Paliperidone Injection

Unless your doctor tells you otherwise, continue your normal diet.

Call your doctor for instructions if you miss an appointment for your paliperidone injection.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include a headache with chest pain, fast or pounding heartbeats, and severe dizziness.

Usual Adult Dose for Schizophrenia:

EXTENDED-RELEASE TABLETS:
-Recommended dose: 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

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:
-Recommended dose: 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

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 per 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

Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective. Ask your doctor before using any new medications during the month(s) between your doses of paliperidone.

Many drugs can interact with paliperidone. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide. Tell your doctor about all your current medicines and any medicine you start or stop using.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of high blood sugar like confusion, feeling sleepy, more thirst, more hungry, passing urine more often, flushing, fast breathing, or breath that smells like fruit.
• Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight.
• If you are planning to harm yourself or the want to harm yourself gets worse.
• Chest pain or pressure.
• Very bad dizziness or passing out.
• Change in how you act.
• Mood changes.
• Shakiness, trouble moving around, or stiffness.
• Slow heartbeat.
• Trouble swallowing or speaking.
• Not able to focus.
• Seizures.
• Change in eyesight.
• Shortness of breath.
• Drooling.
• Any unexplained bruising or bleeding.
• Not able to control eye movements.
• Enlarged breasts.
• Change in sex ability.
• Nipple discharge.
• For women, no period.
• Call your doctor right away if you have a painful erection (hard penis) or an erection that lasts for longer than 4 hours. This may happen even when you are not having sex. If this is not treated right away, it may lead to lasting sex problems and you may not be able to have sex.
• A very bad and sometimes deadly health problem called neuroleptic malignant syndrome (NMS) may happen. Call your doctor right away if you have any fever, muscle cramps or stiffness, dizziness, very bad headache, confusion, change in thinking, fast heartbeat, heartbeat that does not feel normal, or are sweating a lot.
• Very bad irritation where the shot was given.

• If you need to store this medicine at home, talk with your doctor, nurse, or pharmacist about how to store it.

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else's drugs.
• Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
• Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Check with your pharmacist about how to throw out unused drugs.
• Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about paliperidone injection, please talk with your doctor, nurse, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about paliperidone injection. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using paliperidone injection.

Review Date: October 4, 2017