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Iloperidone

Atypical Antipsychotic · Antipsychotic

Atypical AntipsychoticAntipsychotic
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
C
FDA category + note
Top interactionssee all 12
  • AbarelixSevereDatabaseDDInter
  • AbirateroneSevereDatabaseDDInter
  • AdenosineSevereDatabaseDDInter
  • AlfentanilSevereDatabaseDDInter

Mechanism

Iloperidone is a second-generation antipsychotic that acts as an inverse agonist at 5-HT2A receptors, blocking their constitutive activity. This action modulates the release of dopamine, norepinephrine, glutamate, GABA, and acetylcholine. It also blocks D2 receptors and may act as a 5-HT2C inverse agonist, contributing to the inhibition of cortical and limbic dopamine release.

Indications

Schizophrenia

Dosing

Adult
NMDA receptor is not fully saturated. There have been several trials of high doses of glycine to promote glutamatergic activity, but the results are far from convincing. Currently, glycine transport inhibitors are in development as possible psychotropic agents. Ampakines are drugs that potentiate currents mediated by AMPA­type glutamate receptors.…

Pharmacokinetics

Peak effect
2–4 h
Half-life
18 h (CYP2D6 EMs), 33 h (CYP2D6 PMs). P88 t1/2: 26 h (EM), 37 h (PM). P95 t1/2: 23 h (EM), 31 h (PM).
Bioavailability
Well absorbed
Metabolism
CYP2D6/3A4 produce active metabolites P88 and P95.

Contraindications

  • Use in elderly dementia patients (increased mortality risk)

Side effects

Common
Low risk of metabolic adverse effectsorthostasis (requires slow titration)
Serious
  • Neuroleptic malignant syndrome
  • increased mortality in elderly dementia patients

Pregnancy & lactation

Pregnancy

C

Lactation

Not specified

Drug interactions

Abarelix
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Abiraterone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Adenosine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alfentanil
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alfuzosin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alimemazine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amiodarone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amisulpride
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amitriptyline
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amoxapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amprenavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Anagrelide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Related guidelines

Other Atypical Antipsychotic drugs

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Sources: Goodman & Gilman 14e, Katzung·Verified: 2026-05-13 · House clinical team