STIMATE (NEEDS NO REFRIGERATION)
Clinical safety rating: caution
Comprehensive clinical and safety monograph for STIMATE (NEEDS NO REFRIGERATION) (STIMATE (NEEDS NO REFRIGERATION)).
Desmopressin is a synthetic analogue of vasopressin (antidiuretic hormone) that increases cyclic AMP levels in renal collecting duct cells, enhancing water reabsorption and concentrating urine. It also raises plasma levels of von Willebrand factor and factor VIII by stimulating release from endothelial stores.
| Metabolism | Primarily metabolized by the liver via reduction of the disulfide bridge by glutathione, and to a lesser extent by proteolysis. The metabolite is not active. Excretion: renal (filtration and tubular secretion). |
| Excretion | Renal excretion of intact drug and metabolites accounts for >90% of elimination; biliary/fecal excretion is minimal (<5%). |
| Half-life | Terminal elimination half-life is 2-4 hours (mean 3 hours), which supports a dosing interval of 2-4 hours in clinical use. |
| Protein binding | Plasma protein binding is approximately 50-60%, primarily to albumin and to a lesser extent alpha-1 acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 0.2-0.4 L/kg, indicating moderate distribution into total body water and some tissue binding. |
| Bioavailability | Intranasal: 10-20%; Intravenous: 100%; Sublingual: 5-10%; Oral: <1% (extensive first-pass metabolism). |
| Onset of Action | Intranasal: 10-30 minutes; Intravenous: 1-5 minutes; Sublingual: 15-30 minutes; Oral: 30-60 minutes. |
| Duration of Action | Intranasal/IV: 2-4 hours; Sublingual/Oral: 3-6 hours; duration is dose-dependent and may be prolonged in hepatic impairment. |
Intranasal: 1 spray (1.5 mg) into one nostril; may repeat once after 30-60 minutes if needed. Not to exceed 2 doses per bleeding episode.
| Dosage form | SPRAY, METERED |
| Renal impairment | No dose adjustment required for renal impairment. Insufficient data for GFR-based modifications. |
| Liver impairment | No specific Child-Pugh based dose adjustments available. Use with caution in severe hepatic impairment. |
| Pediatric use | Intranasal: <50 kg: 1 spray (1.5 mg) into one nostril; ≥50 kg: same as adult. May repeat once after 30-60 minutes. |
| Geriatric use | No specific dose adjustment recommended. Monitor for adverse effects due to potential comorbidities and concomitant medications. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for STIMATE (NEEDS NO REFRIGERATION) (STIMATE (NEEDS NO REFRIGERATION)).
| Breastfeeding | Desmopressin is excreted into human breast milk in very small amounts. The milk-to-plasma (M/P) ratio is not well established but is estimated to be less than 0.1 based on available data. At therapeutic doses, it is unlikely to affect the nursing infant. However, caution is recommended due to potential for water retention and hyponatremia in the infant. Use only if clearly needed. |
| Teratogenic Risk | Desmopressin is a synthetic analog of vasopressin. Available data in pregnant women are insufficient to determine drug-associated risk of major birth defects and miscarriage. In animal studies, no teratogenic effects were observed at doses up to 100 times the human dose. Desmopressin does not cross the placenta in significant amounts due to its large molecular weight and enzymatic degradation. During the first trimester, theoretical risk of hyponatremia and seizures in the fetus if maternal hyponatremia occurs. In the second and third trimesters, increased uterine contractility has been reported in some cases. Overall, desmopressin is considered low risk, but caution is advised. |
■ FDA Black Box Warning
WARNING: HYPONATREMIA and SEIZURES. Desmopressin can cause severe hyponatremia, which may be life-threatening if not promptly treated. Seizures have been reported. Risk is increased in patients with fluid or electrolyte imbalances, cystic fibrosis, heart failure, or those on medications that increase hyponatremia risk.
| Serious Effects |
["Hypersensitivity to desmopressin or any component of the formulation","Moderate to severe renal impairment (creatinine clearance <50 mL/min)","Hyponatremia or history of hyponatremia","Primary nocturnal enuresis in patients with polydipsia or excessive fluid intake","Uncontrolled hypertension","Coronary artery disease of any cause","Thrombotic states (e.g., deep vein thrombosis, pulmonary embolism)","Patients on medications that increase hyponatremia risk (e.g., SSRIs, NSAIDs, diuretics) unless closely monitored"]
| Precautions | ["Hyponatremia and seizures: monitor serum sodium in patients at high risk; avoid excessive fluid intake.","Cardiovascular: caution in patients with coronary artery disease or hypertension, as increased blood pressure or ischemia may occur.","Fluid retention: avoid in patients with conditions predisposing to fluid overload (e.g., heart failure).","Thrombotic events: use cautiously in patients with risk factors for thrombosis (e.g., advanced atherosclerosis, smoking, oral contraceptives).","Renal impairment: dose reduction may be necessary; monitor renal function.","Cystic fibrosis: increased risk of hyponatremia and seizures.","Hypersensitivity: anaphylactic reactions reported; discontinue if allergic reaction occurs."] |
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| Fetal Monitoring | Monitor serum sodium levels regularly to detect hyponatremia, especially in patients with increased water intake or during treatment for central diabetes insipidus. In pregnancy, monitor blood pressure and urine output. Assess for signs of fluid overload. Fetal monitoring via ultrasound for growth and amniotic fluid index if used long-term. |
| Fertility Effects | No known adverse effects on human fertility. Desmopressin is used to treat central diabetes insipidus and nocturia, and does not interfere with reproductive hormone axes. Animal studies show no impairment of fertility. |