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Gadofosveset

Medically reviewed by Drugs.com. Last updated on Aug 21, 2020.

Pronunciation

(gad oh FOS ve set)

Index Terms

  • Gadofosveset Trisodium

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Intravenous [preservative free]:

Ablavar: 244 mg/mL (10 mL [DSC], 15 mL [DSC])

Brand Names: U.S.

  • Ablavar [DSC]

Pharmacologic Category

  • Diagnostic Agent
  • Gadolinium-Containing Contrast Agent
  • Linear Gadolinium-Based Contrast Agent
  • Radiological/Contrast Media, Nonionic (Low Osmolality)
  • Radiological/Contrast Media, Paramagnetic Agent

Pharmacology

Gadofosveset is a gadolinium-containing paramagnetic agent that reversibly binds to albumin in the plasma. Exposure to an external magnetic field induces a large local magnetic field in exposed blood vessels. This local magnetism disrupts water protons in the vicinity, resulting in a change in proton density and spin characteristics, which can be detected by the imaging device. The binding of gadofosveset to albumin prolongs the period of time gadofosveset resides intravascularly, enhances T1 relaxivity up to 10 times greater than nonprotein bound gadolinium chelates and provides a longer imaging window.

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)

Special Populations: Renal Function Impairment

Clearance decreases substantially as renal function decreases. AUC increased 1.75-fold in patients with moderate (CrCl 30 to 50 mL/minute) and 2.25-fold in patients with severe renal impairment (CrCl <30 mL/minute).

Use: Labeled Indications

Angiography imaging: Contrast medium agent used in magnetic resonance angiography (MRA) to evaluate aortoiliac occlusive disease in adults with known or suspected peripheral vascular disease.

Contraindications

History of prior hypersensitivity to any gadolinium-based contrast agent.

Dosing: Adult

Angiography imaging: IV: 0.03 mmol/kg (0.12 mL/kg).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Administration

IV: Administer as an intravenous bolus injection over a period up to 30 seconds through a dedicated IV line separate from other medications. Flush line with 25-30 mL NS after administration to ensure complete injection of medium. Imaging should be completed within 1 hour of injection.

Storage

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F); do not freeze. Protect from light. Use immediately after opening.

Drug Interactions

Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of Haloperidol. Monitor therapy

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Monitor therapy

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%:

Cardiovascular: Vasodilation (3%), hypertension (1%)

Central nervous system: Headache (4%), paresthesia (3%), burning sensation (2%), dizziness (1%), sensation of cold (1%)

Dermatologic: Pruritus (5%)

Gastrointestinal: Nausea (4%), dysgeusia (2%)

Local: Bruising at injection site (2%)

<1%, postmarketing, and/or case reports: Acute renal failure, anaphylactoid reaction, anaphylaxis, nephrogenic systemic fibrosis (NSF/NFD), prolonged QT interval on ECG

ALERT: U.S. Boxed Warning

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.

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity reactions: Hypersensitivity, including anaphylactic reactions (rare), may occur; appropriate equipment (eg, ventilator) and emergency medications (eg, epinephrine) should be available during use. Delayed reactions may also occur (within several hours of administration). Patients with a history of allergic reactions and/or bronchial asthma may be at an increased risk for developing hypersensitivity reactions; use caution in these patients.

• Nephrogenic systemic fibrosis: [US Boxed Warning]: Gadolinium-based contrast agent (GBCA) exposure may increase the risk for nephrogenic systemic fibrosis (NSF) in patients with renal impairment; avoid use unless GBCA enhanced imaging is essential for diagnostic purposes. The risk is highest in patients with acute kidney injury or chronic, severe renal disease (GFR <30 mL/minute/1.73 m2). The risk appears lower in patients with moderate, chronic renal disease (GFR 30 to 59 mL/minute/1.73 m2) and little, if any, in patients with mild, chronic renal disease (GFR 60 to 89 mL/minute/1.73 m2). NSF, a potentially fatal disease, affects the skin, muscle, and internal organs. All patients should be screened for renal dysfunction prior to administration; estimate GFR in patients at risk for chronic renal disease (diabetes, chronic hypertension, age >60 years). In patients at risk of NSF, do not exceed the recommended dosage and allow sufficient time (ie, several half-lives) for elimination prior to readministration (avoidance of readministration is preferred). In patients receiving hemodialysis, consider prompt initiation of hemodialysis following administration.

• 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.

Disease-related concerns:

• Renal impairment: Use with caution in patients with renal impairment. Dose-dependent worsening of renal function or acute renal failure has occurred in patients with renal insufficiency following use of other gadolinium agents, generally within 48 hours following administration. Dosage reductions may be necessary. Evaluate renal function in patients with renal impairment prior to use; consider follow-up monitoring.

Monitoring Parameters

Baseline ECG if risk factors for QTc prolongation/torsade de pointes; baseline electrolytes (including potassium, calcium and magnesium); screen for renal impairment (all patients); baseline renal function in patients at risk of NSF and follow-up evaluation with renal dysfunction; signs of hypersensitivity (during and for several hours after procedure); short- and long-term monitoring of signs and symptoms of NSF/NFD (eg, burning, itching, swelling, hardening and/or tightening of skin, joint stiffness, deep hip or rib bone pain, muscle weakness, limited range of motion, and/or yellowed/raised spots on whites of eye).

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 (ACR 2018).

Patient Education

What is this drug used for?

• It is used during an MRA (magnetic resonance angiography) test.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Injection site irritation

• Itching

• Nausea

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• 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.

• Severe dizziness

• Passing out

• Abnormal heartbeat

• Fast heartbeat

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.