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Common name
Eldepryl (Selegiline)
Synonyms: Selegin, Selgin, Carbex, Jumex, L-Deprenalin, Sd Deprenyl, Selegilina
Description
ELDEPRYL (selegiline hydrochloride) is a levorotatory acetylenic derivative of phenethylamine. It is commonly referred to in the clinical and pharmacological literature as l-deprenyl. The chemical name is: (R)-(-)-N,2-dimethyl-N-2-propynylphenethylamine hydrochloride. It is a white to near white crystalline powder, freely soluble in water, chloroform, and methanol.
Selegiline prevents the breakdown of a chemical in the brain called dopamine. Low levels of this chemical are associated with Parkinson's disease.
Selegiline is used together with other medicines to treat symptoms of Parkinson's disease.
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Active Ingredients:
Selegiline
Therapeutic actions:
Selegiline is best known as an irreversible inhibitor of monoamine oxidase (MAO), an intracellular enzyme associated with the outer membrane of mitochondria. Selegiline inhibits MAO by acting as a 'suicide' substrate for the enzyme; that is, it is converted by MAO to an active moiety which combines irreversibly with the active site and/or the enzyme's essential FAD cofactor. Because selegiline has greater affinity for type B rather than for type A active sites, it can serve as a selective inhibitor of MAO type B if it is administered at the recommended dose.
MAOs are widely distributed throughout the body; their concentration is especially high in liver, kidney, stomach, intestinal wall, and brain. MAOs are currently subclassified into two types, A and B, which differ in their substrate specificity and tissue distribution. In humans, intestinal MAO is predominantly type A, while most of that in brain is type B.
In CNS neurons, MAO plays an important role in the catabolism of catecholamines (dopamine, norepinephrine and epinephrine) and serotonin. MAOs are also important in the catabolism of various exogenous amines found in a variety of foods and drugs. MAO in the GI tract and liver (primarily type A), for example, is thought to provide vital protection from exogenous amines (e.g., tyramine) that have the capacity, if absorbed intact, to cause a 'hypertensive crisis,' the so-called 'cheese reaction.' (If large amounts of certain exogenous amines gain access to the systemic circulation - e.g., from fermented cheese, red wine, herring, over-the-counter cough/cold medications, etc. - they are taken up by adrenergic neurons and displace norepinephrine from storage sites within membrane bound vesicles. Subsequent release of the displaced norepinephrine causes the rise in systemic blood pressure, etc.)
What is it used for?: (Indications:)
ELDEPRYL is indicated as an adjunct in the management of Parkinsonian patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy.
Contraindications and cautions:
Do not use this medication if you are allergic to selegiline, or if you have used any of the following drugs within the past 14 days:
• cough or cold medicine that contains dextromethorphan;
• meperidine (Demerol), propoxyphene (Darvon, Darvocet), or tramadol (Ultram, Ultracet);
• methadone (Dolophine, Methadose); or
• other MAO inhibitors such as isocarboxazid (Marplan), tranylcypromine (Parnate), phenelzine (Nardil), rasagiline (Azilect), or transdermal selegiline (Emsam).
After you stop taking selegiline, you must wait at least 14 days before taking any of the medications listed above.
Before using this medicine, tell your doctor if you have kidney disease, liver disease, heart disease, high or low blood pressure, or a seizure disorder. If you have any of these conditions, you may need a dose adjustment or special tests to safely take selegiline. FDA pregnancy category C. This medication may be harmful to an unborn baby. It is not known whether selegiline passes into breast milk or if it could harm a nursing baby. Do not take selegiline without telling your doctor if you are breast-feeding a baby. The selegiline disintegrating tablets may contain phenylalanine.
Side effects:
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop taking selegiline and call your doctor at once if you have any of these serious side effects:
• sudden and severe headache, confusion, blurred vision, problems with speech or balance, nausea, vomiting, chest pain, seizure (convulsions), and sudden numbness or weakness (especially on one side of the body);
• feeling light-headed, fainting;
• hallucinations;
• feeling restless, agitated, or irritable;
• twitching muscle movements; or
• painful or difficult urination.
Less serious side effects may include:
• dizziness, weakness;
• sleep problems (insomnia);
• runny or stuffy nose;
• back pain;
• constipation; or
• mouth sores or ulcers, pain with swallowing (while using Zelapar).
Interactions:
Before taking selegiline, tell your doctor if you are using any of the following drugs:
• carbamazepine (Tegretol);
• diet pills or cold medicines that contain ephedrine, pseudoephedrine, or phenylephrine;
• nafcillin (Unipen);
• phenobarbital (Luminal, Solfoton);
• rifampin (Rifadin, Rifater, Rifamate, Rimactane); or
• antidepressants such as amitriptyline (Elavil), amoxapine (Ascendin), bupropion (Wellbutrin, Zyban), citalopram (Celexa), clomipramine (Anafranil), desipramine (Norpramin), doxepin (Sinequan), duloxetine (Cymbalta), escitalopram (Lexapro), fluoxetine (Prozac), fluvoxamine (Luvox), imipramine (Tofranil), nortriptyline (Pamelor), paroxetine (Paxil), protriptyline (Vivactil), sertraline (Zoloft), venlafaxine (Effexor), or trimipramine (Surmontil).
This list is not complete and there are many other medicines that can cause serious medical problems if you take them together with selegiline.
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