Peringatan Keamanan

GBCAs cross the human placenta and result in fetal exposure and gadolinium retention. The human data on the association between GBCAs and adverse fetal outcomes are limited and inconclusive. In animal reproduction studies, there were no adverse developmental effects observed in rats or rabbits with intravenous administration of gadoterate meglumine during organogenesis at doses of 16 and 10 times, respectively, the recommended human dose. Because of the potential risks of gadolinium to the fetus, use gadoterate only if imaging is essential during pregnancy and cannot be delayed.L49911

Gadoterate administered to healthy volunteers and to adult patients at cumulative doses up to 0.3 mmol/kg was tolerated in a manner similar to lower doses. Adverse reactions to overdosage with gadoterate have not been reported. Gadoterate can be removed from the body by hemodialysis.L49911

Long-term animal studies have not been performed to evaluate the carcinogenic potential of gadoterate meglumine.L49911

Gadoterate meglumine did not demonstrate mutagenic potential in in vitro bacterial reverse mutation assays (Ames test) using Salmonella typhimurium, in an in vitro chromosome aberration assay in Chinese hamster ovary cells, in an in vitro gene mutation assay in Chinese hamster lung cells, nor in an in vivo mouse micronucleus assay.L49911

No impairment of male or female fertility and reproductive performance were observed in rats after intravenous administration of gadoterate meglumine at the maximum tested dose of 10 mmol/kg/day (16 times the maximum human dose based on surface area), given during more than 9 weeks in males and more than 4 weeks in females. Sperm counts and sperm motility were not adversely affected by treatment with the drug.L49911

Local intolerance reactions, including moderate irritation associated with infiltration of inflammatory cells were observed after perivenous injection in rabbits suggesting the possibility of local irritation if the contrast medium leaks around the veins in a clinical setting.

Toxicity of gadoterate meglumine was evaluated in neonatal and juvenile (pre- and post-weaning) rats following a single or repeated intravenous administration at doses 1, 2, and 4 times the MHD based on BSA. Gadoterate meglumine was well tolerated at all dose levels tested and had no effect on growth, pre-weaning development, behavior, or sexual maturation.

Gadoteric acid

DB09132

small molecule approved

Deskripsi

Gadoteric acid, commonly used in the salt form gadoterate meglumine, is a macrocyclic, ionic gadolinium-based contrast agent (GBCA).A263131 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+).A263136 Gadoterate meglumine has one of the highest thermodynamic stability, apparent stability, and kinetic stability, partly due to its macrocyclic structure, and thus has a more favorable safety profile due to a decreased tendency of gadolinium dechelation.A263141,A263106

Gadoterate is approved by the FDA under the brand name DOTAREM on 20th March 2013 for intravenous uses with magnetic resonance imaging (MRI) in the 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.L49921

Struktur Molekul 2D

Berat 558.65
Wujud liquid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following an intravenously administered 0.1 mmol/kg, gadoterate demonstrates a mean elimination half-life of about 1.4 ± 0.2 hr and 2.0 ± 0.7 hr in female and male subjects, respectively.L49911]
Volume Distribusi The volume of distribution at steady state of total gadolinium in healthy subjects is 179 ± 26 and 211 ± 35 mL/kg in female and male subjects respectively, roughly equivalent to that of extracellular water. The extent of blood cell partitioning of gadoterate is not known.[L49911]
Klirens (Clearance) In healthy subjects, the renal and total clearance rates of total gadolinium are comparable (1.27 ± 0.32 and 1.74 ± 0.12 mL/min/kg in females; and 1.40 ± 0.31 and 1.64 ± 0.35 mL/min/kg in males, respectively) indicating that the drug is primarily cleared through the kidneys.[L49911]

Absorpsi

Within the studied dose range (0.1 to 0.3 mmol/kg), the kinetics of total gadolinium appear to be linear.L49911 Following the administration of 0.1 mmol/kg of gadoterate meglumine in healthy volunteers, the Cmax, Tmax, AUC0-t, and AUC0-? were measured to be 799.03 (192.63) µmol/L, 5.00 (0.10-10.00) min, 953.51 (76.22) µmol*h/L, and 970.72 (73.34) µmol*h/L for female and 836.85 (451.02) µmol/L, 5.00 (0.11-10.00) min, 1038.74 (240.46) µmol*h/L, and 1061.16 (239.24) µmol*h/L for male subjects respectively.L49916

Metabolisme

Gadoterate is not known to be metabolized.L49911

Rute Eliminasi

Following a 0.1 mmol/kg dose of gadoterate, total gadolinium is excreted primarily in the urine with 72.9 ± 17.0% and 85.4 ± 9.7% (mean ± SD) eliminated within 48 hours, in female and male subjects, respectively. Similar values were achieved after a cumulative dose of 0.3 mmol/kg (0.1 + 0.2 mmol/kg, 20 minutes later), with 85.5 ± 13.2% and 92.0 ± 12.0% recovered in urine within 48 hrs in female and male subjects respectively.L49911

Interaksi Obat

727 Data
Technetium Tc-99m oxidronate Gadoteric acid may decrease effectiveness of Technetium Tc-99m oxidronate as a diagnostic agent.
Cyclosporine Cyclosporine may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Flurbiprofen Flurbiprofen 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.
Pentamidine Pentamidine may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Gadoteric acid 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.
Naproxen Naproxen may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Lopinavir Lopinavir may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Cimicoxib Cimicoxib may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Ceftaroline fosamil Ceftaroline fosamil may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.
Lornoxicam Lornoxicam may decrease the excretion rate of Gadoteric acid which could result in a higher serum level.

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25249313
    Fallenberg EM, Renz DM, Karle B, Schwenke C, Ingod-Heppner B, Reles A, Engelken FJ, Huppertz A, Hamm B, Taupitz M: Intraindividual, randomized comparison of the macrocyclic contrast agents gadobutrol and gadoterate meglumine in breast magnetic resonance imaging. Eur Radiol. 2015 Mar;25(3):837-49. doi: 10.1007/s00330-014-3426-0. Epub 2014 Sep 25.
  • PMID: 24995911
    Xiao Y, Xue R, You T, Li X, Pei F, Wang X, Lei H: Gadolinium-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid conjugate of arabinogalactan as a potential liver-targeting magnetic resonance imaging contrast agent. Carbohydr Res. 2014 Aug 18;395:9-14. doi: 10.1016/j.carres.2014.05.022. Epub 2014 Jun 6.
  • PMID: 20945944
    Ishiguchi T, Takahashi S: Safety of gadoterate meglumine (Gd-DOTA) as a contrast agent for magnetic resonance imaging: results of a post-marketing surveillance study in Japan. Drugs R D. 2010;10(3):133-45. doi: 10.2165/11539140-000000000-00000.
  • PMID: 26606549
    Robert P, Violas X, Grand S, Lehericy S, Idee JM, Ballet S, Corot C: Linear Gadolinium-Based Contrast Agents Are Associated With Brain Gadolinium Retention in Healthy Rats. Invest Radiol. 2016 Feb;51(2):73-82. doi: 10.1097/RLI.0000000000000241.

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