NOCTIVA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NOCTIVA (NOCTIVA).
Desmopressin is a synthetic analog of vasopressin (antidiuretic hormone) that binds to V2 receptors in the renal collecting ducts, increasing water reabsorption and reducing urine volume.
| Metabolism | Primarily metabolized in the liver by disulfide bond reduction; CYP450 enzymes not significantly involved. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 70% of the dose; fecal elimination constitutes about 20%, with the remainder as metabolites. |
| Half-life | Terminal elimination half-life is 2-4 hours (mean 3.2 hours) in adults with normal renal function; prolonged to 6-9 hours in moderate renal impairment (CrCl 30-50 mL/min). |
| Protein binding | Approximately 40% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 1.0-1.5 L/kg, indicating extensive distribution into tissues. |
| Bioavailability | Oral: 10-20% due to extensive first-pass metabolism; transdermal: 30-50% with variable absorption. |
| Onset of Action | Intravenous: within 1 minute; oral: 30-45 minutes; transdermal: 2-4 hours. |
| Duration of Action | Intravenous: 20-30 minutes; oral: 4-6 hours; transdermal: 72 hours (patch applied every 72 hours). |
Desmopressin acetate: 1-2 sprays (10-20 mcg) intranasally once daily at bedtime; or 0.1-0.2 mg orally once daily at bedtime.
| Dosage form | SPRAY, METERED |
| Renal impairment | GFR < 50 mL/min: contraindicated. GFR 50-90 mL/min: use with caution, monitor for hyponatremia. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: contraindicated. |
| Pediatric use | Nocturnal enuresis: 6-12 years: 0.2 mg orally at bedtime; 12+ years: same as adult. Intranasal: 1 spray (10 mcg) per nostril at bedtime for ≥6 years. |
| Geriatric use | Start at 0.1 mg orally at bedtime; monitor serum sodium within 1 week due to increased risk of hyponatremia. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for NOCTIVA (NOCTIVA).
| Breastfeeding | Not recommended. M/P ratio unknown; drug may pass into breast milk and cause infant bradycardia or hypotension. |
| Teratogenic Risk | Pregnancy Category C. First trimester: No adequate human studies; animal studies show fetal harm. Second/third trimester: Risk of fetal bradycardia, hypoglycemia, and respiratory depression if used near term. |
| Fetal Monitoring | Continuous fetal heart rate monitoring during use; maternal blood pressure, heart rate, oxygen saturation, and respiratory status. Monitor for signs of uterine hyperstimulation. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to desmopressin or any component","Moderate to severe renal impairment (CrCl <50 mL/min)","Hyponatremia or history of hyponatremia","Polydipsia (primary or psychogenic)","Decompensated heart failure"]
| Precautions | ["Risk of hyponatremia and water intoxication, especially in elderly and patients with polydipsia","Monitor serum sodium in patients with fluid/electrolyte imbalances","Increased risk of thrombotic events in patients with cardiovascular disease","Allergic reactions possible","Use with caution in patients with cystic fibrosis or renal impairment"] |
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| Fertility Effects | No formal studies in humans. Animal studies suggest no significant effect on fertility. |