Gadobenate DimegluminePronunciation: GAD-oh-BEN-ate di-ME-gloo-meen
Class: Radiopaque agent
- Injection, solution 529 mg/mL
Provides contrast enhancement of the CNS.
Rapid distribution half-life of 0.084 to 0.605 h. Vd of the central compartment is 0.074 to 0.158 L/kg, and Vd by area is 0.17 to 0.282 L/kg.
Excreted mostly in urine (78% to 96%); total plasma and renal Cl ranged from 0.093 to 0.133 L/h/kg and 0.082 to 0.104 L/h/kg, respectively. Mean elimination half-life ranged from 1.17 to 2.02 h; 0.6% to 4% is eliminated via the biliary route and recovered in feces.
Special PopulationsRenal Function Impairment
Elimination half-life was 6.1 and 9.5 h for the moderate and severe renal impairment groups, respectively, compared with 1 to 2 h in healthy patients.Hemodialysis
The mean elimination half-life on dialysis was 1.21 h compared with 42.4 h when off dialysis.Hepatic Function Impairment
Hepatic impairment had little effect on the pharmacokinetics of gadobenate.Elderly
Cl appeared to decrease slightly with increasing age.Gender
There was no significant effect of gender on the pharmacokinetics of gadobenate.Race
Pharmacokinetic differences because of race have not been studied.
Indications and Usage
For IV use in MRI of the CNS to visualize lesions with abnormal blood-brain barrier or abnormal vascularity of the brain, spine, and associated tissues.
Known allergic or hypersensitivity reactions to gadolinium-based contrast agents.
Dosage and AdministrationAdults and Children (older than 2 y)
IV bolus 0.1 mmol/kg (0.2 mL/kg).
- Follow the injection with a sodium chloride flush of at least 5 mL.
- Vials are intended for single use only. Discard any unused product.
- Inspect visually for particulate matter and discoloration prior to administration; do not use if discolored or particulate matter is present.
- Do not mix with IV medications or parenteral nutrition, or administer with other medications in the same IV line.
- Exercise caution to avoid local extravasation during IV administration and treat as necessary if local reactions develop.
Store between 59° and 86°F. Do not freeze.
Drug InteractionsQT prolonging drugs (eg, antiarrhythmic agents [eg, amiodarone, bretylium, disopyramide, dofetilide, procainamide, quinidine, sotalol] , arsenic trioxide, chlorpromazine, cisapride, dolasetron, droperidol, gatifloxacin, halofantrine, levomethadyl, mefloquine, mesoridazine, moxifloxacin, pentamidine, pimozide, probucol, sparfloxacin, thioridazine, ziprasidone)
An additive effect of gadobenate dimeglumine with other drugs that prolong the QT interval cannot be excluded.Transporter-based drug-drug interactions (eg, chemotherapy agents [eg, anthracyclines (eg, daunorubicin, doxorubicin)], cisplatin, etoposide, methotrexate, paclitaxel, tamoxifen, vinca alkaloids [eg, vincristine])
Gadobenate and other drugs may compete for the canalicular multispecific organic anion transporter (CMOAT, also referred to as MRP2 or ABCC2) sites. Therefore, exercise appropriate caution in patients who receive gadobenate concomitantly with such drugs. Consider the potential for prolonged drug exposure in patients with decreased CMOAT activity (eg, Dubin-Johnson syndrome).
Headache (2%); dizziness, paresthesia, taste perversion (1%).
Nausea (2%); vomiting (1%).
Anaphylactic, anaphylactoid, and hypersensitivity reactions, anaphylactic shock, death, loss of consciousness (postmarketing).
Injection-site reaction (1%); extravasation, injection-site reactions (eg, blistering, burning sensation, local pain, necrosis, swelling) (postmarketing).
Feeling hot (1%).
WarningsNephrogenic systemic fibrosis
Gadolinium-based contrast agents increase the risk of nephrogenic systemic fibrosis (NSF) in patients with impaired elimination of the drugs. Increased risk of NSF in patients with chronic, severe renal insufficiency. Avoid use unless the diagnostic information is essential. NSF may result in fatal or debilitating systemic 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 with a history of allergy, drug reactions, or other hypersensitivity-like disorders during the procedure and for several hours after drug administration. Screen all patients for renal impairment by obtaining a history and/or laboratory tests.
Category C .
Undetermined. Breast-feeding should be discontinued before administering gadobenate and should not be resumed for at least 24 h after administration. Per Briggs' Drugs in Pregnancy and Lactation , a similar agent, gadopentetate dimeglumine, is classified as compatible by the American Academy of Pediatrics.
Safety and efficacy in neonates and infants (0 to 2 y of age) have not been established.
Toxic reactions may be greater in patients with renal impairment.
Anaphylactic and anaphylactoid reactions have been reported, and have involved cutaneous, CV, and/or respiratory manifestations. Some reports included circulatory collapse and death. Observe patients for up to 2 h after administration.
In patients with renal insufficiency, acute renal failure requiring dialysis and worsening renal function have occurred. The risk of renal failure may increase with increasing dose of the contrast agent.
Cardiac arrhythmias have been observed.
May occur; treat as necessary if local reactions develop.
Lesions seen on unenhanced images may not all be seen on contrast-enhanced images. Exercise caution when a contrast-enhanced interpretation is made in the absence of a companion unenhanced MRI.
- Advise patients to their inform health care provider if they may be pregnant or are breast-feeding.
- Instruct patients to inform their health care provider if they have ever had an allergic or hypersensitivity reaction to gadolinium-based contrast agents.
- Advise patients that they may experience reactions along the injection site, such as mild and transient burning or pain, or feelings of warmth or coldness.
- Inform patients with impaired renal function who receive repetitive doses of gadolinium-containing contrast agents that they may have an increased risk of developing NSF. Advise patients to contact their health care provider if they develop symptoms of burning, itching, swelling, scaling, hardening, or tightening of the skin; deep pain in the hips, bones, or ribs; muscle weakness; stiffness of joints; or trouble moving, bending, or straightening arms, hands, legs, or feet.
Copyright © 2009 Wolters Kluwer Health.