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Exxua
gepirone
Black Box Warnings .
Suicidality
antidepressants incr. suicidality risk in peds and young adult patients in short-term studies; monitor closely for clinical worsening and suicidality; advise families and caregivers of need for close observation and communication with prescriber; not approved for peds patients
Adult Dosing .
Dosage forms: ER TAB: 18.2 mg, 36.3 mg, 54.5 mg, 72.6 mg; ER TAB (titration pack): 18.2 mg x32
major depressive disorder
- [18.2-72.6 mg PO qd]
- Start: 18.2 mg PO qd x3 days, then may incr. to 36.3 mg PO qd x4 days, then may incr. to 54.5 mg PO qd x1wk, then may incr. to 72.6 mg PO qd; Max: 72.6 mg/day; Info: start 18.2 mg PO qd x7 days, max 36.3 mg/day in elderly patients; give with food; do not cut/crush/chew tab; do not incr. dose if QTc >450 msec
renal dosing
- [adjust dose amount]
- CrCl <50: start 18.2 mg qd x7 days, max 36.3 mg/day
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class B: start 18.2 mg qd x7 days, max 36.3 mg/day; Child-Pugh Class C: contraindicated
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- MAO inhibitor use within 14 days
- hepatic impairment, Child-Pugh Class C
- baseline QTc >450 msec
- electrolyte abnormalities, uncorrected
- long QT syndrome, congenital
- caution: QT prolongation family history
- caution: torsades de pointes history
- caution: ventricular arrhythmia
- caution: AV block, 2nd-3rd degree
- caution: bradycardia
- caution: cardiac disease, uncontrolled
- caution: cardiac disease, significant
- caution: unstable angina
- caution: aortic stenosis, severe
- caution: MI, recent
- caution: heart failure
- caution: HTN, uncontrolled
- caution: hypothyroidism, uncontrolled
- caution: patients <25 yo
- caution: elderly patients
- caution: bipolar disorder
- caution: bipolar disorder risk
- caution: CrCl <50
- caution: hepatic impairment, Child-Pugh Class B
Drug Interactions .
Overview
gepirone
5-HT1A agonist
- CYP3A4 substrate
- prolongs QT interval (conditional)
- serotonergic effects
- add MAO inhibitor to Interaction Check if recent (14 days) use
Contraindicated
Avoid/Use Alternative
Monitor/Modify Tx
Caution Advised
Adverse Reactions .
Serious Reactions
- suicidality
- depression exacerbation
- QT prolongation
- serotonin syndrome
- mania
Common Reactions
- dizziness
- nausea
- headache
- fatigue
- insomnia
- diarrhea
- URI
- xerostomia
- vomiting
- abdominal pain
- dyspepsia
- appetite incr.
- constipation
- nasal congestion
- paresthesia
- hyperhidrosis
- palpitations
- weight incr.
- agitation
- jitteriness
- HR incr.
- lethargy
Safety/Monitoring .
Monitoring Parameters
Cr at baseline; electrolytes including Mg at baseline, then if electrolyte disturbance risk, during dose titration and periodically; ECG at baseline, during dose titration, and periodically, or more frequently if QTc >450 msec during tx or torsades de pointes risk; symptoms of suicidality, clinical worsening, and/or unusual behavior changes, especially during initial tx or after dose changes
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy, especially in 3rd trimester; inadequate human data available, though risk of neonatal withdrawal symptoms or serotonin syndrome based on human data with SSRIs; risk of neonatal persistent pulmonary HTN inconclusive based on human data with SSRIs; risk of decr. embryo-fetal growth and skeletal variations based on animal data at 18x and 24x MRHD
Pregnancy Registry
encourage patients to enroll in National Pregnancy Registry for Antidepressants at 1-866-961-2388 or www.womensmentalhealth.org/research/pregnancyregistry/antidepressants
Lactation
Clinical Summary
weigh risk/benefit while breastfeeding; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: for gepirone: liver extensively; CYP450: 3A4 substrate; Info: active metabolites
Excretion: for gepirone: urine 81% (none unchanged), feces 13% (none unchanged); Half-life: 5h
Subclass: Serotonin 5-HT1A Receptor Agonists
Mechanism of Action
for gepirone: exact mechanism of action unknown; selectively agonizes serotonin 5-HT1A receptors
Formulary .
No Formulary Selected
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