Paliperidone oral prolonged release
- Drugs List
- Therapeutic Indications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
Oral formulations of paliperidone.
Treatment of schizoaffective disorder with psychotic or manic symptoms
Treatment of schizophrenia
6mg once daily, in the morning.
Initial dose titration is not required.
Dosage should only be adjusted following clinical assessment. When dose increases are indicated, increments of 3mg per day are recommended.
Some patients may require higher doses of up to 12mg once daily or lower doses of 3mg once daily.
Increments in dose change should occur at intervals of more than 5 days.
Some patients may require higher doses of up to 12mg once daily.
Increments in dose change should occur at intervals of more than 4 days.
The recommended starting does is 3mg once daily, in the morning.
Adolescents weighing below 51kg: the maximum recommended daily dose of 6mg. Adolescents weighing 51kg or above: the maximum recommended daily dose of 12mg.
Dosage should only be adjusted following clinical assessment. When dose increases are indicated, increments of 3mg per day are recommended, increments in dose change should occur at intervals of more than 5 days.
Patients with Renal Impairment
Mild renal impairment (creatinine clearance 50 to 80ml/minute)
Reduce initial dose to 3mg once daily. This dose may be increased to 6mg once daily depending on tolerability and clinical response.
Moderate to severe renal impairment (creatinine clearance 10 to 50ml/minute)
An initial dose of 3mg every other day is recommended. The dose may be increased to 3mg once daily after clinical assessment.
Children under 15 years
Neutrophil count below 1.0 x 10 to the power of 9 / L
Long QT syndrome
Renal impairment - creatinine clearance below 10ml/minute
Torsade de pointes
Precautions and Warnings
Children weighing less than 51kg
Family history of long QT syndrome
Patients over 65 years
Predisposition to gastrointestinal obstruction
Predisposition to hypotension
Predisposition to venous thromboembolism
Risk of cerebrovascular accident
Delayed intestinal transit
Glucose-galactose malabsorption syndrome
History of seizures
History of torsade de pointes
Peri-operative period in cataract surgery
Renal impairment - creatinine clearance 10-80ml/minute
Severe hepatic impairment
Correct electrolyte disorders before treatment
May mask nausea and vomiting associated with organic disease
Reduce dose in patients with creatinine clearance below 80ml/min
Advise ability to drive/operate machinery may be affected by side effects
May reduce seizure threshold
Some formulations contain lactose
Consider monitoring ECG in patients at risk of QT prolongation
Monitor blood glucose closely in patients with diabetes mellitus
Monitor patient's weight
Monitor patients at risk for signs & symptoms of venous thromboembolism
Monitor patients with existing or tendency towards diabetes mellitus
Monitor periodically for signs or symptoms of hyperglycaemia
Monitor serum electrolytes
Consider discontinuation if signs of tardive dyskinesia occur
Increased risk for venous thromboembolism - take preventive measures
Intraoperative Floppy Iris Syndrome has been reported in cataract surgery
May cause postural hypotension
May cause weight gain
May impair ability to reduce core body temperature
Potential for withdrawal symptoms
Seek medical advice if priapism does not resolve within 4 hours
Avoid abrupt withdrawal
Discontinue if neutrophil count below 1 x 10 to the power of 9/L
Discontinue if patient develops neuroleptic malignant syndrome
Advise patient that the effects of alcohol may be potentiated
Advise patient to avoid alcohol during treatment
Advise that effects are potentiated by CNS depressants (including alcohol)
Advise patient that tablet matrix will be excreted unchanged in the stools
Evaluate the risks and benefits of therapy when treating patients with Parkinson's disease or dementia with Lewy bodies. (DLB). Patients with these conditions may have an increased risk of developing Neuroleptic Malignant Syndrome and may be more sensitive to antipsychotic medications. Increased sensitivity to paliperidone may include symptoms of confusion, obtundation, postural instability with frequent falls, and extrapyramidal symptoms.
Switching to alternative antipsychotic medications if clinically indicated should be supervised closely by a physician.
Patients with schizoaffective disorder treated with paliperidone should be carefully monitored for a potential switch from manic to depressive symptoms.
Use with caution in patients who may experience an elevation in core body temperature and dehydration.
In elderly patients with dementia, antipsychotic drugs are associated with a small increased risk of mortality and an increased risk of stroke or transient ischaemic attack. Furthermore, elderly patients are particularly susceptible to postural hypotension and to hyper and hypothermia in hot or cold weather. It is recommended that: Antipsychotic drugs should not be used in elderly patients to treat mild to moderate psychotic symptoms. Initial doses of antipsychotic drugs in elderly patients should be reduced (to half the adult dose or less), taking into account factors such as the patient's weight, co-morbidity, and concomitant medication. Treatment should be reviewed regularly.
Pregnancy and Lactation
Use paliperidone with caution in pregnancy.
There is no adequate data from the use of paliperidone during human pregnancy. Paliperidone was not teratogenic in animal studies. However, other types of reproductive toxicity were observed.
The use of antipsychotic medication in the last trimester of pregnancy has resulted in long term, but reversible, neurological disturbances (e.g. extrapyramidal effects) in the infant. If paliperidone needs to be discontinued during pregnancy, the medicine should be withdrawn gradually.
The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Paliperidone is contraindicated in breastfeeding.
Paliperidone is excreted in breast milk and effects on the infant are likely.
Although there is insufficient data available for the use of paliperidone during breastfeeding, it is the active metabolite of risperidone. Risperidone data indicate that the concentrations of paliperidone in breast milk are low, and the amounts ingested by the infant are small. Because of the limited published experience with paliperidone during breastfeeding and little long term follow up data, other agents may be preferred, especially whilst nursing newborns or premature infants.
Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1
Advise patient not to drive or operate machinery until they are aware of how they react to paliperidone.
Advise patients that the effects of alcohol may be enhanced by paliperidone.
Advise patient the tablet shell which contains the active ingredient is non-absorbable and should not be concerned if they see a tablet in their stools as the active ingredient will have been released.
Advise patient the tablets should be taken in the morning and should be standardised in relation to food intake and should take the tablets either always in the fasting state or always with breakfast (never alternate between the two).
Advise patient to seek urgent medical care if priapism has not been resolved within 3 to 4 hours.
Gamma glutamyl transferase (GGT) increased
Grand mal seizure
Increases in hepatic enzymes
Intraoperative floppy iris syndrome
Neuroleptic malignant syndrome
Prolongation of QT interval
Transient ischaemic attack
Upper respiratory tract infection
Urinary tract infections
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Last Full Review Date: March 2014
Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 2nd edition (2007) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.
Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 9th edition (2011) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.
Summary of Product Characteristics: Invega 3mg, 6mg, 9mg and 12 mg prolonged release tablets. Janssen-Cilag Ltd. Revised September 2018.
MHRA Drug Safety Update November 2013
Available at: https://www.mhra.gov.uk
Last accessed: March 31, 2014
NICE Evidence Services Available at: www.nice.org.uk
Last accessed: 23 June 2014
US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
Available at: https://toxnet.nlm.nih.gov
Paliperidone Last revised: January 16, 2014
Last accessed: March 07, 2014
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