STIMATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for STIMATE (STIMATE).
Desmopressin acetate is a synthetic analog of the natural pituitary hormone 8-arginine vasopressin (ADH). It acts as a V2 receptor agonist in the renal collecting ducts, increasing water permeability and promoting water reabsorption, thereby reducing urine output. It also increases plasma levels of von Willebrand factor and factor VIII via V2 receptor stimulation on endothelial cells.
| Metabolism | Not extensively metabolized; primarily excreted unchanged in urine. A small fraction may be metabolized by liver or kidney peptidases. |
| Excretion | Desmopressin is primarily excreted renally, with approximately 60-70% of the dose recovered unchanged in urine within 24 hours. The remaining fraction is metabolized hepatically and eliminated via feces. |
| Half-life | Terminal elimination half-life is approximately 3-4 hours in healthy adults, but may be prolonged in patients with renal impairment or in older adults. |
| Protein binding | Desmopressin exhibits low protein binding, approximately 1-2%, primarily to albumin. |
| Volume of Distribution | Volume of distribution is 0.2-0.4 L/kg, indicating distribution primarily in extracellular fluid. |
| Bioavailability | Intranasal: 10-20%; Oral: 5-10% due to extensive first-pass metabolism. |
| Onset of Action | Intranasal: 30-60 minutes; Intravenous: 15-30 minutes; Oral: 1-2 hours. |
| Duration of Action | Antidiuretic effect lasts 8-12 hours after intranasal or intravenous administration, and 6-8 hours after oral administration. Duration may vary based on renal function and fluid intake. |
Intranasal: 1 spray (1.5 mg) into one nostril, 1 hour prior to voiding or on awakening for bedwetting; maximum 2 sprays per day.
| Dosage form | SPRAY, METERED |
| Renal impairment | No specific adjustment; caution in severe impairment (eGFR <15 mL/min). |
| Liver impairment | No specific adjustment; limited data in Child-Pugh C; use cautiously. |
| Pediatric use | Children ≥6 years: same as adult; intranasal 1 spray (1.5 mg) 1 hour before bedtime. Do not exceed 2 sprays per day. |
| Geriatric use | Use caution due to risk of hyponatremia and hypertension; start at lowest effective dose. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for STIMATE (STIMATE).
| Breastfeeding | Desmopressin is excreted in breast milk in low amounts; M/P ratio not established. No adverse effects reported in infants. Use with caution, especially in nursing mothers with preeclampsia due to potential for water intoxication. |
| Teratogenic Risk | Pregnancy Category X. Desmopressin (STIMATE) is contraindicated in pregnancy due to risk of uterine contractions and potential fetal harm. First trimester: No adequate studies; theoretical risk of teratogenicity. Second trimester: Avoid due to risk of preterm labor. Third trimester: May induce premature labor; use only if clearly needed for diabetes insipidus. |
■ FDA Black Box Warning
No FDA black box warning exists for STIMATE.
| Serious Effects |
["Hypersensitivity to desmopressin or any component","Moderate to severe renal impairment (CrCl <50 mL/min)","Hyponatremia or history of hyponatremia","Known platelet-type von Willebrand disease (pseudo-von Willebrand disease)","Unstable angina, decompensated heart failure, or severe coronary artery disease"]
| Precautions | ["Hyponatremia and fluid overload with water intoxication","Seizures due to hyponatremia","Thrombotic events (in patients with predisposing factors)","Caution in patients with cystic fibrosis, coronary artery disease, or hypertension","Risk of arterial or venous thrombosis, especially with desmopressin treatment for bleeding disorders","Elderly patients at increased risk of hyponatremia"] |
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| Fetal Monitoring | Monitor maternal blood pressure, urine output, serum sodium, weight, and signs of water intoxication (headache, nausea, confusion). Fetal monitoring via ultrasound for growth and amniotic fluid index if used in pregnancy. Assess uterine activity for preterm labor. |
| Fertility Effects | No known adverse effects on human fertility. Desmopressin does not affect spermatogenesis or ovulation. In animal studies, no impairment of fertility observed. |