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APO-ROPINIROLE is a brand name for Ropinirole, supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: AND CLINICAL USE ................................................................................................. 3 CONTRAINDICATIONS ...................................................................................................................... 3 WARNINGS AND PRECAUTIONS…
Verbatim from this product's HC label. Tap a section to expand.
Dosing Considerations Renal Impairment:
In patients with mild to moderate renal impairment, APO-ROPINIROLE may be titrated in the recommended manner according to clinical response. 25 mg three times a day. Further dose escalations should be based on tolerability and efficacy.
The recommended maximum dose is 18 mg/day in patients receiving regular dialysis. Supplemental doses after dialysis are not required. Patients with severe renal impairment (creatinine clearance less than 30 mL/min without regular dialysis) have not been studied and administration of APO-ROPINIROLE to such patients is not recommended.
Hepatic Impairment:
Patients with hepatic impairment have not been studied and administration of APO-ROPINIROLE to such patients is not recommended.
Oestrogen Replacement Therapy:
In patients already receiving oestrogen replacement therapy, APO-ROPINIROLE may be titrated in the recommended manner according to clinical response. However, if oestrogen replacement therapy is stopped or started during treatment with APO- ROPINIROLE, adjustment of the APO-ROPINIROLE dosage may be required.
Recommended Dose and Dosage Adjustment APO-ROPINIROLE should be taken three times daily and may be taken with or without food (see ACTION AND CLINICAL PHARMACOLOGY, Pharmacokinetics). 25 mg three times daily. 25 mg per dose as described in the table below.
0 mg per dose on a weekly basis until an optimal therapeutic response is established. Smaller dose increments are recommended for patients who may be at risk for orthostatic symptoms. 0 In clinical trials, initial benefits were observed with 3 mg/day and higher doses.
Doses greater than 24 mg/day have not been included in clinical trials. 0 mg), regardless of levodopa supplementation. Page 24 of 51 When APO-ROPINIROLE is administered as adjunct therapy to levodopa, the dose of levodopa may be decreased gradually as tolerated once a therapeutic effect with ropinirole has been observed (see CLINICAL TRIALS).
A decrease in levodopa dosage may be necessary in order to avoid excessive dopamine stimulation. APO-ROPINIROLE should be discontinued gradually over a 7-day period. The frequency of administration should be reduced from three times daily to twice daily for 4 days.
The following Warnings and Precautions are listed in alphabetical order.
Carcinogenesis and Mutagenesis See PART II:
TOXICOLOGY, Carcinogenicity and Mutagenicity for discussion on animal data. Cardiovascular Patients with pre-existing cardiovascular conditions Since ropinirole has not been studied in patients with a history or evidence of significant cardiovascular disease including myocardial infarction, unstable angina, cardiac decompensation, cardiac arrhythmias, vaso-occlusive disease (including cerebral) or cardiomyopathy, it should be used with caution in such patients.
There is limited experience with ropinirole in patients treated with antihypertensive and antiarrhythmic agents. Consequently, in such patients, the dose of ropinirole should be titrated with caution. Serious Warnings and Precautions Sudden Onset of Sleep Patients receiving treatment with ropinirole and other dopaminergic agents have reported suddenly falling asleep while engaged in activities of daily living, including operating a motor vehicle, which has sometimes resulted in accidents.
Although some of the patients reported somnolence while on ropinirole, others perceived that they had no warning signs, such as excessive drowsiness, and believed that they were alert immediately prior to the event. Physicians should alert patients of the reported cases of sudden onset of sleep, bearing in mind that these events are NOT limited to initiation of therapy.
Patients should also be advised that sudden onset of sleep has occurred without warning signs. If drowsiness or sudden onset of sleep should occur, patients should immediately contact their physician. , operating machines). Episodes of falling asleep while engaged in activities of daily living have also been reported in patients taking other dopaminergic agents, therefore, symptoms may not be alleviated by substituting these products.
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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For the remaining 3 days, the frequency should be reduced to once daily prior to complete withdrawal of APO-ROPINIROLE. Missed Dose Patients should be instructed that, if they miss a dose of APO-ROPINIROLE, they should wait and take the next dose as scheduled.
There is no need to make up for the missed dose. Patients should not take two doses at once. If treatment is interrupted for one day or more, re-initiation by dose titration should be considered (see DOSAGE and ADMINISTRATION). OVERDOSAGE For management of a suspected drug overdose, contact your regional Poison Control Centre.
Symptoms and Signs There were no reports of intentional overdose of ropinirole in the premarketing clinical trials. A total of 27 patients accidentally took more than their prescribed dose of ropinirole, with 10 patients ingesting more than 24 mg/day.
1 mg/day). Of patients who received a dose greater than 24 mg/day, one experienced mild oro-facial dyskinesia, another patient experienced intermittent nausea. Other symptoms reported with accidental overdoses were: agitation, increased dyskinesia, grogginess, sedation, orthostatic hypotension, chest pain, confusion, vomiting and nausea.
Recommended Management It is anticipated that the symptoms of ropinirole overdose will be related to its dopaminergic activity. These symptoms may be alleviated by appropriate treatment with dopamine antagonists such as neuroleptics or metoclopramide.
The efficacy of such drugs in reversing the effects of overdosage however, has not been assessed. General supportive measures are recommended. Vital signs should be maintained, if necessary. ACTION AND CLINICAL PHARMACOLOGY Mechanism of Action Ropinirole is a non-ergoline dopamine agonist, which activates post-synaptic dopamine receptors.
Page 25 of 51 In vitro studies have shown that ropinirole binds with high affinity to cloned human D2, D3, and D4 receptors. The antiparkinson activity of ropinirole is believed to be due to its stimulatory effects on central post-synaptic dopamine D2 receptors within the caudate-putamen.
Ropinirole is a potent agonist both in vitro and in vivo and restores motor function in animal models of Parkinson's disease. Ropinirole has been shown to reverse the motor deficits induced by the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in primates.
Neither ropinirole nor its metabolites bind with high affinity to dopamine D1 receptors. Ropinirole also has very low affinity for 5-HT1, 5-HT2, benzodiazepine, GABAA, muscarinic, alpha- or beta-adrenoreceptors. Ropinirole binds to opiate receptors with low affinity, however, studies show that this weak opiate activity has no consequences at pharmacological doses in vivo.
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Presently, the precise cause of this event is unknown. It is known that many Parkinson's disease patients experience alterations in sleep architecture, which results in excessive daytime sleepiness or spontaneous dozing, and that dopaminergic agents can also induce sleepiness.
There is insufficient information to determine whether this event is associated with ropinirole, all dopaminergic agents or Parkinson's disease itself. Page 5 of 51 Orthostatic hypotension Dopamine agonists appear to impair the systemic regulation of blood pressure with resulting orthostatic symptoms of dizziness or lightheadedness, with or without documented hypotension.
These symptoms appear to occur especially during dose initiation and escalation. Therefore, patients treated with ropinirole and other dopamine agonists should be carefully monitored for signs and symptoms of orthostatic hypotension, especially during dose initiation and escalation (see DOSAGE AND ADMINISTRATION) and should be informed of this risk (see PART III: CONSUMER INFORMATION).
Connective tissue Fibrotic Complications Cases of retroperitoneal fibrosis, pulmonary infiltrates, pleural effusion, pleural thickening, pericarditis, and cardiac valvulopathy have been reported in some patients treated with ergot- derived dopaminergic agents.
While these complications may resolve when the drug is discontinued, complete resolution does not always occur. Although these adverse events are believed to be related to the ergoline structure of these compounds, whether other, nonergot-derived dopamine agonists can cause them is unknown.
A small number of reports have been received of possible fibrotic complications, including pleural effusion, pleural fibrosis, interstitial lung diseases, and cardiac valvulopathy, in the development program and postmarketing experience for ropinirole.
While the evidence is not sufficient to establish a causal relationship between ropinirole and these fibrotic complications, a contribution of ropinirole cannot be completely ruled out in rare cases. Neurologic Neuroleptic Malignant Syndrome A symptom complex resembling the neuroleptic malignant syndrome (characterized by elevated temperature, muscular rigidity, altered consciousness, and autonomic instability), with no other obvious aetiology, has been reported in association with rapid dose reduction, withdrawal of, or changes in antiparkinsonian therapy.
A single spontaneous report of a symptom complex resembling the neuroleptic malignant syndrome has been observed in a 66 year old diabetic male patient with Parkinson's disease, who developed fever, muscle stiffness, and drowsiness 8 days after beginning ropinirole treatment.
The patient also experienced acute bronchitis, which did not respond to antibiotic treatment. Ropinirole was discontinued three days before the patient died. The reporting physician considered these events to be possibly related to ropinirole treatment.
(see DOSAGE AND ADMINISTRATION). A single spontaneous report of severe muscle pain has been reported in a 66 year old male patient around his thigh. The reporting physician considered the event to be probably related to ropinirole treatment.
Page 6 of 51 Dyskinesia with Adjunctive Levodopa Ropinirole may potentiate the dopaminergic side effects of levodopa and may cause or exacerbate pre-existing dyskinesia. Decreasing the dose of levodopa may ameliorate this side effect.
5, 15 and 50 mg/kg/day respectively. The incidence was statistically significant at 50 mg/kg/day. 1 fold (Cmax) greater […]