Selegiline benefit and risks, side effects by Ray Sahelian, M.D.
February 19 2016

 

Selegiline is used to treat the symptoms of Parkinson's disease. You may take selegiline in combination with another medication but with caution. Selegiline is sometimes prescribed for other uses, such as ADHD.

 

Selegiline (deprenyl), a selective, irreversible inhibitor of monoamine oxidase type B (MAO-B) is widely used in the treatment of Parkinson's disease. As the first MAO-B inhibitor approved for the treatment of Parkinson's disease, concerns were raised about the safety of the drug based on the adverse effect profiles of older, nonselective MAO inhibitors. Unlike the nonselective MAO inhibitors, selegiline does not significantly potentiate tyramine-induced hypertension (the 'cheese effect') at the dosages (5 mg daily) used for the treatment of Parkinson's disease. The most frequent adverse events seen during monotherapy with selegiline have been insomnia, nausea, cardiac arrhythmias, dizziness and headache. When combined with levodopa, selegiline can potentiate the typical adverse effects of levodopa, if the dose of levodopa is not reduced sufficiently. Thus, the most common adverse effects associated with this combination are nausea, dizziness, fatigue, constipation and insomnia. At the later stages of Parkinson's disease when fluctuations in disability occur, peak dose dyskinesias, psychiatric complications like hallucinations and insomnia, and orthostatic hypotension are further potentiated by selegiline. Mortality has been reported to be increased when selegiline and levodopa were given together in comparison with treatment with levodopa alone.

 

Availability, where is it sold
Selegiline comes as a tablet to take by mouth. It usually is taken twice a day. Selegiline may be taken for a long time to treat Parkinson's disease but cardiac side effects are of major concern.

 

Zelapar (selegiline HCl, Valeant) Orally Disintegrating Tablets, a monoamine oxidase-B (MAO-B) inhibitor, was approved in 2006 as a once-daily adjunct therapy for Parkinson's disease patients being treated with levodopa / carbidopa who exhibit deterioration in the quality of their response to this therapy.

 

Selegiline side effects are common

Side effects from selegiline occur regularly. Tell your doctor if any of these symptoms are severe or do not go away: dizziness, dry mouth, upset stomach, vomiting, loss of appetite, heartburn, and constipation. Some people may experience chest pain, insomnia at night and sometimes daytime sleepiness, and possible heart rhythm abnormalities.

 

Selegiline combined with other medicines, medications

Several adverse effects have been reported when fluoxetine and selegiline have been used together. When you are taking selegiline, it is especially important that your health care professional know if you are taking any of the following:

Antidepressants, tricyclic (amitriptyline [e.g., Elavil], amoxapine [e.g., Asendin], clomipramine [e.g., Anafranil], desipramine [e.g., Norpramin], doxepin [e.g., Sinequan]imipramine [e.g., Tofranil], nortriptyline [e.g., Pamelor], protriptyline [e.g., Vivactil], trimipramine [e.g., Surmontil]) or
Fluoxetine (e.g., Prozac) or
Fluvoxamine (e.g., Luvox) or
Meperidine (e.g., Demerol) or
Nefazodone (e.g., Serzone) or
Paroxetine (e.g., Paxil) or
Sertraline (e.g., Zoloft) or
Venlafaxine (e.g., Effexor)

 

Using these antidepressants with selegiline may increase the chance of serious side effects.

 

Eur Rev Med Pharmacol Sci. 2014. Comparative efficacy of selegiline versus rasagiline in the treatment of early Parkinson's disease. It appears that selegiline and rasagiline have comparable efficacy in improving Parkinsonian symptoms in patients with early stage disease.

 

Interactions with supplements, herbs, natural pills
Q.
I am emailing this letter on behalf of my husband whom is a Vietnam veteran and was recently diagnosed with Parkinson at the age of 62. His neurologist have prescribed MAO-B Selegiline 5 mg 2x daily. The side effects are minimal if any at all. We were wondering if you knew what supplements would be compatible with this medication to possibly reduce his tremors and any PD symptoms.
   A. One needs to be cautious adding supplements to medications since little research has been done with combinations and this PD medication is already quite potent.

 

Selegeline for ADHD
Placebo-controlled study examining effects of selegiline in children with attention-deficit/hyperactivity disorder.
J Child Adolesc Psychopharmacol. 2006 Aug;16(4):404-15. Division of Neurology, Brain and Behaviour Programme, The Hospital for Sick Children, Toronto, Ontario, Canada.
There is evidence suggesting a role for dopamine in attention-deficit/hyperactivity disorder (ADHD). Pharmacological treatments that act on the dopamine system have been successful in reducing ADHD symptoms. However, unlike traditional stimulants (i.e., methylphenidate), selegiline is a monoamine oxidase inhibitor (MAOI) that has been shown to reduce ADHD symptoms without producing undesirable side effects. In this study using a randomized, double- blind, placebo-controlled, crossover design, cognitive tasks and behavioral rating scales were administered to measure the effectiveness of selegiline in treating different symptoms of ADHD in 11 children aged 6-13. Results indicate that selegiline may target specific symptoms of ADHD including: sustained attention, the learning of novel information, hyperactivity, and peer interactions. Because the drug was not associated with negative side effects and did not specifically reduce symptoms of impulsivity, selegiline may be a preferred treatment for individuals who present with the primarily inattentive subtype of ADHD.
   Dr. Sahelian says: I would be quite worried about the long term use of selegiline in children. I am concerned about cardiac side effects that may occur over time.

 

Protecting brain cells
Expert Rev Neurother. 2013. Revelation in the neuroprotective functions of rasagiline and selegiline: the induction of distinct genes by different mechanisms. Parkinson's disease, cell death of dopamine neurons in the substantia nigra progresses and neuroprotective therapy is required to halt neuronal loss. In cellular and animal models, selegiline [(-)deprenyl] and rasagiline, inhibitors of type B monoamine oxidase (MAO)-B, protect neuronal cells from programmed cell death. In this paper, the authors review their recent results on the molecular mechanisms by which MAO inhibitors prevent the cell death through the induction of antiapoptotic, prosurvival genes. MAO-A mediates the induction of antiapoptotic bcl-2 and mao-a itself by rasagiline, whereas a different mechanism is associated with selegiline. Rasagiline and selegiline preferentially increase GDNF and BDNF in nonhuman primates and Parkinsonian patients, respectively. Enhanced neurotrophic factors might be applicable to monitor the neurorescuing activity of neuroprotection.

 

Selegiline patch
Short-term treatment with selegiline skin patch does not impair sexual function in patients with major depressive disorder. Selegiline, sold as Emsam, is a monoamine oxidase type B inhibitor used to treat patients with major depressive disorder. Journal of Clinical Psychiatry, December 2008.

 

Neuropharmacology. Nov 28 2013. Selegiline normalizes, while l-DOPA sustains the increased number of dopamine neurons in the olfactory bulb in a 6-OHDA mouse model of Parkinson's disease.

 

Emails
Q. Hello, I was wondering if Sinemet is more effective if selegiline is taken with it? Does Sinemet need an MAO inhibitor to work best?
   A. Each parson with Parkinson's disease needs to tailor their medications and combinations for their unique circumstance. Some patients may do well with Sinemet alone, others may find the combination helpful, still others may only need selegiline. When combinations are made, the dosages need to be reduced to avoid overmedication and side effects.

 

If one has ED from antidepressants and diabetes is there any possibilty the Passion Rx (with or without yohimbe) can help based on your experience where some function exists and the diabetes is current controlled as measured by a HBa1C? Any special concerns when a person is using Emsam antidepressant. This is a skin absorbed version of selegeline and MAO inhibitor.
    Caution is advised when herbal supplements used for sexual enhancement are used with prescription medications, especially those that have an influence on neurotransmitter levels. It would be best not to use this aphrodisiac herbal formula in combination with such medications.