STIMATE
Clinical safety rating
cautionComprehensive clinical and safety monograph for STIMATE (STIMATE).
Comprehensive clinical and safety monograph for STIMATE (STIMATE).
Central diabetes insipidusPrimary nocturnal enuresisHemophilia A with factor VIII levels >5%von Willebrand disease (type 1)
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. |
| Molecular Weight | 1069.22 |
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 | Contraindicated due to risk of uterotonic effects and potential for miscarriage; vasoconstrictive properties may impair placental perfusion. |
| 2nd trimester | Not recommended; risk of uterine hyperstimulation and fetal hypoxia. |
| 3rd trimester | Contraindicated for induction of labor; risk of uterine rupture and fetal distress. |
Clinical note
Comprehensive clinical and safety monograph for STIMATE (STIMATE).
| Placental transfer | Desmopressin (STIMATE) is a synthetic analog of vasopressin; molecular weight ~1069 Da suggests potential for placental transfer. Evidence from animal studies and limited human data indicate placental crossing, though clinical significance is uncertain. |
| Breastfeeding | Excreted into breast milk in low amounts; however, due to potent vasoconstrictive and uterotonic effects, it is generally not recommended during breastfeeding. Use only if clearly needed and monitor infant for signs of vasoconstriction or gastrointestinal disturbances. |
| Lactation Rating | L3 - Moderately Safe |
| 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. |
| 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. |
■ FDA Black Box Warning
No FDA black box warning exists for STIMATE.
| Serious Effects |
Hypersensitivity to desmopressin or any component of the formulationHyponatremia or history of hyponatremiaSevere renal impairment (CrCl < 50 mL/min)Syndrome of inappropriate antidiuretic hormone secretion (SIADH)Acute or chronic polydipsia
| 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 |
| Food/Dietary | No specific food interactions. However, avoid excessive fluid intake (more than needed to satisfy thirst) while taking STIMATE to reduce risk of water intoxication and hyponatremia. For patients with nocturnal enuresis, restrict fluids 1 hour before bedtime. |
| Clinical Pearls | STIMATE (desmopressin acetate) is a synthetic analog of vasopressin used for diabetes insipidus and nocturnal enuresis. Monitor for hyponatremia, especially in patients with increased fluid intake, elderly, or those on medications that increase ADH (e.g., SSRIs, NSAIDs). Use with caution in patients with renal impairment, cardiovascular disease, or cystic fibrosis. Avoid use in patients with primary polydipsia or uncontrolled hypertension. For nocturnal enuresis, limit fluid intake 1 hour before dose. Start at lowest effective dose and titrate. Can be administered intranasally, orally, or intravenously. Intranasal route is not recommended for infants due to variable absorption. |
| Patient Advice | Take STIMATE exactly as prescribed; do not increase dose or frequency without consulting your doctor. · For nocturnal enuresis: avoid drinking fluids 1 hour before bedtime and use the bathroom before going to sleep. · Report signs of hyponatremia: headache, nausea, vomiting, confusion, muscle cramps, weakness, or seizures. · Do not use STIMATE if you have allergies to desmopressin or any ingredient in the formulation. · Inform your doctor if you are pregnant, breastfeeding, or have kidney disease, heart disease, or cystic fibrosis. · Store STIMATE at room temperature away from moisture and heat; do not freeze. · For intranasal spray: prime the pump before first use and when not used for 7 days. Blow nose gently before use and do not sniff deeply after spraying. · Do not share your medication with others. |
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