Aurobindo Pharma


Full Prescribing Info
Risperidone Tablets 1mg: Each film coated tablet contains Risperidone 1mg.
Risperidone Tablets 2mg: Each film coated tablet contains Risperidone 2mg.
Risperidone Tablets 3mg: Each film coated tablet contains Risperidone 3mg.
Resicalm 1 (Risperidone Oral Solution 1 mg/mL): Each ml of Risperidone equivalent to Risperidone 1 mg.
Pharmacology: Pharmacodynamics: Risperidone is a selective monoaminergic antagonist with unique properties. It has a high affinity for serotoninergic 5-HT2 and dopaminergic D2 receptors. Risperidone binds also to alpha1 adrenergic receptors, and with lower affinity to H1 histaminergic and alpha2 adrenergic receptors. Risperidone is a potent D2 antagonist, which is considered to improve the positive symptoms of schizophrenia, it causes less depression of motor activity and induction of catalepsy than classical neuroleptics. Balanced central serotonin and dopamine antagonism may reduce extrapyramidal side effects liability and extend the therapeutic activity to the negative and effective symptoms of schizophrenia.
Pharmacokinetics: Risperidone is completely absorbed after oral administration, reaching peak plasma concentrations within 1 to 2 hours. The absorption is not affected by food and thus risperidone can give with or without meals.
Risperidone is metabolized by cytochrome P-450 llD6 to 9-hydroxy-risperidone which has a similar pharmacological activity as risperidone. Risperidone plus 9-hydroxy-risperidone form the active antipsychotic fraction. Another metabolic pathway of risperidone is N-dealkylation. After oral administration to psychotic patients, risperidone is eliminated with a half-life of about 3 hours. The elimination half-life of 9-hydroxy-risperidone and of the active antipsychotic fraction is 24 hours.
Steady-state of risperidone is reached within 1 day in most patients. Steady-state of 9-hydroxy-risperidone is reached within 4-5 days of dosing. Risperidone plasma concentrations are dose-proportional within the therapeutic dose-range.
Risperidone is rapidly distributed. The volume of distribution is 1-2 l/kg. In plasma, risperidone is bound to albumin and alpha1-acid glycoprotein. The plasma protein binding of risperidone is 88% that of 9-hydroxy-risperidone is 77%.
One week after administration, 70% of the dose is excreted in the urine and 14% in faeces. In urine, risperidone plus 9-hydroxy-risperidone represent 35-45% of the dose. The remainders are inactive metabolites.
A single dose study showed higher active plasma concentrations and slower elimination of risperidone in the elderly and in patients with renal insufficiency. Risperidone plasma concentrations were normal in patients with liver insufficiency.
RESICALM is indicated for the treatment of a broad range of patients with schizophrenia, including first episode psychoses, acute schizophrenic exacerbations, chronic schizophrenia, and other psychotic conditions, in which positive symptoms (such as hallucinations, delusions, thought disturbances, hostility, suspiciousness) and/or negative symptoms (such as blunted affect, emotional and social withdrawal, poverty of speech) are prominent. RESICALM alleviates affective symptoms (such as depression, guilt feeling, anxiety) associated with schizophrenia. RESICALM is also effective in maintaining the clinical improvement during continuation therapy in patients who have shown an initial treatment response.
Dosage/Direction for Use
Schizophrenia: Switching from other antipsychotics: When medically appropriate, gradual discontinuation of the previous treatment while RESICALM therapy is initiated is recommended. Also if medically appropriate, when switching patients from depot antipsychotics, initiate RESICALM therapy in place of the next scheduled injection. The need for continuing existing anti-parkinson medications should be re-evaluated periodically.
Adults: RESICALM may be given as tablets or oral solution, once or twice daily.
All patients whether acute or chronic, should start with 2mg/day RESICALM. The dosage may be increased on the second day to 4mg. from then on the dosage can be maintained unchanged or further individualized, if needed. Most patients will benefit from daily doses between 4 and 6mg. 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 16mg/day has not been evaluated, doses above this level should not be used.
A benzodiazepine may be added to RESICALM when additional sedation is required.
Elderly: A starting dose of 0.5mg twice a day is recommended. This dosage can be individually adjusted with 0.5mg twice a day increments to 1 to 2mg twice a day. RESICALM is well tolerated by the elderly.
Children: Experience is lacking in children aged less than 15 years.
Renal and liver disease: A starting dose of 0.5mg twice a day is recommended. This dosage can be individually adjusted with 0.5mg twice a day increments to 1 to 2mg twice a day. RESICALM should be used with caution in this group of patients until further experience is gained.
It is not advisable to take RESICALM Oral Solution in a cup of tea.
Symptoms: In general, reported signs and symptoms have been those resulting from an exaggeration of the drug's known pharmacological effects. These include drowsiness and sedation, tachycardia and hypotension, and extrapyramidal symptoms. Overdosages of up to 360mg have been reported. In case of acute overdosage, the possibility of multiple drug involvement should be considered.
Treatment: Established 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. Cardiovascular monitoring should commence immediately and should include continuous electrocardiographic monitoring to detect possible arrhythmias. There is no specific antidote to RESICALM. 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, anticholinergic medication should be administered. Close medical supervision and monitoring should continue until the patient recovers.
RESICALM is contraindicated in patients with a known hypersensitivity to the components of this product. It is also contraindicated in coma caused by CNS depressants, bone-marrow depression and avoided in phaeochromocytoma.
Special Precautions
Due to the alpha-blocking activity of RESICALM, (orthostatic) hypotension can occur, especially during the initial dose-titration period. RESICALM should be used with caution in patients with known cardiovascular disease (e.g. heart failure, myocardial infarction, conduction abnormalities, dehydration, hypovolaemia or cerebrovascular disease) and the dosage should be gradually titrated as recommended. A dose reduction should be considered if hypotension occurs.
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. It has been reported that the occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. Because RESICALM has a lower potential to induce extrapyramidal symptoms than classical neuroleptics, it should have a reduced risk of inducing tardive dyskinesia as compared to classical neuroleptics. If signs and symptoms of tardive dyskinesia appear, the discontinuation of all antipsychotic drugs should be considered. The Neuroleptic Malignant Syndrome, characterized by hyperthermia, muscle rigidity, autonomic instability, altered consciousness and elevated CPK levels has been reported to occur with classical neuroleptics. In this event, all antipsychotic drugs, including RESICALM, should be discontinued. For specific posology recommendations for elderly patients and patients with renal and liver disease, refer to Dosage & Administration.
Caution is also due when prescribing RESICALM to patients with Parkinson's disease, since theoretically it might cause a deterioration of the disease.
Classical neuroleptics are known to lower the seizure threshold. Caution is recommended when treating patients with epilepsy. Patients may be advised to refrain from excessive eating in view of possibility of weight gain.
Intraoperative Floppy Iris Syndrome: Intraoperative Floppy Iris Syndrome (IFIS) has been observed during cataract surgery in patients treated with medicines with alpha 1a-adrenergic antagonist effects, including risperidone. IFIS may increase the risk of eye complications during and after operation. Current or past use of medicines with alpha-1a-adrenergic antagonist effect should be made known to the ophthalmic surgeon in advance of surgery. The potential benefit of stopping alpha 1 blocking therapy prior to cataract surgery has not been established and must be weighed against the risk of stopping the antipsychotic therapy.
Hyperglycemia and Diabetes Mellitus: Hyperglycemia in some cause extreme and associated with ketoacidosis or hyperosmolar coma or death, has been reported in patients treated with atypical antipysychotics. Assessment of the relationship between atypical antipsychotic use and glucose abnormalities is complicated by the possibility of an increased background risk of diabetes mellitus in patients with schizophrenia and the increasing incidence of diabetes mellitus in the general population. Given this confounders, the relationship between atypical antipsychotics use and hyperglycemia-related adverse events is not completely understood. However, epidemiological studies suggest an increased risk of treatment - emergent hyperglycemia-related events in patients treated with the atypical antipsychotics. Precise risk estimates for hyperglycemia-related adverse events in patients treated with atypical antipsychotics are not available. Patients with an established diagnoses of diabetes mellitus who are started on atypical antipsychotics should be monitored regularly for worsening of glucose control.
Patients with risk factors for diabetes mellitus (e.g obesity, family history of diabetes) who are starting treatment with atypical antipsychotics should undergo fasting blood glucose testing at the beginning of treatment and periodically during treatment. Any patients treated with atypical antipsychotics should be monitored for symptoms of hyperglycemia including polydipsia, polyuria, polyphagia, and weakness. Patients who develop symptoms of hyperglycemia during treatment with atypical antipsychotics should undergo fasting blood glucose testing. In some cases, hyperglycemia has resolved when the atypical antipsychotic was discontinued, however, some patients required continuation of anti-diabetics treatment despite discontinuation of the suspect drug.
Effects on Ability to Drive and Use Machine: RESICALM may interfere with activities requiring mental alertness. Therefore, patients should be advised not to drive or operate machinery until their individual susceptibility is known.
Use In Pregnancy & Lactation
The safety of RESICALM for use during human pregnancy has not been established. Although in experimental animals, risperidone did not show direct reproductive toxicity, some indirect, prolactin and CNS mediated effects were observed. No teratogenic effect of risperidone was noted in any study. Therefore, RESICALM should only be used during pregnancy if the benefits outweigh the risks.
In animal studies, risperidone and 9-hydroxy-risperidone are excreted in the milk. It has been demonstrated that risperidone and 9-hydroxy-risperidone are also excreted in human breast milk. Therefore, women receiving RESICALM should not breast feed.
Side Effects
Based on extensive clinical experience including long term use, RESICALM is generally well tolerated. In many instances, it has been difficult to differentiate adverse events from symptoms of the underlying disease. Adverse events observed in association with the use of RESICALM are listed as follows.
Common: Insomnia, agitation, anxiety, headache.
Less common: Somnolence, fatigue, dizziness, impaired concentration, constipation, dyspepsia, nausea/vomiting, abdominal pain, blurred vision, priapism, erectile dysfunction, organic dysfunction, ejaculatory dysfunction, urinary incontinence, rhinitis, rash and other allergic reactions.
Cerebrovascular adverse events, including cerebrovascular accidents and transient ischemic attacks, have been reported during treatment with risperidone. Hyperglycemia and exacerbation of pre-existing diabetes have been reported in very rare cases during risperidone treatment.
RESICALM has a lower propensity to induce extrapyramidal symptoms than classical neuroleptics. However, in some cases the following extrapyramidal symptoms may occur: tremor, rigidity, hypersalivation, bradykinesia, akathisia, and acute dystonia. These are usually mild and are reversible upon dose reduction and/or administration of antiparkinson medication, if necessary.
Occasionally (orthostatic) hypotension and (reflex) tachycardia or hypertension have been observed following administration of RESICALM (see Precautions). A mild fall in neutrophil and/or thrombocyte count has been reported.
RESICALM can induce a dose-dependent increase in plasma prolactin concentration. Possible associated manifestations are galactorrhoea, gynaecomastia, and disturbances of the menstrual cycle and amenorrhoea. Weight gain (see Precautions), oedema and increased hepatic enzyme levels have been observed during treatment with RESICALM. As with classical neuroleptics, the following have occasionally been reported in psychotic patients: water intoxication due to polydipsia or the syndrome of inappropriate secretion of antidiuretic hormone (SIADH), tardive dyskinesia, neuroleptic malignant syndrome, body temperature dysregulation and seizures.
Post-marketing Data: Eye Disorders Frequency: Not Known: Floppy Iris Syndrome (Intraoperative).
Store below 30°C. Protect from light and moisture.
Shelf-Life: 24 months.
MIMS Class
ATC Classification
N05AX08 - risperidone ; Belongs to the class of other antipsychotics.
FC tab 1 mg (white coloured, biconvex, caplets, debossed on one side with "A" and on the other side with "51". Score line between "5" and "1") x 3 x 10's, 10 x 10's. 2 mg (light orange coloured, biconvex, caplets, debossed on one side with "A" and on the other side with "52". Score line between "5" and "2") x 3 x 10's, 10 x 10's. 3 mg (yellow coloured, biconvex, caplets, debossed on one side with "A" and on the other side with "53". Score line between "5" and "3") x 3 x 10's, 10 x 10's. Oral soln 1 mg/mL (clear, colourless liquid) x 30 mL, 100 mL.
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