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Azilect

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Azilect

Side Effects
Interactions

SIDE EFFECTS

The following adverse reactions are described in more detail in the WARNINGS AND PRECAUTIONS section of the label:

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to the incidence of adverse reactions in the clinical trials of another drug and may not reflect the rates of adverse reactions observed in practice.

During the clinical development of AZILECT, Parkinson's disease patients received AZILECT as initial monotherapy (Study 1) and as adjunct therapy (Study 2, Study 3, Study 4). As the populations in these studies differ, not only in the adjunct use of dopamine agonists or levodopa during AZILECT treatment, but also in the severity and duration of their disease, the adverse reactions are presented separately for each study.

Monotherapy Use of AZILECT

In Study 1, approximately 5% of the 149 patients treated with AZILECT discontinued treatment due to adverse reactions compared to 2% of the 151 patients who received placebo.

The only adverse reaction that led to the discontinuation of more than one patient was hallucinations.

The most commonly observed adverse reactions in Study 1 (incidence in AZILECT-treated patients 3% or greater than the incidence in placebo-treated patients) included flu syndrome, arthralgia, depression, and dyspepsia. Table 1 lists adverse reactions that occurred in 2% or greater of patients receiving AZILECT as monotherapy and were numerically more frequent than in the placebo group in Study 1.

Table 1: Adverse Reactions* in Study 1

  AZILECT 1 mg
(N=149)
Placebo
(N=151)
% of Patients % of Patients
Headache 14 12
Arthralgia 7 4
Dyspepsia 7 4
Depression 5 2
  AZILECT 1 mg (N=149) Placebo (N=151)
  % of Patients % of Patients
Fall 5 3
Flu syndrome 5 1
Conjunctivitis 3 1
Fever 3 1
Gastroenteritis 3 1
Rhinitis 3 1
Arthritis 2 1
Ecchymosis 2 0
Malaise 2 0
Neck Pain 2 0
Paresthesia 2 1
Vertigo 2 1
*Incidence 2% or greater in AZILECT 1 mg group and numerically more frequent than in placebo group

There were no significant differences in the safety profile based on age or gender.

Adjunct Use of AZILECT

AZILECT was studied as an adjunct therapy without levodopa (Study 2), or as an adjunct therapy to levodopa, with some patients also taking dopamine agonists, COMT inhibitors, anticholinergics, or amantadine (Study 3 and Study 4).

In Study 2, approximately 8% of the 162 patients treated with AZILECT discontinued treatment due to adverse reactions compared to 4% of the 164 patients who received placebo.

Adverse reactions that led to the discontinuation of more than one patient were nausea and dizziness.

The most commonly observed adverse reactions in Study 2 (incidence in AZILECT-treated patients 3% or greater than incidence in placebo-treated patients) included peripheral edema, fall, arthralgia, cough, and insomnia. Table 2 lists adverse reactions that occurred in 2% or greater in patients receiving AZILECT as adjunct therapy without levodopa and numerically more frequent than in the placebo group in Study 2.

Table 2: Adverse Reactions* in Study 2

  AZILECT 1 mg
(N=162)
Placebo
(N=164)
% of Patients % of Patients
Dizziness 7 6
Peripheral edema 7 4
Headache 6 4
Nausea 6 4
Fall 6 1
Arthralgia 5 2
Back pain 4 3
Cough 4 1
Insomnia 4 1
Upper respiratory tract infection 4 2
Orthostatic hypotension 3 1
*Incidence 2% or greater in AZILECT 1 mg group and numerically more frequent than in placebo group

There were no significant differences in the safety profile based on age or gender.

In Study 3, adverse event reporting was considered more reliable than Study 4; therefore, only the adverse event data from Study 3 are presented below.

In Study 3, approximately 9% of the 164 patients treated with AZILECT 0.5 mg/day and 7% of the 149 patients treated with AZILECT 1 mg/day discontinued treatment due to adverse reactions, compared to 6% of the 159 patients who received placebo. The adverse reactions that led to discontinuation of more than one AZILECT-treated patient were diarrhea, weight loss, hallucination, and rash.

The most commonly observed adverse reactions in Study 3 (incidence in AZILECT-treated patients 3% or greater than the incidence in placebo-treated patients) included dyskinesia, accidental injury, weight loss, postural hypotension, vomiting, anorexia, arthralgia, abdominal pain, nausea, constipation, dry mouth, rash, abnormal dreams, fall and tenosynovitis.

Table 3 lists adverse reactions that occurred in 2% or greater of patients treated with AZILECT 1 mg/day and that were numerically more frequent than the placebo group in Study 3.

Table 3: Adverse Reactions* in Study 3

  AZILECT 1 mg
(N=149)
AZILECT 0.5 mg
(N=164)
Placebo
(N=159)
% of patients % of patients % of patients
Dyskinesia 18 18 10
Accidental injury 12 8 5
Nausea 12 10 8
Headache 11 8 10
Fall 11 12 8
Weight loss 9 2 3
Constipation 9 4 5
Postural hypotension 9 6 3
Arthralgia 8 6 4
Vomiting 7 4 1
  AZILECT 1 mg (N=149) AZILECT 0.5 mg (N=164) Placebo
(N=159)
  % of patients % of patients % of patients
Dry mouth 6 2 3
Rash 6 3 3
Somnolence 6 4 4
Abdominal pain 5 2 1
Anorexia 5 2 1
Diarrhea 5 7 4
Ecchymosis 5 2 3
Dyspepsia 5 4 4
Paresthesia 5 2 3
Abnormal dreams 4 1 1
Hallucinations 4 5 3
Ataxia 3 6 1
Dyspnea 3 5 2
Infection 3 2 2
Neck pain 3 1 1
Sweating 3 2 1
Tenosynovitis 3 1 0
Dystonia 3 2 1
Gingivitis 2 1 1
Hemorrhage 2 1 1
Hernia 2 1 1
Myasthenia 2 2 1
*Incidence 2% or greater in AZILECT 1 mg group and numerically more frequent than in placebo group Several of the more common adverse reactions seemed dose-related, including weight loss, postural hypotension, and dry mouth. There were no significant differences in the safety profile based on age or gender. During all Parkinson's disease phase 2/3 clinical trials, the long-term safety profile was similar to that observed with shorter duration exposure.

Read the Azilect (rasagiline) Side Effects Center for a complete guide to possible side effects

DRUG INTERACTIONS

Meperidine

Serious, sometimes fatal reactions have been precipitated with concomitant use of meperidine (e.g., Demerol and other tradenames) and MAO inhibitors including selective MAO-B inhibitors [see CONTRAINDICATIONS].

Dextromethorphan

The concomitant use of AZILECT and dextromethorphan was not allowed in clinical studies. The combination of MAO inhibitors and dextromethorphan has been reported to cause brief episodes of psychosis or bizarre behavior. Therefore, in view of AZILECT's MAO inhibitory activity, dextromethorphan is contraindicated for use with AZILECT [see CONTRAINDICATIONS].

MAO Inhibitors

AZILECT is contraindicated for use with other MAO inhibitors because of the increased risk of nonselective MAO inhibition that may lead to a hypertensive crisis [see CONTRAINDICATIONS].

Sympathomimetic Medications

The concomitant use of AZILECT and sympathomimetic medications was not allowed in clinical studies. Severe hypertensive reactions have followed the administration of sympathomimetics and nonselective MAO inhibitors. Hypertensive crisis has been reported in patients taking the recommended dose of AZILECT and sympathomimetic medications. Severe hypertension has been reported in patients taking the recommended dose of AZILECT and ophthalmic drops containing sympathomimetic medications.

Because AZILECT is a selective MAOI, hypertensive reactions are not ordinarily expected with the concomitant use of sympathomimetic medications. Nevertheless, caution should be exercised when concomitantly using recommended doses of AZILECT with any sympathomimetic medications including nasal, oral, and ophthalmic decongestants and cold remedies.

Antidepressants

Concomitant use of AZILECT with one of many classes of antidepressants (e.g., SSRIs, SNRIs, triazolopyridine, tricyclic or tetracyclic antidepressants) is not recommended [see WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY]. Concomitant use of AZILECT and MAO inhibitors is contraindicated [see CONTRAINDICATIONS].

Ciprofloxacin Or Other CYP1A2 Inhibitors

Rasagiline plasma concentrations may increase up to 2 fold in patients using concomitant ciprofloxacin and other CYP1A2 inhibitors. This could result in increased adverse events. Patients taking concomitant ciprofloxacin or other CYP1A2 inhibitors should not exceed a dose of AZILECT 0.5 mg once daily [see WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY].

Tyramine/Rasagiline Interaction

MAO in the gastrointestinal tract and liver (primarily type A) provides protection from exogenous amines (e.g., tyramine) that have the capacity, if absorbed intact, to cause a tyramine reaction with hypertension including clinical syndromes referred to as hypertensive urgency, crisis, or emergency. Foods and medications containing large amounts of exogenous amines (e.g., from fermented cheese, herring, over-the-counter cough/cold medications) may cause release of norepinephrine resulting in a rise in systemic blood pressure.

Results of a special tyramine challenge study indicate that rasagiline is selective for MAO-B at recommended doses and can be used without dietary tyramine restriction. However, certain foods may contain very high amounts (i.e., 150 mg or greater) of tyramine and could potentially cause a hypertensive reaction in individual patients taking AZILECT due to increased sensitivity to tyramine. Selectivity for inhibiting MAO-B diminishes in a dose-related manner as the dose is progressively increased above the recommended daily doses.

There were no cases of hypertensive crisis in the clinical development program associated with 1 mg daily AZILECT treatment, in which most patients did not follow dietary tyramine restriction.

There have been postmarketing reports of patients who experienced significantly elevated blood pressure (including rare cases of hypertensive crisis) after ingestion of unknown amounts of tyramine-rich foods while taking recommended doses of AZILECT. Patients should be advised to avoid foods containing a very large amount of tyramine while taking recommended doses of AZILECT [see WARNINGS AND PRECAUTIONS].

Dopaminergic Antagonists

It is possible that dopamine antagonists, such as antipsychotics or metoclopramide, could diminish the effectiveness of AZILECT.

Drug Abuse And Dependence

Controlled Substance

AZILECT is not a controlled substance.

Abuse

Studies conducted in mice and rats did not reveal any potential for drug abuse and dependence. Clinical trials have not revealed any evidence of the potential for abuse, tolerance or physical dependence; however, systematic studies in humans designed to evaluate these effects have not been performed.

Dependence

Studies conducted in mice and rats did not reveal any potential for drug abuse and dependence. Clinical trials have not revealed any evidence of the potential for abuse, tolerance or physical dependence; however, systematic studies in humans designed to evaluate these effects have not been performed.

Read the Azilect Drug Interactions Center for a complete guide to possible interactions

Last reviewed on RxList: 6/12/2014
This monograph has been modified to include the generic and brand name in many instances.

Side Effects
Interactions
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