Class: Radiopaque agent
- Injection, solution 1 mmol/mL
Provides contrast enhancement of the CNS.
Rapid distribution in the extracellular space.
Excreted unchanged from kidneys. Eliminated from plasma with a mean terminal half-life of 1.81 h; renal Cl is 1.1 to 1.7 mL/min•kg.
Special PopulationsRenal Function Impairment
The elimination half-life was 5.8 h in mild to moderately impaired patients (CrCl 80 to 30 mL/min or more) and 17.6 h in severely impaired patients not on dialysis (CrCl less than 30 mL/min). The mean AUC in patients with healthy renal function was 1.1 mmol•h/L compared with 4 mmol•h/L in patients with mild to moderate renal impairment, and 11.5 mmol•h/L in patients with severe renal impairment. 68% of gadobutrol is removed from the body after dialysis, 94% after a second dialysis, and 98% after a third dialysis session.Elderly
AUC was slightly higher and Cl slightly lower in elderly patients.Children
The median AUC, Cl, and elimination half-life were similar across the range of 2 to 17 y of age.Gender
There was no clinically relevant effect on the pharmacokinetics of gadobutrol.
Indications and Usage
For use in diagnostic MRI to detect and visualize areas with disrupted blood-brain barrier and/or abnormal vascularity of the CNS.
None well documented.
Dosage and AdministrationAdults and Children (2 y and older)
IV bolus 0.1 mmol/kg (0.1 mL/kg).
- Administer as an IV bolus injection, manually or by power injector, at a flow rate of approximately 2 mL/sec. Do not administer IM.
- Flush the IV cannula with physiological saline solution after the injection.
- Inspect visually for particulate matter and discoloration prior to administration and do not use if discolored or particulate matter is present.
- Do not mix gadobutrol with other drugs.
- Exercise caution to avoid local extravasation during IV administration and treat as necessary if local reactions develop.
Store between 59° and 86°F. If freezing occurs, bring to room temperature before use. Discard any unused drug product.
None well documented.
Cardiac arrest (postmarketing).
Dysgeusia, nausea (1%).
Hypersensitivity/anaphylactoid reactions (anaphylactoid shock, angioedema, BP increased, bronchospasm, burning sensation, chest pain, circulatory collapse, conjunctivitis, cough, cyanosis, eyelid edema, face edema, hyperhidrosis, laryngeal edema, oropharyngeal swelling, respiratory arrest, and sneezing) (postmarketing).
Injection-site reaction (1%).
Feeling hot (1%); nephrogenic systemic fibrosis (postmarketing).
WarningsNephrogenic systemic fibrosis
There is an increased risk of nephrogenic systemic fibrosis among patients with impaired elimination of the drugs. The risk for nephrogenic systemic fibrosis appears highest in patients with chronic, severe kidney disease (glomerular filtration rate less than 30 mL/min/1.73 m 2 ) or acute kidney injury. Avoid use unless the diagnostic information is essential and not available with noncontrasted MRI or other modalities. Nephrogenic systemic fibrosis may result in fatal or debilitating fibrosis affecting the skin, muscle, and internal organs. Do not exceed the recommended dose. Allow a sufficient period of time for elimination of the agent from the body prior to any readministration.
Closely observe patients for signs and symptoms of hypersensitivity reactions during and following administration. Screen all patients for renal impairment by obtaining a history and/or laboratory tests.
Category C. Other gadolinium-based contrast agents cross the placenta in humans and result in fetal exposure.
Undetermined. Nonclinical data show that gadobutrol is excreted into breast milk in very small amounts (less than 0.1%) and absorption via the GI tract is poor.
Safety and efficacy in children younger than 2 y have not been established.
Use with caution, reflecting the greater frequency of impaired renal function and concomitant disease or other drug therapy.
Anaphylactoid and anaphylactic reactions with CV, respiratory, or cutaneous manifestations ranging from mild to severe, including death, have occurred. Observe patients during and following administration.
May occur; treat as necessary if local reactions develop. Do not administer IM.
- Advise patients to inform their health care provider if they have a history of kidney and/or liver disease or have recently had a gadolinium-based contrast agent.
- Advise patients to inform their health care provider if they may be pregnant or are breast-feeding or are taking any medications.
- Instruct patients to inform their health care provider if they have ever had an allergic or hypersensitivity reaction to gadolinium-based contrast agents, bronchial asthma, or allergic respiratory disorder.
- Advise patients that they may experience reactions along the injection site, such as mild and transient burning, pain, or feelings of warmth or coldness.
- Inform patients that they may experience adverse reactions, such as headache, nausea, abnormal taste, and feeling hot.
- Instruct patients to contact their health care provider if they develop signs or symptoms of nephrogenic systemic fibrosis following gadobutrol administration, such as burning, itching, swelling, scaling, hardening, and tightening of the skin; red or dark patches on the skin; stiffness in joints with trouble moving, bending, or straightening the arms, hands, legs, or feet; pain in the hip bones or ribs; or muscle weakness.
Copyright © 2009 Wolters Kluwer Health.