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. |
| Molecular Weight | 285.3 |
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 | Avoid. Associated with increased risk of major malformations, particularly cardiovascular and neural tube defects. |
| 2nd trimester | Avoid. Potential risk of fetal growth restriction and oligohydramnios. |
| 3rd trimester | Avoid. Risk of neonatal complications including persistent pulmonary hypertension and withdrawal symptoms. |
Clinical note
Comprehensive clinical and safety monograph for FLUXID (FLUXID).
| Placental transfer | Extensive placental transfer documented; fetal plasma concentrations reach 50-100% of maternal levels. |
| Breastfeeding | Contraindicated during breastfeeding due to high excretion into breast milk and risk of serious adverse effects in the infant, including sedation and respiratory depression. |
| Lactation Rating |
■ 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 |
Hypersensitivity to fluxid or any componentSevere hepatic impairmentNarrow-angle glaucomaUrinary retentionConcurrent use with monoamine oxidase inhibitors (MAOIs)Lactation
| 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 |
| Food/Dietary | No significant food interactions. Avoid excessive alcohol consumption as it may increase bleeding risk. Grapefruit juice does not affect FLUXID. |
Loading safety data…
| L5 - Contraindicated |
| 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 | 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. |
| Clinical Pearls | FLUXID is a novel oral anticoagulant; monitor renal function at baseline and annually. Avoid in CrCl <15 mL/min. No routine coagulation monitoring required but anti-Xa activity correlates with dose. Reversal agent is andexanet alfa. Use with caution in patients with mechanical heart valves or antiphospholipid syndrome. Discontinue 48 hours before elective surgery with standard bleeding risk. |
| Patient Advice | Take exactly as prescribed, with or without food. · Do not stop taking FLUXID without talking to your doctor, as stopping increases risk of blood clots. · You may bruise or bleed more easily; report any unusual bleeding such as blood in urine or stool, or coughing up blood. · If you miss a dose, take it as soon as you remember on the same day; if it is almost time for next dose, skip the missed dose and resume regular schedule. Do not double dose. · Tell all healthcare providers, including dentists, that you take this blood thinner. · Carry a medication card with your FLUXID dose and medical history. |