Gepirone
Generic Name: gepirone
Brand Names:
Exxua
11 DESCRIPTION EXXUA contains gepirone, in the salt form as gepirone hydrochloride (HCl). The chemical name is 2,6- piperidinedione,4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-, monohydrochloride. The molecular weight of gepirone HCl is 395.93 and the structural formula is as follows: Gepirone HCl is a white to off-white crystalline powder, which is readily soluble in water. EXXUA is supplied as extended-release tablets for oral administration.
Overview
11 DESCRIPTION EXXUA contains gepirone, in the salt form as gepirone hydrochloride (HCl). The chemical name is 2,6- piperidinedione,4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-, monohydrochloride. The molecular weight of gepirone HCl is 395.93 and the structural formula is as follows: Gepirone HCl is a white to off-white crystalline powder, which is readily soluble in water. EXXUA is supplied as extended-release tablets for oral administration.
Uses
1 INDICATIONS AND USAGE EXXUA is indicated for the treatment of major depressive disorder (MDD) in adults. EXXUA is indicated for the treatment of major depressive disorder (MDD) in adults ( 1 ).
Dosage
2 DOSAGE AND ADMINISTRATION Correct electrolyte abnormalities and perform electrocardiogram (ECG) prior to initiating treatment with EXXUA. Do not initiate EXXUA if QTc is > 450 msec ( 2.1 ). Perform ECGs during dosage titration and periodically during treatment ( 2.1 ). The recommended starting dose is 18.2 mg administered orally once daily with food at approximately the same time each day ( 2.2 , 2.3 ). Depending on clinical response and tolerability, the dosage may be increased to 36.3 mg once daily on Day 4. Dosage may be further titrated to 54.5 mg once daily after Day 7 and to 72.6 mg once daily after an additional week ( 2.3 ). Geriatric patients: Recommended starting dosage is 18.2 mg once daily. Dosage may be increased to 36.3 mg after 7 days ( 2.4 ).
Side Effects
6 ADVERSE REACTIONS 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, insomnia, abdominal pain, and dyspepsia ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Aytu Therapeutics at 1-855-298-8246 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
Interactions
7 DRUG INTERACTIONS Table 3 displays clinically important drug interactions with EXXUA. Table 3 Clinically 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 CYP3A4 inhibitor increases EXXUA exposure by ~ 2.6-fold [see Clinical Pharmacology (12.3) ] . Intervention Strong CYP3A4 Inhibitors EXXUA is contraindicated in patients taking strong CYP3A4 inhibitors [see Dosage and Administration (2.7) , Contraindications (4) , and Warnings and Precautions (5.2) ] .
Warnings
BOXED WARNING WARNING: SUICIDAL THOUGHTS AND BEHAVIORS Antidepressants increased the risk of suicidal thoughts and behaviors in pediatric and young adult patients in short-term studies. Closely monitor all antidepressant-treated patients for clinical worsening and emergence of suicidal thoughts and behaviors [see Warnings and Precautions (5.1 ) ] . 5 WARNINGS AND PRECAUTIONS 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: Increased risk when co-administered with other serotonergic agents. If serotonin syndrome occurs, discontinue EXXUA and initiate supportive measures ( 5.3 ). Activation of Mania/Hypomania: Screen patients for bipolar disorder ( 5.4 ). 4 CONTRAINDICATIONS 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) ].
Pregnancy
8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to antidepressants, including EXXUA, during pregnancy. Healthcare providers are encouraged to register patients by calling the National Pregnancy Registry for Antidepressants at 1-866-961-2388 or visiting online at https://womensmentalhealth.org/research/pregnancyregistry/antidepressants/. Risk Summary Based on animal reproduction studies, gepirone has been shown to have adverse effects on embryo/fetal and postnatal development.
Storage
16 HOW SUPPLIED How Supplied EXXUA (gepirone) extended-release tablets are supplied in bottles of 30 with child-resistant caps and in four dosage strengths: 18.2-mg Tablets – pink, modified rectangular, with “FK” debossed on one side and “1” on the other side.
Frequently Asked Questions
What is Gepirone used for?▼
1 INDICATIONS AND USAGE EXXUA is indicated for the treatment of major depressive disorder (MDD) in adults. EXXUA is indicated for the treatment of major depressive disorder (MDD) in adults ( 1 ).
What are the side effects of Gepirone?▼
6 ADVERSE REACTIONS 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, insomnia, abdominal pain, and dyspepsia ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Aytu Therapeutics at 1-855-298-8246 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
Can I take Gepirone during pregnancy?▼
8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to antidepressants, including EXXUA, during pregnancy. Healthcare providers are encouraged to register patients by calling the National Pregnancy Registry for Antidepressants at 1-866-961-2388 or visiting online at https://womensmentalhealth.org/research/pregnancyregistry/antidepressants/. Risk Summary Based on animal reproduction studies, gepirone has been shown to have adverse effects on embryo/fetal and postnatal development.
What are the important warnings for Gepirone?▼
BOXED WARNING WARNING: SUICIDAL THOUGHTS AND BEHAVIORS Antidepressants increased the risk of suicidal thoughts and behaviors in pediatric and young adult patients in short-term studies. Closely monitor all antidepressant-treated patients for clinical worsening and emergence of suicidal thoughts and behaviors [see Warnings and Precautions (5.1 ) ] . 5 WARNINGS AND PRECAUTIONS 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: Increased risk when co-administered with other serotonergic agents. If serotonin syndrome occurs, discontinue EXXUA and initiate supportive measures ( 5.3 ). Activation of Mania/Hypomania: Screen patients for bipolar disorder ( 5.4 ). 4 CONTRAINDICATIONS 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) ].
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.