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) |
| Molecular Weight | 500.5 |
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 | Avoid; associated with fetal malformations in animal studies. |
| 2nd trimester | Avoid; potential for fetal toxicity. |
| 3rd trimester | Avoid; risk of neonatal hemorrhage. |
Clinical note
Comprehensive clinical and safety monograph for VOSTALLY (VOSTALLY).
| Placental transfer | High degree of placental transfer observed in animal models. |
| Breastfeeding | Excreted in breast milk; potential for serious adverse reactions in nursing infants. Discontinue drug or nursing. |
| Lactation Rating | L5 |
■ FDA Black Box Warning
There is no FDA black box warning for desmopressin.
| Serious Effects |
PregnancyHistory of hypersensitivity to Vostally or any excipient
| 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 |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they inhibit CYP3A4 metabolism, increasing Vostally levels and risk of toxicity. Limit alcohol intake as it may exacerbate CNS depression and increase the risk of liver toxicity. No significant interaction with high-fat meals; however, taking with food may reduce nausea. |
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| 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 | 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. |
| Clinical Pearls | Vostally (fictitious drug) is a high-affinity serotonin-norepinephrine reuptake inhibitor (SNRI) with a rapid onset of action (within 3-5 days). Monitor for serotonin syndrome when co-prescribed with other serotonergic agents. Abrupt discontinuation may cause withdrawal symptoms such as dizziness, nausea, and paresthesias; taper over 2-4 weeks. Use with caution in patients with uncontrolled hypertension due to dose-dependent blood pressure elevation. May cause mild platelet dysfunction; consider bleeding risk in surgical patients. |
| Patient Advice | Take Vostally at the same time each day to maintain steady blood levels. · Do not stop taking Vostally suddenly; a gradual dose reduction is necessary to avoid withdrawal symptoms. · Report any signs of serotonin syndrome (e.g., agitation, hallucinations, rapid heart rate, fever, muscle stiffness) immediately. · Avoid driving or operating heavy machinery until you know how Vostally affects you, as it may cause drowsiness or dizziness. · Inform your healthcare provider of all medications you are taking, including over-the-counter drugs and supplements, to avoid interactions. |