Azilect

Name: Azilect

How should this medicine be used?

Rasagiline comes as a tablet to take by mouth. It is usually taken once a day with or without food. Take rasagiline at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take rasagiline exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Your doctor may start you on a low dose of rasagiline and may increase your dose based upon your body's response to this medication.

Do not stop taking rasagiline without talking to your doctor. Your doctor will probably decrease your dose gradually. If you suddenly stop taking rasagiline, you may experience withdrawal symptoms such as a fever; muscle stiffness; unsteadiness, wobbliness, or lack of coordination; or changes in consciousness. Tell your doctor if you experience any of these symptoms when your dose of rasagiline is decreased.

Other uses for this medicine

This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

Rasagiline Side Effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using rasagiline and call your doctor at once if you have:

  • extreme drowsiness, falling asleep suddenly, even after feeling alert;
  • unusual changes in mood or behavior;
  • a light-headed feeling, like you might pass out;
  • worsening symptoms of Parkinson's disease (especially uncontrolled muscle movements); or
  • dangerously high blood pressure--severe headache, blurred vision, pounding in your neck or ears, nosebleed, anxiety, confusion, severe chest pain, shortness of breath, irregular heartbeats, seizure.

Some people taking rasagiline with levodopa have fallen asleep during normal daytime activities such as working, talking, eating, or driving. Tell your doctor if you have any problems with daytime sleepiness or drowsiness.

You may have increased sexual urges, unusual urges to gamble, or other intense urges while taking this medicine. Talk with your doctor if this occurs.

Common side effects may include:

  • dizziness, drowsiness;
  • sleep problems (insomnia), strange dreams;
  • depressed mood;
  • upset stomach, nausea, vomiting, stomach pain;
  • loss of appetite, weight loss;
  • constipation;
  • joint pain or stiffness;
  • swelling in your hands or feet;
  • dry mouth, cough; or
  • flu symptoms (fever, chills, body aches).

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Rasagiline Dosage

Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Your dose may be different if you take rasagiline alone than if you take rasagiline with other Parkinson's medications. Follow your doctor's dosing instructions very carefully.

Rasagiline is only part of a complete program of treatment that may include a diet plan created for you by your doctor or nutrition counselor.

Call your doctor if your Parkinson's symptoms do not improve, or if they get worse while using rasagiline.

Do not stop using rasagiline suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to safely stop using rasagiline.

Store at room temperature away from moisture and heat.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include drowsiness, dizziness, severe headache, hallucinations, feeling agitated or irritable, fast and uneven heart rate, muscle spasms, sweating, cold or clammy skin, shallow breathing, fainting, or seizure (convulsions).

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Description

AZILECT® tablets contain rasagiline (as the mesylate), a propargylamine-based drug indicated for the treatment of idiopathic Parkinson's disease. It is designated chemically as: 1H-Inden-1amine, 2, 3-dihydro-N-2-propynyl-, (1R)-, methanesulfonate. The empirical formula of rasagiline mesylate is (C12H13N)CH4SO3 and its molecular weight is 267.34.

Its structural formula is:

Rasagiline mesylate is a white to off-white powder, freely soluble in water or ethanol and sparingly soluble in isopropanol. Each AZILECT tablet for oral administration contains rasagiline mesylate equivalent to 0.5 mg or 1 mg of rasagiline base.

Each AZILECT tablet also contains the following inactive ingredients: mannitol, starch, pregelatinized starch, colloidal silicon dioxide, stearic acid and talc.

Manufacturer

  • Teva CNS

Side Effects of Azilect

Common side effects of Azilect when taken alone are:

  • flu syndrome
  • joint pain
  • depression
  • indigestion

 When taken with levodopa common side effects include:

  • uncontrolled movements (dyskinesia)
  • accidental injury
  • weight loss
  • low blood pressure when standing
  • vomiting
  • anorexia
  • joint pain
  • abdominal pain
  • nausea
  • constipation
  • dry mouth
  • rash
  • abnormal dreams
  • fall

This is not a complete list of Azilect side effects. Ask your doctor or pharmacist for more information.

Azilect Interactions

Tell your doctor about all the medicines you take including prescription or non-prescription medicines, vitamins, or herbal supplements. Especially tell your doctor if you take:

  • meperidine
  • tramadol
  • methadol
  • propoxyphene
  • dextromethorphan (found in many non-prescription cough medicines)
  • other monoamine oxidase inhibitors (MAOIs)
  • St. John's wort
  • cyclobenzaprine
  • medicines for depression (antidepressants)
  • ciprofloxacin

This is not a complete list of Azilect drug interactions. Ask your doctor or pharmacist for more information.

Azilect Precautions

Serious side effects have occurred with Azilect when taken with antidepressant medicines. Tell your doctor if you are taking an antidepressant.

You should not take Azilect if you have moderate to severe liver disease.

You should not take more than 1 mg of Azilect per day. When taken in amounts greater than 1 mg per day, Azilect may cause a serious and possibly dangerous increase in blood pressure called hypertensive crisis.

Talk to your doctor about monitoring for skin cancer (melanoma) on a regular basis. People taking Azilect may have a higher risk of melanoma.

Azilect and Pregnancy

It is not known if Azilect will harm an unborn baby if taken during pregnancy. Azilect should be used during pregnancy only if the potential benefit justifies the potential risk to the unborn baby.

Azilect and Lactation

Azilect inhibits prolactin secretion and may inhibit breast milk secretion. It is not known if Azilect is excreted in human breast milk or if it will harm your baby.

Dosing & Uses

Dosage Forms & Strengths

tablet

  • 0.5mg
  • 1mg

Parkinson Disease

Monotherapy: 1 mg PO qDay

Adjunct without levodopa: 1 mg PO qDay

Adjunct to levodopa: 0.5 mg PO qDay initially, may increase to 1 mg/day if needed and tolerated; consider reducing levodopa dose

Dosage Modifications

Coadministration with CYP1A2 inhibitors (eg, ciprofloxacin): Not to exceed 0.5 mg/day

Renal impairment: No dosage adjustment required for mild-to-moderate; not studied in severe

Hepatic impairment

  • Mild (Child-Pugh A): Not to exceed 0.5 mg/day
  • Moderate-to-severe (Child-Pugh B/C): Do not use

Dosing Considerations

Do not exceed recommended doses because of risk for hypertension

<18 years: Safety and efficacy not established

Patient Handout

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What is the most important information I should know about rasagiline?

Many medicines can interact with rasagiline and should not be used at the same time. Your doctor may need to change your treatment plan if you use any of the following drugs: cyclobenzaprine (a muscle relaxer), dextromethorphan (a cough medicine), meperidine (Demerol), methadone, St. John's wort, or tramadol.

Do not use rasagiline if you have used any other MAO inhibitor in the past 14 days. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, methylene blue injection, phenelzine, selegiline, tranylcypromine, and others.

What should I discuss with my health care provider before taking rasagiline?

You should not take rasagiline if you are allergic to it.

Many medicines can interact with rasagiline and should not be used at the same time. Your doctor may need to change your treatment plan if you use any of the following drugs:

  • cyclobenzaprine (a muscle relaxer);

  • dextromethorphan (contained in many over-the-counter cough medicines);

  • meperidine (Demerol);

  • methadone;

  • St. John's wort; or

  • tramadol (Ultram, Ultracet).

Do not use rasagiline if you have used any other MAO inhibitor in the past 14 days. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, methylene blue injection, phenelzine, selegiline, tranylcypromine, and others.

To make sure rasagiline is safe for you, tell your doctor if you have:

  • high or low blood pressure;

  • liver disease;

  • if you take an antidepressant; or

  • if you take ciprofloxacin (an antibiotic).

People with Parkinson's disease may have a higher risk of skin cancer (melanoma). Talk to your doctor about this risk and what skin symptoms to watch for.

It is not known whether rasagiline will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medicine.

It is not known whether rasagiline passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Azilect Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed following oral administration, with peak plasma concentration attained within approximately 1 hour.1 2

Absolute bioavailability is about 36%.1 2

Duration

Inhibition of platelet MAO-B in humans persists ≥1 week after last dose.1

Food

High-fat meals decrease peak plasma concentrations and AUC of rasagiline by approximately 60 and 20%, respectively.1 2 Because of modest effect on AUC, may administer rasagiline without regard to meals.1 2

Special Populations

Mild hepatic impairment (Child-Pugh score of 5–6) increases rasagiline AUC and peak plasma concentration by twofold and 1.4-fold, respectively; moderate hepatic impairment (Child-Pugh score of 7–9) increases rasagiline AUC and peak plasma concentration by sevenfold and twofold, respectively.1 (See Hepatic Impairment under Dosage and Administration.)

Moderate renal impairment increases AUC of 1-aminoindan (major metabolite of rasagiline) by1.5-fold.1 Because 1-aminoindan does not inhibit MAO, no dosage adjustment needed in patients with mild or moderate renal impairment.1 Data not available for patients with severe renal impairment.1

Distribution

Extent

Readily crosses the blood-brain barrier.2 8

Plasma Protein Binding

Approximately 88–94% (with 61–63% bound to albumin).1

Elimination

Metabolism

Undergoes almost complete biotransformation in the liver prior to excretion.1 Metabolized via dealkylation and/or hydroxylation by CYP isoenzymes, principally CYP1A2.1 2

Elimination Route

Excreted in urine (62%) and feces (7%) as metabolites over 7 days; <1% excreted as unchanged drug in urine.1 2

Half-life

Mean steady-state or terminal half-life is 31 or 1.342 hours, respectively.1 2 However, no correlation between pharmacokinetic profile and pharmacologic effects because rasagiline irreversibly inhibits MAO-B, and restoration of normal enzyme activity depends on the rate of de novo enzyme synthesis.1 2

Commonly used brand name(s)

In the U.S.

  • Azilect

Available Dosage Forms:

  • Tablet

Therapeutic Class: Antiparkinsonian

Pharmacologic Class: Monoamine Oxidase Inhibitor, Type B

What are some other side effects of Azilect?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Flu-like signs.
  • Headache.
  • Upset stomach or throwing up.
  • Hard stools (constipation).
  • Loose stools (diarrhea).
  • Dizziness.
  • Feeling sleepy.
  • Dry mouth.
  • Not hungry.
  • Belly pain.
  • Weight loss.
  • Bad dreams.
  • Joint pain.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

How do I store and/or throw out Azilect?

  • Store at room temperature.
  • Store in a dry place. Do not store in a bathroom.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Check with your pharmacist about how to throw out unused drugs.

Consumer Information Use and Disclaimer

  • If your symptoms or health problems do not get better or if they become worse, call your doctor.
  • Do not share your drugs with others and do not take anyone else's drugs.
  • Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
  • Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
  • Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about this medicine, please talk with your doctor, nurse, pharmacist, or other health care provider.
  • If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take Azilect or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to Azilect. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Review Date: October 4, 2017

Dosage Forms and Strengths

Azilect 0.5 mg Tablets: White to off-white, round, flat, beveled tablets, debossed with “GIL 0.5” on one side and plain on the other side containing, as the active ingredient, rasagiline mesylate equivalent to 0.5 mg of rasagiline base.

Azilect 1 mg Tablets: White to off-white, round, flat, beveled tablets, debossed with “GIL 1” on one side and plain on the other side containing, as the active ingredient, rasagiline mesylate equivalent to 1 mg of rasagiline base.

What is rasagiline (azilect)?

Rasagiline is a monoamine oxidase-B (MAO-B) inhibitor. It works by increasing the levels of certain chemicals in the brain.

Rasagiline is used to treat the symptoms of Parkinson's disease. Rasagiline is sometimes used with another drug called levodopa.

Rasagiline may also be used for other purposes not listed in this medication guide.

Important information

Many medicines can interact with Azilect and should not be used at the same time. Your doctor may need to change your treatment plan if you use any of the following drugs: cyclobenzaprine (a muscle relaxer), dextromethorphan (a cough medicine), meperidine (Demerol), methadone, St. John's wort, or tramadol.

Do not use Azilect if you have used any other MAO inhibitor in the past 14 days. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, methylene blue injection, phenelzine, selegiline, tranylcypromine, and others.

Before you take Azilect, tell your doctor if you have liver disease.

There are many other drugs that can cause serious medical problems if you take them together with Azilect. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor. Keep a list of all your medicines and show it to any healthcare provider who treats you. While you are taking this medicine and for 2 weeks after you stop taking it, you may not be able to eat certain types of cheese. Follow your doctor's instructions. Rasagiline may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

What should I avoid while taking Azilect?

Azilect may impair your thinking or reactions. Avoid driving or operating machinery until you know how this medicine will affect you. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

Drinking alcohol can increase certain side effects of rasagiline.

Also avoid eating foods that are high in tyramine, such as aged cheeses, sour cream, yogurt, avocados, bananas, soy sauce, and pepperoni or other dried meats. Eating tyramine while you are taking Azilect can raise your blood pressure to dangerous levels which could cause life-threatening side effects.

What other drugs will affect Azilect?

Taking Azilect while you are also taking an antidepressant can cause high levels of serotonin in your body. Symptoms of this condition include agitation, hallucinations, fever, fast heart rate, overactive reflexes, nausea, vomiting, diarrhea, loss of coordination, and fainting. Tell your doctor if you have taken an antidepressant during the 2-week period before you start taking Azilect.

Taking Azilect with other drugs that make you sleepy can worsen this effect. Ask your doctor before taking this medicine with a sleeping pill, narcotic pain medicine, muscle relaxer, or medicine for anxiety or seizures.

Many drugs can interact with rasagiline, and some drugs should not be used together. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide. Tell your doctor about all medicines you use, and those you start or stop using during your treatment with Azilect. Give a list of all your medicines to any healthcare provider who treats you.

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