EXXUA (gepirone hydrochloride)

The pharmacokinetics of EXXUA are linear and dose proportional from 18.2 mg to 72.6 mg. Steady-state plasma concentration are typically achieved within two to four days of daily dosing.

AbsorptionThe absolute bioavailability is 14% to 17%. The maximal plasma EXXUA concentration (C max­ ) after dosing is reached within 6 hours post dose (T max ). Effect of Food After a high fat meal, T max is reached at 3 hours. A significant effect of food has been observed on the peak plasma concentration (C m...

The efficacy of EXXUA for the treatment for major depressive disorder (MDD) in adults was evaluated in two eight-week randomized, double-blind, placebo-controlled, flexible-dose studies in adults (age 18 to 69 years) meeting Diagnostic and Statistical Manual of Mental Disorders (DSM-IV) criteria for MDD. In Study 1, adult patients (18 to 69 years) who met DSM-IV diagnostic criteria for MDD were included in the trial. Patients in Study 1 had a median age of 39 years and were 61% female, 73% Caucasian, 9% Black, 2% Asian, and 16% Other (Hispanic or Native American). After an initial dosage of 18...

The following adverse reactions are discussed in greater detail in other sections of the labeling: Suicidal Thoughts and Behaviors in Adolescents and Young Adults [see Warnings and Precautions (5.1) ] QT Prolongation [see Warnings and Precautions (5.2) ] Serotonin Syndrome [see Warnings and Precautions (5.3) ] Activation of Mania or Hypomania [see Warnings and Precautions (5.4) ] Most common adverse reactions (incidence of ≥ 5% and at least twice incidence of placebo) were dizziness, nausea, ins...

EXXUA is contraindicated in patients: with known hypersensitivity to gepirone or components of EXXUA [see Adverse Reactions (6.1) ] . with prolonged QTc interval > 450 msec at baseline [see Warnings and Precautions (5.2) ]. with congenital long QT syndrome [see Warnings and Precautions (5.2) ]. receiving concomitant strong CYP3A4 inhibitors [see Warnings and Precautions (5.2) and Drug Interactions...

QT Interval Prolongation: EXXUA prolongs the QTc. Correct electrolyte abnormalities. Perform ECGs prior to initiation, during dose titration, and periodically during treatment with EXXUA. Monitor ECGs more frequently when EXXUA is used concomitantly with drugs known to prolong the QT interval, in patients who develop QTc ≥ 450 msec during treatment or are at significant risk of developing torsade de pointes. Do not escalate dosage if QTc > 450 msec ( 2.1 , 5.2 , 7 ). Serotonin Syndrome: Increase...

7 DRUG INTERACTIONS Table 3 displays clinically important drug interactions with EXXUA.

Table 3Clinically Important Drug Interactions with EXXUA CYP3A4 Inhibitors Clinical Impact Strong CYP3A4 Inhibitors Concomitant use of EXXUA with a strong CYP3A4 inhibitor increases EXXUA exposure by ~ 5-fold [see Clinical Pharmacology (12.3) ] . Moderate CYP3A4 Inhibitors Concomitant use with a moderate CYP3A...