FLUXID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FLUXID (FLUXID).
FLUXID is a selective serotonin reuptake inhibitor (SSRI) that potentiates serotonergic activity by blocking the reuptake of serotonin at the presynaptic neuronal membrane, increasing serotonin availability in the synaptic cleft.
| Metabolism | Primarily metabolized by CYP2D6 and CYP2C19 isoenzymes to its active metabolite, norfluxid. Inhibits CYP2D6, leading to potential drug-drug interactions. |
| Excretion | Renal: 70% unchanged; Fecal: 20%; Biliary: 10%. |
| Half-life | Terminal half-life: 12 hours (range 10–14 hours). In renal impairment (CrCl <30 mL/min), half-life prolonged to 24–36 hours; dose adjustment required. |
| Protein binding | 95% bound primarily to albumin; minor binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8 L/kg (range 0.6–1.0 L/kg), indicating distribution into total body water and moderate tissue binding. |
| Bioavailability | Oral: 85% (range 75–95%); no significant first-pass metabolism. |
| Onset of Action | Oral: 30–60 minutes; Intravenous: 5–10 minutes. |
| Duration of Action | Oral: 8–12 hours; Intravenous: 6–8 hours. Duration may be prolonged in hepatic impairment. |
1-2 g IV every 8 hours; maximum 6 g/day.
| Dosage form | TABLET, ORALLY DISINTEGRATING |
| Renal impairment | GFR >50 mL/min: no adjustment; GFR 10-50 mL/min: 1 g every 12 hours; GFR <10 mL/min: 1 g every 24 hours. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25%; Child-Pugh C: reduce dose by 50% or consider alternative. |
| Pediatric use | 50 mg/kg IV every 8 hours (max 2 g/dose) for children >1 month; adjust for renal function. |
| Geriatric use | Use with caution; monitor renal function; dose adjustment per CrCl. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FLUXID (FLUXID).
| Breastfeeding | FLUXID is excreted in breast milk with a milk-to-plasma ratio of 0.8. Due to potential for infant toxicity, breastfeeding is not recommended during therapy. |
| Teratogenic Risk | FLUXID is contraindicated in pregnancy. First trimester exposure is associated with a significant risk of major congenital malformations, particularly neural tube defects and cardiovascular anomalies. Second and third trimester exposure may cause fetal growth restriction, oligohydramnios, and neonatal nephrotoxicity. |
| Fetal Monitoring |
■ FDA Black Box Warning
Increased risk of suicidal thinking and behavior in children, adolescents, and young adults taking antidepressants. Closely monitor for clinical worsening, suicidality, or unusual changes in behavior.
| Serious Effects |
["Concurrent use of MAOIs (risk of serotonin syndrome)","Hypersensitivity to FLUXID or any excipient","Concurrent use of pimozide (risk of QT prolongation)","Concurrent use of thioridazine (risk of cardiac arrhythmias)","Use within 14 days of MAOI discontinuation (allow washout)"]
| Precautions | ["Serotonin syndrome: risk with concurrent serotonergic drugs","Discontinuation syndrome: gradual taper recommended","Hyponatremia: particularly in elderly or volume-depleted patients","Increased bleeding risk: especially with NSAIDs or anticoagulants","Activation of mania/hypomania: screen for bipolar disorder before initiation","Angle-closure glaucoma: potential for mydriasis","Serotonin syndrome: potentially life-threatening condition requiring immediate discontinuation"] |
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| Pregnancy test before initiation. In pregnant patients with unavoidable exposure, monitor fetal ultrasound for anomalies, amniotic fluid index, and fetal growth. Monitor maternal renal function and blood pressure. |
| Fertility Effects | FLUXID may impair fertility in both sexes. In males, reduced spermatogenesis and testicular atrophy have been reported. In females, menstrual irregularities and anovulation may occur. Contraception counseling is required for patients of reproductive potential. |