Overview
11 DESCRIPTION Gadobutrol injection is a paramagnetic macrocyclic contrast agent administered for magnetic resonance imaging. The chemical name for gadobutrol is 10–[(1SR,2RS)–2,3–dihydroxy–1–hydroxymethylpropyl]–1,4,7,10–tetraazacyclododecane–1,4,7–triacetic acid, gadolinium complex. Gadobutrol has a molecular formula of C 18 H 31 GdN 4 O 9 and a molecular weight of 604.72.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action In MRI, visualization of normal and pathological tissue depends in part on variations in the radiofrequency signal intensity that occurs with: • Differences in proton density • Differences of the spin-lattice or longitudinal relaxation times (T 1 ) • Differences in the spin-spin or transverse relaxation time (T 2 ) When placed in a magnetic field, gadobutrol shortens the T 1 and T 2 relaxation times. The extent of decrease of T 1 and T 2 relaxation times, and therefore the amount of signal enhancement obtained from gadobutrol, is based upon several factors including the concentration of gadobutrol in the tissue, the field strength of the MRI system, and the relative ratio of the longitudinal and transverse relaxation times.
Indications
- 1 INDICATIONS AND USAGE Gadobutrol injection is a gadolinium-based contrast agent indicated for use with magnetic resonance imaging (MRI): • To detect and visualize areas with disrupted blood brain barrier and/or abnormal vascularity of the central nervous system in adult and pediatric patients, including term neonates ( 1.1 ) • To assess the presence and extent of malignant breast disease in adult patients ( 1.2 ) • To evaluate known or suspected supra-aortic or renal artery disease in adult and pediatric patients, including term neonates ( 1.
Common Doses
- 0.1 mL
- 2 mL
- 1.5 mL
- 30 mL
Dosage
2 DOSAGE AND ADMINISTRATION • Recommended dose for adults and pediatric patients (including term neonates) is 0.1 mL/kg body weight ( 2.1 ) • Administer as an intravenous bolus injection ( 2.2 ) • Follow injection with a normal saline flush ( 2.2 ) 2.1 Recommended Dose The recommended dose of gadobutrol injection for adult and pediatric patients (including term neonates) is 0.1 mL/kg body weight (0.1 mmol/kg). Refer to Table 1 to determine the volume to be administered. Table 1: Volume of Gadobutrol Injection by Body Weight* Body Weight (kg) Volume to be Administered (mL) 2.5 0.25 5 0.
Black Box Warning
WARNING: RISK ASSOCIATED WITH INTRATHECAL USE and NEPHROGENIC SYSTEMIC FIBROSIS Risk Associated with Intrathecal Use Intrathecal administration of gadolinium-based contrast agents (GBCAs) can cause serious adverse reactions including death, coma, encephalopathy, and seizures. Gadobutrol injection is not approved for intrathecal use [see Warnings and Precautions ( 5.1 )] . Nephrogenic Systemic Fibrosis GBCAs increase the risk for nephrogenic systemic fibrosis (NSF) among patients with impaired elimination of drugs.
Contraindications
- 4 CONTRAINDICATIONS Gadobutrol injection is contraindicated in patients with history of severe hypersensitivity reactions to gadobutrol injection. History of severe hypersensitivity reaction to gadobutrol injection ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following clinically significant adverse reactions are discussed elsewhere in labeling: • Nephrogenic Systemic Fibrosis (NSF) [see Boxed Warning and Warnings and Precautions ( 5.2 )] . • Hypersensitivity reactions [see Contraindications ( 4 ) and Warnings and Precautions ( 5.3 )] . • Acute Respiratory Distress Syndrome [see Warnings and Precautions ( 5.4 )] . • Gadolinium Retention [see Warnings and Precautions ( 5.5 )] . Most common adverse reactions (incidence ≥ 0.5%) are headache, nausea, and dizziness ( 6.
Interactions
- No major interactions listed on the FDA label. Always consult a healthcare professional.