LYPQOZET

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LYPQOZET (LYPQOZET).

How it works

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.

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for LYPQOZET (LYPQOZET).

Breastfeeding	Excreted in breast milk; M/P ratio 1.2. Avoid breastfeeding due to potential neonatal toxicity.
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.

Warnings & precautions

■ 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.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Concomitant use of MAOIs (monoamine oxidase inhibitors) or within 14 days of MAOI discontinuation.","Hypersensitivity to LYPQOZET or any inactive ingredient.","Concomitant use of linezolid or intravenous methylene blue (due to risk of serotonin syndrome)."]

Clinical Precautions

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."]

Clinical Tips & Counseling

Drug interactions

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LYPQOZET

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LYPQOZET (LYPQOZET).

How it works

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for LYPQOZET (LYPQOZET).

Breastfeeding	Excreted in breast milk; M/P ratio 1.2. Avoid breastfeeding due to potential neonatal toxicity.
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.