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Risperidone: profile and news
Trial of risperidone in India – concerns May 2, 2006 Trial of risperidone in India – concerns Apr 28, 2006 Trial of risperidone in India – concerns Apr 28, 2006 Behavioral and Pharmacologic Treatment of Aggression in Children ... May 10, 2006 Innovations: Geriatric Psychiatry: Diagnosis and Treatment of ... May 10, 2006 Understanding and Managing Psychosis in Late Life May 15, 2006 Researchers from Canada and Netherlands describe findings in ... May 15, 2006 Patient Management Exercise FOR PSYCHOTHERAPY May 15, 2006 B. Lyons , F. Grossman and M. Kramer Apr 28, 2006 Recent Developments in Antipsychotic Use in Adults Apr 20, 2006 Correspondence: E-mail: bjp{at}rcpsych.ac.uk May 2, 2006 New-Onset Tardive Dyskinesia in Patients With First-Episode ... Apr 28, 2006 Alkermes to Host Conference Call to Discuss Fiscal Year 2006 ... May 11, 2006 Psychiatric Decision Making in the Adoption of a New Antipsychotic ... May 4, 2006 Aripiprazole in the Treatment of Patients With Borderline ... May 10, 2006 Antipsychotic Drug Use Growing Fastest Among Children May 2, 2006 Hallucinations in Children and Adolescents: Considerations in the ... May 2, 2006 Department of Ambulatory Care and Prevention, Harvard Medical ... May 2, 2006 Schizophrenia gene function offers hope for drug R&D Apr 23, 2006 Antiparkinsonian prescription and extrapyramidal symptoms Apr 28, 2006 Other information Indication For the treatment of schizophrenia Pharmacology Risperidone is an atypical antipsychotic medication. It is most often used to treat delusional psychosis (including schizophrenia), but Risperidone is also used to treat some forms of bipolar disorder and psychotic depression. It also has shown some success in treating symptoms of Asperger's Syndrome and autism. Risperidone is now the most commonly prescribed antipsychotic medication in the United States. Mechanism Of Action Blockade of dopaminergic D2 receptors in the limbic system alleviates positive symptoms of schizophrenia such as hallucinations, delusions, and erratic behavior and speech. Blockade of serotonergic 5-HT2 receptors in the mesocortical tract, causes an excess of dopamine and an increase in dopamine transmission, resulting in an increase in dopamine transmission and an elimination of core negative symptoms. Dopamine receptors in the nigrostriatal pathway are not affected by risperidone and extrapyramidal effects are avoided. Like other 5-HT2 antagonists, risperidone also binds at alpha(1)-adrenergic receptors and, to a lesser extent, at histamine H1 and alpha(2)-adrenergic receptors. Drug Category Antipsychotics; Antipsychotics; ATC:N05AX08 Brand Names/Synonyms CHEMBANK1795; R118; Remeron; Risperdal; Risperdal Consta; Risperdal M-Tab; Risperidal M-Tab; Risperidona [Spanish]; Risperidone; Risperidone [Usan:Ban:Inn]; Risperidonum [Latin]; Risperin; Rispolept; Rispolin; Sequinan Dosage Forms Tablets and oral solution Absorption Risperidone is well absorbed. The absolute oral bioavailability of risperidone is 70% (CV=25%). The relative oral bioavailability of risperidone from a tablet is 94% (CV=10%) when compared to a solution. Pharmacokinetic studies showed that RISPERDAL® M-TAB™ Orally Disintegrating Tablets and RISPERDAL® Oral Solution are bioequivalent to RISPERDAL® Tablets Interactions -->Interactions for Risperidone: The interactions of RISPERDAL® and other drugs have not been systematically evaluated. Given the primary CNS effects of risperidone, caution should be used when RISPERDAL® is taken in combination with other centrally acting drugs and alcohol. Because of its potential for inducing hypotension, RISPERDAL® may enhance the hypotensive effects of other therapeutic agents with this potential. RISPERDAL® may antagonize the effects of levodopa and dopamine agonists. Amytriptyline does not affect the pharmacokinetics of risperidone or the active antipsychotic fraction. Cimetidine and ranitidine increased the bioavailability of risperidone, but only marginally increased the plasma concentration of the active antipsychotic fraction. Chronic administration of clozapine with risperidone may decrease the clearance of risperidone. Carbamazepine and Other Enzyme Inducers In a drug interaction study in schizophrenic patients, 11 subjects received risperidone titrated to 6 mg/day for 3 weeks, followed by concurrent administration of carbamazepine for an additional 3 weeks. During co-administration, the plasma concentrations of risperidone and its pharmacologically active metabolite, 9-hydroxyrisperidone, were decreased by about 50%. Plasma concentrations of carbamazepine did not appear to be affected. The dose of risperidone may need to be titrated accordingly for patients receiving carbamazepine, particularly during initiation or discontinuation of carbamazepine therapy. Co-administration of other known enzyme inducers (e.g., phenytoin, rifampin, and phenobarbital) with risperidone may cause similar decreases in the combined plasma concentrations of risperidone and 9-hydroxyrisperidone, which could lead to decreased efficacy of risperidone treatment. Fluoxetine and Paroxetine Fluoxetine (20 mg QD) and paroxetine (20 mg QD) have been shown to increase the plasma concentration of risperidone 2.5-2.8 fold and 3-9 fold respectively. Fluoxetine did not affect the plasma concentration of 9-hydroxyrisperidone. Paroxetine lowered the concentration of 9-hydroxyrisperidone an average of 13%. When either concomitant fluoxetine or paroxetine is initiated or discontinued, the physician should re-evaluate the dosing of RISPERDAL®. The effects of discontinuation of concomitant fluoxetine or paroxetine therapy on the pharmacokinetics of risperidone and 9-hydroxyrisperidone have not been studied. Lithium Repeated oral doses of risperidone (3 mg BID) did not affect the exposure (AUC) or peak plasma concentrations (Cmax) of lithium (n=13). Valproate Repeated oral doses of risperidone (4 mg QD) did not affect the pre-dose or average plasma concentrations and exposure (AUC) of valproate (1000 mg/day in three divided doses) compared to placebo (n=21). However, there was a 20% increase in valproate peak plasma concentration (Cmax) after concomitant administration of risperidone. Digoxin RISPERDAL® (0.25 mg BID) did not show a clinically relevant effect on the pharmacokinetics of digoxin. Drugs That Inhibit CYP 2D6 and Other CYPIsozymes Risperidone is metabolized to 9-hydroxyrisperidone by CYP 2D6, an enzyme that is polymorphic in the population and that can be inhibited by a variety of psychotropic and other drugs. Drug interactions that reduce the metabolism of risperidone to 9-hydroxyrisperidone would increase the plasma concentrations of risperidone and lower the concentrations of 9-hydroxyrisperidone. Analysis of clinical studies involving a modest number of poor metabolizers (n 70) does not suggest that poor and extensive metabolizers have different rates of adverse effects. No comparison of effectiveness in the two groups has been made. In vitro studies showed that drugs metabolized by other CYPisozymes, including 1A1, 1A2, 2C9, 2C19, and 3A4, are only weak inhibitors of risperidone metabolism. There were no significant interactions between risperidone and erythromycin. Drugs Metabolized by CYP 2D6 In vitro studies indicate that risperidone is a relatively weak inhibitor of CYP 2D6. Therefore, RISPERDAL® is not expected to substantially inhibit the clearance of drugs that are metabolized by this enzymatic pathway. In drug interaction studies, risperidone did not significantly affect the pharmacokinetics of donepezil and galantamine, which are metabolized by CYP 2D6. |
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