paliperidone INVEGA

Class: Second Generation Antipsychotic/​Benzisothiazole Derivative
FDA Indications: Schizophrenia, Schizoaffective Disorder
Off-Label Use: Bipolar Disorder
Prescribing
Forms: 1.5, 3, 6, 9mg ER Tablets; LAI: INVEGA SUSTENNA, 39 mg, 78 mg, 117 mg, 156 mg, or 234 mg
Dose Range: 3-12 mg/day
Starting: 6 mg qd, can titrate to 9 mg qd on week 2, or up to max dose 12 mg qd on week 3
Stopping: Taper 6-8 weeks, rapid d/c can lead to rebound psychosis
Monitoring:

NAMI drug fact sheet

Precautions
Serious Side Effects: , , , , Hyperprolactinemia, QTc prolongation
Possible Risk of TdP, Drugs to Avoid in Congenital Long QT
Side Effects: headache, sedation/somnolence, dizziness, constipation, weight gain, nausea, insomnia, sexual dysfunction, anxiety, tachycardia, orthostatic hypotension, EPS
Pharmacodynamics
1° MOA: 5HT2A–D2 antagonist
Target: Antagonism at:
Pharmacokinetics
t½: 23° TMAX: 24°
Substrate of: 1A2, 3A4
Inhibits: ∅ ; Induces:
Active Metabolites:
DDIs
  • - caution when co-prescribed with other medications that may cause orthostatic hypotension
  • - oral bioavailability was increased by 51% when coadministered with valproic acid
  • - Co-administration with carbamazepine can ↓ mean steady-state Cmax and AUC by ~37%
Misc
  • - active metabolite of risperidone, a.k.a. 9-hydroxy-risperidone
  • - not hepatically metabolized; its elimination is based upon urinary excretion, and it thus has few pharmacokinetic DDIs
  • - despite a similar receptor profile, paliperidone is better tolerated (less sedation, orthostasis & fewer EPS) than risperidone because its sustained-release formulation results in a much smoother dose-response curve (risperidone's side effects may may be related to its faster Tmax, higher Cmax & drug-level fluctuations)
  • - trilayer tablet consists of 3 compartments (2 containing drug, 1 a "push" compartment) and an orifice at the head of the first drug compartment; water fills the push compartment and gradually pushes drug up and out of the tablet through the orifice
  • - good evidence for treating violence
Special Populations

Category C

RID: No data available


All atypicals may increase mortality in elderly patients by 1.7 times greater than placebo.

Max recommended dose 3 mg/day in moderate or severe renal impairment (CrCl < 50 mL/ min). Dose reduction (max 6 mg/day) is recommended with mild renal impairment (CrCl ≥50 mL/ min to <80 mL/ min)

No dose adjustment is required in patients with mild or moderate hepatic impairment.

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Last updated January 22 2018 19:18:05. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.