COMPOSITIONS :
Risperidone Film coated tablet 2 mg, each film coated tablet contains : Risperidone 2 mg.
PHARMACOLOGY :
Risperidone is a selective monoaminergic antagonist with unique efficacy. It has a high affinity for serotonin 5-HT2 and dopamine D2 receptors. Risperidone also binds to α1 adrenergic receptors and has low affinity for H1 histaminergic and α2 adrenergic receptors. Risperidone has no affinity for cholinergic receptors. Although Risperidone is a strong D2 antagonist, which improves 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 and extend the therapeutic activity against negative symptoms of schizophrenia.
INDICATIONS :
Acute and chronic schizophrenia, another psychiatric condition in which both positive and negative reactions occur. It is also effective in reducing the symptoms of schizophrenia.
DOSAGE AND ADMINISTRATIONS :
Schizophrenia
Patients switching from other antipsychotics : At the time of starting Risperidone therapy, patients are recommended to discontinue their previous antipsychotic use gradually, also when Risperidone therapy is started in patients who have previously used antiparkinsonian drugs, the patient should be evaluated gradually.
- Adults :
Risperidone may be given once daily or twice daily.
Risperidone should be started at a dose of 2 mg/day. The dosage may be increased on the second day to 4 mg. Subsequently, the dosage can be maintained or adjusted according to the condition of each patient, if needed. Most patients experienced marked improvement at doses of 4 mg/day and 6 mg/day. In some patients, a slower titration phase, with a lower starting and maintenance dose may be appropriate. Doses above 10 mg/day are no more effective than a lower doses and may cause increased of extrapyramidal symptoms. The safety of giving doses above 16 mg/day has not been evaluated, so do not use drugs in excess of this dose. Benzodiazepines may be given with Risperidone if additional sedation is required.
- Elderly:
The recommended starting dose is 0.5 mg, twice daily. This dosage can be individually adjusted with 0.5 mg, twice daily increments to 1 – 2 mg, twice daily. Risperidone is well tolerated in the elderly.
- Children :
No experience of use in paediatric patients < 15 years with schizophrenia.
- Renal and hepatic impairment :
Patients with renal impairment will have less ability to eliminate the active antipsychotic fraction compared to normal patients. Patients with impaired hepatic function will experience an increase plasma concentration of the free fraction of Risperidone. Irrespective of the indication, the initial and maintenance doses should be half of the normal dose and dose titration should be slower for patients with renal and hepatic impairment.
OVERDOSAGE :
Symptoms :
In general, reported signs and symptoms have been those resulting from an exaggeration of the known pharmacological effects of the drug. These symptoms include drowsiness and sedation, tachycardia and hypotension, and extrapyramidal symptoms. Overdosage of up to 360 mg has been reported. The available evidence suggests a broad range of security. In rare cases, QT-prolongation have been reported in overdose.
In case of acute overdose, the possibility of multiple drug involvement shoul be considered.
Treatment :
Establish and maintain a clear airway and ensure adequate oxygen and ventilation. Gastric lavage (after intubation, if the patient is unconscious) and administration of activated charcoal together with laxatives should be considered. Cardiovascular monitoring should be commence immediately and should include continuous electrocardiographic monitoring to detect possible arrhythmias.
There is no specific antidote to Risperidone. Therefore, appropriate action must be taken. Hypotension and circulatory collapse should be treated with appropriate medications such as intravenous fluids and/or sympathomimetic drugs. In case of severe extrapyramidal symptoms, an anticholinergic drugs should be given. Close medical supervision and monitoring should continue until the patient recoveres.
CONTRAINDICATION :
Hypersensitivity to any component of this drug.
WARNINGS AND PRECAUTIONS :
- Patients with known cardiovascular disease, the dose should be titrated gradually.
- Dose should be reduced if hypotension occurs.
- Caution when given to patients with renal or hepatic failure, as well as in elderly and Parkinson’s patients.
- Be careful when operating machinery or motor vehicles. Risperidone may affect activities that require alertness.Therefore, patients are advised not to drive or operate machinery until the effects of the drug on alertness are known.
- Monitor for signs of tardive dyskinesia.
- Be careful when given to pregnant and lactating women. The safety of use Risperidone in pregnant women is unknown.It has been observed that Risperidone and 9-Hydroxy-Risperidone are also excreted in human breast milk. Therefore, women who are given Risperidone are advised not to breastfeeding.
- Discontinue the drug if there is a neuroleptic malignant syndrome with symptoms of hyperthermia, muscle rigidity, autonomic instability, impaired consciousness and elevated CPK levels.
- Use with caution in patients with unstable epilepsy.
- Patients are advised not to overeat considering the possibility of weight gain.
DRUG INTERACTIONS :
- Risperidonemay antagonize the effects of Levodopa and other Dopamine agonists.
- Because Risperidone has an effect on the central nervous system, caution should be exercised when combined with other centrally acting drugs.
- Phenothiazines, tricyclic antidepressants and some beta-blockers may increase the plasma concentrations of Risperidone, but not change its pharmacological effect.
- Carbamazepine may decrease plasma concentrations of the active antipsychotic fraction of Risperidone.Similar effects may be observed with other hepatic enzyme-inducing drugs. On discontinuation of carbamazepine or other hepatic enzymes, the dose of Risperidone should be re-evaluated and reduced if necessary.
- Phenotiazine, tricyclic antidepressants and some beta-blockers may increase the plasma concentrations of Risperidone, but not those of the active antipsychotic fraction.
- Food does not affect the absorption of Risperidone.
ADVERSE REACTIONS :
- Insomnia, anxiety agitation, headache, drowsiness, fatigue, dizziness, extrapyramidal symptoms, weight gain.
- Less common: Drowsiness, fatigue, impaired concentration, dyspepsia, constipation, nausea, abdominal pain, blurred vision, impaired erection and ejaculation, impaired orgasm, rhinitis, redness from other allergic reactions.
- Risperidone may cause an increase in plasma prolactin concentrations depending on the dose used.Possible associated manifestations are galactorrhea, gynaecomastia, menstrual cycle disorder and amenorrhea. Weight gain, oedema and elevated hepatic enzymes have been reported during treatment with risperidone.
PRESENTATIONS :
Risperidone 2 mg is available in the form of a peach film-coated tablet with the marking b breakline f on one side and plain on the other, packaged in :
Box, 3 strips @ 10 film coated tablets No. Reg. : GKL2202365717A1
STORAGE:
STORE BELOW 30°C, PROTECT FROM LIGHT
ON MEDICAL PRESCRIPTION ONLY
Manufactured by :
PT. BERNOFARM
Sidoarjo – Indonesia
