GADOBUTROL
Clinical safety rating: safe
Animal studies have demonstrated safety
Gadobutrol is a gadolinium-based contrast agent (GBCA) that shortens T1 relaxation time in magnetic resonance imaging (MRI), enhancing signal intensity in tissues where it distributes. It is a paramagnetic agent that increases the relaxation rate of water protons in the vicinity of the gadolinium ion.
| Metabolism | Gadobutrol is eliminated unchanged via glomerular filtration. No metabolism occurs; it is exclusively excreted by the kidneys. |
| Excretion | Primarily renal (90-95% unchanged within 24 hours); less than 0.3% fecal. |
| Half-life | Terminal elimination half-life: 1.24-2.23 hours (healthy); may be prolonged in renal impairment (up to 9.6 hours in severe impairment). |
| Protein binding | Negligible (less than 5% bound to plasma proteins). |
| Volume of Distribution | Approximately 0.17-0.26 L/kg (distributes primarily in extracellular fluid; does not cross intact blood-brain barrier except in areas of disruption). |
| Bioavailability | Not applicable (administered intravenously only; bioavailability is 100% by IV route). |
| Onset of Action | Intravenous: Immediate enhancement of signal intensity on T1-weighted MRI (within minutes of injection). |
| Duration of Action | 30-60 minutes after injection; contrast enhancement declines rapidly with T1 shortening effects lasting up to 60-90 minutes. |
0.1 mmol/kg (0.1 mL/kg) intravenous bolus; maximum dose 0.1 mmol/kg per contrast study. Repeat dosing up to 0.2 mmol/kg total during a single session may be considered on clinical judgment.
| Dosage form | SOLUTION |
| Renal impairment | For GFR 30-59 mL/min/1.73 m²: standard dose can be used but do not exceed 0.1 mmol/kg per study. For GFR 15-29 mL/min/1.73 m²: contraindicated. For GFR <15 mL/min/1.73 m² or on dialysis: contraindicated unless no alternative and benefit clearly outweighs risk; if used, minimum dose necessary and do not re-administer within 7 days. |
| Liver impairment | No specific dose adjustment required for Child-Pugh A, B, or C; caution in severe hepatic impairment due to potential gadolinium retention. |
| Pediatric use | 0.1 mmol/kg (0.1 mL/kg) intravenous; maximum 0.1 mmol/kg per single dose. Infants and children: same weight-based dose; approved for all pediatric age groups including term neonates. |
| Geriatric use | No specific dose adjustment; use lowest effective dose due to age-related GFR decline; assess renal function before administration; consider risk of nephrogenic systemic fibrosis in elderly with renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
No significant drug interactions Contraindicated in patients with known gadolinium sensitivity.
| Breastfeeding | Gadobutrol is excreted into breast milk in very small amounts (M/P ratio not established). The absolute dose received by an infant is less than 0.04% of the maternal dose. Consider interrupting breastfeeding for 12-24 hours after administration to minimize infant exposure. |
| Teratogenic Risk | Gadobutrol crosses the placenta. In animal studies, no teratogenic effects were observed at doses up to 2.5 times the human dose. However, gadolinium-based contrast agents are associated with a risk of nephrogenic systemic fibrosis (NSF) and should be used in pregnancy only if clearly needed. First trimester: avoid unless essential; second and third trimesters: use only if diagnostic benefit outweighs potential fetal risks due to gadolinium accumulation. |
■ FDA Black Box Warning
Gadobutrol is associated with a risk of nephrogenic systemic fibrosis (NSF) in patients with chronic severe kidney disease (CKD stage 4/5) or acute kidney injury. Do not use in such patients unless diagnostic information is essential and not available with non-contrast MRI or other modalities.
| Common Effects | Headache |
| Serious Effects |
["History of severe hypersensitivity reaction to gadobutrol or any GBCA.","Chronic severe kidney disease (eGFR < 30 mL/min/1.73 m²) unless risk-benefit justifies use.","Acute kidney injury due to hepatorenal syndrome or perioperative liver transplantation."]
| Precautions | ["Risk of NSF in patients with advanced renal impairment.","Acute adverse reactions including anaphylaxis, hypotension, bronchospasm, and urticaria.","Extravasation leading to tissue necrosis.","Gadolinium retention in tissues (brain, bone, skin) especially with repeated use.","Interference with serum calcium measurements (pseudohypocalcemia) when using certain calcium assays."] |
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| Fetal Monitoring | Monitor maternal renal function before administration. Assess vital signs during injection. For fetus, no specific monitoring required. Observe for hypersensitivity reactions. |
| Fertility Effects | No adverse effects on fertility have been reported in animal studies at clinically relevant doses. Human data are lacking. |