Selegeline (l-deprenyl, Alzene, Carbex, Deprenyl, Eledeprine, Eldepryl, Zelapor) Jumex, Anipryl, EMS

Selegeline is a mono amine oxidase inhibitor that has different effects at different doses. It has been used to treat Parkinson's disease since 1986. In 2006, it was approved as an add-on (adjunct) treatment for Parkinson's sufferers who are already taking levodopa or carbidopa and are no longer responding well to it. In 2006, a transdermal form of selegiline, EMSAM, was also introduced for treating depression.

The Bottom Line: What You Really Need to Know

Uses of selegeline

The indications for selegeline are dose-related.

At low doses (5 mg twice a day) selegeline is prescribed to treat Parkinson's disease and senile dementia. At this level, it inhibits mostly MAO-B.

At higher doses, selegeline is no longer selective and it inhibits MAO-A and -B, and it is used to treat depression. Oral high-dose selegiline is helpful in treating atypical depression and symptoms such as overeating, excessive sleeping and extreme sensitivity to rejection by others.

EMSAM, the transdermal form of selegeline, is the only transdermal medication used to treat depression.

Sometimes selegeline is used to treat narcolepsy or loss of libido.

Selegeline has antioxidant properties, blocks free radical formation, stimulates growth hormone, stops neurodegeneration and stimulates immune system functioning. Some people believe selegeline could be a "longevity drug," delaying aging and prolonging life expectancy. In rat studies, life expectancy increased by 20% with selegeline.

Studies are being done to determine if selegeline is effective in treating cigarette addiction, marijuana addiction or ADHD.

Dosage and instructions

Parkinson's: Selegiline is usually a second-line drug for treating Parkinson's. Most people take levodopa or carbidopa initially, but eventually they begin to respond less to those drugs. At that point, selegiline is added. The dose is 5 mg twice a day.

Atypical depression: 10 mg/day by mouth. It is started at a lower dose and gradually increased to the maintenance dose.

EMSAM: 6mg, 9mg or 12 mg patch once every 24 hours.

How selegiline works

Selegeline's actions on neurotransmitters are dose dependent.

At low doses-10 mg/day or less-selegiline exerts an irreversible selective inhibitory effect on MAO-B and has little effect on MAO-A. MAO-B metabolizes dopamine and phenylethylamine; MAO-B inhibitors are effective in treating Parkinson's disease. At this dose, selegiline also inhibits the effect of tyramine, so dietary restrictions are not necessary. Selegiline has a weak antidepressant effect at low doses.

At higher doses-20 mg/day or more-selegiline loses its specificity to MAO-B and works like the older MAOI medications, inhibiting both MAO-A and -B and functioning as an antidepressant. At the higher dose, however, it is affected by tyramine, so dietary restrictions are necessary.

Selegiline has several other effects that make it attractive to life extensionists. Some believe selegiline could be a life-extending drug; others believe that it may be the parent drug for a group of life-extenders. Some of the actions that make selegiline promising are:

Selegiline also has veterinary uses. It is used to treat Cushing's syndrome and cognitive dysfunction in dogs.

Side Effects

Most people do not suffer side effects with selegiline, especially at low doses. The most frequently seen side effect is a skin reaction to the transdermal patch with EMSAM. Other side effects do occur, and are more likely to occur at high doses. They include:

Interactions

Interactions also tend to be dose-related. Dietary restrictions are not necessary with lower doses-5 mg twice a day by mouth or 6 mg/24 hour patch. At higher doses, selegiline reacts with tyramine containing foods, especially wine and cheese.

At high doses, selegiline can have a dangerous interaction with serotonergic medications. Chills, high fever, agitation, delirium, seizures, coma and death can result from taking MAOIs with these medications. Do not take selegiline, especially at high doses, when you are taking:

Selegeline interacts with anesthetics and should be stopped 10 days before any scheduled surgery.

Oral contraceptives may increase the level of selegiline in the blood; a lower dose may be necessary if you are taking oral contraceptives.

Warnings, precautions and contraindications

Suicide risk: At this time, it is believed that all antidepressants carry an increased risk of suicide, especially in the early weeks of treatment. Anyone who begins taking an antidepressant should be monitored closely for thoughts of harming self or others, unusual thoughts, deepening depression, mood volatility, agitation and other mental or emotional abnormalities.

Hypertensive crisis: High dose selegiline can cause hypertensive crisis when taken with certain other medications. Extremely high blood pressure can cause heart attack or stroke and can result in death.

Interaction with other antidepressants: Severe, sometimes fatal interactions can occur with other antidepressants.

Activation of mania: Selegiline can activate severe mania and rapid cycling in people with bipolar disease. It can also increase agitation, psychosis and delusional thinking.

PKU: Phenylketonurics should not take selegiline.

False positive drug tests: Selegiline breaks down into inactive forms of methamphetamine in the body and can cause false positive results in drug tests for amphetamines and methamphetamines.

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