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AG-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: AG-Rasagiline (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 rasagiline mesylate was demonstrated in patients with early Parkinson’s disease who…
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 AG-Rasagiline dose for the treatment of Parkinson’s disease patients is 1 mg administered once daily.
Adjunctive Therapy to Dopamine Agonists The recommended AG-Rasagiline 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 AG-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 AG-Rasagiline 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 AG-Rasagiline groups, respectively. In those patients who had levodopa dosage reduced, the also been reported in patients taking other dopaminergic agents, therefore, symptoms may not be alleviated by substituting these products.
Currently, the precise cause of this event is unknown. It is known that patients with Parkinson's disease experience alterations in sleep architecture, which results in excessive daytime sleepiness or spontaneous dozing, and that dopaminergic agents can also induce sleepiness.
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 AG-Rasagiline 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 AG-Rasagiline groups, respectively.
Renal Conclusive data are not available for renally impaired patients. As unconjugated rasagiline is not excreted by the kidney, AG-Rasagiline can be given at usual doses in patients with mild renal impairment. Due to the absence of adequate safety data, AG-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 Product Monograph of AG-Rasagiline Page 15 of 49 well-controlled studies of rasagiline in pregnant women.
Because animal reproduction studies are not always predictive of human response, AG-Rasagiline 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 AG-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 AG-Rasagiline 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 AG-Rasagiline 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 AG-Rasagiline dose for the treatment of Parkinson’s disease patients is 1 mg administered once daily. Adjunctive Therapy to Dopamine Agonists The recommended AG-Rasagiline 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 AG-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 AG-Rasagiline 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 AG-Rasagiline groups, respectively. In those patients who had levodopa dosage reduced, the also been reported in patients taking other dopaminergic agents, therefore, symptoms may not be alleviated by substituting these products.
Currently, the precise cause of this event is unknown. It is known that patients with Parkinson's disease experience alterations in sleep architecture, which results in excessive daytime sleepiness or spontaneous dozing, and that dopaminergic agents can also induce sleepiness.
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 AG-Rasagiline 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 AG-Rasagiline groups, respectively.
4 Drug-Drug Interactions. At least 14 days should elapse between discontinuation of AG-Rasagiline and initiation of treatment with a tricyclic, tetracyclic, triazolopyridine, SSRI, or SNRI antidepressant. Similarly, at least 14 days should elapse after discontinuing treatment with a tricyclic, tetracyclic, triazolopyridine, SSRI, or SNRI antidepressant before starting AG-Rasagiline.
Because of the long half-lives of fluoxetine and its active metabolite, at least five weeks (perhaps longer, especially if fluoxetine has been prescribed chronically and/or at higher doses) should elapse between discontinuation of fluoxetine and initiation of AG-Rasagiline.
5 mg or 1 mg AG-Rasagiline as an adjunct to levodopa and 10% of patients who received placebo as an adjunct to levodopa). Decreasing the dose of levodopa may ameliorate this side effect. 7% of patients treated with placebo. 3% of the 1 mg rasagiline mesylate treated patients and in none of the placebo treated patients.
8% of patients treated with placebo. 6% of patients treated with 1 mg/day rasagiline mesylate and in none of the placebo-treated patients. 5 mg/day, 4% of patients treated with 1 mg/day rasagiline mesylate and 3% of patients treated with placebo.
5 mg/day or 1 mg/day and none of the placebo treated patients. Postmarketing reports indicate that patients may experience new or worsening mental status and behavioral changes, which may be severe, including psychotic-like behavior during treatment with rasagiline mesylate or after starting or increasing the dose of rasagiline mesylate.
Other drugs prescribed to improve the symptoms of Parkinson’s disease can have similar effects on thinking and behavior. This abnormal thinking and behavior can consist of one or more of a variety of manifestations including paranoid ideation, delusions, hallucinations, confusion, psychotic-like behavior, disorientation, aggressive behavior, agitation, and delirium.
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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Patients with Hepatic Impairment:
AG-Rasagiline plasma concentration will increase in patients with hepatic impairment. 5 mg daily of AG-Rasagiline. AG-Rasagiline should not be used in patients with moderate to severe hepatic impairment. If patients progress from mild to moderate hepatic impairment, AG- Rasagiline should be stopped.
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, AG-Rasagiline can be given at usual doses in patients with mild renal impairment. Due to the absence of adequate safety data, AG- 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 AG-Rasagiline. 4 Drug-Drug Interactions. Health Canada has not authorized an indication for pediatric use.
3 Pediatrics. 4 Administration AG-Rasagiline is administered orally and should be taken with water at the same time each day. AG-Rasagiline may be taken with or without food, without regard to meals. 5 Missed Dose Patients should be instructed to take AG-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 AG-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: Product Monograph of AG-Rasagiline Page 16 of 49 In the double-blind, placebo-controlled trial (TEMPO) conducted in patients receiving rasagiline mesylate tablets as monotherapy, approximately 5% of the 149 patients treated with rasagiline mesylate 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 Rasagiline mesylate tablets 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 rasagiline mesylate tablets 1 mg group and numerically more frequent than in placebo group Other events of potential clinical importance reported by 1% or more of Parkinson’s disease Product Monograph of AG-Rasagiline Page 17 of 49 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 discontinued rasagiline mesylate 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 rasagiline mesylate tablet-treated patients was > 3% greater than the […]
Patients with Hepatic Impairment:
AG-Rasagiline plasma concentration will increase in patients with hepatic impairment. 5 mg daily of AG-Rasagiline. AG-Rasagiline should not be used in patients with moderate to severe hepatic impairment. If patients progress from mild to moderate hepatic impairment, AG- Rasagiline should be stopped.
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, AG-Rasagiline can be given at usual doses in patients with mild renal impairment. Due to the absence of adequate safety data, AG- 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 AG-Rasagiline. 4 Drug-Drug Interactions. Health Canada has not authorized an indication for pediatric use.
3 Pediatrics. 4 Administration AG-Rasagiline is administered orally and should be taken with water at the same time each day. AG-Rasagiline may be taken with or without food, without regard to meals. 5 Missed Dose Patients should be instructed to take AG-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 AG-Rasagiline. 5 OVERDOSAGE Symptoms Symptoms reported following overdose of AG-Rasagiline in doses ranging from 3 mg to 100 mg include dysphoria, hypomania, hypertensive crisis, and serotonin syndrome.
Product Monograph of AG-Rasagiline Page 8 of 49 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 for upwards of a day following the overdose. Death has been reported following overdosage.
Therefore, 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 AG-Rasagiline (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 […]
Impulse Control/Compulsive Behaviours Patients and caregivers should be advised to adhere to dosage instructions given by the healthcare professional. Patients should be regularly monitored for the development of impulse control disorders.
Patients and caregivers should be made aware that behavioral symptoms of impulse control disorders including pathological gambling, increased libido, hypersexuality, compulsive spending or buying, binge eating and compulsive eating have been reported in patients treated with dopamine agonists and/or other dopaminergic treatments for Parkinson’s disease, including rasagiline mesylate.
Safety data from various sources including literature, clinical trials, and post-market analysis have described an addictive pattern of dopamine replacement therapy, in which patients use doses in excess of those required to control their motor symptoms.
Because patients may not recognize these behaviors as abnormal, it is important for healthcare professionals to specifically ask patients and caregivers to identify new behavior patterns. Review of treatment is recommended if such symptoms develop.
These symptoms were generally reversible upon dose reduction or treatment discontinuation See 8 ADVERSE REACTIONS. Renal Conclusive data are not available for renally impaired patients. As unconjugated rasagiline is not excreted by the kidney, AG-Rasagiline can be given at usual doses in patients with mild renal impairment.
Due to the absence of adequate safety data, AG-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 Product Monograph of AG-Rasagiline Page 15 of 49 well-controlled studies of rasagiline in pregnant women. Because animal reproduction studies are not always predictive of human response, AG-Rasagiline 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 AG-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 AG-Rasagiline 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 […]