All About Selegiline: Medical Uses, Mechanisms, Side-Effects and More

Eldepryl (Selegiline Hcl): Uses, Dosage, Side Effects, Interactions, Warning

All About Selegiline: Medical Uses, Mechanisms, Side-Effects and More

The number of patients who received selegiline in prospectively monitored pre-marketing studies is limited. While other sources of information about the use of selegiline are available (e.g., literature reports, foreign post-marketing reports, etc.

) they do not provide the kind of information necessary to estimate the incidence of adverse events. Thus, overall incidence figures for adverse reactions associated with the use of selegiline cannot be provided.

Many of the adverse reactions seen have also been reported as symptoms of dopamine excess.

Moreover, the importance and severity of various reactions reported often cannot be ascertained. One index of relative importance, however, is whether or not a reaction caused treatment discontinuation.

In prospective pre-marketing studies, the following events led, in decreasing order of frequency, to discontinuation of treatment with selegiline: nausea, hallucinations, confusion, depression, loss of balance, insomnia, orthostatic hypotension, increased akinetic involuntary movements, agitation, arrhythmia, bradykinesia, chorea, delusions, hypertension, new or increased angina pectoris, and syncope. Events reported only once as a cause of discontinuation are ankle edema, anxiety, burning lips/mouth, constipation, drowsiness/lethargy, dystonia, excess perspiration, increased freezing, gastrointestinal bleeding, hair loss, increased tremor, nervousness, weakness, and weight loss.

Experience with ELDEPRYL (selegiline hcl) obtained in parallel, placebo controlled, randomized studies provides only a limited basis for estimates of adverse reaction rates.

The following reactions that occurred with greater frequency among the 49 patients assigned to selegiline as compared to the 50 patients assigned to placebo in the only parallel, placebo controlled trial performed in patients with Parkinson's disease are shown in the following Table. None of these adverse reactions led to a discontinuation of treatment.


Adverse EventNumber of Patients Reporting Events
selegiline hydrochloride N=49placebo N=50
Abdominal Pain42
Dry mouth31
Vivid Dreams20
The following events were reported once in either or both groups
Ache, generalized10
Hair Loss01
Leg pain10
Low back pain10
Urinary Retention10
Weight Loss10

In all prospectively monitored clinical investigations, enrolling approximately 920 patients, the following adverse events, classified by body system, were reported.


increased tremor, chorea, loss of balance, restlessness, blepharospasm, increased bradykinesia, facial grimace, falling down, heavy leg, muscle twitch*, myoclonic jerks*, stiff neck, tardive dyskinesia, dystonic symptoms, dyskinesia, involuntary movements, freezing, festination, increased apraxia, muscle cramps.

Mental Status/Behavioral/Psychiatric

hallucinations, dizziness, confusion, anxiety, depression, drowsiness, behavior/mood change, dreams/nightmares, tiredness, delusions, disorientation, lightheadedness, impaired memory*, increased energy*, transient high*, hollow feeling, lethargy/malaise, apathy, overstimulation, vertigo, personality change, sleep disturbance, restlessness, weakness, transient irritability.

Pain/Altered Sensation

headache, back pain, leg pain, tinnitus, migraine, supraorbital pain, throat burning, generalized ache, chills, numbness of toes/fingers, taste disturbance.


orthostatic hypotension, hypertension, arrhythmia, palpitations, new or increased angina pectoris, hypotension, tachycardia, peripheral edema, sinus bradycardia, syncope.


nausea/vomiting, constipation, weight loss, anorexia, poor appetite, dysphagia, diarrhea, heartburn, rectal bleeding, bruxism*, gastrointestinal bleeding (exacerbation of preexisting ulcer disease).


slow urination, transient anorgasmia*, nocturia, prostatic hypertrophy, urinary hesitancy, urinary retention, decreased penile sensation*, urinary frequency.

Skin and Appendages

increased sweating, diaphoresis, facial hair, hair loss, hematoma, rash, photosensitivity.


asthma, diplopia, shortness of breath, speech affected.

Postmarketing Reports

The following experiences were described in spontaneous post-marketing reports. These reports do not provide sufficient information to establish a clear causal relationship with the use of ELDEPRYL (selegiline hcl) .


Seizure in dialyzed chronic renal failure patient on concomitant medications.

* indicates events reported only at doses greater than 10 mg/day.


Evidence that Formulations of the Selective MAO-B Inhibitor, Selegiline, which Bypass First-Pass Metabolism, also Inhibit MAO-A in the Human Brain

All About Selegiline: Medical Uses, Mechanisms, Side-Effects and More

  • Parkinson's disease
  • Pharmacokinetics

Selegiline (L-deprenyl) is a selective, irreversible inhibitor of monoamine oxidase B (MAO-B) at the conventional dose (10 mg/day oral) that is used in the treatment of Parkinson’s disease.

However, controlled studies have demonstrated antidepressant activity for high doses of oral selegiline and for transdermal selegiline suggesting that when plasma levels of selegiline are elevated, brain MAO-A might also be inhibited.

Zydis selegiline (Zelapar) is an orally disintegrating formulation of selegiline, which is absorbed through the buccal mucosa producing higher plasma levels of selegiline and reduced amphetamine metabolites compared with equal doses of conventional selegiline.

Although there is indirect evidence that Zydis selegiline at high doses loses its selectivity for MAO-B, there is no direct evidence that it also inhibits brain MAO-A in humans. We measured brain MAO-A in 18 healthy men after a 28-day treatment with Zydis selegiline (2.5, 5.

0, or 10 mg/day) and in 3 subjects receiving the selegiline transdermal system (Emsam patch, 6 mg/day) using positron emission tomography and the MAO-A radiotracer [11C]clorgyline. We also measured dopamine transporter (DAT) availability in three subjects from the 10 mg group. The 10 mg Zydis selegiline dose significantly inhibited MAO-A (36.9±19.7%, range 11–70%, p30% inhibition of MAO-A in two of the three subjects tested.

Our results confirming inhibition of brain MAO-A with high dose Zydis selegiline and with the Emsam patch provide the first direct evidence in the humans that brain MAO-A inhibition may contribute to its pharmacological and therapeutic profile, particularly for depression.

They are consistent with those of Clarke et al who reported that repeated doses of high-dose Zydis selegiline reduces the urinary excretion of 5-hydroxy-indoleacetic acid, a peripheral marker for MAO-A activity (Clarke et al, 2003a, 2003b), and also with preclinical studies with the selegiline transdermal system which showed targeted inhibition of the MAO enzymes in the CNS while limiting MAO-A inhibition in the gut (Mawhinney et al, 2003).

Meyer et al (2006) reported that patients with major depressive disorder have an average 34% elevation of brain MAO-A, which may contribute to the monoamine imbalance in depression.

We can speculate that brain MAO-A inhibition by formulations of selegiline, which result in brain MAO-A inhibition, may contribute to a rebalancing of brain monoamines. Interestingly, there is a high comorbidity between smoking and depression (Glassman et al, 1990).

Biologically based self-medication hypotheses have been proposed to account for this observation including nicotine-induced release of norepinephrine and dopamine, which are neurotransmitters mediating arousal and stimulation (Lerman et al, 1996; Pomerleau and Pomerleau, 1984).

As tobacco smoke inhibits brain MAO-A by ∼30% (Fowler et al, 1996), brain MAO-A inhibition by cigarette smoke may also contribute to a rebalancing of brain monoamines thus alleviating depression symptoms.

Even though the primary pharmacological action of selegiline is MAO-B inhibition, its pharmacology is complex (Finberg, 2014 for review) and other mechanisms including the actions of amphetamine metabolites (Engberg et al, 1991), increased DAT expression (Lamensdorf et al, 1999), and DAT upregulation (Wiener et al, 1989) have also been proposed to account for the antidepressant efficacy of high doses of selegiline (Mann et al, 1989). Significant decreases in amphetamine metabolites with transdermal (Azzaro et al, 2007) and orally disintegrating formulations of selegiline (Clarke et al, 2003a) reduce the lihood that selegiline metabolites play a role in the pharmacological effects of these formulations. Similar to our prior PET study with conventional selegiline (10 mg/day for 1 week; Fowler et al, 2001), we did not find significant brain DAT inhibition by 10 mg Zydis selegiline. We note that DAT inhibitor drugs methylphenidate and modafinil at therapeutic doses inhibit >50% of DAT (Volkow et al, 2002; Volkow et al, 2009), whereas the DAT reduction we observed with Zydis selegiline for three subjects was


Zelapar (Selegiline)

All About Selegiline: Medical Uses, Mechanisms, Side-Effects and More

Zelapar (selegiline) is an oral adjunctive therapy used along with carbidopa and levodopa to treat symptoms of Parkinson’s disease, particularly in patients who experience a deteriorating response to levodopa/carbidopa treatment. Those declining responses include “end-dose” type fluctuations (when the drug wears off), “on-off” symptoms (sudden events when medication works or does not work), or dyskinesias (spontaneous, involuntary movements).

Zelapar is an oral tablet containing a chemical called selegiline hydrochloride that prevents the breakdown of dopamine in the brain and helps levodopa work for a longer period of time.

How Zelapar works

The mechanisms of how Zelapar provides benefits in the treatment of Parkinson’s disease are not fully understood. One main mechanism that is speculated is the selegiline-mediated inhibition of monoamine oxidase type B (MAO-B), an enzyme that catalyzes the breakdown of dopamine in the brain, which would increase the net amount of dopamine available.

In addition, there is evidence that selegiline may act through other mechanisms to increase dopaminergic activity, including interfering with dopamine re-uptake at the junction between nerve cells.

Dosage and administration

The tablet is available for oral administration (dissolved in the mouth) at a strength of 1.25 mg.

Zelapar treatment should be initiated with 1.25 mg given once a day for at least six weeks. If the patient is able to tolerate the drug. But if the desired benefit has not been achieved after six weeks, the dose may be increased to 2.5 mg once a day.

Zelapar should be taken in the morning before breakfast; the tablet should be placed on the tongue and allowed to dissolve. Patients should avoid eating, drinking or mouth-rinsing for five minutes before and after taking it to allow the medicine to be absorbed. Zelapar disintegrates within seconds after being placed on the tongue.

The drug should not be discontinued abruptly as this may cause severe side effects. A missed dose should be skipped to avoid overdose.

While taking Zelapar, alcohol should be avoided. Foods rich in tyramine, a chemical that induces the release of dopamine from nerve cells, should be avoided while taking Zelapar, as should over-the-counter medicines that contain tyramine.

Examples of tyramine-rich foods include air-dried, aged or fermented meats, beef, poultry, fish or liver, unpasteurized beer, aged cheeses, soybeans, soy sauce, sauerkraut, and yeast extracts.

Consuming tyramine while using Zelapar can raise blood pressure to dangerous levels, causing life-threatening side effects.


Serious drug interactions may occur when certain medications are used at the same time as Zelapar. The drug is contraindicated in patients with a known hypersensitivity to any formulation of selegiline, or to any of Zelapar’s inactive ingredients.

It should not be used if the patient has taken fluoxetine (Prozac) within the past five weeks. The drug also should not be used along with other selegiline products such as Eldepryl because it may lead to a severe increase in blood pressure. Zelapar should not be administered with analgesic agents such as tramadol, methadone, and propoxyphene.

Zelapar also is contraindicated for use with meperidine, cyclobenzaprine (Flexeril), antidepressants (citalopram, duloxetine etc.), MAO inhibitors (linezolid, rasagiline etc.), and cough medicines containing dextromethorphan.

The contraindications that apply to levodopa also must be taken into account.

Warnings and precautions

Zelapar should not be used at daily doses exceeding those recommended (2.5 mg/day) because of the risks associated with non-selective inhibition of MAO, which may lead to high blood pressure. Zelapar also may cause irritation of the buccal mucosa.

The drug may increase the dopaminergic side effects of levodopa and may cause or exacerbate pre-existing involuntary movements.

Zelapar should be taken with caution by patients with certain conditions such as liver or kidney disease, high blood pressure, and phenylketonuria.

Patients should be cautioned about the possibility of developing hallucinations.

Although the safety of Zelapar during pregnancy or breastfeeding is not known, the doctor should be informed and caution should be taken for its use in these circumstances.

Side effects

The commonly observed side effects of Zelapar include dizziness, nausea, abdominal pain, constipation, sleep problems, involuntary movements, back pain, and mouth sores or ulcers.


Parkinson’s News Today is strictly a news and information website about the disease. It does not provide medical advice, diagnosis, or treatment. This content is not intended to be a substitute for professional medical advice, diagnosis, or treatment.

Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition. Never disregard professional medical advice or delay in seeking it because of something you have read on this website.


Selegiline Uses, Side Effects & Warnings –

All About Selegiline: Medical Uses, Mechanisms, Side-Effects and More

Generic Name: selegiline (oral) (se LE ji leen)
Brand Name:Eldepryl, Zelapar

Medically reviewed by on Sep 27, 2019 – Written by Cerner Multum

What is selegiline?

Selegiline prevents the breakdown of a chemical in your brain called dopamine (DO pa meen). Low levels of this chemical are associated with Parkinson's disease.

Selegiline is used together with other medicines to treat symptoms of Parkinson's disease.

Selegiline may also be used for purposes not listed in this medication guide.

Serious drug interactions can occur when certain medicines are used together with selegiline. Tell each of your healthcare providers about all medicines you use now, and any medicine you start or stop using.

You should not use selegiline if you are allergic to it, or if you have taken fluoxetine (Prozac, Sarafem and others) within the past 5 weeks.

Some medicines can cause unwanted or dangerous effects when used with selegiline. Your doctor may need to change your treatment plan if you use any of the following drugs:

  • cough medicine that contains dextromethorphan;
  • cyclobenzaprine (Flexeril);
  • meperidine (Demerol) or other narcotic (opioid) pain medicine;
  • methadone;
  • St. John's wort;
  • tramadol (Ultram, Ultracet);
  • an antidepressant–citalopram, desvenlafaxine, duloxetine, escitalopram, fluvoxamine, levomilnacipran, milnacipran, mirtazapine, nefazodone, paroxetine, venlafaxine, vilazodone, vortioxetine, and others; or
  • an MAO inhibitor–isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, tranylcypromine, and others.

After you stop taking selegiline, you must wait at least 14 days before taking any of the medications listed above.

To make sure selegiline is safe for you, tell your doctor if you have:

People with Parkinson's disease may have a higher risk of skin cancer (melanoma). Talk to your doctor about this risk and what skin symptoms to watch for.

It is not known whether selegiline will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

It is not known whether selegiline passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not use this medicine in larger or smaller amounts or for longer than recommended. Do not change your doses or medication schedule without your doctor's advice.

Selegiline capsules are usually taken twice a day, at breakfast and lunch. Follow your doctor's instructions.

The disintegrating tablet form of selegiline (Zelapar) should be taken once a day before breakfast and without any liquid.

While you are using selegiline and for 14 days after you stop, you must not eat foods listed in the “What should I avoid while using selegiline?” section of this leaflet. Eating these foods while you are using selegiline can raise your blood pressure to dangerous levels.

Foods that you MAY eat include:

  • fresh meat, poultry, or fish (including lunch meat, hot dogs, breakfast sausage, and cooked sliced ham);
  • any vegetables except broad bean pods (fava beans);
  • processed cheese, mozzarella, ricotta, cottage cheese;
  • pizza made with cheeses low in tyramine;
  • soy milk, yogurt; or
  • Brewer's or baker's yeast.

To take selegiline orally disintegrating tablets (Zelapar):

  • Keep the tablet in its blister pack until you are ready to take the medicine. Open the package and peel back the foil from the tablet blister. Do not push a tablet through the foil or you may damage the tablet.
  • Using dry hands, remove the tablet and place it on your tongue. It will begin to dissolve right away. Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing. Swallow several times as the tablet dissolves.
  • Do not drink or eat anything for at least 5 minutes after taking a Zelapar orally disintegrating tablet.

Do not stop taking selegiline suddenly or you may have harmful side effects. For best results, keep taking the medicine as prescribed.

Store this medicine at room temperature away from moisture and heat.

Keep each Zelapar tablet in the foil blister pack until you are ready to take it. Throw away any Zelapar tablets not used within 3 months after you have opened the pouch containing the blister pack.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include severe headache, hallucinations, vision problems, sweating, cool or clammy skin, fast or uneven heart rate, feeling light-headed, fainting, or seizure (convulsions).

Avoid drinking alcohol while you are taking selegiline.

While taking selegiline and for 14 days after you stop, you must NOT eat foods that are high in tyramine, including:

  • air dried meats, aged or fermented meats, sausage or salami (including cacciatore and mortadella), pickled herring;
  • any spoiled or improperly stored beef, poultry, fish, or liver;
  • beer from a tap, beer that has not been pasteurized;
  • aged cheeses (such as blue, Swiss, cheddar, Parmesan, or Romano cheese);
  • over-the-counter supplements or cough and cold medicines that contain tyramine;
  • sauerkraut, soy beans, soy sauce, tofu, fava beans; or
  • yeast extracts (such as Marmite).

Eating tyramine while you are using selegiline can raise your blood pressure to dangerous levels which could cause life-threatening side effects. You should become very familiar with the list of foods to avoid while you are using selegiline.

Selegiline may impair your thinking or reactions. Some people taking selegiline have fallen asleep during normal daytime activities such as working, talking, eating, or driving. You may fall asleep suddenly, even after feeling alert. Be careful if you drive or do anything that requires you to be alert.

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • a light-headed feeling, you might pass out;
  • trouble breathing;
  • confusion, hallucinations, unusual thoughts or behavior;
  • increased tremors or uncontrolled muscle movements;
  • worsening side effects of your other medications;
  • high levels of serotonin in the body (when taken with an antidepressant)–agitation, fever, fast heart rate, overactive reflexes, nausea, vomiting, diarrhea, loss of coordination, fainting; or
  • dangerously high blood pressure–severe headache, blurred vision, pounding in your neck or ears, anxiety, nausea, vomiting, severe chest pain, shortness of breath, pounding heartbeats, or seizure (convulsions).

You may have increased sexual urges, unusual urges to gamble, or other intense urges while taking this medicine. Talk with your doctor if this occurs.

Common side effects may include:

  • dizziness;
  • nausea, stomach pain, constipation;
  • skin rash or other irritation;
  • sleep problems (insomnia); or
  • mouth sores or ulcers, pain with swallowing (while using selegiline orally disintegrating tablets).

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Usual Adult Dose for Parkinson's Disease:

Oral tablet: Recommended dose: 5 mg orally twice a dayMaximum dose: 10 mg orally per dayOral disintegrating tablet:Initial dose: 1.25 mg orally once a day for at least 6 weeks. After 6 weeks, the dose may be increased to 2.5 mg orally once a day if needed.Maintenance dose: 1.

25 to 2.5 mg orally once a dayMaximum dose: 2.5 mg orally once a dayComments:

-After two to three days of treatment, an attempt may be made to reduce the dose of concomitant levodopa-carbidopa by 10% to 30%. Further reductions may be possible during continued selegiline therapy.

Use: Adjunct in the management of Parkinson's disease patients being treated with levodopa-carbidopa who exhibit deterioration in the quality of their response to this therapy.

Usual Adult Dose for Depression:

Initial dose: Apply one 6 mg/24 hours transdermal patch to intact skin once every 24 hoursMaintenance dose: One 6 mg/24 hours to 12 mg/24 hours transdermal patch applied to the skin once a day Maximum dose: 12 mg/24 hours transdermal patch applied to the skin once a dayComments:

-Episodes of depression may require several months or more of sustained pharmacologic therapy

-If dose adjustments are necessary, they should be made in increments of 3 mg/24 hours at intervals of at least 2 weeks-Full antidepressant effect may be delayed

Use: Treatment of major depressive disorder (MDD)

What other drugs will affect selegiline?

Many drugs can interact with selegiline, and some drugs should not be used together. This includes prescription and over-the-counter medicines, vitamins, and herbal products.

Not all possible interactions are listed in this medication guide. Tell your doctor about all medicines you use, and those you start or stop using during your treatment with selegiline.

Give a list of all your medicines to any healthcare provider who treats you.

Remember, keep this and all other medicines the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Copyright 1996-2018 Cerner Multum, Inc. Version: 6.01.

Medical Disclaimer


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All About Selegiline: Medical Uses, Mechanisms, Side-Effects and More

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Eldepryl, Zelapar (selegiline) dosing, indications, interactions, adverse effects, and more

All About Selegiline: Medical Uses, Mechanisms, Side-Effects and More

  • 5 mg PO at breakfast & 5 mg at lunch (10 mg/day)
  • After 2-3 days of selegeline therapy, can begin to taper levadopa dose by 10-30% as tolerated; continue to taper based upon patient response
  • Not to exceed 10 mg/day
  • Initial 1.25 mg PO qDay, may increase after 6 weeks if inadequate response, no more than 2.5 mg/day
  • Do not take food or liquid for 5 minutes after dose

Use caution; safety and efficacy not established

Hepatic Impairment

Use caution; safety and efficacy not established

Safety and efficacy not established


– 5 mg PO at breakfast & 5 mg at lunch (10 mg/day)

– After 2-3 days of selegeline therapy, can begin to taper levadopa dose by 10-30% as tolerated; continue to taper based upon patient response

– Not to exceed 10 mg/day

Orally-disintegrating (with levodopa/carbidopa)

– Initial 1.25 mg PO qDay, may increase after 6 weeks if inadequate response, no more than 2.5 mg/day

– Do not take food or liquid for 5 minutes after dose


No Interactions Found

Interactions Found


All Interactions Sort By: SeverityName


Nausea (20%)

Frequency Not Defined (selected)




Generalized pain





Mood changes

Orthostatic hypotension


Urinary retention



Loses selectivity for MAO-B receptors at higher doses

Prescriptions should be written for the smallest quantity consistent with good patient care

May cause exacerbation of hypertension and orthostatic hypotension; use with caution in patients at risk for this effect of those who do not tolerate transient hypotensive episode

May potentiate dopaminergic side effects of levodopa and cause dyskinesia or exacerbate preexisting dyskinesia, which may in turn require a reduction of lovodopa dose

Patients with Parkinson disease treated with drugs that increase dopaminergic tone have reported falling asleep while engaged in activities of daily living, including the operation of motor vehicles

Diminished impulse control; reports of intense urges to gamble, increased sexual urges, intense urges to spend money, binge eating, and/or other intense urges

In patients with bipolar disorder, treating a depressive episode may precipitate a mixed/manic episode; prior to initiating treatment, screen patients for any personal or family history of bipolar disorder, mania, or hypomania

Serotonin syndrome reported with use

Risk of melanoma development increased in Parkinson disease patients; monitor patients closely

The available data on use in pregnant women are not sufficient to inform a drug- associated risk of adverse pregnancy-related outcomes; When treating a pregnant woman, the physician should carefully consider both the potential risks of taking an MAOI, particularly the risk of hypertensive crisis during pregnancy, along with the established benefits of treating depression with an antidepressant


There is no information regarding presence in human milk, or effects on milk production or breastfed infant; because of potential for serious adverse reactions in breastfed infants from therapy, including potential for hypertensive crisis, advise a woman that breastfeeding is not recommended during treatment and for 5 days after final dose

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.

Selective MAO-B inhibitor; may increase dopaminergic activity by interfering with dopamine reuptake at the synapse.


Peak plasma time: (conventional) 0.5-0.9 hr; (ODT) 15-40 min

Concentration: (conventional, 5 mg) 0.9-2.7 ng/mL; (ODT, 1.25 /2.5 mg) 3.34/4.47 ng/mL

Half-life elimination: 10 hr (PO); 18-25hr (TD)

Onset of action: Within 1 hr

Duration: 24-72hr (PO)

Bioavailability: 10%

Protein Bound: 90%

Vd: 300 L

Metabolism: cytochrome P-450 enzymes

Metabolites: L-amphetamine, L-desmethylselegiline, L-methamphetamine

Excretion: Urine

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
  • Manage and view all your plans together – even plans in different states.
  • Compare formulary status to other drugs in the same class.
  • Access your plan list on any device – mobile or desktop.

Medscape prescription drug monographs are FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.