LYPQOZET
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LYPQOZET (LYPQOZET).
LYPQOZET is a selective serotonin reuptake inhibitor (SSRI) that potentiates serotonergic activity in the central nervous system by inhibiting the reuptake of serotonin at the presynaptic serotonin transporter, leading to increased synaptic levels of serotonin.
| Metabolism | Hepatic via CYP2D6, CYP3A4, and CYP2C19. Major metabolite: norLYPQOZET (active). |
| Excretion | Primarily renal (75% unchanged) and fecal/biliary (20% as metabolites); <5% unchanged in feces. |
| Half-life | Terminal elimination half-life is 22-28 hours in adults, allowing once-daily dosing. Extended half-life supports sustained therapeutic levels. |
| Protein binding | 95-98% bound primarily to albumin, with minor binding to α1-acid glycoprotein. |
| Volume of Distribution | 3-5 L/kg, indicating extensive tissue distribution with high concentrations in liver and kidney. |
| Bioavailability | Oral: 90% (high bioavailability with minimal first-pass effect). |
| Onset of Action | Oral: 1-2 hours; IV: 5-10 minutes. |
| Duration of Action | 24 hours (oral), allowing once-daily dosing. Duration may extend in renal impairment. |
| Molecular Weight | 425.5 |
Oral, 75 mg once daily.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min. For GFR <30 mL/min, use 50 mg once daily. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: 50 mg once daily. Child-Pugh C: Not recommended. |
| Pediatric use | Not established in patients <18 years. |
| Geriatric use | No specific dose adjustment, but monitor renal function at baseline and periodically. |
| 1st trimester | Insufficient human data; animal studies suggest risk. Avoid unless benefit outweighs risk. |
| 2nd trimester | Use only if clearly needed; monitor fetal growth. |
| 3rd trimester | May cause adverse effects in the neonate; avoid near term. |
Clinical note
Comprehensive clinical and safety monograph for LYPQOZET (LYPQOZET).
| Placental transfer | Crosses placenta; extent unknown but likely moderate based on molecular weight. |
| Breastfeeding | Excreted in breast milk in low amounts; monitor infant for potential adverse effects. Consider discontinuing breastfeeding if high maternal doses required. |
| Lactation Rating |
■ FDA Black Box Warning
WARNING: SUICIDAL THOUGHTS AND BEHAVIORS - Antidepressants increased the risk of suicidal thoughts and behavior in children, adolescents, and young adults in short-term trials. Closely monitor for clinical worsening, suicidality, or unusual changes in behavior.
| Serious Effects |
Hypersensitivity to LYPQOZET or componentsSevere hepatic impairmentConcomitant use with strong CYP3A4 inhibitors
| Precautions | Serotonin syndrome: Risk with co-administration of serotonergic drugs., Discontinuation syndrome: Gradual dose reduction recommended., Bleeding risk: Increased risk of gastrointestinal or other bleeding, especially with NSAIDs or anticoagulants., Hyponatremia: Especially in elderly or volume-depleted patients., Bone fracture: Increased risk observed in epidemiological studies., Angle-closure glaucoma: May trigger attack in patients with anatomically narrow angles. |
| Food/Dietary | Avoid grapefruit products as they increase systemic exposure. High-fat meals may reduce absorption; take on an empty stomach 1 hour before or 2 hours after meals. Avoid alcohol. |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | First trimester: Major congenital malformations including neural tube defects, cardiovascular anomalies; Second trimester: Growth restriction, oligohydramnios; Third trimester: Preterm labor, placental insufficiency. |
| Fetal Monitoring | Maternal: Blood pressure, renal function, hepatic enzymes; Fetal: Ultrasound for growth and anatomy, amniotic fluid index, fetal heart rate monitoring. |
| Fertility Effects | May impair spermatogenesis and oogenesis; reversible upon discontinuation. |
| Clinical Pearls | LYPQOZET is a high-extraction-ratio hepatically cleared drug; dosage adjustment required in Child-Pugh B/C cirrhosis. Monitor INR if co-administered with warfarin due to CYP2C9 inhibition. Avoid in patients with active hepatitis or ALT >3x ULN. |
| Patient Advice | Take with a full glass of water. · Avoid grapefruit juice or grapefruit products. · Report any unusual bleeding or jaundice immediately. · Do not drink alcohol while taking this medication. · If you miss a dose, skip it; do not double the next dose. |