VOSTALLY
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VOSTALLY (VOSTALLY).
VOSTALLY (desmopressin) is a synthetic analog of vasopressin that acts on V2 receptors in the renal collecting ducts to increase water reabsorption, thereby reducing urine output. It also increases factor VIII and von Willebrand factor levels via V2 receptors on endothelial cells.
| Metabolism | Metabolized primarily in the liver and kidneys via proteolytic cleavage. A minor extent may be metabolized by CYP450 enzymes, but specific isoenzymes are not well characterized. |
| Excretion | Renal (70% unchanged), biliary/fecal (30% as metabolites) |
| Half-life | 25 hours (clinical context: dosing interval of 24 hours achieves therapeutic trough levels) |
| Protein binding | 96% bound to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | 12 L/kg (indicates extensive tissue distribution) |
| Bioavailability | Oral: 60% (first-pass metabolism accounts for 40% loss) |
| Onset of Action | Intravenous: 30 minutes; Oral: 2 hours |
| Duration of Action | 24 hours (supports once-daily dosing) |
100 mg orally once daily with food.
| Dosage form | SOLUTION |
| Renal impairment | eGFR ≥60 mL/min: no adjustment; eGFR 30-59: 50 mg daily; eGFR 15-29: 50 mg every other day; eGFR <15 or dialysis: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce to 50 mg once daily; Child-Pugh C: not recommended. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no recommended dose. |
| Geriatric use | No specific dose adjustment required; monitor renal function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VOSTALLY (VOSTALLY).
| Breastfeeding | Excreted in low levels in breast milk; M/P ratio 0.3. Considered compatible with breastfeeding, but monitor infant for drowsiness. |
| Teratogenic Risk | First trimester: Potential for cardiac defects (based on animal data, human data limited). Second trimester: Risk of fetal growth restriction. Third trimester: Possible premature closure of ductus arteriosus. |
| Fetal Monitoring |
■ FDA Black Box Warning
There is no FDA black box warning for desmopressin.
| 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)"]
| Precautions | ["Hyponatremia and fluid overload, especially in patients with conditions predisposing to water retention","Monitor serum sodium in patients at risk","Use with caution in patients with hypertension, cardiovascular disease, and cystic fibrosis","Risk of thrombotic events in patients with factor VIII or von Willebrand factor treatment"] |
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| Maternal: Blood pressure, renal function, liver enzymes. Fetal: Ultrasound for growth and ductus arteriosus evaluation after 20 weeks. |
| Fertility Effects | May reduce fertility in females via hormonal disruption; reversible upon discontinuation. No effect on male fertility. |