GADAVIST
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GADAVIST (GADAVIST).
Gadovist (gadobutrol) is a macrocyclic gadolinium-based contrast agent (GBCA) that enhances MRI signal intensity by shortening T1 relaxation time in tissues with altered vascularity or blood-brain barrier integrity.
| Metabolism | Not metabolized; excreted unchanged via glomerular filtration in the kidneys. |
| Excretion | Primarily renal; approximately 95% of administered dose excreted unchanged in urine within 72 hours, with 85% eliminated within 6 hours. Less than 1% excreted in feces. |
| Half-life | Plasma terminal elimination half-life is approximately 1.5 hours in patients with normal renal function (GFR >60 mL/min/1.73m²). In renal impairment (GFR <30 mL/min/1.73m²), half-life extends to 10-15 hours; in end-stage renal disease, half-life may exceed 30 hours, necessitating adjustment of imaging timing. |
| Protein binding | Gadobutrol has negligible protein binding (<1%), primarily to albumin and globulins. |
| Volume of Distribution | Volume of distribution is approximately 0.20 L/kg (range 0.16-0.24 L/kg), consistent with extracellular fluid volume, indicating minimal tissue penetration or cellular uptake. |
| Bioavailability | Only administered intravenously; bioavailability is 100% by IV route. Oral bioavailability is negligible (not absorbed orally) and not clinically relevant. |
| Onset of Action | Intravenous administration: Enhancement of magnetic resonance imaging (MRI) signal intensity occurs immediately after injection, with optimal contrast visualization typically achieved within 2-5 minutes post-injection for central nervous system imaging and within 5-10 minutes for vascular or other body regions. |
| Duration of Action | Duration of clinically useful contrast enhancement is approximately 30-60 minutes for central nervous system imaging, with rapid clearance limiting utility beyond 90 minutes. Repeat dosing may be required for prolonged studies. |
0.1 mmol/kg (0.2 mL/kg) IV bolus; maximum dose 0.3 mmol/kg per imaging session.
| Dosage form | SOLUTION |
| Renal impairment | GFR ≥30 mL/min: no adjustment. GFR <30 mL/min or dialysis: contraindicated; do not administer. |
| Liver impairment | No specific dose adjustment recommended; caution with severe hepatic impairment due to potential gadolinium retention. |
| Pediatric use | 0.1 mmol/kg (0.2 mL/kg) IV bolus; maximum dose 0.3 mmol/kg. Approved for children ≥2 years. |
| Geriatric use | No specific adjustment; assess renal function (GFR) prior to use, as elderly patients are at increased risk of nephrogenic systemic fibrosis. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GADAVIST (GADAVIST).
| Breastfeeding | Gadobutrol is excreted into breast milk in very low amounts. M/P ratio is unknown. The manufacturer recommends discontinuing breastfeeding for 12-24 hours after administration to minimize infant exposure. |
| Teratogenic Risk | Gadovist (gadobutrol) is a gadolinium-based contrast agent. In the first trimester, there is theoretical risk of fetal harm due to gadolinium crossing the placenta; however, human data are limited. In the second and third trimesters, gadolinium exposure has been associated with increased risk of stillbirths, neonatal death, and possibly congenital anomalies in animal studies. Avoid use unless essential. |
■ FDA Black Box Warning
Nephrogenic systemic fibrosis (NSF) risk: Gadobutrol increases NSF risk in patients with acute or chronic severe renal insufficiency (eGFR <30 mL/min/1.73m²) or hepatorenal syndrome. Avoid use unless diagnostic information is essential and not available with non-contrast MRI or other modalities.
| Serious Effects |
["Absolute: History of severe hypersensitivity reaction to gadobutrol or any gadolinium-based contrast agent","Absolute: Acute or chronic severe renal insufficiency (eGFR <30 mL/min/1.73m²) unless dialysis is initiated and well-established","Relative: Moderate renal impairment (eGFR 30-59 mL/min/1.73m²) - consider risk/benefit; use lowest dose necessary"]
| Precautions | ["Nephrogenic systemic fibrosis (NSF) - screen all patients for acute or chronic renal impairment; avoid in severe renal impairment if possible","Hypersensitivity reactions including anaphylaxis - observe patient during and after injection; have emergency equipment available","Gadolinium retention - linear GBCAs have higher risk; macrocyclic agents like gadobutrol have lower but not zero retention risk","Contrast-induced acute kidney injury (CI-AKI) - rare, monitor renal function post-procedure in high-risk patients"] |
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| Fetal Monitoring | Monitor for allergic reactions. In pregnant patients, fetal monitoring may be considered after exposure. Assess renal function before use due to risk of nephrogenic systemic fibrosis. |
| Fertility Effects | No specific fertility effects reported in humans. Animal studies showed no impairment of fertility at clinically relevant doses. |