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Dr. Fernandez

Post of the Week: Zelepar

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What about orally-disintegrating selegiline (zelepar)? Is this really worth the added expense?


A new selegiline formulation, zydis selegiline (or orally-disintigrating selegiline), dissolves on contact with saliva and is absorbed mostly in the buccal region. It does not need to go through the stomach to be absorbed. Because it is absorbed through the blood vessels underneath the tongue and goes directly to the blood stream, it bypasses the gut and the “filtration” of the liver. Therefore, it results in a higher concentration of selegiline in the blood stream that enters the brain. Because the drug bypasses “checkpoints” in the liver that break it down into inactive by-products, the amount of amphetamine metabolites are reduced 10-fold using the route of administration (Seager 1998; Clarke et al 2003). Of course these are mostly theoretical advantages. As to whether they translate to clinically meaningful advantages remains to be seen. Having said that, we do know from the pivotal trail on zelepar that led to its FDA approval in the United States that is a safe and well-tolerated drug, taken only once per day (unlike its older predecessor requiring a twice per day dosage), and in lessens the off time of Parkinson’s patients when taken along with levodopa. It is therefore indicated as an add on medication to levodopa in advancing Parkinson’s disease.

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