Paliperidone
Loading...Paliperidone Recall
Get an alert when a recall is issued.
Questions & Answers
Side Effects & Adverse Reactions
There is currently no warning information available for this product. We apologize for any inconvenience.
Legal Issues
There is currently no legal information available for this drug.
FDA Safety Alerts
There are currently no FDA safety alerts available for this drug.
Manufacturer Warnings
There is currently no manufacturer warning information available for this drug.
FDA Labeling Changes
There are currently no FDA labeling changes available for this drug.
Uses
1.1 Schizophrenia
Paliperidone Extended-Release Tablets are indicated for the treatment of schizophrenia [see Clinical Studies (14.1)].
The efficacy of Paliperidone Extended-Release Tablets in schizophrenia was established in three 6-week trials in adults and one 6-week trial in adolescents, as well as one maintenance trial in adults.
1.2 Schizoaffective DisorderPaliperidone Extended-Release Tablets are indicated for the treatment of schizoaffective disorder as monotherapy and an adjunct to mood stabilizers and/or antidepressant therapy [see Clinical Studies (14.2)].
The efficacy of Paliperidone Extended-Release Tablets in schizoaffective disorder was established in two 6-week trials in adults.
History
There is currently no drug history available for this drug.
Other Information
Paliperidone, the active ingredient in Paliperidone Extended-Release Tablets, is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives. Paliperidone Extended-Release Tablets contain a racemic mixture of (+)- and (-)- paliperidone. The chemical name is (±)-3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one. Its molecular formula is C23H27FN4O3 and its molecular weight is 426.49. The structural formula is:
Paliperidone is sparingly soluble in 0.1N HCl and methylene chloride; practically insoluble in water, 0.1N NaOH, and hexane; and slightly soluble in N,N-dimethylformamide.
Paliperidone Extended-Release Tablets are available in 1.5 mg (orange-brown), 3 mg (white), 6 mg (beige), and 9 mg (pink) strengths. Paliperidone Extended-Release Tablets utilizes OROS® osmotic drug-release technology [see Description (11.1)].
Inactive ingredients are carnauba wax, cellulose acetate, hydroxyethyl cellulose, propylene glycol, polyethylene glycol, polyethylene oxides, povidone, sodium chloride, stearic acid, butylated hydroxytoluene, hypromellose, titanium dioxide, and iron oxides. The 3 mg tablets also contain lactose monohydrate and triacetin.
11.1 Delivery System Components and PerformancePaliperidone Extended-Release Tablets use osmotic pressure to deliver paliperidone at a controlled rate. The delivery system, which resembles a capsule-shaped tablet in appearance, consists of an osmotically active trilayer core surrounded by a subcoat and semipermeable membrane. The trilayer core is composed of two drug layers containing the drug and excipients, and a push layer containing osmotically active components. There are two precision laser-drilled orifices on the drug-layer dome of the tablet. Each tablet strength has a different colored water-dispersible overcoat and print markings. In an aqueous environment, such as the gastrointestinal tract, the water-dispersible color overcoat erodes quickly. Water then enters the tablet through the semipermeable membrane that controls the rate at which water enters the tablet core, which, in turn, determines the rate of drug delivery. The hydrophilic polymers of the core hydrate and swell, creating a gel containing paliperidone that is then pushed out through the tablet orifices. The biologically inert components of the tablet remain intact during gastrointestinal transit and are eliminated in the stool as a tablet shell, along with insoluble core components.
Sources
Paliperidone Manufacturers
-
Patriot Pharmaceuticals, Llc
![Paliperidone Tablet, Extended Release [Patriot Pharmaceuticals, Llc]](/wp-content/themes/bootstrap/assets/img/loading2.gif)
Paliperidone | Patriot Pharmaceuticals, Llc
2.1 SchizophreniaAdults
The recommended dose of Paliperidone Extended-Release Tablets for the treatment of schizophrenia in adults is 6 mg administered once daily. Initial dose titration is not required. Although it has not been systematically established that doses above 6 mg have additional benefit, there was a general trend for greater effects with higher doses. This must be weighed against the dose-related increase in adverse reactions. Thus, some patients may benefit from higher doses, up to 12 mg/day, and for some patients, a lower dose of 3 mg/day may be sufficient. Dose increases above 6 mg/day should be made only after clinical reassessment and generally should occur at intervals of more than 5 days. When dose increases are indicated, increments of 3 mg/day are recommended. The maximum recommended dose is 12 mg/day.
In a longer-term study, Paliperidone Extended-Release Tablets have been shown to be effective in delaying time to relapse in patients with schizophrenia who were stabilized on Paliperidone Extended-Release Tablets for 6 weeks [see Clinical Studies (14)]. Paliperidone Extended-Release Tablets should be prescribed at the lowest effective dose for maintaining clinical stability and the physician should periodically reevaluate the long-term usefulness of the drug in individual patients.
Adolescents (12–17 years of age)
The recommended starting dose of Paliperidone Extended-Release Tablets for the treatment of schizophrenia in adolescents 12–17 years of age is 3 mg administered once daily. Initial dose titration is not required. Dose increases, if considered necessary, should be made only after clinical reassessment and should occur at increments of 3 mg/day at intervals of more than 5 days. Prescribers should be mindful that, in the adolescent schizophrenia study, there was no clear enhancement to efficacy at the higher doses, i.e., 6 mg for subjects weighing less than 51 kg and 12 mg for subjects weighing 51 kg or greater, while adverse events were dose-related.
2.2 Schizoaffective DisorderThe recommended dose of Paliperidone Extended-Release Tablets for the treatment of schizoaffective disorder in adults is 6 mg administered once daily. Initial dose titration is not required. Some patients may benefit from lower or higher doses within the recommended dose range of 3 to 12 mg once daily. A general trend for greater effects was seen with higher doses. This trend must be weighed against dose-related increase in adverse reactions. Dosage adjustment, if indicated, should occur only after clinical reassessment. Dose increases, if indicated, generally should occur at intervals of more than 4 days. When dose increases are indicated, increments of 3 mg/day are recommended. The maximum recommended dose is 12 mg/day.
2.3 Administration InstructionsPaliperidone Extended-Release Tablets can be taken with or without food.
Paliperidone Extended-Release Tablets must be swallowed whole with the aid of liquids. Tablets should not be chewed, divided, or crushed. The medication is contained within a nonabsorbable shell designed to release the drug at a controlled rate. The tablet shell, along with insoluble core components, is eliminated from the body; patients should not be concerned if they occasionally notice in their stool something that looks like a tablet.
2.4 Use with RisperidoneConcomitant use of Paliperidone Extended-Release Tablets with risperidone has not been studied. Since paliperidone is the major active metabolite of risperidone, consideration should be given to the additive paliperidone exposure if risperidone is coadministered with Paliperidone Extended-Release Tablets.
2.5 Dosage in Special PopulationsRenal Impairment
Dosing must be individualized according to the patient's renal function status. For patients with mild renal impairment (creatinine clearance ≥ 50 mL/min to < 80 mL/min), the recommended initial dose of Paliperidone Extended-Release Tablets is 3 mg once daily. The dose may then be increased to a maximum of 6 mg once daily based on clinical response and tolerability. For patients with moderate to severe renal impairment (creatinine clearance ≥ 10 mL/min to < 50 mL/min), the recommended initial dose of Paliperidone Extended-Release Tablets is 1.5 mg once daily, which may be increased to a maximum of 3 mg once daily after clinical reassessment. As Paliperidone Extended-Release Tablets have not been studied in patients with creatinine clearance below 10 mL/min, use is not recommended in such patients. [See Clinical Pharmacology (12.3)]
Hepatic Impairment
For patients with mild to moderate hepatic impairment, (Child-Pugh Classification A and B), no dose adjustment is recommended [see Clinical Pharmacology (12.3)]. Paliperidone Extended-Release Tablets have not been studied in patients with severe hepatic impairment.
Elderly
Because elderly patients may have diminished renal function, dose adjustments may be required according to their renal function status. In general, recommended dosing for elderly patients with normal renal function is the same as for younger adult patients with normal renal function. For patients with moderate to severe renal impairment (creatinine clearance 10 mL/min to < 50 mL/min), the maximum recommended dose of Paliperidone Extended-Release Tablets is 3 mg once daily [see Renal Impairment above].
Login To Your Free Account