Paliperidone
Mechanism :
Major metabolite of risperidone; improves negative symptoms of psychoses and reduces incidence of EPS. Has high affinity for serotonin type 2 (5-HT2) receptors; binds to dopamine D2 receptors with 20 times lower affinity than that for 5-HT2 receptors; antagonizes alpha1-adrenergic, alpha2-adrenergic, and histaminergic receptors; has moderate affinity for serotonin type 1 (5-HT1C, 5-HT1D, 5-HT1A) receptors; has weak affinity for dopamine D1 receptors; has no affinity for muscarinic, beta1-adrenergic, and beta2-adrenergic receptors
Indication :
Contraindications :
Documented hypersensitivity to paliperidone or risperidone.
Any condition or drug that prolongs QT interval.
Severe pre-existing GI stenosis.
Dosing :
<12 years:
Safety not established
>12 years (<51 kg):
3 mg/day orally initially; increased in increments of 3 mg/day at intervals of 5 days. Max dose: 6 mg/day in those <51 kg and 12 mg/day in those >51 kg.
Adverse Effect :
Sudden numbness or weakness on one side, stiff muscles, akathisia, somnolence, insomnia, parkinsonism, hyperprolactinemia, high fever, sweating, confusion, arrhythmias, tremor, difficulty in swallowing.
Interaction :
Serious - Use Alternative:
Afatinib, Amiodarone, Apomorphine, Arsenic Trioxide, Astemizole, Bromocriptine, Cabergoline.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 50-80 | 3 mg once daily and increase according to response |
| 30-50 | 3 mg once daily and increase according to response |
| 10-30 | 3 mg alternate days, increasing to 3 mg daily according to response |
| <10 | 3 mg alternate days, increasing to 3 mg daily according to response. Use with caution |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unknown dialysability. Dose as in GFR<10 mL/min |
| HD | Unknown dialysability. Dose as in GFR<10 mL/min |
| HDF/High flux | Unknown dialysability. Dose as in GFR<10 mL/min |
| CAV/VVHD | Unknown dialysability. Dose as in GFR=10–30 mL/min |
Hepatic Dose :
Mild to moderate hepatic impairment: No dose adjustment is required.
Severe impairment: Dosing has not been studied but caution should be taken.