GADOTERIDOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GADOTERIDOL (GADOTERIDOL).
Gadoteridol is a paramagnetic gadolinium-based contrast agent that increases signal intensity in T1-weighted magnetic resonance imaging by shortening the T1 relaxation time of protons in water molecules. It distributes in the extracellular fluid compartment and does not cross the intact blood-brain barrier, thus enhancing imaging in areas of disrupted barrier or abnormal vascularity.
| Metabolism | Gadoteridol is not metabolized; it is excreted unchanged primarily via glomerular filtration in the kidneys. |
| Excretion | Renal: >95% unchanged via glomerular filtration. Biliary/fecal: <5%. |
| Half-life | Terminal half-life 1.5-2 hours in normal renal function; prolonged to 10-18 hours in moderate renal impairment (CrCl 30-60 mL/min) and up to 30 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | Negligible (<3%), does not bind significantly to plasma proteins. |
| Volume of Distribution | 0.22 L/kg (approximately 15.4 L in 70 kg adult), consistent with extracellular fluid distribution. |
| Bioavailability | IV only (100% bioavailable); not administered via other routes. |
| Onset of Action | IV: Immediate enhancement begins during injection, peak enhancement within 2-4 minutes post-injection for CNS imaging. |
| Duration of Action | IV: Diagnostic enhancement lasts 30-60 minutes for CNS imaging; complete elimination by 24 hours in normal renal function. |
0.2 mL/kg (0.1 mmol/kg) IV bolus, max 20 mL per dose; additional doses up to 0.4 mL/kg may be given within 30 minutes if needed.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-59 mL/min: consider not exceeding single dose and avoiding repeat dosing; GFR <30 mL/min or dialysis: contraindicated due to risk of nephrogenic systemic fibrosis (NSF). |
| Liver impairment | No dose adjustment required for hepatic impairment as gadoteridol is not significantly metabolized by the liver. |
| Pediatric use | 0.2 mL/kg (0.1 mmol/kg) IV bolus, max 20 mL; for children 2 years and older. Safety for repeated doses not established. |
| Geriatric use | No specific dose adjustment except based on renal function; monitor GFR 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 GADOTERIDOL (GADOTERIDOL).
| Breastfeeding | Limited data: Gadoteridol is excreted into breast milk in very small amounts (M/P ratio not established; estimated less than 0.04% of maternal dose per 24 hours). The American College of Radiology considers it acceptable with a 12-24 hour interruption of breastfeeding after administration to minimize any risk. |
| Teratogenic Risk | Gadoteridol is a gadolinium-based contrast agent. Animal studies have shown adverse effects including skeletal and visceral abnormalities at high doses. No adequate human studies exist. The risk to the fetus during the first trimester is uncertain; use is contraindicated unless essential. During second and third trimesters, gadolinium agents can cross the placenta and are associated with increased risk of nephrogenic systemic fibrosis in neonates if used in pregnancy. |
■ FDA Black Box Warning
Gadolinium-based contrast agents (GBCAs) increase the risk for nephrogenic systemic fibrosis (NSF) in patients with acute or chronic severe renal insufficiency (glomerular filtration rate <30 mL/min/1.73m²) or in patients with acute kidney injury. Avoid use in these populations unless the diagnostic information is essential and not available with non-contrast MRI or other imaging modalities.
| Serious Effects |
["History of hypersensitivity to gadoteridol or any component of the formulation","Severe renal impairment (GFR <30 mL/min/1.73m²) or acute kidney injury (unless benefit outweighs risk)"]
| Precautions | ["Risk of nephrogenic systemic fibrosis (NSF) in patients with severe renal impairment","Acute kidney injury may increase risk of NSF","Hypersensitivity reactions, including anaphylaxis, may occur","Gadolinium retention for months to years in brain and other tissues; clinical significance unknown","Use with caution in patients with history of allergic or hypersensitivity reactions","Administration may cause acute reactions (e.g., nausea, headache) at injection site"] |
| Food/Dietary |
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| Fetal Monitoring | No specific fetal monitoring required. Maternal renal function assessment recommended prior to use. Monitor for signs of allergic reaction or nephrogenic systemic fibrosis (noted in patients with renal impairment). |
| Fertility Effects | Animal studies at high doses showed no significant effects on fertility or reproductive performance. No human data available on fertility impact. |
| No specific food interactions. Encourage adequate hydration (e.g., water) before and after administration to minimize renal toxicity. Avoid fasting or dehydration before scan. |
| Clinical Pearls | Gadoteridol is a macrocyclic gadolinium-based contrast agent (GBCA) with high stability and lower risk of nephrogenic systemic fibrosis (NSF) compared to linear agents. Pre-scan eGFR assessment is mandatory; avoid in acute kidney injury or severe chronic kidney disease (eGFR <30 mL/min/1.73m²) unless benefit outweighs risk. Recognize subtle signs of gadolinium deposition (e.g., T1 hyperintensity in dentate nucleus) on unenhanced MRI after repeated doses. Administer as slow IV bolus (0.1 mmol/kg); flush line to minimize extravasation. Have resuscitation equipment ready for hypersensitivity reactions (rare but potentially severe). |
| Patient Advice | Inform your doctor if you have kidney disease, diabetes, or high blood pressure. · Drink plenty of water before and after the scan unless otherwise instructed. · Report any prior allergic reaction to contrast agents. · You may experience a cool sensation or metallic taste during injection. · Breastfeeding: Do not breastfeed for 24 hours after receiving this drug. · Pregnancy: Use only if clearly needed; discuss risks with your doctor. |