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AZILECT is a brand name for Rasagiline, supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: AZILECT (rasagiline tablets) is indicated for: the treatment of the signs and symptoms of idiopathic Parkinson’s disease as initial monotherapy, and as adjunct therapy to dopamine agonists or to levodopa. The effectiveness of AZILECT was demonstrated in patients with early Parkinson’s disease who were receiving…
Verbatim from this product's HC label. Tap a section to expand.
1 Dosing Considerations There is no evidence that additional benefit will be obtained from the administration of doses higher than that recommended. Furthermore, higher doses will likely result in a loss of selectivity of rasagiline towards MAO-B with an increase in the inhibition of MAO-A.
There is an increased risk of adverse reactions with higher doses as well as an increased risk of hypertensive episode (“cheese reaction”). See 7 WARNINGS AND PRECAUTIONS, Hypertension and Tyramine/rasagiline interaction. 2 Recommended Dose and Dosage Adjustment Monotherapy The recommended AZILECT dose for the treatment of Parkinson’s disease patients is 1 mg administered once daily.
Adjunctive Therapy to Dopamine Agonists The recommended AZILECT dose as adjunctive therapy to dopamine agonists is 1 mg administered once daily. 5 – 1 mg once daily. 5 mg administered once daily. If a sufficient clinical response is not achieved, the dose may be increased to 1 mg administered once daily.
Change of levodopa dose in adjunct therapy:
When AZILECT is used in combination with levodopa a reduction of the levodopa dosage may be considered based upon individual response. During the controlled trials of AZILECT as adjunct therapy to levodopa, levodopa dosage was reduced in some patients.
In clinical studies, dosage reduction of levodopa was allowed within the first 6 weeks if dopaminergic side effects, including dyskinesia and hallucinations, emerged. 5 mg/day and 1 mg/day AZILECT groups, respectively. 5 mg/day, and 1 mg/day groups, respectively.
In the LARGO study levodopa dosage reduction occurred in 6% of patients in the placebo group and in 9% in the AZILECT 1 mg/day group. In patients who had their levodopa dosage reduced, the dose was reduced on average by about 13% and 11% in the placebo and the AZILECT groups, respectively.
AZILECT (rasagiline) Page 7 of 48 Patients with Hepatic Impairment:
AZILECT plasma concentration will increase in patients with hepatic impairment. 5 mg daily of AZILECT. AZILECT should not be used in patients with moderate to severe hepatic impairment. If patients progress from mild to moderate hepatic impairment, AZILECT should be stopped.
Renal Conclusive data are not available for renally impaired patients. As unconjugated rasagiline is not excreted by the kidney, AZILECT can be given at usual doses in patients with mild renal impairment. Due to the absence of adequate safety data, AZILECT should not be administered to patients with moderate to severe renal impairment.
1 Pregnant Women Reproductive studies conducted with rasagiline in animals did not reveal any negative effect at doses much higher than those used in the clinical studies. However, there are no adequate and well-controlled studies of rasagiline in pregnant women.
Because animal reproduction studies are not always predictive of human response, AZILECT should be used during pregnancy only if clearly needed. 2 Breast-feeding Experimental data indicated that rasagiline inhibits prolactin secretion and, thus, may inhibit lactation.
It is not known whether rasagiline is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when AZILECT is administered to a nursing woman. 3 Pediatrics Pediatrics (< 18 years of age): Based on the data submitted and reviewed by Health Canada, the safety and efficacy of AZILECT in pediatric patients has not been established; therefore, Health Canada has not authorized an indication for pediatric use.
4 Geriatrics Geriatrics (≥ 65 years of age): Approximately half of patients in clinical trials were 65 years and over. There were no significant differences in the safety profile of the geriatric and non -geriatric patients. 1 Adverse Reaction Overview The most commonly observed adverse events seen with Azilect were: abdominal pain, accidental injury, anorexia, arthralgia, constipation, cough, depression, dry mouth, dyskinesia, dyspepsia, ecchymosis, fall, flu syndrome, insomnia, nausea, paresthesia, peripheral edema, postural hypotension, rash, somnolence, vomiting, and weight loss.
, Hypertension and Tyramine/rasagiline interaction. 2 Recommended Dose and Dosage Adjustment Monotherapy The recommended AZILECT dose for the treatment of Parkinson’s disease patients is 1 mg administered once daily. Adjunctive Therapy to Dopamine Agonists The recommended AZILECT dose as adjunctive therapy to dopamine agonists is 1 mg administered once daily.
5 – 1 mg once daily. 5 mg administered once daily. If a sufficient clinical response is not achieved, the dose may be increased to 1 mg administered once daily.
Change of levodopa dose in adjunct therapy:
When AZILECT is used in combination with levodopa a reduction of the levodopa dosage may be considered based upon individual response. During the controlled trials of AZILECT as adjunct therapy to levodopa, levodopa dosage was reduced in some patients.
In clinical studies, dosage reduction of levodopa was allowed within the first 6 weeks if dopaminergic side effects, including dyskinesia and hallucinations, emerged. 5 mg/day and 1 mg/day AZILECT groups, respectively. 5 mg/day, and 1 mg/day groups, respectively.
In the LARGO study levodopa dosage reduction occurred in 6% of patients in the placebo group and in 9% in the AZILECT 1 mg/day group. In patients who had their levodopa dosage reduced, the dose was reduced on average by about 13% and 11% in the placebo and the AZILECT groups, respectively.
AZILECT (rasagiline) Page 7 of 48 Patients with Hepatic Impairment:
AZILECT plasma concentration will increase in patients with hepatic impairment. 5 mg daily of AZILECT. AZILECT should not be used in patients with moderate to severe hepatic impairment. If patients progress from mild to moderate hepatic impairment, AZILECT should be stopped.
3 Pharmacokinetics, Special Populations and Conditions and 7 WARNINGS AND PRECAUTIONS, Hepatic Impairment.
AZILECT is contraindicated for: concomitant use with opioid analgesics, including meperidine and its derivatives, tramadol, methadone, tapentadol, and propoxyphene. concomitant use with serotonin-specific reuptake inhibitors (SSRIs), serotonin- norepinephrine reuptake inhibitors (SNRIs); tricyclic, tetracyclic or triazolopyridine antidepressants; concomitant use with cyclobenzaprine (a tricyclic muscle relaxant).
concomitant use with St. John’s wort Serious, sometimes fatal reactions have been precipitated with concomitant use of the above drugs and MAO inhibitors including selective MAO-B inhibitors. These reactions have been characterized by coma, severe hypertension or hypotension, severe respiratory depression, AZILECT (rasagiline) Page 5 of 48 convulsions, malignant hyperpyrexia, excitation, peripheral vascular collapse and death.
At least 14 days should elapse between discontinuation of AZILECT and initiation of treatment with meperidine. concomitant use with the antitussive agent dextromethorphan. The combination of MAO inhibitors and dextromethorphan has been reported to cause brief episodes of psychosis or bizarre behavior.
concomitant use with other MAO inhibitors because of the increased risk of non-selective MAO inhibition that may lead to a hypertensive crisis. At least 14 days should elapse between discontinuation of AZILECT and initiation of treatment with MAO inhibitors.
patients who are hypersensitive to this drug or to any ingredient in the formulation, including any non-medicinal ingredient, or component of the container. For a complete listing, see 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING.
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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3 Pharmacokinetics, Special Populations and Conditions and 7 WARNINGS AND PRECAUTIONS, Hepatic Impairment.
Patients with Renal Impairment:
Conclusive data are not available for renally impaired patients. As unconjugated rasagiline is not excreted by the kidney, AZILECT can be given at usual doses in patients with mild renal impairment. Due to the absence of adequate safety data, AZILECT should not be administered to patients with moderate to severe renal impairment.
Patients Taking Ciprofloxacin and Other CYP1A2 Inhibitors:
Rasagiline plasma concentrations are expected to double in patients taking concomitant ciprofloxacin and o ther CYP1A2 inhibitors. 5 mg daily of AZILECT. 4 Drug-Drug Interactions. Health Canada has not authorized an indication for pediatric use .
3 Pediatrics. 4 Administration AZILECT is administered orally and should be taken with water at the same time each day. AZILECT may be taken with or without food, without regard to meals. 5 Missed Dose Patients should be instructed to take AZILECT as prescribed.
If a dose is missed the next dose should be taken at the usual time on the following day. The patient should not double -up the dose of AZILECT.
The adverse events that led to the discontinuation of more than one patient were hallucinations, nausea, dizziness, diarrhea, weight loss, and rash. 2 Clinical Trial Adverse Reactions Clinical trials are conducted under very specific conditions.
The adverse reaction rates observed in the clinical trials; therefore, may not reflect the rates observed in practice and should not be compared to the rates in the clinical trials of another drug. Adverse reaction information from clinical trials may be useful in identifying and approximating rates of adverse drug reactions in real-world use.
Patients Receiving AZILECT as Initial Monotherapy AZILECT (rasagiline) Page 16 of 48 Adverse events leading to discontinuation in controlled clinical studies: In the double-blind, placebo-controlled trial (TEMPO) conducted in patients receiving AZILECT as monotherapy, approximately 5% of the 149 patients treated with AZILECT discontinued treatment due to adverse events compared to 2% of the 151 patients who received placebo.
The only adverse event that led to the discontinuation of more than one patient was hallucinations. 5 times the incidence in the placebo group (n=151), were: flu syndrome, arthralgia, depression, dyspepsia and fall. Table 2 lists treatment emergent adverse events that occurred in ≥ 2% of patients receiving AZILECT as monotherapy participating in the double-blind, placebo-controlled trial and were numerically more frequent than in the placebo group.
Table 2. Treatment Emergent* Adverse Events in AZILECT 1 mg-Treated Monotherapy Patients in TEMPO Placebo-Controlled Studies Without Levodopa Treatment AZILECT 1 mg (N=149) Placebo (N=151) % of Patients % of Patients Headache 14 12 Arthralgia 7 4 Dyspepsia 7 4 Depression 5 2 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% in AZILECT 1 mg group and numerically more frequent than in placebo group AZILECT (rasagiline) Page 17 of 48 Other events of potential clinical importance reported by 1% or more of Parkinson’s disease patients receiving AZILECT as monotherapy, and at least as frequent as in the placebo group, in descending order of frequency include: dizziness, diarrhea, chest pain, albuminuria, allergic reaction, alopecia, angina pectoris, anorexia, asthma, hallucinations, impotence, leukopenia, libido decreased, liver function tests abnormal, skin carcinoma, syncope, vesiculobullous rash, vomiting.
There were no significant differences in the safety profile based on age or gender. Patients Receiving AZILECT as Adjunct to Dopamine Agonists Therapy Adverse events leading to discontinuation in a controlled clinical study: In a double-blind, randomized, placebo-controlled trial (ANDANTE) conducted in patients receiving AZILECT as add-on therapy to dopamine agonists, approximately 8% of the 162 patients treated with AZILECT discontinued AZILECT treatment due to adverse reactions compared to 4% of the 164 patients who received placebo.
The adverse reactions that led to the discontinuation of more than one patient were nausea and dizziness. Adverse Events Incidence in a Controlled Clinical Study The most commonly observed adverse reactions were those in which the treatment difference for the incidence in AZILECT-treated patients was > 3% greater than the incidence in the placebo-treated patients and included peripheral edema, fall, arthralgia, cough, and insomnia.
Table 3 lists treatment-emergent adverse events that occurred in ≥ 2% of patients receiving AZILECT as add-on therapy to dopamine agonists and were numerically more frequent than in the placebo group. Table 3. […]
Patients with Renal Impairment:
Conclusive data are not available for renally impaired patients. As unconjugated rasagiline is not excreted by the kidney, AZILECT can be given at usual doses in patients with mild renal impairment. Due to the absence of adequate safety data, AZILECT should not be administered to patients with moderate to severe renal impairment.
Patients Taking Ciprofloxacin and Other CYP1A2 Inhibitors:
Rasagiline plasma concentrations are expected to double in patients taking concomitant ciprofloxacin and o ther CYP1A2 inhibitors. 5 mg daily of AZILECT. 4 Drug-Drug Interactions. Health Canada has not authorized an indication for pediatric use .
3 Pediatrics. 4 Administration AZILECT is administered orally and should be taken with water at the same time each day. AZILECT may be taken with or without food, without regard to meals. 5 Missed Dose Patients should be instructed to take AZILECT as prescribed.
If a dose is missed the next dose should be taken at the usual time on the following day. The patient should not double -up the dose of AZILECT. 5 OVERDOSAGE Symptoms Symptoms reported following overdose of AZILECT in doses ranging from 3 mg to 100 mg include dysphoria, hypomania, hypertensive crisis, and serotonin syndrome.
The following description of presenting symptoms and clinical course is based upon overdose descriptions of non-selective MAO inhibitors. Characteristically, signs and symptoms of non-selective MAOI overdose may not appear immediately.
Delays of up to 12 hours between ingestion of drug and the appearance of signs may occur. Importantly, the peak intensity of the syndrome may not be reached f or upwards of a day following the overdose. Death has been reported following overdosage.
Therefore, AZILECT (rasagiline) Page 8 of 48 immediate hospitalization, with continuous patient observation and monitoring for a period of at least two days following the ingestion of such drugs in overdose, is strongly recommended.
The clinical picture of MAOI overdose varies considerably; its severity may be a function of the amount of drug consumed. The central nervous and cardiovascular systems are prominently involved. Signs and symptoms of overdosage may include, alone or in combination, any of the following: drowsiness, dizziness, faintness, irritability, hyperactivity, agitation, severe headache, hallucinations, trismus, opisthotonos, convulsions, and coma; rapid and irregular pulse, hypertension, hypotension and vascular collapse; precordial pain, respiratory depression and failure, hyperpyrexia, diaphoresis, and cool, clammy skin.
In the post-marketing period, serotonin syndrome has been reported in a patient erroneously treated with a higher than recommended dose of AZILECT (4 mg daily) and tramadol. Treatment There is no specific antidote for rasagiline overdose.
The following suggestions are offered based upon the assumption that rasagiline overdose may be modeled after non-selective MAO inhibitor poisoning. Treatment of overdose with non-selective MAO inhibitors is symptomatic and supportive.
Respiration should be supported by appropriate measures, including management of the airway, use of supplemental oxygen, and mechanical ventilator assistance, as required. Body temperature should be monitored closely. Intensive management of hyperpyrexia may be required.
Maintenance of fluid and electrolyte balance is essential. For this reason, in cases of overdose with AZILECT, dietary tyramine restriction should be observed […]