Peringatan Keamanan

GBCAs cross the 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, gadobenate dimeglumine has been shown to be teratogenic in rabbits following repeated intravenous administration during organogenesis at doses up to 6 times the recommended human dose. There were no adverse developmental effects observed in rats with intravenous administration of gadobenate dimeglumine during organogenesis at doses up to three times the recommended human dose. Because of the potential risks of gadolinium to the fetus, use gadobenate dimeglumine only if imaging is essential and cannot be delayed.L49936

Clinical consequences of overdosage with gadobenate dimeglumine have not been reported. Treatment of an overdosage should be directed toward support of vital functions and prompt institution of symptomatic therapy. In a Phase 1 clinical study, doses up to 0.4 mmol/kg were administered to patients. Gadobenate dimeglumine has been shown to be dialyzable.L49936

Long-term animal studies have not been performed to evaluate the carcinogenic potential of gadobenate dimeglumine.L49936

The results for gadobenate dimeglumine were negative in the following genetic toxicity studies: 1) in vitro bacteria reverse mutation assays, 2) an in vitro gene mutation assay in mammalian cells, 3) an in vitro chromosomal aberration assay, 4) an in vitro unscheduled DNA synthesis assay, and 5) an in vivo micronucleus assay in rats.L49936

Gadobenate dimeglumine had no effect on fertility and reproductive performance at IV doses of up to 2 mmol/kg/day (3 times the human dose on body surface basis) for 13 weeks in male rats and for 32 days in female rats. However, vacuolation in testes and abnormal spermatogenic cells were observed when gadobenate dimeglumine was intravenously administered to male rats at 3 mmol/kg/day (5 times the human dose on body surface basis) for 28 days. The effects were not reversible following 28-day recovery period. The effects were not reported in dog and monkey studies (at doses up to about 11 and 10 times the human dose on body surface basis for dogs (28 days dosing) and monkeys (14 days dosing), respectively).L49936

Gadobenic acid

DB00743

small molecule approved investigational

Deskripsi

Gadobenic acid, usually available in the salt form gadobenate dimeglumine, is a linear MRI gadolinium-based contrast agent (GBCA) used primarily for MR imaging of the liver.A263086 It differs from other GBCAs due to the benzene ring that confers weak protein binding, thus leading to an increased R1 and R2 relaxivity.A263166 As gadobenate dimeglumine is specifically taken up by hepatocytes and excreted through the biliary system, it is a useful contrast agent for liver MRI.A1139

Gadobenate dimeglumine was approved by the FDA in November 2004 under the brand name MultiHance.A263166

Struktur Molekul 2D

Berat 667.73
Wujud liquid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Gadobenate ion has a rapid distribution half-life (reported as mean ± SD) of 0.084 ± 0.012 to 0.605 ± 0.072 hours. The mean elimination half-life ranged from 1.17 ± 0.26 to 2.02 ± 0.60 hours.[L49936]
Volume Distribusi The volume of distribution of the central compartment ranged from 0.074 ± 0.017 to 0.158 ± 0.038 L/kg, and estimates of volume of distribution by area ranged from 0.170 ± 0.016 to 0.282 ± 0.079 L/kg.[L49936]
Klirens (Clearance) The total plasma clearance and renal clearance estimates of gadobenate ion were similar, ranging from 0.093 ± 0.010 to 0.133 ± 0.270 L/hr/kg and 0.082 ± 0.007 to 0.104 ± 0.039 L/hr/kg, respectively. The clearance is similar to that of substances that are subject to glomerular filtration.[L49936]

Absorpsi

Three single-dose intravenous studies were conducted in 32 healthy male subjects to assess the pharmacokinetics of gadobenate dimeglumine. The doses administered in these studies ranged from 0.005 to 0.4 mmol/kg. Upon injection, the meglumine salt is completely dissociated from the gadobenate dimeglumine complex. Thus, the pharmacokinetics is based on the assay of gadobenate ion, the MRI contrast effective ion in gadobenate dimeglumine. Data for plasma concentration and area under the curve demonstrated linear dependence on the administered dose. The pharmacokinetics of gadobenate ion following intravenous administration can be best described using a two-compartment model.L49936 A population pharmacokinetic analysis incorporated data from 25 healthy subjects (14 males and 11 females) and 15 subjects undergoing MR imaging of the central nervous system (7 males and 8 females) between ages of 2 and 16 years. The subjects received a single intravenous dose of 0.1 mmol/kg of gadobenate dimeglumine. The geometric mean Cmax was 62.3 µg/mL (n=16) in children 2 to 5 years of age, and 64.2 µg/mL (n=24) in children older than 5 years. The geometric mean AUC0-? was 77.9 ?g?h/mL in children 2-5 years of age (n=16) and 82.6 ?g?h/mL in children older than 5 years (n=24). The geometric mean half-life was 1.2 hours in children 2 to 5 years of age and 0.93 hours in children older than 5 years. There was no significant gender-related difference in the pharmacokinetic parameters in the pediatric patients. Pharmacokinetic simulations indicate similar AUC and Cmax values for gadobenate dimeglumine in pediatric subjects less than 2 years when compared to those reported for adults; no age-based dose adjustment is necessary for this pediatric population.L49936

Metabolisme

There was no detectable biotransformation of gadobenate ion. Dissociation of gadobenate ion in vivo has been shown to be minimal, with less than 1% of the free chelating agent being recovered alone in feces.L49936

Rute Eliminasi

Gadobenate ion is eliminated predominately via the kidneys, with 78% to 96% of an administered dose recovered in the urine. A small percentage of the administered dose (0.6% to 4%) is eliminated via the biliary route and recovered in feces.L49936

Interaksi Obat

1028 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Gadobenic acid.
Dofetilide The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Dofetilide.
Citalopram The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Citalopram.
Anagrelide The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Anagrelide.
Disopyramide The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Disopyramide.
Clemastine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Clemastine.
Ibutilide The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Ibutilide.
Valproic acid The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Valproic acid.
Terfenadine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Terfenadine.
Grepafloxacin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Grepafloxacin.
Quinine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Quinine.
Sotalol The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Sotalol.
Erlotinib The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Erlotinib.
Toremifene The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Toremifene.
Cisapride The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Cisapride.
Imatinib The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Imatinib.
Astemizole The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Astemizole.
Thioridazine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Thioridazine.
Trovafloxacin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Trovafloxacin.
Mifepristone The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Mifepristone.
Cocaine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Cocaine.
Quinidine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Quinidine.
Procainamide The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Procainamide.
Pimozide The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Pimozide.
Amiodarone The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Amiodarone.
Arsenic trioxide The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Arsenic trioxide.
Escitalopram The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Escitalopram.
Domperidone The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Domperidone.
Sparfloxacin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Sparfloxacin.
Halofantrine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Halofantrine.
Bepridil The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Bepridil.
Paliperidone The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Paliperidone.
Lithium cation The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Lithium cation.
Temafloxacin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Temafloxacin.
Zuclopenthixol The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Zuclopenthixol.
Tetrabenazine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Tetrabenazine.
Dronedarone The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Dronedarone.
Nilotinib The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Nilotinib.
Iloperidone The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Iloperidone.
Vandetanib The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Vandetanib.
Romidepsin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Romidepsin.
Asenapine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Asenapine.
Artemether The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Lumefantrine.
Vemurafenib The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Vemurafenib.
Eliglustat The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Eliglustat.
Ribociclib The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Gadobenic acid.
Glasdegib The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Glasdegib.
Deutetrabenazine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Deutetrabenazine.
Macimorelin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Macimorelin.
Terodiline The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Terodiline.
Leuprolide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Gadobenic acid.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Gadobenic acid.
Erythromycin The risk or severity of QTc prolongation can be increased when Erythromycin is combined with Gadobenic acid.
Azithromycin The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Gadobenic acid.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Gadobenic acid.
Ranolazine The risk or severity of QTc prolongation can be increased when Ranolazine is combined with Gadobenic acid.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Gadobenic acid.
Methadone The risk or severity of QTc prolongation can be increased when Methadone is combined with Gadobenic acid.
Diltiazem The risk or severity of QTc prolongation can be increased when Diltiazem is combined with Gadobenic acid.
Clozapine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Clozapine.
Sulpiride The risk or severity of QTc prolongation can be increased when Sulpiride is combined with Gadobenic acid.
Nimodipine The risk or severity of QTc prolongation can be increased when Nimodipine is combined with Gadobenic acid.
Promazine The risk or severity of QTc prolongation can be increased when Promazine is combined with Gadobenic acid.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Prochlorperazine is combined with Gadobenic acid.
Droperidol The risk or severity of QTc prolongation can be increased when Droperidol is combined with Gadobenic acid.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Chlorpromazine is combined with Gadobenic acid.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Gadobenic acid.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Ciprofloxacin is combined with Gadobenic acid.
Fluorouracil The risk or severity of QTc prolongation can be increased when Fluorouracil is combined with Gadobenic acid.
Perflutren The risk or severity of QTc prolongation can be increased when Perflutren is combined with Gadobenic acid.
Cinnarizine The risk or severity of QTc prolongation can be increased when Cinnarizine is combined with Gadobenic acid.
Atropine The risk or severity of QTc prolongation can be increased when Atropine is combined with Gadobenic acid.
Chloroquine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Gadobenic acid.
Efavirenz The risk or severity of QTc prolongation can be increased when Efavirenz is combined with Gadobenic acid.
Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Gadobenic acid.
Pentamidine The risk or severity of QTc prolongation can be increased when Pentamidine is combined with Gadobenic acid.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Carbinoxamine.
Dolasetron The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Dolasetron.
Roxithromycin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Roxithromycin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Cinoxacin.
Loperamide The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Loperamide.
Granisetron The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Granisetron.
Ondansetron The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Ondansetron.
Levosimendan The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Desloratadine.
Telithromycin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Telithromycin.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Dimenhydrinate.
Primaquine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Primaquine.
Papaverine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Papaverine.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Chlorpheniramine.
Nifedipine The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Nifedipine.
Levofloxacin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Levofloxacin.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Ofloxacin.
Propafenone The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Propafenone.
Flecainide The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Flecainide.

Target Protein

Albumin ALB

Referensi & Sumber

Synthesis reference: Pier Lucio Anelli, Pierfrancesco Morisini, Silvia Ceragioli, Fulvio Uggeri, Luciano Lattuada, Roberta Fretta, Aurelia Ferrigato, "Process for the Preparation of Gadobenate Dimeglumine Complex in a Solid Form." U.S. Patent US20120232151, issued September 13, 2012.
Artikel (PubMed)
  • PMID: 10608412
    de Haen C, Cabrini M, Akhnana L, Ratti D, Calabi L, Gozzini L: Gadobenate dimeglumine 0.5 M solution for injection (MultiHance) pharmaceutical formulation and physicochemical properties of a new magnetic resonance imaging contrast medium. J Comput Assist Tomogr. 1999 Nov;23 Suppl 1:S161-8.
  • PMID: 17921081
    Morana G, Salviato E, Guarise A: Contrast agents for hepatic MRI. Cancer Imaging. 2007 Oct 1;7 Spec No A:S24-7.
  • PMID: 1546612
    Vogl TJ, Pegios W, McMahon C, Balzer J, Waitzinger J, Pirovano G, Lissner J: Gadobenate dimeglumine--a new contrast agent for MR imaging: preliminary evaluation in healthy volunteers. AJR Am J Roentgenol. 1992 Apr;158(4):887-92.
  • PMID: 9818314
    Kirchin MA, Pirovano GP, Spinazzi A: Gadobenate dimeglumine (Gd-BOPTA). An overview. Invest Radiol. 1998 Nov;33(11):798-809.
  • PMID: 10608397
    Clement O, Siauve N, Cuenod CA, Vuillemin-Bodaghi V, Leconte I, Frija G: Mechanisms of action of liver contrast agents: impact for clinical use. J Comput Assist Tomogr. 1999 Nov;23 Suppl 1:S45-52.
  • PMID: 16118549
    Port M, Corot C, Violas X, Robert P, Raynal I, Gagneur G: How to compare the efficiency of albumin-bound and nonalbumin-bound contrast agents in vivo: the concept of dynamic relaxivity. Invest Radiol. 2005 Sep;40(9):565-73.
  • PMID: 9406019
    Cavagna FM, Maggioni F, Castelli PM, Dapra M, Imperatori LG, Lorusso V, Jenkins BG: Gadolinium chelates with weak binding to serum proteins. A new class of high-efficiency, general purpose contrast agents for magnetic resonance imaging. Invest Radiol. 1997 Dec;32(12):780-96.
  • PMID: 25794059
    Fakhran S, Alhilali L, Kale H, Kanal E: Assessment of rates of acute adverse reactions to gadobenate dimeglumine: review of more than 130,000 administrations in 7.5 years. AJR Am J Roentgenol. 2015 Apr;204(4):703-6. doi: 10.2214/AJR.14.13430.
Menampilkan 8 dari 9 artikel.
Textbook
  • ISBN: 978-0-85369-840-1
    Sweetman, Sean C. (2009). Contrast Media. In Martindale : The Complete Drug Reference, 36th Edition 2 Volume Set (36th ed., pp. 1478). Pharmaceutical Press.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • MultiHance
    Injection, solution • 529 mg/1mL • Intravenous • US • Approved
  • MultiHance
    Injection, solution • 529 mg/1mL • Intravenous • US • Approved
  • MultiHance
    Solution • 529 mg / mL • Intravenous • Canada • Approved
International Brands
  • Multihance Multipack — Bracco

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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