Description

Simple

A substance that helps produce clearer images in magnetic resonance imaging (MRI) of the liver.

Clinical

A gadolinium-based contrast agent used in magnetic resonance imaging (MRI) to help characterize lesions in the liver.

Overview

Gadoxetic acid (gadoxetate) is a paramagnetic gadolinium-containing contrast agent in which its salt form, gadoxetate disodium, is used for intravenous injection. Ethoxybenzyl diethylenetriaminepentaacetic acid is the moiety that chelates with a gadolinium ion and forms a stable complex with it to make up the drug. It is marketed by Bayer HealthCare Pharmaceuticals and FDA approved on July 3, 2008.

Pharmacology

Indication

Gadoxetate is used as a contrast medium for magnetic resonance imaging (MRI) to detect and characterize lesions in the liver.

Pharmacodynamic

Gadoxetate disodium is an amphipathic compound in which gadoxetate is hydrophillic and its moiety, the ethoxybenyzl group, is lipophillic. Consequently, gadoxetate disodium has a biphasic mode of action in which it first distributes into the extracellular space after bolus injection and then hepatoc... Read more

Mechanism of action

When gadoxetate disodium is placed in an external magnetic field, a large magnetic moment is produced. As a result, a magnetic field is induced around the tissue. The water protons in the vicinity are disrupted such that the change the proton density and spin characteristics are detected and visuali... Read more

Absorption

Information currently not available.

Protein binding

Volume of distribution

Total volume of distribution at steady state is 0.21 L/kg. Gadoxetate disodium cannot diffuse through the blood brain barrier. The two transporters that gadoxetate disodium can enter the hepatocyte through are OATP1B1 and OATP1B3. Gadoxetate disodium may also exit the heptaocyte and go back into sin... Read more

Clearance

Clearance may be lower in older patients.Total serum clearance (CLtot) = 250 mL/min;Renal clearance (CLr) = 120 mL/min

Half life

Terminal elimination half-life, healthy subjects, adults = 0.91 - 0.95 hours

Route of elimination

Gadoxetate disodium is eliminated equally via urine and feces. Multidrug resistance protein 2 actively transports/excretes gadoxetate disodium into the bile.

Toxicity

LD50, oral, rat = 18100 mg/kg;
LD50, oral, mouse = 14500 mg/kg;
LD50, IV, rat = 3600 - 7300 mg/kg;
LD50, IV, mouse = 5400 - 10900 mg/kg;
LD50, IV, dog = >2200 mg/kg

Adverse Effects

Contraindications

  • Hypersensitivity:
    • false
  • Regions: US

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Acetylcysteine
The excretion of Gadoxetic acid can be decreased when combined with Acetylcysteine.
Aminohippuric acid
The excretion of Gadoxetic acid can be decreased when combined with Aminohippuric acid.
Amprenavir
The excretion of Gadoxetic acid can be decreased when combined with Amprenavir.
Apalutamide
The excretion of Gadoxetic acid can be increased when combined with Apalutamide.
Asunaprevir
The excretion of Gadoxetic acid can be decreased when combined with Asunaprevir.
Ataluren
The excretion of Gadoxetic acid can be decreased when combined with Ataluren.
Atazanavir
The excretion of Gadoxetic acid can be decreased when combined with Atazanavir.
Atorvastatin
The excretion of Gadoxetic acid can be decreased when combined with Atorvastatin.
Axitinib
The excretion of Gadoxetic acid can be decreased when combined with Axitinib.
Baricitinib
The excretion of Gadoxetic acid can be decreased when combined with Baricitinib.
Beclomethasone dipropionate
The excretion of Gadoxetic acid can be decreased when combined with Beclomethasone dipropionate.
Bempedoic acid
The excretion of Gadoxetic acid can be decreased when combined with Bempedoic acid.
Benzbromarone
The excretion of Gadoxetic acid can be decreased when combined with Benzbromarone.
Bezafibrate
The excretion of Gadoxetic acid can be decreased when combined with Bezafibrate.
Cabazitaxel
The excretion of Gadoxetic acid can be decreased when combined with Cabazitaxel.
Candesartan
The excretion of Gadoxetic acid can be decreased when combined with Candesartan.
Caspofungin
The excretion of Gadoxetic acid can be decreased when combined with Caspofungin.
Cerivastatin
The excretion of Gadoxetic acid can be decreased when combined with Cerivastatin.
Cholecystokinin
The excretion of Gadoxetic acid can be decreased when combined with Cholecystokinin.
Cholic Acid
The excretion of Gadoxetic acid can be decreased when combined with Cholic Acid.
1 References
  1. 1 . Van Beers BE, Pastor CM, Hussain HK: Primovist, Eovist: what to expect? J Hepatol. 2012 Aug;57(2):421-9. doi: 10.1016/j.jhep.2012.01.031. Epub 2012 Apr 12.PubMed: 22504332