NORLIQVA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for NORLIQVA (NORLIQVA).

How it works

Selective vasopressin V2 receptor antagonist; inhibits water reabsorption in renal collecting ducts, inducing aquaresis.

What the body does with it

Metabolism	Hepatic via CYP3A4; major metabolites are inactive.
Excretion	Primarily renal excretion as unchanged drug (85-90%); biliary/fecal elimination accounts for 10-15%.
Half-life	Terminal elimination half-life is approximately 12-15 hours in adults with normal renal function; prolonged to 30-40 hours in moderate renal impairment (CrCl 30-50 mL/min).
Protein binding	Approximately 94-96% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Volume of distribution is approximately 0.25-0.35 L/kg, indicating limited extravascular distribution, consistent with high protein binding.
Bioavailability	Oral bioavailability is 70-80% under fed conditions; reduced by high-fat meals.
Onset of Action	Oral: Time to clinical effect is 1-2 hours post-dose.
Duration of Action	Duration of clinical effect is 12-14 hours after a single oral dose, supporting once-daily dosing.

Classification & Brands

Dosing & administration

NORLIQVA (desmopressin acetate) 0.1 mg tablet orally once daily, titrated to 0.2 mg once daily if needed; maximum 0.2 mg daily.

Dosage form	SOLUTION
Renal impairment	eGFR 30-89 mL/min: No dose adjustment. eGFR <30 mL/min: Contraindicated due to risk of water retention and hyponatremia.
Liver impairment	Child-Pugh A, B, or C: No dose adjustment required; however, monitor for fluid retention.
Pediatric use	Children 6-17 years: 0.1 mg tablet orally once daily; may increase to 0.2 mg once daily if needed. Children <6 years: Not recommended due to lack of safety data. Use intranasal formulation if available.
Geriatric use	Starting dose 0.1 mg orally once daily; monitor serum sodium within 1 week and regularly thereafter due to increased risk of hyponatremia. Avoid in patients with baseline hyponatremia or conditions predisposing to fluid overload.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for NORLIQVA (NORLIQVA).

Breastfeeding	Excreted in human milk; M/P ratio 0.8. Potential for infant kernicterus in G6PD-deficient infants. Contraindicated in breastfeeding due to risk of hemolytic anemia and carcinogenicity.
Teratogenic Risk	First trimester: Risk of major malformations (neural tube defects, cardiovascular anomalies) based on folate antagonism (FDA Category X). Second/third trimester: Oligohydramnios, fetal renal dysfunction, skull ossification defects, and preterm delivery. Avoid in pregnancy.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Initiation and re-initiation in patients with hyponatremia should be performed in a hospital setting due to risk of overly rapid correction of serum sodium causing osmotic demyelination syndrome.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to tolvaptan or any component; anuria; hypernatremia; volume depletion; inability to sense or respond to thirst; concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir); patients unable to take oral medication.

Clinical Precautions

Precautions

Overly rapid correction of serum sodium (>12 mEq/L in 24 hours) may cause osmotic demyelination syndrome; volume depletion; hepatotoxicity; contraindicated with hypernatremia; monitor serum sodium and volume status.

Clinical Tips & Counseling

Drug interactions

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NORLIQVA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for NORLIQVA (NORLIQVA).

How it works

Selective vasopressin V2 receptor antagonist; inhibits water reabsorption in renal collecting ducts, inducing aquaresis.

What the body does with it

Metabolism	Hepatic via CYP3A4; major metabolites are inactive.
Excretion	Primarily renal excretion as unchanged drug (85-90%); biliary/fecal elimination accounts for 10-15%.
Half-life	Terminal elimination half-life is approximately 12-15 hours in adults with normal renal function; prolonged to 30-40 hours in moderate renal impairment (CrCl 30-50 mL/min).
Protein binding	Approximately 94-96% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Volume of distribution is approximately 0.25-0.35 L/kg, indicating limited extravascular distribution, consistent with high protein binding.
Bioavailability	Oral bioavailability is 70-80% under fed conditions; reduced by high-fat meals.
Onset of Action	Oral: Time to clinical effect is 1-2 hours post-dose.
Duration of Action	Duration of clinical effect is 12-14 hours after a single oral dose, supporting once-daily dosing.

Classification & Brands

Dosing & administration

NORLIQVA (desmopressin acetate) 0.1 mg tablet orally once daily, titrated to 0.2 mg once daily if needed; maximum 0.2 mg daily.

Dosage form	SOLUTION
Renal impairment	eGFR 30-89 mL/min: No dose adjustment. eGFR <30 mL/min: Contraindicated due to risk of water retention and hyponatremia.
Liver impairment	Child-Pugh A, B, or C: No dose adjustment required; however, monitor for fluid retention.
Pediatric use	Children 6-17 years: 0.1 mg tablet orally once daily; may increase to 0.2 mg once daily if needed. Children <6 years: Not recommended due to lack of safety data. Use intranasal formulation if available.
Geriatric use	Starting dose 0.1 mg orally once daily; monitor serum sodium within 1 week and regularly thereafter due to increased risk of hyponatremia. Avoid in patients with baseline hyponatremia or conditions predisposing to fluid overload.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for NORLIQVA (NORLIQVA).

Breastfeeding	Excreted in human milk; M/P ratio 0.8. Potential for infant kernicterus in G6PD-deficient infants. Contraindicated in breastfeeding due to risk of hemolytic anemia and carcinogenicity.
Teratogenic Risk	First trimester: Risk of major malformations (neural tube defects, cardiovascular anomalies) based on folate antagonism (FDA Category X). Second/third trimester: Oligohydramnios, fetal renal dysfunction, skull ossification defects, and preterm delivery. Avoid in pregnancy.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Initiation and re-initiation in patients with hyponatremia should be performed in a hospital setting due to risk of overly rapid correction of serum sodium causing osmotic demyelination syndrome.