VIBISONE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VIBISONE (VIBISONE).
VIBISONE (budesonide) is a corticosteroid with potent glucocorticoid activity that binds to the glucocorticoid receptor, leading to inhibition of pro-inflammatory mediators such as cytokines and chemokines, and suppression of immune cell activation.
| Metabolism | Metabolized primarily via CYP3A4 to its major metabolite, 16α-hydroxyprednisolone, which has negligible glucocorticoid activity. |
| Excretion | Primarily renal excretion of unchanged drug (65%) and metabolites (25%); biliary/fecal elimination accounts for 10%. |
| Half-life | Terminal elimination half-life of 12-15 hours in patients with normal renal function; prolonged to 24-30 hours in moderate renal impairment (CrCl <50 mL/min). |
| Protein binding | 98% bound, primarily to albumin. |
| Volume of Distribution | 0.8 L/kg, indicating moderate tissue distribution. |
| Bioavailability | Oral: 45% due to extensive first-pass metabolism; Intravenous: 100%. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes. |
| Duration of Action | Oral: 8-12 hours; Intravenous: 6-10 hours. Duration may be extended in hepatic impairment. |
Adults: 5 mg orally once daily with or without food.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-89 mL/min: No adjustment. GFR <30 mL/min: Not recommended. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose to 2.5 mg once daily. Child-Pugh C: Not recommended. |
| Pediatric use | Not approved for pediatric use; no established dosing. |
| Geriatric use | No dose adjustment required; monitor for renal function and potential hypotension. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VIBISONE (VIBISONE).
| Breastfeeding | Contraindicated during breastfeeding. VIBISONE is excreted in human milk with an estimated M/P ratio of 0.8. Potential for serious adverse reactions in nursing infants, including immunosuppression and growth suppression. |
| Teratogenic Risk | FDA Pregnancy Category X. First trimester: significant risk of major congenital malformations, including neural tube defects, craniofacial anomalies, and cardiac defects. Second and third trimesters: increased risk of spontaneous abortion, intrauterine growth restriction, and fetal death. Contraindicated in pregnancy. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to budesonide or any component of the formulation.","Patients with known or suspected systemic infections (e.g., untreated tuberculosis, fungal, bacterial, viral, or parasitic infections) unless specific anti-infective therapy is administered."]
| Precautions | ["Hypothalamic-pituitary-adrenal (HPA) axis suppression, particularly at higher doses or prolonged use.","Increased risk of infections, including tuberculosis, fungal, bacterial, viral, or parasitic infections.","Systemic corticosteroid effects such as Cushing's syndrome, hyperglycemia, and psychiatric disturbances.","May mask signs of infection or decrease resistance to new infections.","Monitor for growth suppression in pediatric patients.","Use with caution in patients with osteoporosis, hypertension, diabetes, or glaucoma."] |
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| Fetal Monitoring |
| Monitor maternal complete blood count, liver function tests, and renal function monthly. Perform fetal ultrasound for growth and anatomy at 18-20 weeks and monthly thereafter. Assess amniotic fluid index weekly from 32 weeks. |
| Fertility Effects | VIBISONE may impair fertility in males and females. In males, reversible oligospermia or azoospermia. In females, anovulation and menstrual irregularities. Effects are dose-dependent and may persist after discontinuation. |