Risperdal Consta(j&j)

Uses

Risperdal Consta(j&j) tablet is used for the treatment of acute and chronic schizophrenic psychoses, 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. Risperdal Consta(j&j) also alleviate affective symptoms (such as depression, guilt feelings, anxiety) associated with schizophrenia. Risperdal Consta(j&j) is also effective inmaintaining the clinical improvement during continuation therapy in patients who have shown an initial treatment response. Risperdal Consta(j&j) is in dicated for the treatment of mania in bipolar disorder.

Risperdal Consta(j&j) is also used to associated treatment for these conditions: Acute Mania, Irritability, Mixed manic depressive episode, Psychosis, Schizophrenia, Acute Manic episode, Agitated psychotic state

How Risperdal Consta(j&j) works

Though its precise mechanism of action is not fully understood, current focus is on the ability of risperidone to inhibit the D2 dopaminergic receptors and 5-HT2A serotonergic receptors in the brain. Schizophrenia is thought to result from an excess of dopaminergic D2 and serotonergic 5-HT2A activity, resulting in overactivity of central mesolimbic pathways and mesocortical pathways, respectively.

D2 dopaminergic receptors are transiently inhibited by risperidone, reducing dopaminergic neurotransmission, therefore decreasing positive symptoms of schizophrenia, such as delusions and hallucinations. Risperdal Consta(j&j) binds transiently and with loose affinity to the dopaminergic D2 receptor, with an ideal receptor occupancy of 60-70% for optimal effect. Rapid dissociation of risperidone from the D2 receptors contributes to decreased risk of extrapyramidal symptoms (EPS), which occur with permanent and high occupancy blockade of D2 dopaminergic receptors. Low-affinity binding and rapid dissociation from the D2 receptor distinguish risperidone from the traditional antipsychotic drugs. A higher occupancy rate of D2 receptors is said to increase the risk of extrapyramidal symptoms and is therefore to be avoided.

Increased serotonergic mesocortical activity in schizophrenia results in negative symptoms, such as depression and decreased motivation. The high-affinity binding of risperidone to 5-HT2A receptors leads to a decrease in serotonergic activity. In addition, 5-HT2A receptor blockade results in decreased risk of extrapyramidal symptoms, likely by increasing dopamine release from the frontal cortex, and not the nigrostriatal tract. Dopamine level is therefore not completely inhibited. Through the above mechanisms, both serotonergic and D2 blockade by risperidone are thought to synergistically work to decrease the risk of extrapyramidal symptoms.

Risperdal Consta(j&j) has also been said to be an antagonist of alpha-1 (α1), alpha-2 (α2), and histamine (H1) receptors.[L1212] Blockade of these receptors is thought to improve symptoms of schizophrenia, however the exact mechanism of action on these receptors is not fully understood at this time.

Dosage

Risperdal Consta(j&j) dosage

Psychoses: 2 mg in 1-2 divided doses on 1st day then 4 mg in 1-2 divided doses on second day (Slower titration appropriate in some patients); usual dose range 4-6 mg daily; doses above 10 mg daily only if benefit considered to outweigh risk (max. 16 mg daily). Elderly (or in hepatic or renal impairment) initially 1 mg daily in two divided doses increased in steps of 1-2 mg twice daily. Child under 15 years not recommended.

Mania:Initially 2 mg once daily increased if necessary in step of 1 mg daily; usual dose range 1-6 mg daily; Elderly (or in hepatic or renal impairment) initially 1 mg daily in two divided doses increased in steps of 1-2 mg twice daily.

Schizophrenia: Risperdal Consta(j&j) should be generally administered at 1 mg BID initially, with increases in increments of 1 mg BID on the second and third day, as tolerated, to a target dose of 3 mg BID by the third day. Further dosage adjustments, if indicated, should generally occur at intervals of not less than 1 week. When dosage adjustments are necessary, small dose increments or decrements of 1-2 mg are recommended.

Side Effects

Insomnia, agitation, anxiety, headache, less commonly drowsiness, impaired concentration, fatigue, blurred vision, constipation, nausea and vomiting, dyspepsia, abdominal pain, hyperprolactinaemia, urine incontinence, tachycardia, hypertension, edema, rash, rhinitis, cerebrovascular accident, neurtropenia and thrombocytopenia have been reported.

Toxicity

Symptoms of overdose include lethargy, dystonia/spasm, tachycardia, bradycardia, and seizures. LD₅₀=57.7 mg/kg (rat, oral) and 34 mg/kg (rat, intravenous).

Precaution

Special precaution should be taken in case of preexisting cardiovascular diseases, discontinue use if signs and symptoms of tardive dyskinesia occur, renal and hepatic impairment, elderly epilepsy, Parkinson's disease and in pregnancy.

Interaction

Risperdal Consta(j&j) May antagonize the effects of levodopa and dopamine agonists. Chronic administration with Carbamazepine reduces plasma clearance of Risperdal Consta(j&j). Chronic administration with Clozapine may decrease the clearance of Risperdal Consta(j&j). Risperdal Consta(j&j) may enhance the effects of certain antihypertensives.

Food Interaction

• Take with or without food. Food does not affect the rate or extent of absorption.

[Moderate] GENERALLY AVOID: Risperdal Consta(j&j) oral solution is not compatible with either tea or cola.

In addition, alcohol may potentiate some of the pharmacologic effects of risperidone.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Risperdal Consta(j&j) oral solution should not be mixed with tea or cola.

It may be taken with water, coffee, orange juice, or lowfat milk.

Patients should also be advised to avoid consumption of alcohol.

Risperdal Consta(j&j) Cholesterol interaction

[Moderate] Atypical antipsychotic drugs have been associated with undesirable alterations in lipid levels.

While all agents in the class have been shown to produce some changes, each drug has its own specific risk profile.

Before or soon after initiation of antipsychotic medication, obtain a fasting lipid profile at baseline and monitor periodically during treatment.

Risperdal Consta(j&j) Drug Interaction

Major: escitalopramModerate: aripiprazole, lorazepam, duloxetine, divalproex sodium, clonazepam, lamotrigine, lithium, pregabalin, polyethylene glycol 3350, fluoxetine, quetiapine, lisdexamfetamine, alprazolam, sertralineUnknown: amphetamine / dextroamphetamine, omega-3 polyunsaturated fatty acids, acetaminophen, cyanocobalamin, cholecalciferol

Risperdal Consta(j&j) Disease Interaction

Major: dementia, acute alcohol intoxication, CNS depression, NMS, tardive dyskinesia, liver disease, QT interval prolongation, renal dysfunctionModerate: depression, aspiration, seizure, hematologic abnormalities, hyperglycemia/diabetes, hypotension, lipid alterations, priapism, renal impairment, weight gain, hyperprolactinemia, parkinsonism

Volume of Distribution

The volume of distribution of risperidone is approximately 1 to 2 L/kg.

Elimination Route

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.

Half Life

3 hours in extensive metabolizers Up to 20 hours in poor metabolizers

Clearance

Risperdal Consta(j&j) is cleared by the kidneys. Clearance is decreased in the elderly and those with a creatinine clearance (ClCr) between 15-59 mL/min, in whom clearance is decreased by approximately 60%.

Elimination Route

Risperdal Consta(j&j) is extensively metabolized in the liver. In healthy elderly subjects, renal clearance of both risperidone and 9-hydroxyrisperidone was decreased, and elimination half-lives are prolonged compared to young healthy subjects.

Pregnancy & Breastfeeding use

Pregnancy: Although, in experimental animals, Risperdal Consta(j&j) did not show direct reproductive toxicity, some indirect, prolactin- and CNS-mediated effects were observed, No teratogenicity effect of Risperdal Consta(j&j) was noted in any study. The safety of Risperdal Consta(j&j) for use during human pregnancy has not been established.

Lactation: In animal studies, Risperdal Consta(j&j) and 9-hydroxyrisperidone are excreted in the milk. It has been demonstrated that Risperdal Consta(j&j) and 9-hydroxyrisperidone are also excreted in human breast milk. Therefore, women receiving Risperdal Consta(j&j) should not breast feed.

Contraindication

Risperdal Consta(j&j) is contraindicated in patients with a known hypersensitivity to the product.

Acute Overdose

Drowsiness, sedation, tachycardia, hypotension, and extrapyramidal symptoms may occur. In case of severe extrapyramidal symptoms, anticholinergic medication should be administered. Close medical supervision and monitoring should continue until the patient recovers. There is no specific antidote to Risperdal Consta(j&j).

Storage Condition

Store in a cool and dry place, protected from light.

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