Selegiline Hydrochloride

Name: Selegiline Hydrochloride

Description

ZELAPAR Orally Disintegrating Tablets contain selegiline hydrochloride, a levorotatory acetylenic derivative of phenethylamine. Selegiline hydrochloride is described chemically as: (-)-(R)-N, α- dimethyl-N-2-propynylphenethylamine hydrochloride and its structural formula is:

Its empirical formula is C13H17N·HCl, representing a molecular weight of 223.75. Selegiline hydrochloride is a white to almost white crystalline powder that is freely soluble in water, chloroform, and methanol.

ZELAPAR Orally Disintegrating Tablets are available for oral administration (not to be swallowed) in a strength of 1.25 mg. Each lyophilized orally disintegrating tablet contains the following inactive ingredients: gelatin, mannitol, glycine, aspartame, citric acid, yellow iron oxide, and grapefruit flavor.

Side effects

The following adverse reactions are discussed in more detail in the Warnings and Precautions section of labeling.

  • Risk for Hypertension [see WARNINGS AND PRECAUTIONS]
  • Risk of Serotonin Syndrome [see WARNINGS AND PRECAUTIONS]
  • Falling Asleep During Activities of Daily Living and Somnolence [see WARNINGS AND PRECAUTIONS]
  • Hypotension/Orthostatic Hypotension [see WARNINGS AND PRECAUTIONS]
  • Dyskinesia [see WARNINGS AND PRECAUTIONS]
  • Hallucinations/Psychotic-Like Behavior [see WARNINGS AND PRECAUTIONS]
  • Impulse Control / Compulsive Behaviors [see WARNINGS AND PRECAUTIONS]
  • Withdrawal Emergent Hyperpyrexia and Confusion [see WARNINGS AND PRECAUTIONS]
  • Melanoma [see WARNINGS AND PRECAUTIONS]
  • Irritation of the Buccal Mucosa [see WARNINGS AND PRECAUTIONS]
  • Risk for Phenylketonuric Patients [see WARNINGS AND PRECAUTIONS]
  • Effect on Renal Function [see WARNINGS AND PRECAUTIONS]

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, the incidence of adverse reactions (number of unique patients experiencing an adverse reaction per total number of patients treated) observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the incidence of adverse reactions observed in clinical practice.

Because the controlled trials performed during premarketing development both used a titration design (1.25 mg per day for 6 weeks, followed by 2.5 mg per day for 6 weeks), with a resultant confounding of time and dose, it was impossible to adequately evaluate the effects of dose on the incidence of adverse events.

The most common adverse reactions (treatment difference incidence at least 3% greater than placebo incidence) reported in the double-blind, placebo-controlled trials during ZELAPAR treatment were constipation, skin disorders, vomiting, dizziness, dyskinesia, insomnia, dyspnea, myalgia, and rash (see Table 1).

Of the 194 patients treated with ZELAPAR in the double-blind, placebo-controlled trials, 5% discontinued due to adverse reactions compared to 1% of the 98 patients who received placebo. Most common adverse reactions causing discontinuation of treatment included dizziness, chest pain, accidental injury, and myasthenia.

Incidence In Controlled Clinical Trials

Table 1 lists the adverse events reported in the placebo-controlled trials after at least one dose of ZELAPAR (incidence 2% or greater).

Table 1: Treatment-Emergent Adverse Events* Incidence in Double-Blind, Placebo- Controlled Trials (Events ≥2% of Patients Treated with ZELAPAR and Numerically More Frequent than the Placebo Group)

Body System/ Adverse Event ZELAPAR†
1.25/2.5 mg
N=194
%
Placebo†
N=98
%
Body as a Whole    
Back Pain 5 3
Chest Pain 2 0
Pain 8 7
Cardiovascular System    
Hypertension 3 2
Digestive System    
Constipation 4 0
Diarrhea 2 1
Dysphagia 2 1
Dyspepsia 5 3
Flatulence 2 1
Nausea 11 9
Stomatitis 5 4
Tooth Disorder 2 1
Vomiting 3 0
Hemic and Lymphatic System    
Ecchymosis 2 0
Metabolic and Nutritional Disorders    
Hypokalemia 2 0
Musculoskeletal System    
Leg Cramps 3 1
Myalgia 3 0
Nervous System    
Ataxia 3 1
Depression 2 1
Dizziness 11 8
Dry Mouth 4 2
Dyskinesia 6 3
Hallucinations 4 2
Headache 7 6
Insomnia 7 4
Somnolence 3 2
Tremor 3 1
Respiratory System    
Dyspnea 3 0
Pharyngitis 4 2
Rhinitis 7 6
Skin and Appendages    
Rash 4 1
Skin Disorders‡ 6 2
*Patients may have reported multiple adverse experiences during the study or at discontinuation; thus patients may be included in more than one category.
†Patients received concomitant levodopa.
‡Skin disorders represent any new skin abnormality that would not be characterized as rash or neoplastic lesion. These include events such as skin ulcer, fungal dermatitis, skin hypertrophy, contact dermatitis, herpes simplex, dry skin, sweating, urticaria, and pruritus.

Treatment-emergent adverse reactions for certain events were reported at a higher frequency by patients ≥65 years of age compared to patients <65 years [see Use In Specific Populations]. No consistent differences in the incidences of adverse reactions were observed between male and female patients.

There were insufficient data to assess the impact of race on the incidence of adverse reactions.

What is the most important information i should know about selegiline (eldepryl, zelapar)?

There are many other medicines that can cause serious medical problems if you take them together with selegiline. Tell your doctor about all other prescription and over-the-counter medications you use, including vitamins, minerals, and herbal products.

While taking selegiline, do not drink alcohol or eat foods that are high in tyramine, listed in the "What should I avoid while using selegiline?" section of this leaflet. Eating tyramine while you are using selegiline can raise your blood pressure to dangerous levels and cause life-threatening symptoms.

You should become very familiar with the list of foods to avoid while you are using selegiline.

Do not stop taking selegiline suddenly or you may have harmful side effects. Keep taking the medicine as prescribed. Talk with your doctor before stopping the medication.

You may have increased sexual urges, unusual urges to gamble, or other intense urges while taking this medication. Talk with your doctor if you believe you have any intense or unusual urges while taking selegiline.

What happens if i miss a dose (eldepryl, zelapar)?

Take the medication as soon as you remember. If it is almost time for the next dose, skip the missed dose and wait until your next regularly scheduled dose. Do not take extra medicine to make up the missed dose.

What should i avoid while using selegiline (eldepryl, zelapar)?

You must NOT eat foods that are high in tyramine, including:

  • air dried meats, aged or fermented meats, sausage or salami (including cacciatore and mortadella), pickled herring, and any spoiled or improperly stored beef, poultry, fish, or liver;
  • beer from a tap, beer that has not been pasteurized;
  • aged cheeses, including blue, boursault, brick, brie, camembert, cheddar, emmenthaler, gruyere, parmesan, romano, roquefort, stilton, and swiss;
  • over-the-counter supplements or cough and cold medicines that contain tyramine;
  • sauerkraut, soy beans, soy sauce, tofu, miso soup, bean curd, fava beans; or
  • yeast extracts (such as Marmite).

Eating tyramine while you are taking selegiline can raise your blood pressure to dangerous levels which could cause life-threatening side effects.

You should become very familiar with the list of foods to avoid while you are taking selegiline.

Avoid drinking alcohol while taking selegiline.

Selegiline can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert.

Where can i get more information?

Your pharmacist can provide more information about selegiline.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2013 Cerner Multum, Inc. Version: 5.03. Revision date: 12/15/2010.

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Stability

Storage

Oral

Capsules and Tablets

20–25°C.1 2

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Selegiline Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules

5 mg*

Eldepryl

Somerset

Selegiline Hydrochloride Capsules

Tablets

5 mg*

Selegiline Hydrochloride Tablets

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