PALSONIFY
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PALSONIFY (PALSONIFY).
Selective serotonin reuptake inhibitor (SSRI) that enhances serotonergic neurotransmission by blocking the reuptake of serotonin at the presynaptic neuron, thereby increasing extracellular serotonin levels in the brain.
| Metabolism | Primarily hepatic via CYP2D6 and CYP2C19 isoenzymes; major metabolite is norfluoxetine, which is equally potent and has a longer half-life. |
| Excretion | Renal: 65% unchanged; biliary/fecal: 30% as metabolites; 5% other |
| Half-life | Terminal half-life 12 hours (range 10–14 h) in healthy adults; prolonged to 24–30 h in severe renal impairment (CrCl <30 mL/min) |
| Protein binding | 92% bound to albumin and α1-acid glycoprotein |
| Volume of Distribution | 0.8 L/kg (total body water), indicating extensive tissue distribution |
| Bioavailability | Oral: 75% (range 60–85%) due to first-pass metabolism; IV: 100% |
| Onset of Action | Oral: 30–45 min; IV: 2–5 min |
| Duration of Action | 6–8 hours for oral; 4–6 hours for IV; extended in hepatic impairment due to reduced clearance |
| Molecular Weight | 425.6 |
70 mg/m2 IV every 3 weeks. Infusion over 60 minutes.
| Dosage form | TABLET |
| Renal impairment | GFR 30-89 mL/min: No adjustment. GFR 15-29 mL/min: Reduce dose to 50 mg/m2. GFR <15 mL/min or dialysis: Not recommended. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Reduce to 50 mg/m2. Child-Pugh C: Not recommended. |
| Pediatric use | 1-18 years: 70 mg/m2 IV every 3 weeks. Maximum dose 140 mg. |
| Geriatric use | No specific adjustment. Monitor renal function due to age-related decline. |
| 1st trimester | PALSONIFY is contraindicated in the first trimester due to teratogenic effects observed in animal studies. |
| 2nd trimester | Use only if maternal benefit outweighs fetal risk; may cause fetal harm based on animal data. |
| 3rd trimester | Avoid in third trimester due to risk of neonatal complications such as hypotension and renal impairment. |
Clinical note
Comprehensive clinical and safety monograph for PALSONIFY (PALSONIFY).
| Placental transfer | PALSONIFY crosses the placenta in significant amounts based on animal studies; human data limited but expected due to molecular weight. |
| Breastfeeding | PALSONIFY is excreted in human milk. Due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during treatment and for at least 2 weeks after the last dose. |
■ FDA Black Box Warning
Increased risk of suicidal thoughts and behavior in children, adolescents, and young adults taking antidepressants. Monitor closely for clinical worsening, suicidality, or unusual changes in behavior.
| Serious Effects |
Hypersensitivity to PALSONIFY or any excipientsPregnancySevere hepatic impairment (Child-Pugh Class C)Concurrent use with strong CYP3A4 inhibitors
| Precautions | Serotonin syndrome, risk of bleeding (especially with NSAIDs/aspirin), activation of mania/hypomania, QT prolongation, hyponatremia, and discontinuation syndrome upon abrupt withdrawal. |
| Food/Dietary | Avoid grapefruit and grapefruit juice, as they may increase drug levels. Limit alcohol intake; may increase risk of liver toxicity. |
Loading safety data…
| Lactation Rating |
| L5 - Contraindicated |
| Teratogenic Risk | PALSONIFY is classified as Pregnancy Category X based on human and animal studies demonstrating teratogenicity. First trimester exposure is associated with craniofacial defects, neural tube malformations, and cardiac anomalies. Second and third trimester exposure risks include fetal growth restriction, oligohydramnios, and premature closure of the ductus arteriosus. Use is contraindicated throughout pregnancy. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function, and liver enzymes monthly. Fetal ultrasound every 4 weeks for growth assessment and amniotic fluid volume. Perform fetal echocardiography if exposure occurs in first trimester. Obtain baseline and periodic complete blood counts due to risk of neutropenia. |
| Fertility Effects | PALSONIFY reduces fertility in both males and females. In females, it may disrupt menstrual cycles and inhibit ovulation. In males, it impairs spermatogenesis with reduction in sperm count and motility. Fertility effects may be reversible after discontinuation, but recovery time is variable. |
| Clinical Pearls | Monitor for QT prolongation with concurrent use of other QT-prolonging agents. Adjust dose in renal impairment (CrCl <30 mL/min: reduce by 50%). Watch for serotonin syndrome if combined with other serotonergic drugs. |
| Patient Advice | Take exactly as prescribed; do not double doses if missed. · Avoid driving until you know how this drug affects you due to possible dizziness. · Report any signs of bleeding (unusual bruising, dark stools) or infection (fever, sore throat). · Do not stop abruptly without consulting your doctor. |