in combination with GLP1-agonist
- drug interaction(s) of benzodiazepines with antidepressants
- drug interaction(s) of antidepressants with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists with MAO inhibitors
- drug interaction(s) of NSAIDs with antidepressants
- drug interaction(s) of antidepressant with opiates
- drug interaction(s) of gabapentinoid with psychotropic agent
- drug interaction(s) of MAO inhibitor with caffeine
Mechanism of action
- selective MAO-B inhibitor
- 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
- inhibits CNS degradation of dopamine
- potentiates the effects of L-dopa
- metabolized to 2 amphetamine derivatives that enhance release & decrease re-uptake of dopamine
- it has been suggested that MAO-B inhibitors may slow the progression of Parkinson's disease; however, this issue is controversial
- symptomatic improvement in Alzheimer's disease
- does not alter the course of the disease[8]
More general terms
- monoamine oxidase [MAO] inhibitor
- aromatic compound
- amine
- alkyne
- pharmacologic agents for treatment of Parkinson's disease
Additional terms
References
- ↑ Merck Index 11th ed #2893
- ↑ Research Biochemicals International 1993-94 catalog
- ↑ The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill pg 475
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 1051-52
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Jump up to: 8.0 8.1 Alafuzoff et al Eur J Clin Pharmacol 55:815, 2000
- ↑ Jump up to: 9.0 9.1 9.2 9.3 Prescriber's Letter 13(4): 2006 New Drug: Emsam (Selegiline) Transdermal Patch Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220407&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Prescriber's Letter 13(7): 2006 New treatments for Parkinson's Disease (Azilect and Zelapar) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220710&pb=PRL (subscription needed) http://www.prescribersletter.com
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5195
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5288103
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=26758
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=92913
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=199604
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=26757