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(selegiline HCl) Orally Disintegrating Tablets
Zelapar (selegiline HCl) is indicated as an adjunct in the management of patients with Parkinson's disease being
treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. Zelapar is
a once-daily treatment for Parkinson's disease patients experiencing wearing off and demonstrates excellent safety and
tolerability. Zelapar uses an innovative transmucosal drug delivery that improves bioavailability so that patients can
get more free hours.
Zelapar is for patients with Parkinson's disease and deteriorating response to levodopa/carbidopa. Zelapar adds more
active hours to the lives of people with Parkinson's disease (PD) by significantly bypassing the gut and first-pass
hepatic metabolism thereby delivering more active drug, at a lower dose. Studies have shown that adding Zelapar to
l-dopa reduces OFF time by up to 2.2 hours per day.
Zelapar is a selective and irreversible MAO-B inhibitor. Put simply, Zelapar makes more dopamine available in the
brain by preventing its breakdown. Dopamine is the chemical in the brain responsible for the control of movement - the
very substance that people with Parkinson's disease need. Levodopa, a dopamine replacer, is converted into dopamine by
the brain. Adding Zelapar boosts the brain's natural supply of dopamine. It is added to levodopa/carbidopa treatment to
help manage the symptoms of PD when there is a reduced response to this therapy.
One concern with conventional swallowed selegiline is that much of the active drug is broken down during digestion.
Increasing the dose to deliver more drug to the brain also increases the level of metabolites (including amphetamine and
methamphetamine, substances associated with toxicity) made during digestion. Zelapar utilizes a unique, Zydis
technology which allows it to pass through the body in a different way. Zelapar tablets dissolve within seconds in the
mouth, and the active drug moves into the bloodstream directly into systemic circulation and ultimately to the brain,
were it is needed. Because the digestive system is bypassed, there are fewer metabolites and side effects.
Phase 4 multi-center studies are enrolling patients with Parkinson's Disease who are receiving Zelapar as adjunctive treatment to L-dopa.
Named after Dr. James Parkinson, a London physician who first described the disease in 1817, Parkinson's disease (PD) is
a chronic, progressive disorder of the central nervous system. Once you get PD, it does not go away and the symptoms get
worse over time. In general, tremor is followed by stiffness, slowness of movement (bradykinesia), and in the later
stages, lack of balance. Emotional symptoms such as depression and anxiety are also characteristic of Parkinson's
disease.
Although the exact cause of PD is unknown, many of the symptoms occur when certain brain cells, called neurons, die or
become damaged. Neurons produce a chemical substance called dopamine that is important in the control of movement. Over
time, the dopamine level in the brain decreases and a chemical imbalance is caused that makes movement more difficult
and less fluid. By the time characteristics of Parkinson's disease like tremor and stiffness are visible, the normal
level of dopamine has been greatly reduced.
Perhaps the biggest adjustment PD patients will have to make is learning to live with the "ON-OFF" cycle. This is the
back and forth between periods of time with and without symptoms. During "ON" times patients report that they feel
relatively fluid, clear, and in control of their movements. On the contrary, during "OFF" periods, patients experience
stiffness, lack of muscular coordination and pain. Most patients have visible symptoms. Typically, patients cycle
between ON and OFF periods 3 - 4 times every day.
Detecting PD in its early stages can be difficult, but most skilled practitioners can usually diagnose PD accurately.
If you think you might have Parkinson's disease, or if your doctor suspects that you may, he will perform an assessment
to detect Parkinson's disease that consists of
- Taking your medical history
- Questions about things you do at home on a regular basis such as dressing, showering, bathing, walking, and
eating
- A special exam by a neurologist
More sophisticated tests are available if a diagnosis is uncertain, but these are generally not used due to their cost
and the overall strength of the standard exam.
Zelapar is a special formulation of the drug selegiline that adds more active hours for patients with Parkinson's disease (PD). Doctors may recommend adding Zelapar to levodopa/carbidopa treatment when patients are experiencing a reduced response to this therapy.
Do not take Zelapar if you are allergic to selegiline or any of the other ingredients in Zelapar. Zelapar should not be taken with certain medications. Discuss any medicine you are taking with your doctor. Zelapar should not be taken with meperedine (DEMEROL®) or other opiods. Rare cases of high blood pressure have been associated with taking conventional forms of selegiline with foods containing tyramine. Zelapar may cause you to have low blood pressure when you stand (this is more common in older patients than in younger ones). If you are pregnant, you must speak to your doctor about whether to take Zelapar. (Zelapar should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.) Do not take more than 2 tablets (2.5 mg) a day.
Zelapar was very well tolerated in clinical trials. The most commonly reported side effects were dizziness, nausea, pain, headache, trouble sleeping, runny nose, involuntary movements, back pain, skin disorders, mouth inflammation, and upper stomach pain. In addition, 5.2% of patients discontinued Zelapar therapy due to side effects (vs. 1% with placebo).
You may need your levodopa dose reduced after starting Zelapar therapy. Be sure to speak with your doctor if you experience any side effects.
Please see full Prescribing Information at www.zelapar.com |
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