Selegiline is a relatively selective, irreversible monoamine oxidase type B (MAO-B) inhibitor. In the brain, MAO-B is partly responsible for the catabolism of dopamine. Selegiline boosts the symptomatic effect of levodopa by slowing the breakdown of levodopa-derived dopamine. Selegiline is known as deprenyl or 1-deprenyl.
Selegiline is beneficial as an adjunct to levodopa for patients who are experiencing a deterioration in the quality of their response. Selegiline delays the need for levodopa in early patients. For patients with motor fluctuations, selegiline reduces "off" time and extends the short duration response of levodopa. Thus, selegiline provides symptomatic benefit for advanced patients with motor fluctuations. In addition, there is interest in whether selegiline can slow progression of Parkinson's disease. An early retrospective study found that patients on selegiline lived longer than those not on selegiline. In laboratory models, selegiline provides a neuroprotective effect. Although several clinical studies have yielded results which are consistent with a neuroprotective action, this has yet to be conclusively demonstrated in Parkinson's disease patients.
Important Information About Selegiline
Side effects of selegiline
Selegiline is generally very well tolerated. Because it is metabolized to amphetamine derivatives, it is typically administered in the morning and at midday rather than in the evening to minimize the potential for insomnia. Some patients experience gastrointestinal side effects. Unusual side effects include increased liver enzymes and aggravation of peptic ulcer disease. When administered concurrently with levodopa, the most common side effect is an exacerbation of dopaminergic adverse effects. if a patient has peak-dose dyskinesias or hallucinations on levodopa, these may worsen with the addition of selegiline. The physician should then lower the levodopa dose to alleviate these symptoms. For patients who have side effects on levodopa/PDI alone, it may be helpful to introduce selegiline at a low dose (one half tablet). This will allow an opportunity to reduce the levodopa dose in response to a worsening of side effects as the selegiline dose is escalated. A reduction of levodopa/PDI of approximately 20% is often required.
If you experience any of the following serious side effects, stop taking selegiline and seek emergency medical attention:
In case of the following less serious side effects , continue to take selegiline and talk to your doctor.
A constellation of symptoms known as the serotonin syndrome may occur with the use of serotomimetic agents, taken alone or in combination with MAO inhibitors including selegiline. These agents include serotonin reuptake inhibitors, tricyclic and tetracyclic antidepressants, meperidine and other opiates, dextromethorphan, and tryptophan. The syndrome is characterized by various combinations of confusion, agitation, restlessness, rigidity, hyperreflexia, shivering, autonomic instability, myocionus, coma, low grade fever, nausea, diarrhea, diaphoresis, flushing, and rarely rhabdomyolysis and death. Patients taking selegiline should therefore avoid meperidine and other opiates. The actual incidence of serious events when selegiline is used in combination with antidepressants is unclear. As many patients with Parkinson's disease suffer with depression, this issue raises difficult management questions.
Do Not Take Selegiline If
Selegiline should not be taken if you are taking meperidine (Demerol).
Before taking selegiline, tell your doctor if you are taking:
Before taking selegiline, tell your doctor if you have any other medical conditions. You may require special monitoring or a special dosage because of other conditions or other medicines that you are taking.
Selegiline is in the FDA pregnancy category C. This means that it is not known whether selegiline will harm an unborn baby. Do not take selegiline without first talking to your doctor if you are pregnant.
It is also not known whether selegiline will harm a nursing infant. Do not take selegiline without first talking to your doctor if you are breast-feeding a baby.
Overdosing on Selegiline
If you take an overdose, seek emergency medical attention.
Symptoms of a selegiline overdose include excitement, irritability, nervousness, insomnia, dizziness, severe headache, hallucinations, weakness, sweating, and seizures.
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