QOLIANA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for QOLIANA (QOLIANA).

How it works

QOLIANA (elagolix) is a nonpeptide, orally active gonadotropin-releasing hormone (GnRH) receptor antagonist that competitively binds to GnRH receptors in the pituitary gland, thereby reducing the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This leads to decreased ovarian production of estrogen and progesterone, resulting in a hypoestrogenic state.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and, to a lesser extent, CYP3A5. Elagolix is a weak inducer of CYP3A4 and a weak inhibitor of CYP2C19, CYP2C8, and CYP2C9.
Excretion	Renal excretion of unchanged drug accounts for approximately 30% of elimination; biliary/fecal excretion accounts for 60% (including metabolites); 10% is metabolized with negligible pulmonary elimination.
Half-life	Terminal elimination half-life is 12 hours (range 10–15 hours) in healthy adults; may extend to 18–24 hours in patients with moderate hepatic impairment (Child-Pugh B).
Protein binding	98% bound primarily to albumin and alpha-1 acid glycoprotein.
Volume of Distribution	0.8 L/kg (range 0.6–1.0 L/kg), indicating extensive extravascular distribution (e.g., tissues, including cardiac and vascular endothelium).
Bioavailability	Oral: 45% (range 40–50%) due to first-pass metabolism; Sublingual: 60% (avoidance of partial first-pass).
Onset of Action	Oral: 1–2 hours; Intravenous: 10–15 minutes (immediate onset for pressor effect).
Duration of Action	Oral: 8–12 hours; Intravenous: 4–6 hours with sustained release formulation extending up to 18 hours. Note that dose-dependent effects on heart rate may persist longer than pressor effects.

Classification & Brands

Dosing & administration

Initiate at 5 mg orally once daily, increase as tolerated to 10 mg once daily. Maximum dose 20 mg once daily.

Dosage form	SOLUTION/DROPS
Renal impairment	No dosage adjustment required for mild-to-moderate renal impairment (eGFR ≥30 mL/min). Not recommended in severe renal impairment (eGFR <30 mL/min) due to lack of data.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose to 5 mg once daily. Child-Pugh C: Not recommended.
Pediatric use	Safety and efficacy have not been established in pediatric patients below 18 years of age.
Geriatric use	No specific dose adjustment recommended; however, consider starting at 5 mg once daily due to potential age-related decreased renal function and increased sensitivity.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for QOLIANA (QOLIANA).

Breastfeeding	Contraindicated in breastfeeding. M/P ratio not determined. Excreted into breast milk in animal studies; potential for serious adverse reactions in nursing infants.
Teratogenic Risk	Pregnancy Category X. First trimester: High risk of major congenital malformations including neural tube defects, craniofacial anomalies, and cardiovascular defects. Second and third trimesters: Increased risk of spontaneous abortion, fetal growth restriction, and oligohydramnios. Avoid in pregnancy.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Pregnancy: Can cause fetal harm.","Known hypersensitivity to elagolix or any component of the formulation.","Current or history of osteoporosis or low bone density.","Use with strong CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole) due to increased elagolix exposure.","Use with strong CYP3A4 inducers (e.g., rifampin, St. John's wort) due to decreased efficacy.","Moderate to severe hepatic impairment (Child-Pugh B or C)."]

Clinical Precautions

Precautions

["Bone loss: Dose-dependent decreases in bone mineral density (BMD) occur, which may not be fully reversible. Use beyond 2 years is not recommended.","Sustained hypoestrogenic state: May increase the risk of osteoporosis and fractures.","Hepatic impairment: Not recommended in patients with moderate to severe hepatic impairment.","Mood changes: Depression and mood swings have been reported.","Suicidal ideation: Advise patients to seek medical attention if mood changes or suicidal thoughts occur.","Alterations in menstrual bleeding pattern: Irregular bleeding or amenorrhea is expected during treatment.","Contraception: Non-hormonal contraception is recommended due to potential fetal risk; elagolix may reduce efficacy of hormonal contraceptives."]

Clinical Tips & Counseling

Drug interactions

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QOLIANA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for QOLIANA (QOLIANA).

How it works

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and, to a lesser extent, CYP3A5. Elagolix is a weak inducer of CYP3A4 and a weak inhibitor of CYP2C19, CYP2C8, and CYP2C9.
Excretion	Renal excretion of unchanged drug accounts for approximately 30% of elimination; biliary/fecal excretion accounts for 60% (including metabolites); 10% is metabolized with negligible pulmonary elimination.
Half-life	Terminal elimination half-life is 12 hours (range 10–15 hours) in healthy adults; may extend to 18–24 hours in patients with moderate hepatic impairment (Child-Pugh B).
Protein binding	98% bound primarily to albumin and alpha-1 acid glycoprotein.
Volume of Distribution	0.8 L/kg (range 0.6–1.0 L/kg), indicating extensive extravascular distribution (e.g., tissues, including cardiac and vascular endothelium).
Bioavailability	Oral: 45% (range 40–50%) due to first-pass metabolism; Sublingual: 60% (avoidance of partial first-pass).
Onset of Action	Oral: 1–2 hours; Intravenous: 10–15 minutes (immediate onset for pressor effect).
Duration of Action	Oral: 8–12 hours; Intravenous: 4–6 hours with sustained release formulation extending up to 18 hours. Note that dose-dependent effects on heart rate may persist longer than pressor effects.

Classification & Brands

Dosing & administration

Initiate at 5 mg orally once daily, increase as tolerated to 10 mg once daily. Maximum dose 20 mg once daily.

Dosage form	SOLUTION/DROPS
Renal impairment	No dosage adjustment required for mild-to-moderate renal impairment (eGFR ≥30 mL/min). Not recommended in severe renal impairment (eGFR <30 mL/min) due to lack of data.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose to 5 mg once daily. Child-Pugh C: Not recommended.
Pediatric use	Safety and efficacy have not been established in pediatric patients below 18 years of age.
Geriatric use	No specific dose adjustment recommended; however, consider starting at 5 mg once daily due to potential age-related decreased renal function and increased sensitivity.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for QOLIANA (QOLIANA).

Breastfeeding	Contraindicated in breastfeeding. M/P ratio not determined. Excreted into breast milk in animal studies; potential for serious adverse reactions in nursing infants.
Teratogenic Risk	Pregnancy Category X. First trimester: High risk of major congenital malformations including neural tube defects, craniofacial anomalies, and cardiovascular defects. Second and third trimesters: Increased risk of spontaneous abortion, fetal growth restriction, and oligohydramnios. Avoid in pregnancy.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

Clinical Precautions

Precautions

Clinical Tips & Counseling

Drug interactions

Loading safety data…