Paliperidone

By

Generic Name: Paliperidone Brand Name(s): Generics only. No brands available.

Uses

What is Paliperidone used for?

Paliperidone is used to treat certain mental/mood disorders (such as schizophrenia, schizoaffective disorder). This medication can decrease hallucinations and help you to think more clearly and positively about yourself, feel less agitated, and take a more active part in everyday life.

Paliperidone belongs to a class of drugs called atypical antipsychotics. It works by helping to restore the balance of certain natural substances in the brain.

How should I take Paliperidone?

Take this medication by mouth with or without food as directed by your doctor, usually once daily. Swallow the tablets whole with liquid. Do not crush or chew the tablets. Doing so can release all of the drug at once, increasing the risk of side effects.

The dosage is based on your age, medical condition, and response to treatment.

Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day. It is important to continue taking this medication as prescribed even if you feel well. Do not stop taking this medication without consulting your doctor.

Tell your doctor if your condition persists or worsens.

How do I store Paliperidone?

Paliperidone is best stored at room temperature away from direct light and moisture. To prevent drug damage, you should not store Paliperidone in the bathroom or the freezer. There may be different brands of Paliperidone that may have different storage needs. It is important to always check the product package for instructions on storage, or ask your pharmacist. For safety, you should keep all medicines away from children and pets.

You should not flush Paliperidone down the toilet or pour them into a drain unless instructed to do so. It is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.

Precautions & warnings

What should I know before using Paliperidone?

Before taking paliperidone, tell your doctor or pharmacist if you are allergic to it; or to risperidone; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease, seizures, low white blood cell count, Parkinson’s disease, dementia, esophagus/stomach/intestinal movement or blockage disorders (such as difficulty swallowing, peritonitis, cystic fibrosis, Meckel’s diverticulum), certain eye problems (cataracts, glaucoma), personal or family history of diabetes, high cholesterol/triglyceride levels, heart disease, breathing trouble during sleep (sleep apnea).

Paliperidone may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.

The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using paliperidone, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/”water pills”) or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using paliperidone safely.

This drug may make you dizzy or drowsy. Alcohol or marijuana can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana.

Before having surgery (including cataract/glaucoma eye surgery), tell your doctor or dentist if you are taking or have ever taken this medication, and about all the other products you use (including prescription drugs, nonprescription drugs, and herbal products).

This medication may make you sweat less, making you more likely to get heat stroke. Avoid doing things that may cause you to overheat, such as hard work or exercise in hot weather, or using hot tubs. When the weather is hot, drink a lot of fluids and dress lightly. If you overheat, quickly look for a place to cool down and rest. Get medical help right away if you have a fever that does not go away, mental/mood changes, headache, or dizziness.

Older adults may be more sensitive to the side effects of this drug, especially drowsiness, dizziness, lightheadedness, and QT prolongation (see above). Drowsiness, dizziness, and lightheadedness can increase the risk of falling.

During pregnancy, this medication should be used only when clearly needed. Babies born to mothers who have used this drug during the last 3 months of pregnancy may rarely develop symptoms including muscle stiffness or shakiness, drowsiness, feeding/breathing difficulties, or constant crying. If you notice any of these symptoms in your newborn especially during their first month, tell the doctor right away.

Since untreated mental/mood problems (such as schizophrenia, schizoaffective disorders, depression) can be a serious condition, do not stop taking this medication unless directed by your doctor. If you are planning pregnancy, become pregnant, or think you may be pregnant, immediately discuss with your doctor the benefits and risks of using this medication during pregnancy.

This medication passes into breast milk and may have undesirable effects on a nursing infant. Consult your doctor before breast-feeding.

Is it safe during pregnancy or breast-feeding?

There are no adequate studies in women for determining risk when using this Paliperidone during pregnancy or while breastfeeding. Please always consult with your doctor to weigh the potential benefits and risks before taking Paliperidone. Paliperidone is pregnancy risk category N according to the US Food and Drug Administration (FDA).

FDA pregnancy risk category reference below:

  • A=No risk,
  • B=No risk in some studies,
  • C=There may be some risk,
  • D=Positive evidence of risk,
  • X=Contraindicated,
  • N=Unknown

Side effects

What side effects can occur from Paliperidone?

Drowsiness, dizziness, lightheadedness, drooling, stomach/abdominal pain, weight gain, or tiredness may occur. If any of these side effects persist or worsen, tell your doctor promptly.

Dizziness and lightheadedness can increase the risk of falling. Get up slowly when rising from a sitting or lying position.

An empty tablet shell may appear in your stool. This effect is harmless because your body has already absorbed the medication.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: difficulty swallowing, muscle spasms, shaking (tremor), mental/mood changes (such as restlessness), signs of infection (such as fever, persistent sore throat), interrupted breathing during sleep.

This drug may rarely make your blood sugar rise, which can cause or worsen diabetes. Tell your doctor right away if you have symptoms of high blood sugar such as increased thirst/urination. If you already have diabetes, check your blood sugar regularly as directed and share the results with your doctor. Your doctor may need to adjust your diabetes medication, exercise program, or diet.

This drug may also cause significant weight gain and a rise in your blood cholesterol (or triglyceride) levels. These effects, along with diabetes, may increase your risk for developing heart disease. Discuss the risks and benefits of treatment with your doctor.

Paliperidone may rarely cause a condition known as tardive dyskinesia. In some cases, this condition may be permanent. Tell your doctor right away if you develop any unusual/uncontrolled movements (especially of the face, lips, mouth, tongue, arms, or legs).

This medication may increase a certain natural substance (prolactin) made by your body. For females, this increase in prolactin may result in unwanted breast milk, missed/stopped periods, or difficulty becoming pregnant. For males, it may result in decreased sexual ability, inability to produce sperm, or enlarged breasts. If you develop any of these symptoms, tell your doctor right away.

Get medical help right away if you have any very serious side effects, including: severe dizziness, fainting, seizures.

This medication may rarely cause a very serious condition called neuroleptic malignant syndrome (NMS). Get medical help right away if you have any of the following symptoms: fever, muscle stiffness/pain/tenderness/weakness, severe tiredness, severe confusion, sweating, fast/irregular heartbeat, dark urine, signs of kidney problems (such as change in the amount of urine).

Rarely, males may have a painful or prolonged erection lasting 4 or more hours. If this occurs, stop using this drug and get medical help right away, or permanent problems could occur.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Not everyone experiences these side effects. There may be some side effects not listed above. If you have any concerns about a side-effect, please consult your doctor or pharmacist.

Interactions

What drugs may interact with Paliperidone?

A product that may interact with this drug is: metoclopramide.

Many drugs besides paliperidone may affect the heart rhythm (QT prolongation), including amiodarone, chlorpromazine, moxifloxacin, quinidine, sotalol, procainamide, thioridazine, among others.

Tell your doctor or pharmacist if you are taking other products that cause drowsiness such as opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana, drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), muscle relaxants (such as carisoprodol, cyclobenzaprine), or antihistamines (such as cetirizine, diphenhydramine).

Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.

Paliperidone may interact with other drugs that you are currently taking, which can change how your drug works or increase your risk for serious side effects. To avoid any potential drug interactions, you should keep a list of all the drugs you are using (including prescription drugs, nonprescription drugs and herbal products) and share it with your doctor and pharmacist. For your safety, do not start, stop, or change the dosage of any drugs without your doctor’s approval.

Does food or alcohol interact with Paliperidone?

Paliperidone may interact with food or alcohol by altering the way the drug works or increase the risk for serious side effects. Please discuss with your doctor or pharmacist any potential food or alcohol interactions before using this drug.

What health conditions may interact with Paliperidone?

Paliperidone may interact with your health condition. This interaction may worsen your health condition or alter the way the drug works. It is important to always let your doctor and pharmacist know all the health conditions you currently have.

Dosage

The information provided is not a substitute for any medical advice. You should ALWAYS consult with your doctor or pharmacist before using this Paliperidone.

What is the dose of Paliperidone for an adult?

Usual Adult Dose for Schizophrenia

EXTENDED-RELEASE TABLETS:

6 mg orally once a day

-Dose range: 3 to 12 mg per day; dose increases may be made in increments of 3 mg per day and should occur at intervals of more than 5 days.

-Maximum dose: 12 mg/day

Comments:

-Initial dose titration is not required.

-Greater effects may be seen with higher doses, however this must be weighed against dose-related increases in adverse events.

-Doses above 6 mg per day have not been systematically studied for additional benefit.

-Efficacy was established with 3 trials using patients with schizophrenia for 6-weeks; efficacy in maintenance therapy was established with one adult trial.

1-MONTH EXTENDED-RELEASE INJECTABLE SUSPENSION:

-For patients who have never taken oral paliperidone or oral or injectable risperidone, tolerability should be established with oral paliperidone or oral risperidone prior to initiating treatment with paliperidone extended-release injectable suspension.

-Dosing in the US and Canada is the same; however, paliperidone extended-release injectable suspension is dosed as the salt (paliperidone palmitate) in the US and as the base (paliperidone) in Canada:

Paliperidone palmitate:

-Initial dose: 234 mg IM on day 1 followed by 156 mg IM one week later; administer IM into deltoid muscle

-Maintenance dose: 117 mg IM monthly; administer into deltoid or gluteal muscle

-Dose range: 39 to 234 mg based on patient tolerability and efficacy; dose adjustments may be made monthly, although full effect may not be evident for several months

-Maximum dose: 234 mg/month

Paliperidone (base):

-Initial dose: 150 mg IM on day 1 followed by 100 mg IM one week later; administer IM into deltoid muscle

-Maintenance dose: 75 mg IM monthly; administer into deltoid or gluteal muscle

-Dose range: 25 to 150 mg based on patient tolerability and efficacy; dose adjustments may be made monthly, although full effect may not be evident for several months

Comments:

-The dosing window for maintenance doses is 7 days before or after monthly time point.

-If a dose is missed during initial titration or maintenance dosing, see dosage adjustment section for guidance.

3-MONTH EXTENDED-RELEASE INJECTABLE SUSPENSION:

-Patients should be adequately treated for at least 4 months with the 1-month extended-release suspension prior to starting on the 3-month extended-release formulation.

-In order to establish a consistent maintenance dose, it is recommended that the last 2 doses of the 1-month extended-release suspension be of the same dosage strength.

-Initiate with the 3-month extended release injection when the next 1-month extended-release suspension dose is scheduled (up to 7-days before or after the monthly dose is scheduled).

Initial dose (based on the 1-month extended-release suspension dose):

-Initiate with 273 mg IM every 3 months if the last dose of the 1-month extended-release suspension was 78 mg

-Initiate with 410 mg IM every 3 months if the last dose of the 1-month extended-release suspension was 117 mg

-Initiate with 546 mg IM every 3 months if the last dose of the 1-month extended-release suspension was 156 mg

-Initiate with 819 mg IM every 3 months if the last dose of the 1-month extended-release suspension was 234 mg

Dose adjustments may be made every 3 months in increments within the range of 273 mg to 819 mg based on efficacy and tolerability; due to long-acting nature of the formulation, it may take several months for the patient’s response to be apparent.

Comments:

-The initial dose will be 3.5-fold higher than monthly dose.

-The dosing window is 2 weeks before or after the 3-month time point.

-Missed doses should be avoided. If a dose is missed, see dosage adjustment section for guidance.

-Conversion from 39 mg IM once-monthly was not studied.

-If the needle becomes clogged during administration, the remaining dose should not be re-injected. Instead, the patient should be monitored and treated with oral supplementation until the next scheduled 3-month injection.

Use: For the treatment of schizophrenia

Usual Adult Dose for Schizoaffective Disorder

EXTENDED RELEASE TABLETS:

6 mg orally once a day

-Dose range: 3 to 12 mg per day; dose increases may be made in increments of 3 mg per day and should occur at intervals of more than 4 days.

-Maximum dose: 12 mg/day

Comments:

-Initial dose titration is not required.

-Greater effects may be seen with higher doses; however, this must be weighed against dose-related increases in adverse events.

-Doses above 6 mg per day have not been systematically studied for additional benefit.

-Efficacy was established with 2 trials using patients with schizoaffective disorder for 6 weeks.

1-MONTH EXTENDED-RELEASE INJECTABLE SUSPENSION:

-For patients who have never taken oral paliperidone or oral or injectable risperidone, tolerability should be established with oral paliperidone or oral risperidone prior to initiating treatment with paliperidone extended-release injectable suspension.

-Dosing in the US and Canada is the same; however, paliperidone extended-release injectable suspension is dosed as the salt (paliperidone palmitate) in the US and as the base (paliperidone) in Canada:

Paliperidone palmitate:

-Initial dose: 234 mg IM on day 1 followed by 156 mg IM one week later; administer IM into deltoid muscle

-Dose range: 78 to 234 mg based on patient tolerability and efficacy; dose adjustments may be made monthly, although full effect may not be evident for several months

-Maximum dose: 234 mg/month

Paliperidone (base):

-Initial dose: 150 mg IM on day 1 followed by 100 mg IM one week later; administer IM into deltoid muscle

-Dose range: 50 to 150 mg based on patient tolerability and efficacy; dose adjustments may be made monthly, although full effect may not be evident for several months

Comments:

-The dosing window for maintenance doses is 7 days before or after monthly time point.

-If a dose is missed during initial titration or maintenance dosing, see dosage adjustment section for guidance.

Use: Treatment of schizoaffective disorder as monotherapy and as an adjunct to mood stabilizers and/or antidepressants

Renal Dose Adjustments

EXTENDED-RELEASE TABLETS:

Mild renal dysfunction (CrCl 50 mL/min to less than 80 mL/min): Initial dose: 3 mg orally once a day; may increase to a maximum of 6 mg orally once a day based on efficacy and tolerability.

Moderate to severe renal dysfunction (CrCl 10 mL/min to less than 50 mL/min): Initial dose: 1.5 mg orally once a day; may increase to a maximum of 3 mg orally once a day based on efficacy and tolerability.

CrCl less than 10 mL/min: Use not recommended

1-MONTH EXTENDED-RELEASE IM SUSPENSION:

Paliperidone palmitate:

Mild renal dysfunction (CrCl 50 to less than 80 mL/min):

-Initial dose: 156 mg IM on day 1 followed by 117 mg IM one week later; administer IM into deltoid muscle

-Maintenance dose: 78 mg IM monthly; administer IM into deltoid or gluteal muscle

Moderate to severe renal dysfunction (CrCl less than 50 mL/min): Use not recommended

Paliperidone base:

Mild renal dysfunction (CrCl 50 to less than 80 mL/min:

-Initial dose: 100 mg IM on day 1 followed by 75 mg IM one week later; administer IM into deltoid muscle

-Maintenance dose: 50 mg IM monthly, adjusted within the range of 25 to 100 mg based on individual efficacy and tolerability; administer IM into deltoid or gluteal muscle

Moderate to severe renal dysfunction (CrCl less than 50 mL/min): Use not recommended

3-MONTH EXTENDED-RELEASE IM SUSPENSION:

Mild renal dysfunction (CrCl 50 to less than 80 mL/min): Adjust dosage and stabilize patient using the 1-month extended-release suspension and then transition to 3-month suspension.

Moderate to severe renal dysfunction (CrCl less than 50 mL/min): Use not recommended

Liver Dose Adjustments

Mild to moderate hepatic impairment (Child-Pugh Class A and B): No dosage adjustments required

Severe hepatic impairment: Data not available

Dose Adjustments

Concomitant Administration with Strong CYP450 3A4/P-glycoprotein (P-gp) Inducers:

EXTENDED RELEASE TABLETS: May be necessary to increase the dose of paliperidone when coadministered with a strong inducer of both CYP450 3A4 and P-gp (e.g., carbamazepine, rifampin, St John’s wort).

1-MONTH EXTENDED RELEASE IM SUSPENSION: Avoid use of strong CYP450 3A4/P-gp inducers and/or consider switching to oral extended-release tablets.

Paliperidone base and 3-MONTH EXTENDED-RELEASE IM SUSPENSION: When switching patients currently at steady-state on a long acting antipsychotic injection; initiate paliperidone extended-release injection at next scheduled injection; the 1-week initiation dosing regimen will not be necessary.

MISSED DOSES: 1-MONTH Extended-Release Suspension:

-Dosing window: Patients may receive second dose 4 days before or after the 1-week time point; third and subsequent doses may be given up to 7 days before or after monthly time point.

Missed INITIATION Doses:

-If second initiation dose is missed and it is less than 4 weeks since first injection: Administer 156 mg paliperidone palmitate OR 100 mg paliperidone base IM into deltoid muscle as soon as possible; maintenance dose should begin 5 weeks after the first injection.

-If second initiation dose is missed and it is 4 to 7 weeks from first injection: Administer 2 injections (156 mg paliperidone palmitate OR 100 mg paliperidone base), with the first as soon as possible and the second 1 week later, both IM into deltoid muscle, then resume normal monthly cycle.

-If second initiation dose is missed and it is more than 7 weeks from the first injection: Re-initiate initial dosing schedule.

Missed MAINTENANCE Doses:

-If less than 6 weeks have elapsed since last maintenance dose: Administer as soon as possible followed by injections at monthly intervals.

-If greater than 6 weeks but less than 6 months have elapsed since last monthly maintenance dose, and dose was less than 234 mg paliperidone palmitate OR 150 mg paliperidone base: Administer maintenance dose IM into deltoid muscle as soon as possible and repeat same dose IM into deltoid muscle 1 week later; then resume monthly dosing.

-If greater than 6 weeks but less than 6 months have elapsed since monthly maintenance dose of 234 mg paliperidone palmitate OR 150 mg paliperidone base: Administer 156 mg paliperidone palmitate OR 100 mg paliperidone base IM into deltoid muscle as soon as possible followed by the same dose IM into deltoid muscle one week later; then resume normal monthly cycle.

-If more than 6 months have elapsed since last maintenance injection: Re-initiate initial dosing schedule.

MISSED DOSES: 3-MONTH Extended-Release Suspension:

Dosing window: Up to 2 weeks before or after 3-month time point.

-If more than 3.5 months (up to but less than 4 months) have elapsed: Administer as soon as possible, then continue with the 3-month injections following this dose.

-If 4 months up to and including 9 months have elapsed: Re-initiation using the 1-month extended release suspension is necessary as follows:

—If the last dose of the 3-month suspension was 273 mg, give the 1-month extended release suspension at 78 mg IM into the deltoid muscle on Day 1 and Day 8, then 1 month after Day 8, resume 3-month extended-release suspension with 273 mg IM into deltoid or gluteal muscle

—If the last dose of the 3-month suspension was 410 mg, give the 1-month extended release suspension at 117 mg IM into the deltoid muscle on Day 1 and Day 8, then 1 month after Day 8, resume 3-month extended-release suspension with 410 mg IM into deltoid or gluteal muscle

—If the last dose of the 3-month suspension was 546 mg, give the 1-month extended release suspension at 156 mg IM into the deltoid muscle on Day 1 and Day 8, then 1 month after Day 8, resume 3-month extended-release suspension with 546 mg IM into deltoid or gluteal muscle

—If the last dose of the 3-month suspension was 819 mg, give the 1-month extended release suspension at 156 mg IM into the deltoid muscle on Day 1 and Day 8, then 1 month after Day 8, resume 3-month extended-release suspension with 819 mg IM into deltoid or gluteal muscle

-If more than 9 months have elapsed since last injection of the 3-month extended release suspension: Re-initiate with the 1-month extended release suspension; the 3-month extended-release suspension can be resumed after the patient has been adequately treated with the 1-month extended-release suspension for at least 4 months.

SWITCHING From 3-Month Extended-Release IM Suspension TO 1-Month Extended-Release IM Suspension:

-If the last dose of the 3-month extended-release suspension was 273 mg, after 3 months, switch to the 1-month extended-release suspension at 78 mg IM once a month

-If the last dose of the 3-month extended-release suspension was 410 mg, after 3 months, switch to the 1-month extended-release suspension at 117 mg IM once a month

-If the last dose of the 3-month extended-release suspension was 546 mg, after 3 months, switch to the 1-month extended-release suspension at 156 mg IM once a month

-If the last dose of the 3-month extended-release suspension was 819 mg, after 3 months, switch to the 1-month extended-release suspension at 234 mg IM once a month

SWITCHING From 3-Month Extended-Release IM Suspension TO Oral Paliperidone Extended-Release Tablets:

-If the last dose of the 3-month extended-release IM suspension was 273 mg, after 3 months start extended-release tablets at 3 mg orally once a day.

-If the last dose of the 3-month extended-release IM suspension was 410 mg, after 3 months start extended-release tablets at 3 mg orally once a day; at 24-weeks from last IM dose, increase oral dose to 6 mg once a day.

-If the last dose of the 3-month extended-release suspension was 546 mg, after 3 months start extended-release tablets at 3 mg orally once a day, at 18 weeks from last IM dose, increase oral dose to 6 mg orally once a day, at 24 weeks from last IM dose, increase oral dose to 9 mg orally once a day.

-If the last dose of the 3-month extended-release suspension was 819 mg, after 3 months start extended-release tablets at 6 mg orally once a day, at 18 weeks from last IM dose, increase oral dose to 9 mg orally once a day, at 24 weeks from last IM dose, increase oral dose to 12 mg orally once a day.

What is the dose of Paliperidone for a child?

Usual Pediatric Dose for Schizophrenia

EXTENDED-RELEASE TABLETS:

12 to 17 years old:

-Initial dose: 3 mg orally once a day

-Dose range: 3 to 12 mg per day; dose increases may be made in increments of 3 mg per day and should occur at intervals of more than 5 days.

-Maximum dose: 12 mg/day

Comments:

-Initial dose titration is not required.

-In the adolescent schizophrenia trials, higher doses (6 mg per day in patients weighing less than 51 kg; 12 mg per day in patients weighing 51 kg or more) did not demonstrate greater efficacy, while adverse events were dose-related.

-Efficacy was established with a 6-week trial in adolescent patients with schizophrenia.

Use: Treatment of schizophrenia

Precautions

Safety and efficacy of the long-acting injection in patients younger than 18 years have not been established.

Safety and efficacy of paliperidone in patients younger than 12 years in the treatment of schizophrenia have not been established.

Safety and efficacy of paliperidone in patients younger than 18 years in the treatment of schizoaffective disorder have not been established.

How is Paliperidone available?

Paliperidone is available in the following dosage forms and strengths:

  • Oral tablet, extended release.

What should I do in case of an emergency or overdose?

In case of an emergency or an overdose, call your local emergency services or go to your nearest emergency room.

What should I do if I miss a dose?

If you miss a dose of Paliperidone, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and take your regular dose as scheduled. Do not take a double dose.

Hello Health Group does not provide medical advice, diagnosis or treatment.

Review Date: April 11, 2018 | Last Modified: April 11, 2018

Sources
You might also like