Description

Simple

A medication used to enhance MRI images to detect abnormalities in the blood, blood vessels, and various locations of the body.

Clinical

A diagnostic contrast agent used with magnetic resonance imaging to provide contrast enhancement for intracranial and spinal lesions with abnormal blood brain barrier or abnormal vascularity, and for whole body imaging.

Overview

Gadoteric acid is a macrocycle-structured gadolinium-based MRI contrast agent. It is composed of the organic acid DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) used for its chelating properties, and gadolinium (Gd3+). As a paramagnetic molecule, gadoterate develops a magnetic moment when placed in a magnetic field. This magnetic moment enhances the relaxation rates of water protons in its vicinity, leading to an increase in signal intensity (brightness) of tissues. More specifically, it reduces the T1 relaxation time (and to some extent the T2 and T2* relaxation times) in NMR, which is the source of its clinical utility. Increased signal brightness allows it to be used in imaging of blood vessels and of inflamed or diseased tissue where the blood vessels become 'leaky'.

Gadoteric acid, as the FDA approved product Dotarem, is indicated for intravenous use with magnetic resonance imaging (MRI) in brain (intracranial), spine and associated tissues in adult and pediatric patients (2 years of age and older) to detect and visualize areas with disruption of the blood brain barrier (BBB) and/or abnormal vascularity.

Pharmacology

Indication

Gadoteric acid is indicated for intravenous use with magnetic resonance imaging (MRI) in brain (intracranial), spine and associated tissues in adult and pediatric patients (2 years of age and older) to detect and visualize areas with disruption of the blood brain barrier (BBB) and/or abnormal vascul... Read more

Pharmacodynamic

Gadoterate affects proton relaxation times and consequently the MR signal, and the contrast obtained is characterized by the relaxivity of the gadoterate molecule. The relaxivity values for gadoterate are similar across the spectrum of magnetic field strengths used in clinical MRI (0.2 - 1.5 T).
Ga... Read more

Mechanism of action

Gadoterate is a paramagnetic molecule that develops a magnetic moment when placed in a magnetic field. The magnetic moment enhances the relaxation rates of water protons in its vicinity, leading to an increase in signal intensity (brightness) of tissues. When placed in a magnetic field, gadoterate s... Read more

Absorption

Information currently not available.

Protein binding

Gadoterate does not undergo protein binding in vitro.

Volume of distribution

The volume of distribution at steady state of total gadolinium in normal subjects is 179 and 211 mL/kg in female and male subjects respectively, roughly equivalent to that of extracellular water.

Clearance

In healthy subjects, the renal and total clearance rates of total gadolinium are comparable (1.27 and 1.74 mL/min/kg in females; and 1.40 and 1.64 mL/min/kg in males, respectively).

Half life

Gadoteric acid demonstrates a mean elimination half-life of about 1.4 hr and 2.0 hr in female and male subjects, respectively.

Route of elimination

Gadoteric acid is excreted primarily in urine.

Toxicity

The most frequent adverse reactions in clinical studies were nausea, headache, injection site pain, injection site coldness, and burning sensation. Nephrogenic Systemic Fibrosis has occurred in patients with impaired elimination of GBCAs.

Adverse Effects

Contraindications

Information currently not available.

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)
Abacavir
Abacavir may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Acarbose
Acarbose may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Acetaminophen
Acetaminophen may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Gadoteric acid which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid
Acetylsalicylic acid may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Aclidinium
Aclidinium may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Acrivastine
Gadoteric acid may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir
Acyclovir may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Adefovir
Adefovir may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Adefovir dipivoxil
Adefovir dipivoxil may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Albutrepenonacog alfa
Gadoteric acid may decrease the excretion rate of Albutrepenonacog alfa which could result in a higher serum level.
Alclofenac
Alclofenac may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Aldesleukin
Aldesleukin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Allopurinol
Allopurinol may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Allylestrenol
Allylestrenol may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Almasilate
Gadoteric acid may decrease the excretion rate of Almasilate which could result in a higher serum level.
Alminoprofen
Alminoprofen may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Almotriptan
Almotriptan may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.