Iloperidone

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

North America

USA: Fanapt.

Drug combinations

Chemistry

Iloperidone: C~24~H~27~FN~2~O~4~. Mw: 426.48. (1) 1-[4-[3-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]propoxy]-3-methoxyphenyl]ethanone; (2) 4′-[3-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3′-methoxyacetophenone. CAS-133454-47-4.

Pharmacologic Category

Atypical Antipsychotics. (ATC-code: N05AX14).

Mechanism of action

Iloperidone is a piperidinyl-benzisoxazole atypical antipsychotic with mixed D~2~/5-HT~2~ antagonist activity. It exhibits high affinity for 5-HT~2A~, D~2~, and D~3~ receptors, low to moderate affinity for D~1~, D~4~, H~1~, 5-HT~1A~, 5-HT~6~, 5HT~7~, and NE~α1~ receptors, and no affinity for muscarinic receptors. The addition of serotonin antagonism to dopamine antagonism (classic neuroleptic mechanism) is thought to improve negative symptoms of psychoses and reduce the incidence of extrapyramidal side-effects. Iloperidone’s low affinity for histamine H~1~ receptors may decrease the risk for weight gain and somnolence while its affinity for NE~α1/α2C~ may provide antidepressant and anxiolytic activity and improved cognitive function.

Therapeutic use

Acute treatment of schizophrenia.

Pregnancy and lactiation implications

Animal studies have shown an increased risk of developmental toxicity and fetal mortality; use during pregnancy only if clearly needed. Not recommended in nursing women.

Unlabeled use

Contraindications

Hypersensitivity to iloperidone or any component of the formulation. Not recommended in hepatic impairment. Not approved for use in dementia-related psychosis.

Warnings and precautions

Elderly patients with dementia-related psychosis who are treated with atypical antipsychotic drugs are at an increased risk of death and cerebrovascular-related adverse events, including stroke. Prolongs QT interval and may be associated with arrhythmia and sudden death. Neuroleptic malignant syndrome (immediate discontinuation), tardive dyskinesia, hyperglycemia and diabetes mellitus, seizure, and orthostatic hypotension (dizziness, tachycardia, and syncope) can occur. Leukopenia, neutropenia, and agranulocytosis have been reported with antipsychotics (should be discontinued at the first sign of a decline in WBC in the absence of other causative factors). Suicide, priapism, sedation, impaired core body temperature regulation, weight gain, and potential for cognitive and motor impairment have also been observed. May cause anticholinergic effects (confusion, agitation, constipation, xerostomia, blurred vision, urinary retention). Antipsychotic use has been associated with esophageal dysmotility and aspiration. Extrapyramidal symptoms (EPS) including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia (risk of these reactions is generally much lower relative to typical/conventional antipsychotics) may occur. Risk of dystonia (and probably other EPS) may be greater with increased doses, use of conventional antipsychotics, males, and younger patients.

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