Drug Index

Paliperidone

 
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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 :

• Schizophrenia


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)
50-803 mg once daily and increase according to response
30-503 mg once daily and increase according to response
10-303 mg alternate days, increasing to 3 mg daily according to response
<103 mg alternate days, increasing to 3 mg daily according to response. Use with caution

Dose in Patients undergoing Renal Replacement Therapies
CAPDUnknown dialysability. Dose as in GFR<10 mL/min
HDUnknown dialysability. Dose as in GFR<10 mL/min
HDF/High fluxUnknown dialysability. Dose as in GFR<10 mL/min
CAV/VVHDUnknown 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.
06/24/2020 06:48:59 Paliperidone
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