DESMOPRESSIN ACETATE PRESERVATIVE FREE
Clinical safety rating: safe
Other drugs that may increase the risk of water intoxication and hyponatremia Can cause hyponatremia and water intoxication monitor sodium levels.
Synthetic analog of antidiuretic hormone (ADH, vasopressin) that binds to V2 receptors in renal collecting ducts, increasing water permeability and reabsorption, thereby reducing urine volume and increasing urine osmolality. Also increases factor VIII and von Willebrand factor levels via V2 receptor activation on endothelial cells.
| Metabolism | Primarily metabolized by reduction of the disulfide bond to form inactive metabolites. Not significantly metabolized by CYP450 enzymes. Minor degradation by peptidases. |
| Excretion | Primarily renal (filtration and tubular secretion); approximately 60-70% of the administered dose is excreted unchanged in urine; minor biliary/fecal elimination (<5%). |
| Half-life | 1.5-2.5 hours (terminal elimination half-life); prolonged in renal impairment (up to 5-6 hours in severe renal failure). |
| Protein binding | Low; approximately 30-40% bound mainly to serum albumin. |
| Volume of Distribution | Approximately 0.3-0.5 L/kg; reflects distribution primarily in extracellular fluid with limited tissue binding. |
| Bioavailability | Intranasal: 5-15% (mean 10%); Oral: 0.1-1% (mean 0.5%); Subcutaneous: 100% (bioequivalent to intravenous). |
| Onset of Action | Intravenous: 15-30 minutes; Intranasal: 30-60 minutes; Oral: 60-120 minutes; Subcutaneous: 30-60 minutes. |
| Duration of Action | Antidiuretic effect: 6-24 hours (intravenous/intranasal), 6-12 hours (oral); dose-dependent; hemostatic effect: 6-8 hours (intravenous). |
0.2-0.4 mg (200-400 mcg) orally once daily at bedtime, or 0.1-0.2 mg (100-200 mcg) orally two to three times daily. Alternatively, 1-4 mcg (0.001-0.004 mg) intravenously or subcutaneously once daily.
| Dosage form | INJECTABLE |
| Renal impairment | eGFR <50 mL/min: avoid use due to risk of water intoxication. eGFR 50-90 mL/min: reduce dose by 50% and monitor serum sodium. No adjustment for eGFR >90 mL/min. |
| Liver impairment | No specific dose adjustment recommended for Child-Pugh Class A or B; caution and monitoring advised due to potential fluid retention. Child-Pugh Class C: use with extreme caution, reduce dose by 50%. |
| Pediatric use | Central diabetes insipidus: 0.1-1.2 mg (100-1200 mcg) orally daily, divided into 2-3 doses; or 0.4-2 mcg (0.4-2 mcg) IV/SC once daily. Primary nocturnal enuresis: 0.2-0.6 mg (200-600 mcg) orally at bedtime; start at 0.2 mg and titrate. No weight-based dosing recommended; adjust based on response and serum sodium. |
| Geriatric use | Start at lowest dose (0.1 mg orally once daily) and titrate slowly. Monitor serum sodium and fluid balance closely due to increased risk of hyponatremia and water intoxication. Avoid in patients with eGFR <50 mL/min. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Other drugs that may increase the risk of water intoxication and hyponatremia Can cause hyponatremia and water intoxication monitor sodium levels.
| FDA category | Animal |
| Breastfeeding | Desmopressin is excreted into breast milk in very low concentrations (M/P ratio approximately 0.1–0.3), unlikely to affect the nursing infant. No adverse effects have been reported. It is considered compatible with breastfeeding; however, monitor the infant for signs of hyponatremia (irritability, seizures) if the mother requires high doses. |
| Teratogenic Risk |
■ FDA Black Box Warning
None
| Common Effects | enuresis |
| Serious Effects |
["Hypersensitivity to desmopressin or any component of the formulation","Moderate to severe renal impairment (CrCl <50 mL/min)","Hyponatremia or history of hyponatremia","Polydipsia (primary or psychogenic)","Uncontrolled hypertension or coronary artery disease (for intranasal formulations)"]
| Precautions | ["Risk of hyponatremia and water intoxication, especially with high doses or in patients with conditions predisposing to fluid overload","Seizures, coma, and death have been reported secondary to hyponatremia","Monitor serum sodium, urine output, and urine osmolality","Avoid fluid overload; restrict water intake in patients with normal thirst mechanism","Caution in patients with cardiovascular disease or hypertension due to possible pressor effects at high doses","Use with caution in patients with cystic fibrosis or other conditions associated with fluid/electrolyte imbalances"] |
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| Desmopressin acetate does not cross the placenta in significant amounts due to its high molecular weight and enzymatic degradation by placental aminopeptidases. No increased risk of major congenital malformations has been reported with first-trimester exposure. Late pregnancy use is not associated with fetal harm but may rarely cause maternal hyponatremia or uterine hyperstimulation (oxytocin-like effect). There is no evidence of teratogenicity in animal studies. FDA Pregnancy Category B (prior to 2015 removal of letter categories). |
| Fetal Monitoring | Monitor maternal serum sodium and urine osmolality at baseline and periodically during therapy, especially in patients at risk of hyponatremia (excessive fluid intake, concurrent medications). Assess maternal fluid balance (intake/output) and weight. Fetal monitoring: standard prenatal care; no specific fetal surveillance required unless signs of uterine contractions or preeclampsia develop. |
| Fertility Effects | No known direct effects on fertility in males or females. Desmopressin does not alter ovulation, spermatogenesis, or implantation. Use for central diabetes insipidus or nocturnal enuresis does not impair reproductive function. |
| Food/Dietary |
| No significant food interactions. However, avoid excessive fluid intake (e.g., water, juice) around dosing to reduce hyponatremia risk. Use caution with alcohol and caffeine due to diuretic effects. |
| Clinical Pearls | Desmopressin acetate (preservative-free) is a synthetic analog of vasopressin used for diabetes insipidus (central), nocturnal enuresis, and hemophilia A/von Willebrand disease (type I). Preservative-free formulation reduces risk of mucosal irritation. Monitor serum sodium and urine osmolality; risk of hyponatremia, especially in elderly and patients on thiazides or SSRIs. Administer intranasally (0.1-0.4 mL) or subcutaneously (2-4 mcg). Onset: 15-30 min intranasal, 30-60 min SQ. Duration: 6-12 hours. Avoid overhydration during treatment. For hemophilia, use with factor VIII monitoring. |
| Patient Advice | Use exactly as prescribed; do not increase dose without consulting your doctor. · Monitor fluid intake: drink only when thirsty to avoid low sodium levels (hyponatremia). · Report symptoms of hyponatremia: headache, nausea, vomiting, confusion, seizures. · For nocturnal enuresis: take last dose at bedtime and avoid fluids 1 hour before and 8 hours after. · Intranasal: use preservative-free spray as directed; do not share with others. · Contact healthcare provider if urination decreases or if you gain weight suddenly. · Store at room temperature; protect from light and freezing. |