Mechanism of effect
Pharmacodynamic
Pharmacokinetics
Distribution
Vdss: 148 ± 16 mL/kg
:Metabolism
Negligible
Excretion
Urine (79% to 94% as unchanged drug); feces (~5%)
Onset of Action
5 to 7 minutes
Duration of Action
~1 hour
Half-Life Elimination
16.3 ± 2.6 hours; moderate renal impairment: 49 hours; severe renal impairment: 70 hours
Protein Binding
80% to 87% (predominantly to albumin)
Drug indications
contrast agent during coronary angiographyGadofosost is a paramagnetic contrast agent from the non-ionic spectrum based on the element galadynium, which is used as a contrast agent in MRI imaging.
Dosage
Angiography imaging: IV: 0.03 mmol/kg ، 0.12 mL/kg
Drug contraindications
Kidney function abnormal , Hypersensitivity to this drugAny history of sensitivity to galadynium derivatives.
Patients with renal impairment and drug dysfunction
Patients prone to systemic nephrotic fibrosis
NFS
Side effects
Headache , Nephrotic syndrome , vertigo , Chills , Hypertension , Injection-site reaction , itchingHeadache. Injection site reactions. Paresthesia. Vasodilatation of peripheral arteries
Nephrogenic systemic fibrosis:
Gadolinium-based contrast agents increase the risk of nephrogenic systemic fibrosis (NSF) in patients with impaired elimination of the drugs. In these patients, avoid use of gadolinium-based contrast agents unless the diagnostic information is essential and not available with noncontrast-enhanced magnetic resonance imaging (MRI) or other modalities. NSF may result in fatal or debilitating fibrosis affecting the skin, muscle, and internal organs.
The risk for NSF appears highest among patients with chronic, severe kidney disease (glomerular filtration rate [GFR] <30 mL/minute per 1.73 m2) or acute kidney injury.
Screen patients for acute kidney injury and other conditions that may reduce renal function. For patients at risk of chronically reduced renal function (eg, >60 years, hypertension, diabetes), estimate the GFR through laboratory testing.
For patients at highest risk for NSF, do not exceed the recommended gadofosveset dose. Allow a sufficient period of time for elimination of the drug from the body prior to readministration.
Interactions
Amitriptyline , Amiodarone , Erythromycin , Imipramine , Pimozide , Tacrolimus , Quinidine , Thioridazine , Disopyramide , Cisapride , Haloperidol , Dapoxetine , TamoxifenAlerts
Nephrogenic systemic fibrosis:
Gadolinium-based contrast agents increase the risk of nephrogenic systemic fibrosis (NSF) in patients with impaired elimination of the drugs. In these patients, avoid use of gadolinium-based contrast agents unless the diagnostic information is essential and not available with noncontrast-enhanced magnetic resonance imaging (MRI) or other modalities. NSF may result in fatal or debilitating fibrosis affecting the skin, muscle, and internal organs.
The risk for NSF appears highest among patients with chronic, severe kidney disease (glomerular filtration rate [GFR] <30 mL/minute per 1.73 m2) or acute kidney injury.
Screen patients for acute kidney injury and other conditions that may reduce renal function. For patients at risk of chronically reduced renal function (eg, >60 years, hypertension, diabetes), estimate the GFR through laboratory testing.
For patients at highest risk for NSF, do not exceed the recommended gadofosveset dose. Allow a sufficient period of time for elimination of the
drug from the body prior to readministration.
QTc prolongation: Rare cases of QTc prolongation have been observed with gadofosveset use. Data from pooled safety studies have demonstrated that the administration of gadofosveset resulted in minimal changes to the QTc interval as compared to placebo (means of 2.8 msec and 3.2 msec respectively). Consider baseline and follow up ECG in patients at increased risk of arrhythmias due to QTc prolongation (eg, underlying cardiac disease, concurrent medications). Patients should be monitored for at least 1 hour after the administration of gadofosveset.
Points of recommendation
What is this drug used for?
• It is used during an MRA (magnetic resonance angiography) test.
Frequently reported side effects of this drug
• Injection site irritation
• Itching
• Nausea
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
• Nephrogenic systemic fibrosis like skin burning, itching, swelling, or scaling; red or dark spots on the skin; hard or tight skin; stiff joints; muscle weakness; hip or rib pain; trouble moving, bending, or straightening arms, hands, legs, or feet.
• Kidney problems like unable to pass urine, blood in urine, change in amount of urine passed, weight gain.
Pregnancy level
Group c - Not adequate studies in pregnant women
Pregnancy Risk Factor
C
Pregnancy Considerations
Gadolinium-based contrast agents may cross the placenta (ACOG 723 2017; ACR 2018).
Use of gadolinium-based contrast agents in pregnancy is controversial and should be limited. A gadolinium-based contrast agent may be considered for use in pregnancy if it will significantly improve diagnostic performance and is expected to improve fetal or maternal outcome (ACOG 723 2017). In addition, use should only be considered if information needed from the study cannot be acquired without using a contrast agent and cannot be deferred until after delivery. Agents with a low risk for development of nephrogenic systemic fibrosis should be used at the lowest effective dose
Breast feeding warning
There is no published experience with gadofosveset during breastfeeding. Guidelines developed by several North American professional organizations state that breastfeeding need not be disrupted after a nursing mother receives a gadolinium-containing contrast medium.Related drugs
Gadobutrol , Gadopentetic acid , Gadoteric acid , Gadodiamide , DotaremGadobutrol
Gadodiamide
Gadolinium
Gadopentetic acid
Gadoteric acid
Gadoteridol
Gadoversetamide
Gadoxetic acid
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