Paliperidone
Paliperidone Uses, Dosage, Side Effects, Food Interaction and all others data.
Paliperidone is an atypical antipsychotic developed by Janssen Pharmaceutica. Chemically, paliperidone is primary active metabolite of the older antipsychotic risperidone (paliperidone is 9-hydroxyrisperidone). While its specific mechanism of action is unknown, it is believed paliperidone and risperidone act via similar, if not the same, pathways.
Paliperidone is the major active metabolite of risperidone. The mechanism of action of paliperidone, as with other drugs having efficacy in schizophrenia, is unknown, but it has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism.
Paliperidone is an atypical antipsychotic developed by Janssen Pharmaceutica. Chemically, paliperidone is primary active metabolite of the older antipsychotic risperidone (paliperidone is 9-hydroxyrisperidone). The mechanism of action is unknown but it is likely to act via a similar pathway to risperidone.
| Trade Name | Paliperidone |
| Availability | Prescription only |
| Generic | Paliperidone |
| Paliperidone Other Names | 9-hydroxyrisperidone, Paliperidona, Paliperidone |
| Related Drugs | fluoxetine, quetiapine, lamotrigine, Abilify, Prozac, Seroquel, aripiprazole, olanzapine, risperidone, lithium |
| Weight | 1.5mg, 3mg, 6mg, 9mg, |
| Type | Oral Tablet, Extended Release, Intramuscular, Intramuscular Suspension, Injection |
| Formula | C23H27FN4O3 |
| Weight | Average: 426.4839 Monoisotopic: 426.206718955 |
| Protein binding | The plasma protein binding of racemic paliperidone is 74%. |
| Groups | Approved |
| Therapeutic Class | Atypical neuroleptic drugs |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Schizophrenia: Paliperidone Extended-Release Tablets are used for the treatment of schizophrenia
The efficacy of Paliperidone 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.
Schizoaffective Disorder: Paliperidone Extended-Release Tablets are used for the treatment of schizoaffective disorder as monotherapy and an adjunct to mood stabilizers and/or antidepressant therapy
The efficacy of Paliperidone in schizoaffective disorder was established in two 6-week trials in adults.
Paliperidone is also used to associated treatment for these conditions: Delusional Parasitosis, Schizoaffective Disorders, Schizophrenia
How Paliperidone works
Paliperidone is the major active metabolite of risperidone. The mechanism of action of paliperidone, as with other drugs having efficacy in schizophrenia, is unknown, but it has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism.
Dosage
Paliperidone dosage
Schizophrenia:
- Adults: 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.
- 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.
Schizoaffective Disorder: The 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.
Paliperidone can be taken with or without food. Paliperidone 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.
Side Effects
The following adverse reactions are observed:Increased mortality in elderly patients with dementia-related psychosis, Cerebrovascular adverse reactions, including stroke, in elderly patients with dementia-related psychosis, Neuroleptic malignant syndrome, QT prolongation, Tardive dyskinesia, Metabolic changes, Hyperprolactinemia, Potential for gastrointestinal obstruction, Orthostatic hypotension and syncope, Falls, Leukopenia, neutropenia, and agranulocytosis, Potential for cognitive and motor impairment, Seizures, Dysphagia, Suicide, Priapism, Thrombotic thrombocytopenic purpura (TTP), Disruption of body temperature regulation, Antiemetic effect, Increased sensitivity in patients with Parkinson's disease or those with dementia with Lewy bodies, Diseases or conditions that could affect metabolism or hemodynamic responses
Toxicity
The possibility of obtundation, seizures, or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis.
Food Interaction
- Avoid alcohol.
[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of paliperidone.
Use in combination may result in additive central nervous system depression and In healthy ambulatory subjects, administration of a 12 mg paliperidone extended release tablet with a standard high-fat The clinical significance of these changes is unknown. Since clinical trials establishing the safety and efficacy of paliperidone were carried out without regard to the timing of meals, presumably paliperidone may be administered with or without food.
Administration with food may increase the bioavailability of paliperidone from the extended release tablets.
MANAGEMENT: Patients receiving paliperidone should be advised to avoid the consumption of alcohol.
Paliperidone 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.
Paliperidone Drug Interaction
Major: haloperidol, escitalopram, topiramateModerate: aripiprazole, lorazepam, diphenhydramine, duloxetine, lamotrigine, lurasidone, lithium, pregabalin, brexpiprazole, quetiapine, diazepam, cariprazineUnknown: amphetamine / dextroamphetamine, omega-3 polyunsaturated fatty acids, acetaminophen, cyanocobalamin, cholecalciferol
Paliperidone Disease Interaction
Major: dementia, QT Prolongation, NMS, tardive dyskinesiaModerate: depression, aspiration, seizure, hematologic abnormalities, hyperglycemia/diabetes, hypotension, lipid alterations, priapism, weight gain, hyperprolactinemia, antiemetic effect, gastrointestinal obstruction
Volume of Distribution
- 487 L
Elimination Route
The absolute oral bioavailability of paliperidone following paliperidone administration is 28%.
Half Life
The terminal elimination half-life of paliperidone is approximately 23 hours.
Elimination Route
One week following administration of a single oral dose of 1 mg immediate-release 14C-paliperidone to 5 healthy volunteers, 59% (range 51% – 67%) of the dose was excreted unchanged into urine, 32% (26% – 41%) of the dose was recovered as metabolites, and 6% – 12% of the dose was not recovered.
Pregnancy & Breastfeeding use
Pregnancy Category C. There are no adequate and well controlled studies of Paliperidone in pregnant women.
Use of first generation antipsychotic drugs during the last trimester of pregnancy has been associated with extrapyramidal symptoms in the neonate. These symptoms are usually self- limited. It is not known whether paliperidone, when taken near the end of pregnancy, will lead to similar neonatal signs and symptoms.
Nursing Mothers: Paliperidone is excreted in human breast milk. The known benefits of breastfeeding should be weighed against the unknown risks of infant exposure to paliperidone.
Contraindication
Paliperidone is contraindicated in patients with a known hypersensitivity to either paliperidone or risperidone, or to any of the excipients in the Paliperidone formulation. Hypersensitivity reactions, including anaphylactic reactions and angioedema, have been reported in patients treated with risperidone and in patients treated with paliperidone. Paliperidone is a metabolite of risperidone.
Interaction with other Medicine
Renal Impairment: Dosing must be individualized according to the patient's renal function status
Hepatic Impairment: No dosage adjustment is required in patients with mild to moderate hepatic impairment. Paliperidone has not been studied in patients with severe hepatic impairment.
Elderly: No dosage adjustment is recommended based on age alone. However, dose adjustment may be required because of age-related decreases in creatinine clearance
Storage Condition
Store up to 25°C; excursions permitted to 15 -30°C. Protect from moisture. Keep out of reach of children.
Innovators Monograph
You find simplified version here Paliperidone
Paliperidone contains Paliperidone see full prescribing information from innovator Paliperidone Monograph, Paliperidone MSDS, Paliperidone FDA label
FAQ
What is Paliperidone used for?
Paliperidone is an antipsychotic medicine that is used to treat schizophrenia in adults and teenagers who are at least 12 years old.Paliperidone may also be used for purposes not listed in this medication guide.
How safe is Paliperidone?
Paliperidone is effective and safe in treatment of schizophrenic patients and in switching to PP treatment in patients with schizophrenia, which reduced the percentage of patients admitted to the hospital for relapse and the median number hospitalization, and has positive effects on functionality.
How does Paliperidone work?
Paliperidone work by blocking the receptors for the neurotransmitters dopamine and 5-hydroxytryptamine, which are involved in schizophrenia. By blocking these receptors.Paliperidone helps to normalise the activity of the brain and reduce symptoms.
What are the common side effects of Paliperidone?
Common side effects of Paliperidone are include:
- pain, swelling, redness at injection site
- extreme tiredness
- dizziness, feeling unsteady, or having trouble keeping your balance
- restlessness
- agitation
- headache
- dry mouth
- weight gain
- stomach pain or discomfort
- breast discharge
- missed menstrual period
- breast enlargement in males
- decreased sexual ability
Is Paliperidone safe during pregnancy?
Paliperidone should not be used during pregnancy unless the benefit outweighs the risk to the fetus. No data available on use of Paliperidone in pregnant women to inform a drug-related risk.
Is Paliperidone safe during breastfeeding?
Risperidone data indicate that the concentrations of Paliperidone in breastmilk are low, and amounts ingested by the infant are small. A safety scoring system finds Paliperidone possible to use cautiously during breastfeeding,although others do not recommend it.
Can I drink alcohol with Paliperidone?
You should avoid the use of alcohol while being treated with Paliperidone .Combining alcohol with Paliperidone can increase side effects like dizziness, drowsiness,and trouble concentrating.
Can I drive after taking Paliperidone?
Paliperidone may make you dizzy or drowsy. Alcohol can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely.
When should be taken of Paliperidone?
It is usually taken once a day in the morning with or without food. Take Paliperidone at around the same time every day.
What time of day should I take Paliperidone?
Take Paliperidone once a day at breakfast time. Even if you don't eat breakfast, you should still take paliperidone first thing each morning.
Can Paliperidone be taken at night?
Paliperidone was administered once daily in the morning, but it was allowed in the evening in the case of excessive sedation.
How fast does Paliperidone work?
To begin with, most people find that this medication will help them feel more relaxed and calm. Later, after one or two weeks, other symptoms should begin to improve. Some people may get some side effects before they start to feel any better. Most side effects should go away after a few weeks.
How long should I take Paliperidone?
The Sustenna Paliperidone of long-acting injection Paliperidone is administered twice in the first 8 days of treatment, then every 4 weeks.
How long does Paliperidone stay in my system?
Release of Paliperidone starts as early as one day after the injection and lasts for as long as 126 days.
Does Paliperidone make I tired?
You should know that receiving Paliperidone extended-release injection may make you drowsy and may affect your ability to think clearly, make decisions, and react quickly.
Can Paliperidone cause permanent damage?
Paliperidone may rarely cause a condition known as tardive dyskinesia. In some cases, this condition may be permanent.
Does Paliperidone cause shortness of breath?
Fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness.
How does Paliperidone make me feel?
Paliperidone can make some people feel dizzy, sleepy, or less alert.
Can I overdose on Paliperidone?
Overdose symptoms may include severe drowsiness, fast heartbeats, and fainting. While you are taking Paliperidone, you may be more sensitive to heat. Avoid getting too hot, or becoming overheated or dehydrated.
Does Paliperidone make my gain weight?
Paliperidone caused significant weight gain.
What happens if I miss a dose?
Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.Get your prescription refilled before you run out of medicine completely.
