Drug Action
Paliperidone is a metabolite of risperidone.
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Drug reference
Paliperidone is a metabolite of risperidone.
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Schizophrenia| Psychotic or manic symptoms of schizoaffective disorder ▶BY MOUTH ▶Adult: 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 TREVICTA ® PRE-FILLED SYRINGES Maintenance of schizophrenia in patients who are clinically stable on once-monthly intramuscular paliperidone ▶BY DEEP INTRAMUSCULAR INJECTION ▶Adult: Initially 175–525 mg every 3 months, adjusted according to response, to be administered into the deltoid or gluteal muscle, dose is based on previous once-monthly intramuscular paliperidone and should be initiated in place of the next scheduled dose— consult product literature XEPLION ® PRE-FILLED SYRINGES Maintenance in schizophrenia in patients previously responsive to paliperidone or risperidone ▶BY DEEP INTRAMUSCULAR INJECTION ▶Adult: 150 mg for 1 dose on day 1, then 100 mg for 1 dose on day 8, to be injected into the deltoid muscle, dose subsequently adjusted at monthly intervals according to response; maintenance 75 mg once a month, alternatively maintenance 25–150 mg once a month, following the second dose, monthly maintenance doses can be administered into either the deltoid or gluteal muscle
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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
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XEPLION ® PRE-FILLED SYRINGES Xeplion ® 25 mg pre- filled syringes may be difficult to obtain.
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TREVICTA ® PRE-FILLED SYRINGES Scottish Medicines Consortium (SMC) decisions The Scottish Medicines Consortium has advised (September 2016) that paliperidone palmitate (Trevicta ®) is accepted for use within NHS Scotland for the maintenance treatment of schizophrenia in patients who are clinically stable on one-monthly paliperidone palmitate injectable product.
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→Appendix 1: paliperidone
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GENERAL SIDE-EFFECTS ▶Common or very common Anxiety. appetite abnormal. asthenia. cardiac conduction disorders. cough. depression. diarrhoea. fever. gastrointestinal discomfort. headache. hyperglycaemia. hypertension. increased risk of infection. joint disorders. laryngeal pain. mood altered . nasal congestion. nausea. oral disorders. pain. skin reactions. vision disorders ▶Uncommon Alopecia. anaemia. breast abnormalities. chest discomfort. chills. conjunctivitis. cystitis. dry eye. dysarthria. dysphagia. dyspnoea. ear pain. epistaxis. fall. gait abnormal. gastrointestinal disorders. generalised tonic-clonic seizure. hypoglycaemia. induration. malaise . menstrual cycle irregularities. muscle spasms. muscle weakness. oedema. palpitations. respiratory disorders. 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. eye disorders. flushing. glaucoma. hypothermia. ischaemia. jaundice. pancreatitis. polydipsia. posture abnormal. rhabdomyolysis. SIADH. sleep apnoea. vaginal discharge. water intoxication. withdrawal syndrome SPECIFIC SIDE-EFFECTS ▶Common or very common ▶With oral use Weight decreased ▶Uncommon ▶With oral use Concentration impaired. confusion. diabetes mellitus ▶Frequency not known ▶With intramuscular use Injection site necrosis
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Use only if potential benefit outweighs risk— toxicity in animal studies; if discontinuation during pregnancy is necessary, withdraw gradually. TREVICTA ® PRE-FILLED SYRINGES Manufacturer advises to consider long-acting nature of formulation—paliperidone detected in plasma up to 18 months after single dose.
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Manufacturer advises avoid—present in milk. TREVICTA ® PRE-FILLED SYRINGES Manufacturer advises to consider long-acting nature of formulation—paliperidone detected in plasma up to 18 months after single dose.
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Manufacturer advises caution in severe impairment (no information available).
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▶With oral use Manufacturer advises avoid if creatinine clearance less than 10 mL/minute. ▶With intramuscular use Manufacturer advises avoid if creatinine clearance less than 50 mL/minute. Dose adjustments ▶With oral use Manufacturer advises reduce initial dose to 3 mg once daily if creatinine clearance 50–80 mL/minute (max. 6 mg once daily). Manufacturer advises reduce initial dose to 1.5 mg once daily if creatinine clearance 10–50 mL/minute (max. 3 mg once daily). TREVICTA ® PRE-FILLED SYRINGES Dose adjustments Manufacturer advises dose should be adjusted and stabilised using once-monthly injectable paliperidone before switching to three-monthly injectable paliperidone, if creatinine clearance 50–80 mL/minute. XEPLION ® PRE-FILLED SYRINGES Dose adjustments Manufacturer advises initial dose 100 mg on day 1 and then 75 mg on day 8 if creatinine clearance 50–80 mL/minute; recommended maintenance dose 50 mg (range 25–100 mg) monthly if creatinine clearance 50–80 mL/minute.
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▶With intramuscular use Treatment requires careful monitoring for optimum effect.
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▶With intramuscular use Correct injection technique (including the use of z-track technique) and rotation of injection sites are essential. ▶With oral use Always take with breakfast or always take on an empty stomach.
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There can be variation in the licensing of different medicines containing the same drug. Prolonged-release suspension for injection ▶Trevicta (Janssen-Cilag Ltd) Paliperidone (as Paliperidone palmitate) 200 mg per 1 ml Trevicta 175mg/0.875ml prolonged-release suspension for injection pre-filled syringes | 1 pre-filled disposable injection P £551.76 DT = £551.76 Trevicta 263mg/1.315ml prolonged-release suspension for injection pre-filled syringes | 1 pre-filled disposable injection P £734.70 DT = £734.70 Trevicta 350mg/1.75ml prolonged-release suspension for injection pre-filled syringes | 1 pre-filled disposable injection P £942.21 DT = £942.21 Trevicta 525mg/2.625ml prolonged-release suspension for injection pre-filled syringes | 1 pre-filled disposable injection P £1,177.77 DT = £1,177.77 Modified-release tablet CAUTIONARY AND ADVISORY LABELS 2, 25 ▶Invega (Janssen-Cilag Ltd) Paliperidone 3 mg Invega 3mg modified-release tablets | 28 tablet P £97.28 DT = £97.28 Paliperidone 6 mg Invega 6mg modified-release tablets | 28 tablet P £97.28 DT = £97.28 Paliperidone 9 mg Invega 9mg modified-release tablets | 28 tablet P £145.92 DT = £145.92 Suspension for injection ▶Xeplion (Janssen-Cilag Ltd) Paliperidone (as Paliperidone palmitate) 100 mg per 1 ml Xeplion 150mg/1.5ml suspension for injection pre-filled syringes | 1 pre-filled disposable injection P £392.59 DT = £392.59 Xeplion 75mg/0.75ml suspension for injection pre-filled syringes | 1 pre-filled disposable injection P £244.90 DT = £244.90 Xeplion 100mg/1ml suspension for injection pre-filled syringes | 1 pre-filled disposable injection P £314.07 DT = £314.07 Xeplion 50mg/0.5ml suspension for injection pre-filled syringes | 1 pre-filled disposable injection P £183.92 DT = £183.92 eiiii F 401
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▶With oral use Patients or carers should be given advice on how to administer paliperidone tablets. Missed doses ▶With intramuscular use For missed doses see product literature.
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6 mg once daily, dose to be taken in the
First-line fragment. Read the complete Indications and Dose section above.
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Initially 175–525 mg every 3 months, adjusted
First-line fragment. Read the complete Indications and Dose section above.
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150 mg for 1 dose on day 1, then 100 mg for
First-line fragment. Read the complete Indications and Dose section above.
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