Fanapt Titration Pack
Fanapt Titration Pack Uses, Dosage, Side Effects, Food Interaction and all others data.
Fanapt Titration Pack 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. Fanapt Titration Pack also binds with high affinity to serotonin 5-HT2a and dopamine 3 receptors. Fanapt Titration Pack 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 | Fanapt Titration Pack |
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 | Oral |
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 | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Fanapt Titration Pack 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
Fanapt Titration Pack is also used to associated treatment for these conditions: Schizophrenia
How Fanapt Titration Pack works
Fanapt Titration Pack is a dopamine D2 and 5-HT2A receptor antagonist and acts as a neuroleptic agent.
Dosage
Fanapt Titration Pack 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.
Fanapt Titration Pack 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.
Fanapt Titration Pack Drug Interaction
Major: hydroxyzine, citalopram, clozapine, ziprasidone, haloperidol, paliperidone, lithium, thioridazine, risperidoneModerate: aripiprazole, divalproex sodium, clonazepam, lamotrigine, lurasidone, eszopiclone, molindone, thiothixeneUnknown: amphetamine / dextroamphetamine, methylphenidate, methylphenidate
Fanapt Titration Pack Disease Interaction
Major: dementia, QT Prolongation, NMS, tardive dyskinesiaModerate: depression, aspiration, seizure, hematologic abnormalities, hyperglycemia/diabetes, hypotension, lipid alterations, priapism, weight gain, hyperprolactinemia
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 Fanapt Titration Pack
Fanapt Titration Pack contains Iloperidone see full prescribing information from innovator Fanapt Titration Pack Monograph, Fanapt Titration Pack MSDS, Fanapt Titration Pack FDA label