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Selegiline or L-Deprenyl (trade names include Eldepryl, Emsam, Deprenyl, Anipryl, Egibren, Jumex, Jumexil, Moverdin, Selegos, Selgian, Selgin, Zelapar) is an antiparkinsonian drug from monoamine oxidase type B (MAO-B) inhibitors pharmacological group. This medication is used to treat symptoms of Parkinson's disease, parkinsonism, shaking palsy, paralysis agitans, such as dementia in Alzheimer's disease, shakiness (tremor), muscle stiffness, loss of normal movement, sudden switching between normal movement and stiffness, other movement disorders. This is a cognitive enhancing smart anti aging drug that improves brain functions, cognitive actions, concentration, the range of motion and ability to walk, dress, exercise. Selegiline works by increasing and extending the effects of levodopa, and helping to slow the progress of Parkinson's disease. Deprenyl is usually used in combination with other antiparkinson medications (e.g., levodopa, carbidopa).
Emsam (Selegiline in the form of transdermal patch) is prescribed for the therapy of depression and major depressive disorder.
This medication is also indicated to treat the symptoms of Cushing's disease and cognitive dysfunction in veterinary medicine for dogs, pets and animals.
Selegiline was tested and studied for the treatment of attention deficit hyperactivity disorder (ADHD); to stop smoking tobacco or cannabis.
How and where to order Deprenyl, Eldepryl (Selegiline) 5 mg tablets or capsules online on FLCPR:
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Forms: | Selegiline Hydrochloride 5 mg capsules or tablets
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Related medications:
Amantadine (Symmetrel)
Apomorphine (Taluvian)
Bromocriptine (Parlodel)
Budipine (Parkinsan)
Cabergoline (Dostinex)
Carbidopa, Entacapone, Levodopa (Stalevo)
Carbidopa, Levodopa (Sinemet)
Dihydroergocryptine Mesylate (Almirid)
Donepezil (Aricept)
Entacapone (Comtan)
Galantamine (Reminyl)
Levodopa (Larodopa)
Memantine (Namenda)
Pergolide (Permax)
Piracetam (Nootropil)
Piribedil (Trivastal)
Pramipexole (Mirapex)
Procyclidine (Kemadrin)
Rasagiline (Azilect)
Rivastigmine (Exelon)
Ropinirole (Requip)
Rotigotine (Neupro)
Tolcapone (Tasmar)
Trihexyphenidyl (Artane)
Pharmacological and medical categories:
Anti aging drugs
Antidepressants
Antiparkinson medicines
Pharmaceutical drugs for the treatment of Parkinson's disease
Central nervous system agents
Dopaminergic antiparkinsonism agents
Meds to treat ADHD
Monoamine oxidase B (MAO-B) inhibitors
Stop smoking pills
Substituted phenethylamines
Veterinary medications, pet meds
ATC codes:
N - Nervous system
N04 - Anti-parkinson drugs
N04B - Dopaminergic agents
N04BD - Monoamine oxidase B inhibitors
N04BD01 - Selegiline
ICD-10 codes:
Cushing's syndrome - E24
Dementia in Alzheimer's disease ( G30.-+ ) - F00*
Cannabis related disorders - F12
Major depressive disorder, single episode - F32
Major depressive disorder, recurrent - F33
Attention-deficit hyperactivity disorders - F90
Parkinson's disease - G20
Other specified degenerative diseases of nervous system - G31.8
Mild cognitive impairment, so stated - G31.84
Tobacco abuse counseling - Z71.6
Indications and usage:
Eldepryl (Selegiline Hydrochloride) capsules or tablets is indicated as an adjunct in the management of Parkinsonian patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. There is no evidence from controlled studies that selegiline has any beneficial effect in the absence of concurrent levodopa therapy.
Evidence supporting this claim was obtained in randomized controlled clinical investigations that compared the effects of added selegiline or placebo in patients receiving levodopa/carbidopa. Selegiline was significantly superior to placebo on all three principal outcome measures employed: change from baseline in daily levodopa/carbidopa dose, the amount of "off" time, and patient self-rating of treatment success. Beneficial effects were also observed on other measures of treatment success (e.g., measures of reduced end of dose akinesia, decreased tremor and sialorrhea, improved speech and dressing ability and improved overall disability as assessed by walking and comparison to previous state).
Dosage and administration:
Selegiline is administered as monotherapy in the early phase of the disease, or as adjunctive therapy with levodopa (with / without a peripheral decarboxylase inhibitor). In each case the initial dose is 5 mg taken at breakfast and lunch. There is no evidence that additional benefit will be obtained from the administration of higher doses.
After two to three days of adjunctive therapy, an attempt may be made to reduce the dose of levodopa (10-30%) if levodopa-related adverse reactions occur. Further reductions of levodopa may be possible during continued selegiline therapy.
Double-blind studies on early-phase parkinsonian patients showed that patients receiving selegiline monotherapy manage significantly longer without levodopa therapy than controls receiving placebo. These patients could also maintain their ability to work longer.
After the initiation of levodopa therapy, selegiline potentiates and extends the effect of levodopa, and thus a reduction of levodopa dosage is possible. By adding selegiline to levodopa therapy the fluctuations in disability, e.g.end-of-dose type fluctuations, can be reduced.
Dosage forms and strengths:
Eldepryl (Selegiline Hydrochloride) 5 mg and 10 mg capsules or tablets for oral use.
Overdosage:
No cases of overdosage by selegiline pills are known. However, experience gained during selegiline's development reveal that some individuals exposed to doses of 600 mg/day selegiline suffered severe hypotension and psychomotor agitation.
Theoretically, overdosage causes significant inhibition of both MAO-A and MAO-B and thus, symptoms may resemble those observed with non-selective MAOIs, particularly disorders of the central nervous and cardiovascular systems (e.g. drowsiness, dizziness, faintness, irritability, hyperactivity, agitation, severe headache, hallucination, hypertension, hypotension, vascular collapse, rapid and irregular pulse, precordial pain, respiratory depression and failure, hyperpyrexia, diaphoresis). There is no specific antidote and the treatment is symptomatic.
Contraindications:
Selegiline is contraindicated in patients with a known hypersensitivity to this drug. This medication is also is contraindicated for use with meperidine. This contraindication is often extended to other opioids.
Warnings:
Selegiline should not be used at daily doses exceeding those recommended (10 mg/day) because of the risks associated with non-selective inhibition of MAO.
The selectivity of selegiline for MAO-B may not be absolute even at the recommended daily dose of 10 mg a day. Rare cases of hypertensive reactions associated with ingestion of tyramine-containing foods have been reported in patients taking the recommended daily dose of selegiline. The selectivity is further diminished with increasing daily doses. The precise dose at which selegiline becomes a non-selective inhibitor of all MAO is unknown, but may be in the range of 30 to 40 mg a day.
Severe CNS toxicity associated with hyperpyrexia and death have been reported with the combination of tricyclic antidepressants and non-selective MAOIs (Nardil, Parnate). A similar reaction has been reported for a patient on amitriptyline and Eldepryl. Another patient receiving protriptyline and selegiline pills developed tremors, agitation, and restlessness followed by unresponsiveness and death two weeks after Eldepryl was added. Related adverse events including hypertension, syncope, asystole, diaphoresis, seizures, changes in behavioral and mental status, and muscular rigidity have also been reported in some patients receiving Eldepryl and various tricyclic antidepressants.
Serious, sometimes fatal, reactions with signs and symptoms that may include hyperthermia, rigidity, myoclonus, autonomic instability with rapid fluctuations of the vital signs, and mental status changes that include extreme agitation progressing to delirium and coma have been reported with patients receiving a combination of fluoxetine hydrochloride (Prozac) and non-selective MAOIs. Similar signs have been reported in some patients on the combination of Selegiline (10 mg a day) and selective serotonin re-uptake inhibitors including fluoxetine, sertraline and paroxetine.
Since the mechanisms of these reactions are not fully understood, it seems prudent, in general, to avoid this combination of Eldepryl and tricyclic antidepressants as well as Selegiline HCl and selective serotonin re-uptake inhibitors. At least 14 days should elapse between discontinuation of Eldepryl and initiation of treatment with a tricyclic antidepressant or selective serotonin re-uptake inhibitors. Because of the long half-lives of fluoxetine and its active metabolite, at least five weeks (perhaps longer, especially if fluoxetine has been prescribed chronically and/or at higher doses) should elapse between discontinuation of fluoxetine and initiation of treatment with selegiline tablets or capsules.
Precautions:
General
Some patients given selegiline may experience an exacerbation of levodopa associated side effects, presumably due to the increased amounts of dopamine reaction with super sensitive, post-synaptic receptors. These effects may often be mitigated by reducing the dose of levodopa/carbidopa by approximately 10 to 30%.
The decision to prescribe selegiline should take into consideration that the MAO system of enzymes is complex and incompletely understood and there is only a limited amount of carefully documented clinical experience with selegiline. Consequently, the full spectrum of possible responses to selegiline may not have been observed in pre-marketing evaluation of the drug. It is advisable, therefore, to observe patients closely for atypical responses.
Melanoma
Epidemiological studies have shown that patients with Parkinson's disease have a higher risk (2- to approximately 6-fold higher) of developing melanoma than the general population. Whether the increased risk observed was due to Parkinson's disease or other factors, such as drugs used to treat Parkinson's disease, is unclear. For the reasons stated above, patients and providers are advised to monitor for melanomas frequently and on a regular basis when using Eldepryl for any indication. Ideally, periodic skin examinations should be performed by appropriately qualified individuals (e.g., dermatologists).
Information for patients:
Patients should be advised of the possible need to reduce levodopa dosage after the initiation of Eldepryl therapy.
Patients (or their families if the patient is incompetent) should be advised not to exceed the daily recommended dose of 10 mg. The risk of using higher daily doses of selegiline should be explained, and a brief description of the "cheese reaction" provided. Rare hypertensive reactions with selegiline at recommended doses associated with dietary influences have been reported.
Consequently, it may be useful to inform patients (or their families) about the signs and symptoms associated with MAOI induced hypertensive reactions. In particular, patients should be urged to report, immediately, any severe headache or other atypical or unusual symptoms not previously experienced.
There have been reports of patients experiencing intense urges to gamble, increased sexual urges, and other intense urges and the inability to control these urges while taking one or more of the medications that increase central dopaminergic tone, that are generally used for the treatment of Parkinson's disease, including Eldepryl. Although it is not proven that the medications caused these events, these urges were reported to have stopped in some cases when the dose was reduced or the medication was stopped. Prescribers should ask patients about the development of new or increased gambling urges, sexual urges or other urges while being treated with Selegiline. Patients should inform their physician if they experience new or increased gambling urges, increased sexual urges or other intense urges while taking Eldepryl. Physicians should consider dose reduction or stopping the medication if a patient develops such urges while taking Selegiline HCl pills.
Drug interactions:
The occurrence of stupor, muscular rigidity, severe agitation, and elevated temperature has been reported in some patients receiving the combination of selegiline and meperidine. Symptoms usually resolve over days when the combination is discontinued. This is typical of the interaction of meperidine and MAOIs. Other serious reactions (including severe agitation, hallucinations, and death) have been reported in patients receiving this combination. Severe toxicity has also been reported in patients receiving the combination of tricyclic antidepressants, selective serotonin re-uptake inhibitors and selegiline. One case of hypertensive crisis has been reported in a patient taking the recommended doses of selegiline and a sympathomimetic medication (ephedrine).
Side effects, adverse reactions:
The most common side effects of selegiline tablets and capsules in conjunction with levodopa include, in decreasing order of frequency, nausea, hallucinations, confusion, depression, loss of balance, insomnia, increased involuntary movements, agitation, slow or irregular heart rate, delusions, hypertension, new or increased angina pectoris, and syncope.
Use in specific populations:
Pregnancy
There are no adequate and well-controlled studies in pregnant women. Selegiline should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing mothers
It is not known whether selegiline hydrochloride is excreted in human milk. Because many drugs are excreted in human milk, consideration should be given to discontinuing the use of all but absolutely essential drug treatments in nursing women.
Pediatric use
The effects of Selegiline HCl in children have not been evaluated.
Pregnancy categories:
B2 - Australia
C - United States (Risk cannot be ruled out)
Salts and other forms:
Selegiline Base
Selegiline Citrate
Selegiline Hydrochloride
Synonyms, international and chemical names:
(-)-Deprenil
(R)-(-)-N,alpha-Dimethyl-N-2-propinylphenethylamine
(R)-(-)-N-Methyl-N-(1-phenyl-2-propyl)-2-propinylamin
Benzeneethanamine, N,alpha-dimethyl-N-2-propynyl-, (R)-
Deprenil
Deprenyl
L-Deprenalin
L-Deprenil
L-Deprenyl
Selegelin
Selegeline
Selegiliini
Selegilin
Selegilina
Selegiline HCl
Selegilinehydrochloride
Selegilinhydrochlorid
Selegilini Hydrochloridum
Selegilinum
Szelegilin
Brands, generics, trade names:
Anipryl - Pfizer, Zoetis
Cognitive - Ebewe Pharma, Ever Pharma
Deprenyl - Orion Pharma, Sanofi-Aventis
Deprilan - Biosintetica Laboratorios
Egibren - Chiesi
Eldepryl - Orion Corporation
Emsam - Mylan
Jumex - Sanofi-Aventis, Armstrong Laboratorios de Mexico, Chiesi, Chinoin Pharmaceutical and Chemical Works, Dexxon, DKSH, IDS Group, IVAX, Lexapharm, Metro Drug Distribution, Novartis, Paranova, The Glory Medicina, Torrent Pharmaceuticals, Zuellig Pharma
Jumexil - Farmalab Industrias Quimicas e Farmaceuticas
Moverdin - Kocak Farma Ilac
Niar - Abbott, Knoll
Otrasel - Cephalon, Lafon Laboratoires
Plurimen - Orion Pharma, Asta Medica, Viatris
Selegilin - AbZ-Pharma, Azupharma, CT-Arzneimittel, Mepha, Ratiopharm
Selegilina - Davur Laboratorios, Generis Farmaceutica
Selegiline - Alphapharm, Apotex, Biogaran, Generics UK, Mylan, Sandoz, Teva
Selegos - Medochemie, Britton Distributions, Derek Marketing, Komedic, Star Medical Supplies
Selerin - Cipla, Protec
Selgian - Ceva Animal Health, Biokema, Ceva Sante Animale, Sanofi-Aventis
Selgin - Intas Pharmaceuticals
Tonus - Acapi
Xilopar - Teva, Cephalon, Elan Pharmaceuticals, Esteve, Segix Italia
Zelapar - Teva, B & S Healthcare, Cardinal Health, Cephalon, Elan Pharmaceuticals, Lexon UK, Servipharm, Star Pharmaceuticals, Valeant Pharmaceuticals, Zeneus Pharma
Here is a list of popular medications containing selegiline as a main active pharmaceutical ingredient; their trade names, forms, doses, companies - manufacturers, distributors, suppliers, researchers and developers:
Trade name of the drug |
Pharmaceutical forms and doses |
Companies |
Deprenyl |
Tablets; Oral; Selegiline Hydrochloride 5 mg |
Sanofi-Aventis |
Eldepryl |
Capsules; Oral; Selegiline Hydrochloride 5 mgSyrup; Oral; Selegiline Hydrochloride 10 mg / 5 mlTablets; Oral; Selegiline Hydrochloride 5 mgTablets; Oral; Selegiline Hydrochloride 10 mg |
Orion CorporationAllphar ServicesAspenAsta MedicaDeprenyl ResearchDouglas PharmaceuticalsDraxis HealthEisaiErcopharmEumedica PharmaceuticalsGenepharmMylanPolyfarmaReckitt BenckiserServipharmSomerset PharmaceuticalsStar PharmaceuticalsThemis MedicareViatris |
Emsam |
Transdermal Systems; Topical; Selegiline 6 mg / 24 hTransdermal Systems; Topical; Selegiline 9 mg / 24 hTransdermal Systems; Topical; Selegiline 12 mg / 24 h |
MylanBristol-Myers SquibbSomerset Pharmaceuticals |
Selgin |
Tablets; Oral; Selegiline Hydrochloride 5 mg |
Intas Pharmaceuticals |
References:
Selegiline main article on Wikipedia: https://en.wikipedia.org/wiki/Selegiline
D-Deprenyl article on Wikipedia: https://en.wikipedia.org/wiki/Selegiline
Selegiline compound on PubChem: https://pubchem.ncbi.nlm.nih.gov/compound/Selegiline
Selegiline Hydrochloride compound on PubChem: https://pubchem.ncbi.nlm.nih.gov/compound/Selegiline-hydrochloride
Selegiline medicine on DrugBank: https://www.drugbank.ca/drugs/DB01037
Selegiline Hydrochloride on DrugBank: https://www.drugbank.ca/salts/DBSALT000260
Selegiline FAQ on MedlinePlus (revised 01/15/2018): https://medlineplus.gov/druginfo/meds/a697046.html
Apotex Selegiline Hydrochloride tablets drug label on DailyMed (revised November 28, 2018): https://dailymed.nlm.nih.gov/dailymed/lookup...
Zelapar (Selegiline Hydrochloride) orally disintegrating tablets drug label on DailyMed (revised February 3, 2020): https://dailymed.nlm.nih.gov/dailymed/drugInfo...
Emsam (Selegiline) patch drug label on DailyMed (revised May 15, 2020): https://dailymed.nlm.nih.gov/dailymed/drugInfo...
Selegiline containing drugs on Drugs-About.com: https://drugs-about.com/ing/selegiline.html
Selegiline for sale on Pharma Doctor: https://pharma-doctor.com/selegiline.html
Eldepryl (Selegiline Hydrochloride) capsules official prescribing information from the U.S. FDA (issued January 2008): https://www.accessdata.fda.gov/drugsatfda_docs/label/...
EMSAM (Selegiline Transdermal System) official prescribing information from the U.S. FDA (issued June 2007): https://www.accessdata.fda.gov/drugsatfda_docs/label/...
Eldepryl (Selegiline Hydrochloride) 5 mg tablets product information from GP2U TeleHealth (revised 28 October 2010): https://gp2u.com.au/static/pdf/E/ELDEPRYL-PI.pdf
Eldepryl (Selegiline Hydrochloride) 5 mg and 10 mg tablets patient information leaflet from Medicines.org.uk (revised January 2021): https://www.medicines.org.uk/emc/files/pil.2251.pdf
Revised: February 2021
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