Iloperidonum

Iloperidonum Uses, Dosage, Side Effects, Food Interaction and all others data.

Iloperidonum 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. Iloperidonum also binds with high affinity to serotonin 5-HT2a and dopamine 3 receptors. Iloperidonum 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.

Trade Name Iloperidonum
Availability Prescription only
Generic Iloperidone
Iloperidone Other Names Iloperidona, Iloperidone, Ilopéridone, Iloperidonum
Related Drugs quetiapine, Abilify, Seroquel, aripiprazole, olanzapine, risperidone, haloperidol, prochlorperazine, Haldol, Compazine
Type
Formula C24H27FN2O4
Weight Average: 426.4806
Monoisotopic: 426.195485567
Protein binding

95% of iloperidone is bound to protein. Percent bound is not altered by renal or hepatic impairment or combination therapy with ketoconazole.

Groups Approved
Therapeutic Class Piperidinyl-benzisoxazole derivative
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Iloperidonum
Iloperidonum

Uses

Iloperidonum is used for the treatment of schizophrenia in adults.

When deciding among the alternative treatments available for this condition, the prescriber should consider the finding that iloperidone is associated with prolongation of the QTc interval. Prolongation of the QTc interval is associated in some other drugs with the ability to cause torsade de pointestype arrhythmia, a potentially fatal polymorphic ventricular tachycardia which can result in sudden death. In many cases this would lead to the conclusion that other drugs should be tried first. Whether iloperidone will cause torsade de pointes or increase the rate of sudden death is not yet known.

Patients must be titrated to an effective dose of iloperidone. Thus, control of symptoms may be delayed during the first 1 to 2 weeks of treatment compared to some other antipsychotic drugs that do not require a similar titration. Prescribers should be mindful of this delay when selecting an antipsychotic drug for the treatment of schizophrenia

Iloperidonum is also used to associated treatment for these conditions: Schizophrenia

How Iloperidonum works

Iloperidonum is a dopamine D2 and 5-HT2A receptor antagonist and acts as a neuroleptic agent.

Dosage

Iloperidonum dosage

Initial dose: 1 mg orally twice a day

Titration: Increase in increments of not more than 2 mg twice daily as tolerated.

Target dose: 6 to 12 mg twice a day

Maximum 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.

Side Effects

Dizziness (20%), Dry mouth (15%), Nausea (10%), Somnolence (10%), Tachycardia, Diarrhea, Ejaculation failure, Myalgia, Nasal congestion, Orthostatic hypotension, Palpitations, Urinary incontinence, Weight gain

Toxicity

Commonly observed adverse reactions (incidence ≥5% and two-fold greater than placebo) were: dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence, tachycardia, and weight increased.

Precaution

This drug 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.

Interaction

There are no known drug interactions and none well documented.

Food Interaction

  • Take with or without food. High fat meals may delay the Tmax of iloperidone and its metabolites P88, P95 by 1,2, and 6 hours respectively, without significantly changing the Cmax or AUC.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Iloperidonum Cholesterol interaction

[Moderate] Atypical antipsychotic drugs have been associated with undesirable alterations in lipid levels.

While all agents in the class have been shown to produce some changes, each drug has its own specific risk profile.

Before or soon after initiation of antipsychotic medication, obtain a fasting lipid profile at baseline and monitor periodically during treatment.

Volume of Distribution

Apparent Vd = 1340-2800 L

Elimination Route

Well absorbed from the GI tract and Cmax is reached within 2-4 hours. Steady-state concentration is achieved in 3-4 days post-administration of iloperidone. Relative bioavailability of the tablet formulation compared to oral solution is 96%. Accumulation occurs in a predictable fashion.

Half Life

The observed mean elimination half-lives for iloperidone, P88 and P95 in CYP2D6 extensive metabolizers (EM) are 18, 26 and 23 hours, respectively, and in poor metabolizers (PM) are 33, 37 and 31 hours, respectively.

Clearance

Apparent clearance (clearance/bioavilability) = 47-102 L/h.

Elimination Route

Renal (in which <1% of iloperidone is excreted unchanged).

Pregnancy & Breastfeeding use

Pregnancy Category-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 risks

Lactation: Not known if excreted in breast milk, do not nurse.

Contraindication

Hypersensitivity.

Special Warning

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.

Innovators Monograph

You find simplified version here Iloperidonum

Iloperidonum contains Iloperidone see full prescribing information from innovator Iloperidonum Monograph, Iloperidonum MSDS, Iloperidonum FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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