Iloperidone
Iloperidone shows high affinity and maximal receptor occupancy for dopamine D2 receptors in the caudate nucleus and putamen of the brains of schizophrenic patients. The improvement in cognition is attributed to iloperidone's high affinity for α adrenergic receptors. Iloperidone also binds with high affinity to serotonin 5-HT2a and dopamine 3 receptors. Iloperidone binds with moderate affinity to dopamine D4, serotonin 5-HT6 and 5-HT7, and norepinephrine NEα1 receptors. Furthermore, iloperidone binds with weak affinity to serotonin 5-HT1A, dopamine D1, and histamine H1 receptors.
Initial dose: 1 mg orally twice a dayTitration: Increase in increments of not more than 2 mg twice daily as tolerated.Target dose: 6 to 12 mg twice a dayMaximum dose: 24 mg/dayThis drug must be titrated slowly to avoid orthostatic hypotension; because of the need to titrate slowly, control of symptoms may be delayed during the first 1 to 2 weeks of treatment.
There are no known drug interactions and none well documented.
Hypersensitivity.
Dizziness (20%), Dry mouth (15%), Nausea (10%), Somnolence (10%), Tachycardia, Diarrhea, Ejaculation failure, Myalgia, Nasal congestion, Orthostatic hypotension, Palpitations, Urinary incontinence, Weight gain
PregnancyCategory-C. Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risksLactation: Not known if excreted in breast milk, do not nurse.
Ilodon is not approved for the treatment of patients with dementia-related psychosis. Prolongs QT interval; caution with other drugs/conditions that increase QTc. Risk of neuroleptic malignant syndrome and extrapyramidal symptoms. May cause anticholinergic side effects (eg., confusion, agitation). Blood dyscrasias (leukopenia, neutropenia, agranulocytosis) may occur. Orthostatic hypotension may occur.
Piperidinyl-benzisoxazole derivative
Renal Dose Adjustments: No adjustment recommended.Liver Dose Adjustments-Mild hepatic impairment: No adjustment recommended.Moderate hepatic impairment: Use with caution.Severe hepatic impairment: Not recommended.
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