Formulary
Paliperidone: Indications, Dosing, Side Effects and Interactions
Paliperidone is a metabolite of risperidone.
MedNext Academy | 8 min read
Paliperidone: Indications, Dosing, Side Effects and Interactions
Paliperidone is a metabolite of risperidone.
Drug action
Paliperidone is a metabolite of risperidone.
Indications and dose
**Schizophrenia,Psychotic or manic symptoms of schizoaffective disorder**
- **Adult** (By Mouth): 6 mg once daily, dose to be taken in the morning, then adjusted in steps of 3 mg if required, dose to be adjusted over at least 5 days; usual dose 3-12 mg daily.
**Schizophrenia [in patients stabilised on oral paliperidone or oral risperidone],Schizophrenia [in patients previously responsive to oral paliperidone or risperidone]**
- **Adult** (By Deep Intramuscular Injection): 150 mg for 1 dose on day 1, followed by 100 mg for 1 dose on day 8, then maintenance 75 mg once a month, alternatively maintenance 25-150 mg once a month, dose to be adjusted according to response, for maintenance doses required to achieve similar previous steady-state levels of paliperidone or risperidone-consult product literature, for advice on missed doses-consult product literature.
**Schizophrenia [in patients stabilised on intramuscular risperidone]**
- **Adult** (By Deep Intramuscular Injection): 25-150 mg once a month, dose to be adjusted according to response, starting dose is based on previous intramuscular risperidone and should be initiated in place of the next scheduled dose-consult product literature, for advice on missed doses-consult product literature.
**Schizophrenia [in patients stabilised on once- or three-monthly intramuscular paliperidone]**
- **Adult** (By Deep Intramuscular Injection): 700-1000 mg every 6 months, dose to be adjusted according to response, starting dose is based on previous once- or three-monthly intramuscular paliperidone and should be initiated in place of the next scheduled dose-consult product literature, for advice on missed doses-consult product literature.
**Schizophrenia [in patients stabilised on once-monthly intramuscular paliperidone]**
- **Adult** (By Deep Intramuscular Injection): 175-525 mg every 3 months, dose to be adjusted according to response, starting dose is based on previous once-monthly intramuscular paliperidone and should be initiated in place of the next scheduled dose-consult product literature, for advice on missed doses-consult product literature.
Cautions
For all antipsychotic drugs Blood dyscrasias; cardiovascular disease; conditions predisposing to seizures; depression; diabetes (may raise blood glucose); epilepsy; history of jaundice; myasthenia gravis; Parkinson's disease (may be exacerbated); photosensitisation (may occur with higher dosages); prostatic hypertrophy; severe respiratory disease; susceptibility to angle-closure glaucoma Cautions, further information Cardiovascular disease An ECG may be required, particularly if physical examination identifies cardiovascular risk factors, personal history of cardiovascular disease, or if the patient is being admitted as an inpatient. Elderly Screening Tool of Older Persons' potentially inappropriate Prescriptions (STOPP) criteria to aid medication reviews (see Prescribing in the elderly for information). Potentially inappropriate: for all antipsychotics (other than quetiapine and clozapine) in patients with parkinsonism or Lewy Body Disease (risk of severe extrapyramidal symptoms) in behavioural and psychological symptoms of dementia (BPSD), unless symptoms are severe and other non-pharmacological treatments have failed (increased risk of stroke) for use as a hypnotic, unless sleep disorder is due to psychosis or dementia (risk of confusion, hypotension, extrapyramidal side-effects, and falls) in patients prone to falls (may cause gait dyspraxia, parkinsonism) if prescribed a phenothiazine (other than prochlorperazine for nausea, vomiting, or vertigo; chlorpromazine for relief of persistent hiccups; levomepromazine as an antiemetic in palliative care) as first-line treatment (sedative, significant antimuscarinic (anticholinergic) toxicity in older people, and safer and more efficacious alternatives exist) if prescribed an antipsychotic drug with moderate or marked antimuscarinic effects (e.g. chlorpromazine, clozapine, flupenthixol, fluphenazine, pipothiazine, promazine, and zuclopenthixol) in patients with a history of prostatism or urinary retention (high risk of urinary retention) Cautions For paliperidone General cautions: Cataract surgery (risk of intraoperative floppy iris syndrome); dementia with Lewy bodies; elderly patients with dementia; elderly patients with risk factors for stroke; predisposition to gastro-intestinal obstruction; prolactin-dependent tumours Specific cautions: With intramuscular use When transferring from oral to depot therapy, the dose by mouth should be reduced gradually
Side effects
For all antipsychotic drugs Common or very common Agitation; amenorrhoea; arrhythmias; constipation; dizziness; drowsiness; dry mouth; erectile dysfunction; fatigue; galactorrhoea; gynaecomastia; hyperglycaemia; hyperprolactinaemia; hypersalivation; hypotension (dose-related); insomnia; leucopenia; movement disorders; muscle rigidity; neutropenia; parkinsonism; postural hypotension (dose-related); QT interval prolongation; rash; seizure; tremor; urinary retention; vomiting; weight increased Uncommon Agranulocytosis; confusion; neuroleptic malignant syndrome (discontinue-potentially fatal) Rare or very rare Sudden death; withdrawal syndrome neonatal Side-effects, further information For depot antipsychotics-side-effects may persist until the drug has been cleared from its depot site. Overdose Phenothiazines cause less depression of consciousness and respiration than other sedatives. Hypotension, hypothermia, sinus tachycardia, and arrhythmias may complicate poisoning. For details on the management of poisoning see Antipsychotics under Emergency treatment of poisoning . Side-effects For paliperidone General side-effects: Common or very common Anxiety; appetite abnormal; asthenia; cardiac conduction disorders; cough; depression; diarrhoea; drooling; eye disorders; facial spasm; fever; gastrointestinal discomfort; glabellar reflex abnormal; headache; hypertension; increased risk of infection; joint disorders; laryngeal pain; mood altered; muscle complaints; muscle contracture; musculoskeletal stiffness; nasal congestion; nausea; neuromuscular dysfunction; oral disorders; oropharyngeal spasm; pain; respiratory disorders; skin reactions; vision disorders; weight decreased Uncommon Alopecia; anaemia; breast abnormalities; chest discomfort; chills; concentration impaired; conjunctivitis; cystitis; diabetes mellitus; dry eye; dysarthria; dysphagia; dyspnoea; ear pain; epistaxis; fall; gait abnormal; gastrointestinal disorders; generalised tonic-clonic seizure; hypoglycaemia; induration; malaise; menstrual cycle irregularities; muscle weakness; oedema; palpitations; sensation abnormal; sexual dysfunction; sleep disorders; syncope; taste altered; thirst; thrombocytopenia; tinnitus; urinary disorders; vertigo Rare or very rare Angioedema; cerebrovascular insufficiency; coma; consciousness impaired; dandruff; diabetic ketoacidosis; dysphonia; embolism and thrombosis; flushing; glaucoma; hypothermia; ischaemia; jaundice; pancreatitis; polydipsia; posture abnormal; rhabdomyolysis; SIADH; sleep apnoea; vaginal discharge; water intoxication; withdrawal syndrome Frequency not known Severe cutaneous adverse reactions (SCARs) Specific side-effects: Common or very common With intramuscular use Cervical spasm; tetany Rare or very rare With intramuscular use Catatonia; unresponsive to stimuli Frequency not known With intramuscular use Injection site necrosis
Interactions
**Severe interactions:**
- Potential for other medicines to affect INVEGA In vitro studies indicate that CYP2D6 and CYP3A4 may be minimally involved in paliperidone metabolism, but there are no indications in vitro nor in...
- Concomitant administration of INVEGA with paroxetine, a potent CYP2D6 inhibitor, showed no clinically significant effect on the pharmacokinetics of paliperidone.
**Other interactions (19):**
- Caution is advised when prescribing INVEGA with medicines known to prolong the QT interval, e.g., class IA antiarrhythmics (e.g., quinidine, disopyramide) and class III antiarrhythmics (e.g.,...
- In vitro studies indicate that paliperidone is not an inducer of CYP1A2 activity.
- Given the primary CNS effects of paliperidone (see section 4.8), INVEGA should be used with caution in combination with other centrally acting medicines, e.g., anxiolytics, most antipsychotics,...
- Paliperidone may antagonise the effect of levodopa and other dopamine agonists.
- Because of its potential for inducing orthostatic hypotension (see section 4.4), an additive effect may be observed when INVEGA is administered with other therapeutic agents that have this...
- Caution is advised if paliperidone is combined with other medicines known to lower the seizure threshold (i.e., phenothiazines or butyrophenones, clozapine, tricyclics or SSRIs, tramadol,...
Pregnancy
For all antipsychotic drugs Extrapyramidal effects and withdrawal syndrome have been reported occasionally in the neonate when antipsychotic drugs are taken during the third trimester of pregnancy. Following maternal use of antipsychotic drugs in the third trimester, neonates should be monitored for symptoms including agitation, hypertonia, hypotonia, tremor, drowsiness, feeding problems, and respiratory distress. Pregnancy For paliperidone Use only if potential benefit outweighs risk (toxicity in animal studies). M With oral use: If discontinuation during pregnancy is necessary, withdraw gradually. M Pregnancy For Byannli pre-filled syringes Consider long-acting nature of formulation (paliperidone may be detected in plasma up to 4 years after single dose). M Pregnancy For Trevicta pre-filled syringes Consider long-acting nature of formulation (paliperidone may be detected in plasma up to 18 months after single dose). M
Breast feeding
For all antipsychotic drugs There is limited information available on the short- and long-term effects of antipsychotic drugs on the breast-fed infant. Animal studies indicate possible adverse effects of antipsychotic medicines on the developing nervous system. Chronic treatment with antipsychotic drugs whilst breast-feeding should be avoided unless absolutely necessary. Phenothiazine derivatives are sometimes used in breast-feeding women for short-term treatment of nausea and vomiting. Breast feeding For paliperidone Avoid (present in milk). M Breast feeding For Byannli pre-filled syringes Consider long-acting nature of formulation (paliperidone may be detected in plasma up to 4 years after single dose). M Breast feeding For Trevicta pre-filled syringes Consider long-acting nature of formulation (paliperidone may be detected in plasma up to 18 months after single dose). M
Hepatic impairment
Caution in severe impairment (no information available). M
Renal impairment
Prescribing in renal impairment . With oral use: Avoid if creatinine clearance less than 10 mL/minute. M With intramuscular use: Avoid if creatinine clearance less than 50 mL/minute. M Dose adjustments With oral use: Reduce initial dose to 3 mg once daily if creatinine clearance 50-79 mL/minute (max. 6 mg once daily). M Reduce initial dose to 3 mg on alternate days if creatinine clearance 10-49 mL/minute (max. 3 mg once daily). M With intramuscular use: For once-monthly formulations, reduce initial dose to 100 mg on day 1 then 75 mg on day 8 if creatinine clearance 50-79 mL/minute; recommended maintenance dose 50 mg (range 25-100 mg) once a month if creatinine clearance 50-79 mL/minute. M Renal impairment For Byannli pre-filled syringes Dose adjustments Max. dose 700 mg every 6 months if creatinine clearance 50-80 mL/minute. M
Medicinal forms
Tablet,Injection
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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