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RISPERIDEX 2MG

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RISPERIDEX 1,2,3,4 MG

Central Nervous System-Antipsychotics

Central Nervous System

ACTIVE INGREDIENTS

= Additional active ingredients

Risperidone.

RISPERIDONE

PRESENTATION AND DOSSAGE

TABS: 20 X 1 mg

TABS: 20 X 2 mg

TABS: 20 X 3 mg

TABS:20 X 4 mg

RELATED INFORMATION



CONTAINS LACTOSE

INDICATIONS

For the management schizophrenia, and the manifestations of psychotic disorders. The antipsychotic efficacy of Risperidone was established in short-term (6 to 8-weeks) controlled trials of schizophrenic inpatients. Also effective in maintaining the clinical improvement during continuation therapy in patients who have shown an initial treatment response. For the short-term treatment (up to 6 weeks) of persistent aggression in patients with moderate to severe Alzheimer’s dementia unresponsive to non-pharmacological approaches and when there is a risk of harm to self or others. Conduct and other disruptive disorders: Treatment of behavioral disorders expressed by impulse control disorders or self-alienated-aggressive or treatment-requiring behavioral disorders with reduced or substandard intelligence. Treatment should not be given to children under the age of 5 years.

For the treatment of mania in bipolar disorder. These episodes are characterized by symptoms such as elevated, expansive or irritable mood, inflated self-esteem, decreased need for sleep, pressured speech, racing thoughts, distractibility, or poor judgment, including disruptive or aggressive behaviors.


DRUG INTERACTION

As with other antipsychotics, caution is advised when prescribing this drug with medicinal products known to prolong the QT interval, such as antiarrhythmics (e.g., quinidine, dysopiramide, procainamide, propafenone, amiodarone, sotalol), tricyclic antidepressant (i.e., amitriptyline), tetracyclic antidepressants (i.e., maprotiline), some antihistaminics, other antipsychotics, some antimalarials (i.e., quinine and mefloquine), and with medicines causing electrolyte imbalance (hypokalaemia, hypomagnesiaemia), bradycardia, or those which inhibit the hepatic metabolism of risperidone. This list is indicative and not exhaustive.

Potential for Risperidone to affect other medicinal products: This drug should be used with caution in combination with other centrally-acting substances notably including alcohol, opiates, antihistamines and benzodiazepines due to the increased risk of sedation. It may antagonize the effect of levodopa and other dopamine agonists. If combination is necessary, (e.g. in end-stage Parkinson’s disease), the lowest effective dose of each treatment should be prescribed. Clinically significant hypotension has been observed post marketing with concomitant use and antihypertensive treatment. No clinically relevant effect on the pharmacokinetics of lithium, valproate, digoxin or topiramate.

Potential for other medicinal products to affect risperidone: Carbamazepine decreases the plasma concentrations of the active antipsychotic fraction. Similar effects may be observed with e.g. rifampicin, phenytoin and phenobarbital which also include CYP 3A4 hepatic enzyme as well as P-glycoprotein. When carbamazepine or other CYP 3A4 hepatic enzyme/P-glycoprotein (P-gp) inducers are initiated or discontinued, the physician should reevaluate the dosing of this drug. Fluoxetine and paroxetine, CYP 2D6 inhibitors, increase the plasma concentration of this drug, but less so of the active antipsychotic fraction. Other CYP2D6 inhibitors, such as quinidine may affect the plasma concentrations of this drug in a similar way. When concomitant fluoxetine or paroxetine is initiated or discontinued, the physician should re-evaluate the dosing of this drug. Verapamil, an inhibitor of CYP 3A4 and P-gp, increases the plasma concentration it. Galantamine and donepezil: no clinically relevant effect on the pharmacokinetics of it and on the active antipsychotic fraction. Phenothiazines, tricyclic antidepressants, and some beta-blockers may increase the plasma concentrations of it but not those of the active antipsychotic fraction. Amytriptyline does not affect the pharmacokinetics of this drug or the active antipsychotic fraction. Cimetidine and ranitidine increased the bioavailability of it, but only marginally that of the active antipsychotic fraction. Erythromycin, a CYP 3A4 inhibitor, does not change the pharmacokinetics and the active antipsychotic fraction. The combined use of psychostimulants (e.g., methylphenidate) with risperidone in children and adolescents did not alter the pharmacokinetics and efficacy. Increased mortality in elderly patients with dementia concomitantly receiving furosemide. Concomitant use of oral risperidone with paliperidone is not recommended as paliperidone is the active metabolite and the combination of the two may lead to additive active antipsychotic fraction exposure.

Pediatric population: Interaction studies have only been performed in adults


CONTRA-INDICATIONS

Hypersensitivity to Risperidone or to any of the additional ingredients.


SPECIAL PRECAUTIONS

Increased mortality in elderly people with dementia: In a meta-analysis of 17 controlled trials of atypical antipsychotics, including this drug, elderly patients with dementia treated with atypical antipsychotics have an increased mortality compared to placebo. In placebo-controlled trials with oral risperidone in this population, the incidence of mortality was 4.0% for this drug treated patients compared to 3.1% for placebo-treated patients. The odds ratio (95% exact confidence interval) was 1.21 (0.7, 2.1). The mean age (range) of patients who died was 86 years (range 67-100). Data from two large observational studies showed that elderly people with dementia who are treated with conventional antipsychotics are also at a small increased risk of death compared with those who are not treated. There are insufficient data to give a firm estimate of the precise magnitude of the risk and the cause of the increased risk is not known. The extent to which the findings of increased mortality in observational studies may be attributed to the antipsychotic drug as opposed to some characteristic(s) of the patients is not clear.

Concomitant use with furosemide: In this drug placebo-controlled trials in elderly patients with dementia, a higher incidence of mortality was observed in patients treated with furosemide plus risperidone (7.3%; mean age 89 years, range 75-97) when compared to patients treated with this drug alone (3.1%; mean age 84 years, range 70-96) or furosemide alone (4.1%; mean age 80 years, range 67-90). The increase in mortality in patients treated with furosemide plus this drug was observed in two of the four clinical trials. No pathophysiological mechanism has been identified to explain this finding, and no consistent pattern for cause of death observed. Nevertheless, caution should be exercised and the risks and benefits of this combination should be considered prior to the decision to use. There was no increased incidence of mortality among patients taking other diuretics as concomitant medication with it. Irrespective of treatment, dehydration was an overall risk factor for mortality and should therefore be carefully avoided in elderly patients with dementia.

Cerebrovascular Adverse Events (CVAE): An approximately 3-fold increased risk of cerebrovascular adverse events have been seen in randomized placebo controlled clinical trials in the dementia population with some atypical antipsychotics. The pooled data from six placebo-controlled studies with it in mainly elderly patients (>65 years of age) with dementia showed that CVAEs (serious and non-serious, combined) occurred in 3.3% (33/1009) of patients treated with this drug and 1.2% (8/712) of patients treated with placebo. The odds ratio (95% exact confidence interval) was 2.96 (1.34, 7.50). The mechanism for this increased risk is not known. An increased risk cannot be excluded for other antipsychotics or other patient populations.

This drug should be used with caution in patients with risk factors for stroke. The risk of CVAEs was significantly higher in patients with mixed or vascular type of dementia when compared to Alzheimer’s dementia. Therefore, patients with other types of dementias than Alzheimer’s should not be treated with it. Physicians are advised to assess the risks and benefits of the use of this drug in elderly patients with dementia, taking into account risk predictors for stroke in the individual patient. Patients/caregivers should be cautioned to immediately report signs and symptoms of potential CVAEs such as sudden weakness or numbness in the face, arms or legs, and speech or vision problems. All treatment options should be considered without delay, including discontinuation of it. This drug should only be used short term for persistent aggression in patients with moderate to severe Alzheimer’s dementia to supplement non-pharmacological approaches which have had limited or no efficacy and when there is potential risk of harm to self or others. Patients should be reassessed regularly, and the need for continuing treatment reassessed.

Orthostatic Hypotension: Due to the alpha-blocking activity of this drug, (orthostatic) hypotension can occur, especially during the initial dose-titration period. Clinically significant hypotension has been observed post marketing with concomitant use of it and antihypertensive treatment. This drug should be used with caution in patients with known cardiovascular disease (e.g. heart failure, myocardial infarction, conduction abnormalities, dehydration, hypovolemia, or cerebrovascular disease), and the dosage should be gradually titrated as recommended. A dose reduction should be considered if hypotension occurs.

Leukopenia, Neutropenia, and Agranulocytosis: Events of leucopenia, neutropenia and agranulocytosis have been reported with antipsychotic agents, including this drug. Agranulocytosis has been reported very rarely (< 1/10,000 patients) during post-marketing surveillance. Patients with a history of a clinically significant low white blood cell count (WBC) or a drug-induced leukopenia/neutropenia should be monitored during the first few months of therapy and discontinuation should be considered at the first sign of a clinically significant decline in WBC in the absence of other causative factors. Patients with clinically significant neutropenia should be carefully monitored for fever or other symptoms or signs of infection and treated promptly if such symptoms or signs occur. Patients with severe neutropenia (absolute neutrophil count < 1 X 109/L) should discontinue it and have their WBC followed until recovery.

Venous thromboembolism: Cases of venous thromboembolism (VTE) have been reported with antipsychotic drugs. Since patients treated with antipsychotics often present with acquired risk factors for VTE, all possible risk factors for VTE should be identified before and during treatment with it and preventive measures undertaken.

Tardive Dyskinesia/Extrapyramidal Symptoms (TD/EPS): Drugs with dopamine receptor antagonistic properties have been associated with the induction of tardive dyskinesia characterized by rhythmical involuntary movements, predominantly of the tongue and/or face. The onset of extrapyramidal symptoms is a risk factor for tardive dyskinesia. If signs and symptoms of tardive dyskinesia appear, the discontinuation of all antipsychotic drugs should be considered.

Neuroleptic Malignant Syndrome (NMS): Neuroleptic Malignant Syndrome, characterized by hyperthermia, muscle rigidity, autonomic instability, altered consciousness and elevated serum creatine phosphokinase levels has been reported to occur with antipsychotics. Additional signs may include myoglobinuria (rhabdomyolysis) and acute renal failure. In this event, all antipsychotic drugs, including this drug, should be discontinued.

Parkinson’s disease and Dementia with Lewy Bodies: Physicians should weigh the risks versus the benefits when prescribing antipsychotics, including this drug, to patients with Parkinson’s disease or Dementia with Lewy Bodies (DLB) since both groups may be at increased risk of Neuroleptic Malignant Syndrome as well as having an increased sensitivity to antipsychotic medications. Manifestation of this increased sensitivity can include confusion, obtundation, and postural instability with frequent falls, in addition to extrapyramidal symptoms.

Hyperglycemia and Diabetes Mellitus: Hyperglycemia, diabetes mellitus and exacerbation of pre-existing diabetes have been reported during treatment with it. In some cases, a prior increase in body weight has been reported which may be a predisposing factor. Association with ketoacidosis has been reported very rarely and rarely with diabetic coma. Appropriate clinical monitoring is advisable in accordance with utilized antipsychotic guidelines. Patients treated with any atypical antipsychotic, including it should be monitored for symptoms of hyperglycemia (such as polydipsia, polyuria, polyphagia and weakness) and patients with diabetes mellitus should be monitored regularly for worsening of glucose control.

Weight Gain: Significant weight gain has been reported with use. Weight should be monitored regularly.

Hyperprolactinemia: Tissue culture studies suggest that cell growth in human breast tumors may be stimulated by prolactin. Although no clear association with the administration of antipsychotics has so far been demonstrated in clinical and epidemiological studies, caution is recommended in patients with relevant medical history. This drug should be used with caution in patients with pre-existing hyperprolactinemia and in patients with possible prolactin-dependent tumors.

QT prolongation:  Has very rarely been reported post marketing. As with other antipsychotics, caution should be exercised when it is prescribed in patients with known cardiovascular disease, family history of QT prolongation, bradycardia, or electrolyte disturbances (hypokalemia, hypomagnesaemia), as it may increase the risk of arrythmogenic effects, and in concomitant use with medicines known to prolong the QT interval.

Priapism: Drugs with alpha-adrenergic blocking effects have been reported to induce priapism. Priapism has been reported with it during post marketing surveillance.

Body Temperature Regulation: Disruption of the body’s ability to reduce core body temperature has been attributed to antipsychotic agents. Appropriate care is advised when prescribing it to patients who will be experiencing conditions which may contribute to an elevation in core body temperature, e.g., exercising strenuously, exposure to extreme heat, receiving concomitant medication with anticholinergic activity, or being subject to dehydration.

Antiemetic Effect: An antiemetic effect was observed in preclinical studies with it. This effect, if it occurs in humans, may mask the signs and symptoms of overdose with certain medicines or of conditions such as intestinal obstruction, Reye’s syndrome, and brain tumor.

Seizures: This drug should be used cautiously in patients with a history of seizures or other conditions that potentially lower the seizure threshold.

Renal and hepatic impairment: Patients with renal impairment have less ability to eliminate the active antipsychotic fraction than adults with normal renal function. Patients with impaired hepatic function have increases in plasma concentration of the free fraction of it.

Intraoperative Floppy Iris Syndrome: Intraoperative Floppy Iris Syndrome (IFIS) has been observed during cataract surgery in patients treated with medicines with alpha1a-adrenergic antagonist effect, including this drug. IFIS may increase the risk of eye complications during and after the operation. Current or past use of medicines with alpha1a-adrenergic antagonist effect should be made known to the ophthalmic surgeon in advance of surgery. The potential benefit of stopping alpha1-blocking therapy prior to cataract surgery has not been established and must be weighed against the risk of stopping the antipsychotic therapy.

Pediatric population: Before this drug is prescribed to a child or adolescent with conduct disorder they should be fully assessed for physical and social causes of the aggressive behavior such as pain or inappropriate environmental demands. The sedative effect of it should be closely monitored in this population because of possible consequences on learning ability. A change in the time of administration of it could improve the impact of the sedation on attention faculties of children and adolescents. This drug was associated with mean increases in body weight and body mass index (BMI). Baseline weight measurement prior to treatment and regular weight monitoring are recommended. Changes in height in the long-term open-label extension studies were within expected age appropriate norms. The effect of long-term treatment on sexual maturation and height has not been adequately studied. Because of the potential effects of prolonged hyperprolactinemia on growth and sexual maturation in children and adolescents, regular clinical evaluation of endocrinological status should be considered, including measurements of height, weight, sexual maturation, monitoring of menstrual functioning, and other potential prolactin-related effects. During treatment regular examination for extrapyramidal symptoms and other movement disorders should also be conducted.


SIDE EFFECTS

Very common: Insomnia, sedation/somnolence, parkinsonism, headache.

Common: Pneumonia, bronchitis, upper respiratory tract infection, sinusitis, urinary tract infection, ear infection, influenza, hyperprolactinaemia, weight increased, increased appetite, decreased appetite, sleep disorder, agitation, depression, anxiety, akathisia, dystonia, dizziness, dyskinesia, tremor, vision blurred, conjunctivitis, tachycardia, hypertension, dyspnoea, pharyngolaryngeal pain, cough, epistaxis, nasal congestion, abdominal pain, abdominal discomfort, vomiting, nausea, constipation, diarrhoea, dyspepsia, dry mouth, toothache, rash, erythema, muscle spasms, musculoskeletal pain, back pain, arthralgia, urinary incontinence, oedema, pyrexia, chest pain, asthenia, fatigue, pain, fall.


DOSAGE

Schizophrenia

Adults: This drug may be given once daily or twice daily. Patients should start with 2 mg/day. The dosage may be increased on the second day to 4 mg. From then on the dosage can be maintained unchanged, or further individualized, if needed. Most patients will benefit from daily doses between 4 and 6 mg. In some patients, a slower titration phase and a lower starting and maintenance dose may be appropriate. Doses above 10 mg/day have not been shown to be superior in efficacy to lower doses and may cause extrapyramidal symptoms. Since the safety of doses above 16 mg/day has not been evaluated, doses above this level should not be used. A benzodiazepine may be added to it when additional sedation is required.

Elderly: A starting dose of 0.5 mg twice daily is recommended. This dosage can be individually adjusted with 0.5 mg twice daily increments to 1 to 2 mg twice daily.

Adolescents: A starting dose of 0.5 mg daily is recommended, administered as a single-daily dose either in the morning or evening. If indicated, this dosage can then be adjusted at intervals not less than 24 hours in increments of 0.5 or 1 mg/day, as tolerated, to a recommended dose of 3 mg/day. Efficacy has been demonstrated at doses between 1 and 6 mg/day. Doses higher than 6 mg/day have not been studied. Patients experiencing persistent somnolence may benefit from administering half the daily dose twice daily.

Children: Experience in schizophrenia is lacking in children aged less than 13 years of age.

Bipolar Mania

Adults: This drug should be administered on a once daily schedule, starting with 2 or 3 mg. Dosage adjustments, if indicated, should occur at intervals of not less than 24 hours and in dosage increments of 1 mg per day. Efficacy was demonstrated in flexible doses over a range of 1 to 6 mg per day. As with all symptomatic treatments, the continued use of it must be evaluated and justified on an ongoing basis.

Children and Adolescents: A starting dose of 0.5mg once daily is recommended, administered as a single-daily dose in either the morning or evening. If indicated, this dosage can then be adjusted at intervals not less than 24 hours in increments of 0.5 or 1 mg/day, as tolerated, to a recommended dose of 2.5 mg/day. Although efficacy has been demonstrated at doses between 0.5 and 6 mg/day. No additional benefit was seen above 2.5 mg/day, and higher doses were associated with more adverse events. Doses higher than 6 mg/day have not been studied. Patients experiencing persistent somnolence may benefit from administering half the daily dose twice daily. As with all symptomatic treatments, the continued use of this drug must be evaluated and justified on an ongoing basis. Experience is lacking in bipolar mania in children less than 10 years of age.

Psychotic manifestations of dementia: A starting dose of 0.25 mg twice daily is recommended. This dosage can be individually adjusted by increments of 0.25 mg twice daily not more frequently than every other day, if needed. The optimum dose is 0.5 mg twice daily for most patients. Some patients, however, may benefit from doses up to 1 mg twice daily. This drug should not be used more than 6 weeks in patients with persistent aggression in Alzheimer’s dementia. During treatment, patients must be evaluated frequently and regularly, and the need for continuing treatment reassessed.

Conduct and other disruptive behavior disorders

Subjects ≥ 50 kg: A starting dose of 0.5 mg once daily is recommended. This dosage can be individually adjusted by increments of 0.5 mg once daily not more frequently than every other day, if needed. The optimum dose is 1 mg once daily for most patients. Some patients, however, may benefit from 0.5 mg once daily while others may require 1.5 mg once daily.

Subjects < 50 kg: A starting dose of 0.25 mg once daily is recommended. This dosage can be individually adjusted by increments of 0.25 mg once daily not more frequently than every other day, if needed. The optimum dose is 0.5 mg once daily for most patients. Some patients, however, may benefit from 0.25 mg once daily while others may require 0.75 mg once daily. As with all symptomatic treatments, the continued use of it must be evaluated and justified on an ongoing basis. Experience is lacking in children aged less than 5 years of age.

Renal & Hepatic Impairment: Patients with renal impairment have less ability to eliminate the active antipsychotic fraction than normal adults. Patients with impaired hepatic function have increases in plasma concentration of the free fraction of this drug.

Irrespective of the indication, starting and consecutive dosing should be halved, and dose titration should be slower for patients with renal or hepatic impairment. This drug should be used with caution in these groups of patients.

Method of administration: This drug is for oral use. Food does not affect the absorption of risperidone. Upon discontinuation, gradual withdrawal is advised. Acute withdrawal symptoms, including nausea, vomiting, sweating, and insomnia have very rarely been described after abrupt cessation of high doses of antipsychotic medicines. Recurrence of psychotic symptoms may also occur, and the emergence of involuntary movement disorders (such as akathisia, dystonia and dyskinesia) has been reported.

Switching from other antipsychotics: When medically appropriate, gradual discontinuation of the previous treatment while this therapy is initiated is recommended. Also, if medically appropriate, when switching patients from depot antipsychotics, initiate therapy in place of the next scheduled injection. The need for continuing existing anti-Parkinson medications should be re-evaluated periodically.


OVERDOSE

Symptoms: drowsiness, sedation, tachycardia, hypotension, extrapyramidal symptoms, QT-prolongation, convulsions. Combined overdose with paroxetine: Torsade de pointes. In case of acute overdose, the possibility of multiple drug involvement should be considered. Treatment: Establish and maintain a clear airway and ensure adequate oxygenation and ventilation. Gastric lavage (after intubation, if the patient is unconscious) and administration of activated charcoal together with a laxative should be considered only when drug intake was less than one hour before. Cardiovascular monitoring should commence immediately and should include continuous electrocardiographic monitoring to detect possible arrhythmias.

There is no specific antidote to this drug. Therefore, appropriate supportive measures should be instituted. Hypotension and circulatory collapse should be treated with appropriate measures such as intravenous fluids and/or sympathomimetic agents. In case of severe extrapyramidal symptoms, an anticholinergic medicinal product should be administered. Close medical supervision and monitoring should continue until the patient recovers.


PREGNANCY & LACTATION

Pregnancy: There are no adequate data from the use of this drug in pregnant women. Risperidone was not teratogenic in animal studies but other types of reproductivetoxicity were seen. The potential risk for humans is unknown.Neonates exposed to antipsychotic drugs (including this drug) during the third trimester of pregnancy are at risk of adverse reactions including extrapyramidal and/or withdrawal symptoms that may vary in severity following delivery. There have been reports of agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, or feeding disorder. Consequently, newborns should be monitored carefully. This drug should not be used during pregnancy unless clearly necessary. If discontinuation during pregnancy is necessary, it should not be done abruptly.

Lactation: In animal studies, this drug and 9-hydroxy-risperidone are excreted in the milk. It has been demonstrated that this drug and 9-hydroxy-risperidone are also excreted in human breast milk in small quantities. There are no data available on adverse reactions in breast-feeding infants. Therefore, the advantage of breast-feeding should be weighed against the potential risks for the child.

Fertility: As with other drugs that antagonize dopamine D2 receptors, this drug elevates prolactin level. Hyperprolactinemia may suppress hypothalamic GnRH, resulting in reduced pituitary gonadotropin secretion. This, in turn, may inhibit reproductive function by impairing gonadal steroidogenesis in both female and male patients. There were no relevant effects observed in the non-clinical studies.


MANUFACTURER & DISTRIBUTER:

Manufacturer: Dexcel Ltd.

License Holder: Dexcel Pharma Technologies


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