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APO-RASAGILINE 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: APO-RASAGILINE (rasagiline mesylate 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 rasagiline mesylate tablets was demonstrated in patients with early…
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 APO-RASAGILINE dose for the treatment of Parkinson’s disease patients is 1 mg administered once daily.
Adjunctive Therapy to Dopamine Agonists The recommended APO-RASAGILINE dose as adjunctive therapy to dopamine agonists is 1 mg administered once daily. 5 to 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 APO-RASAGILINE is used in combination with levodopa a reduction of the levodopa dosage may be considered based upon individual response. During the controlled trials of rasagiline mesylate tablets 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 rasagiline mesylate tablets 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 rasagiline mesylate tablets 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 APO-RASAGILINE (Rasagiline Mesylate Tablets) Page 8 of 52 rasagiline mesylate tablets groups, respectively.
Patients with Hepatic Impairment:
APO-RASAGILINE plasma concentration will increase in patients with hepatic impairment. 5 mg daily of APO-RASAGILINE. APO-RASAGILINE should not be used in patients with moderate to severe hepatic impairment. If patients progress from mild to moderate hepatic impairment, APO-RASAGILINE should be stopped.
Renal Conclusive data are not available for renally impaired patients. As unconjugated rasagiline is not excreted by the kidney, APO-RASAGILINE can be given at usual doses in patients with mild renal impairment. Due to the absence of adequate safety data, APO-RASAGILINE 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, APO-RASAGILINE should be used during APO-RASAGILINE (Rasagiline Mesylate Tablets) Page 16 of 52 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 APO-RASAGILINE 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 rasagiline mesylate tablets 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 rasagiline mesylate tablets 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.
09/2023 TABLE OF CONTENTS Sections or subsections that are not applicable at the time of authorization are not listed. RECENT MAJOR LABEL CHANGES........................................................................................
2 TABLE OF CONTENTS .......................................................................................................... 2 PART I: HEALTH PROFESSIONAL INFORMATION .................................................................
5 1 INDICATIONS ............................................................................................................... 1 Pediatrics.................................................................................................................
2 Geriatrics ................................................................................................................. 5 2 CONTRAINDICATIONS .................................................................................................
5 3 SERIOUS WARNINGS AND PRECAUTIONS BOX ............................................................ 6 4 DOSAGE AND ADMINISTRATION ................................................................................. 1 Dosing Considerations .............................................................................................
2 Recommended Dose and Dosage Adjustment ........................................................ 4 Administration ........................................................................................................ 5 Missed Dose ............................................................................................................
8 5 OVERDOSAGE.............................................................................................................. 8 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING ................................. 9 7 WARNINGS AND PRECAUTIONS ................................................................................
09/2023 7 WARNINGS AND PRECAUTIONS 09/2023 TABLE OF CONTENTS Sections or subsections that are not applicable at the time of authorization are not listed. RECENT MAJOR LABEL CHANGES........................................................................................
2 TABLE OF CONTENTS .......................................................................................................... 2 PART I: HEALTH PROFESSIONAL INFORMATION .................................................................
5 1 INDICATIONS ............................................................................................................... 1 Pediatrics.................................................................................................................
2 Geriatrics ................................................................................................................. 5 2 CONTRAINDICATIONS .................................................................................................
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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/Biliary/Pancreatic.
Patients with Renal Impairment:
Conclusive data are not available for renally impaired patients. As unconjugated rasagiline is not excreted by the kidney, APO-RASAGILINE can be given at usual doses in patients with mild renal impairment. Due to the absence of adequate safety data, APO-RASAGILINE 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 other CYP1A2 inhibitors. 5 mg daily of APO-RASAGILINE. 4 Drug-Drug Interactions. Health Canada has not authorized an indication for pediatric use.
3 Pediatrics. 4 Administration APO-RASAGILINE is administered orally and should be taken with water at the same time each day. APO-RASAGILINE may be taken with or without food, without regard to meals. 5 Missed Dose Patients should be instructed to take APO-RASAGILINE 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 APO-RASAGILINE.
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 Rasagiline Mesylate Tablets as Initial Monotherapy Adverse events leading to discontinuation in controlled clinical studies: In the double-blind, placebo-controlled trial (TEMPO) conducted in patients receiving rasagiline APO-RASAGILINE (Rasagiline Mesylate Tablets) Page 17 of 52 mesylate tablets as monotherapy, approximately 5% of the 149 patients treated with rasagiline mesylate tablets 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 rasagiline mesylate tablets 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 Rasagiline Mesylate Tablets 1 mg-Treated Monotherapy Patients in TEMPO Placebo-Controlled Studies Without Levodopa Treatment Rasagiline mesylate tablets 1mg (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 rasagiline mesylate tablets 1 mg group and numerically more frequent than in placebo group APO-RASAGILINE (Rasagiline Mesylate Tablets) Page 18 of 52 Other events of potential clinical importance reported by 1% or more of Parkinson’s disease patients receiving rasagiline mesylate tablets 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 Rasagiline Mesylate Tablets 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 rasagiline mesylate tablets as add-on therapy to dopamine agonists, approximately 8% of the 162 patients treated with rasagiline mesylate tablets discontinued rasagiline mesylate tablets 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 […]
1 Special Populations ............................................................................................... 1 Pregnant Women ......................................................................................... 2 Breast-feeding..............................................................................................
3 Pediatrics ..................................................................................................... 4 Geriatrics...................................................................................................... 16 8 ADVERSE REACTIONS ................................................................................................
1 Adverse Reaction Overview .................................................................................. 2 Clinical Trial Adverse Reactions ............................................................................. 5 Post-Market Adverse Reactions ............................................................................
23 9 DRUG INTERACTIONS ................................................................................................ 1 Serious Drug Interactions ......................................................................................
3 Drug-Behavioural Interactions .............................................................................. 4 Drug-Drug Interactions.......................................................................................... 5 Drug-Food Interactions .........................................................................................
6 Drug-Herb Interactions ......................................................................................... 7 Drug-Laboratory Test Interactions ........................................................................ 29 10 CLINICAL PHARMACOLOGY .......................................................................................
1 Mechanism of Action ............................................................................................ 2 Pharmacodynamics ............................................................................................... 3 Pharmacokinetics ..................................................................................................
30 11 STORAGE, STABILITY AND DISPOSAL ......................................................................... 31 12 SPECIAL HANDLING INSTRUCTIONS ........................................................................... 32 PART II: SCIENTIFIC INFORMATION ..................................................................................
33 13 PHARMACEUTICAL INFORMATION ............................................................................ 33 14 CLINICAL TRIALS ........................................................................................................
1 Clinical Trials by Indication .................................................................................... 2 Comparative Bioavailability Studies ...................................................................... 39 APO-RASAGILINE (Rasagiline Mesylate Tablets) Page 4 of 52 15 MICROBIOLOGY ........................................................................................................
40 16 NON-CLINICAL TOXICOLOGY ..................................................................................... 40 17 SUPPORTING PRODUCT MONOGRAPHS .................................................................... 44 PATIENT MEDICATION INFORMATION .............................................................................
45 APO-RASAGILINE (Rasagiline Mesylate Tablets) Page 5 of 52 PART I: HEALTH PROFESSIONAL INFORMATION 1 INDICATIONS APO-RASAGILINE (rasagiline mesylate tablets) is indicated for: • the treatment of the signs and symptoms of idiopathic […]