Perflubron (Oral-Local)


VA CLASSIFICATION
Primary: DX900

Commonly used brand name(s): Imagent GI.

Another commonly used name is
perfluorooctylbromide .
Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).

Not commercially available in Canada.



Category:


Diagnostic aid, radiopaque (gastrointestinal disorders)—

Indications

Accepted

Gastrointestinal imaging, magnetic resonance—Perflubron is indicated to enhance delineation of the bowel during magnetic resonance imaging (MRI) in order to differentiate it from adjacent structures and from pathologic masses. {01} {02} {03} {04} {05} {07}


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    498.96

Mechanism of action/Effect:

Perflubron acts as a negative bowel contrast agent. It generates no signal during proton MRI. Bowel loops filled with perflubron appear black with all pulse sequences because the contrast agent lacks mobile protons (hydrogen has been replaced with halogen atoms). Due to its insolubility in water it does not mix with intestinal secretions; thus bowel lumina appear homogeneously black on MR images when perflubron replaces bowel contents. {01} {05} {07}

Absorption:

Minimal absorption (less than 0.001% of the administered dose) has occurred in persons with normal gastrointestinal tracts. {01} {06} {09}

Distribution:

Rapid transit through the gastrointestinal tract; reaches rectum within 30 to 40 minutes in most patients. {01} {05} {06} {07}

Elimination:
    Through rectum within 30 minutes of ingestion; usually completely eliminated within 24 to 48 hours. {01} {06}


Precautions to Consider

Carcinogenicity

Long-term animal studies to evaluate carcinogenic potential of perflubron have not been performed. {01}

Mutagenicity

In the Ames test, in a chromosome aberration study conducted in cultured human lymphocytes, and in a mouse micronucleus assay in vivo, perflubron was not shown to cause mutagenesis. {01}

Pregnancy/Reproduction

Pregnancy—
Adequate and well-controlled studies in humans have not been done. However, although there is no evidence that the magnetic and electric fields associated with MRI have an effect on human development, in vitro studies and theoretical predictions raise concern regarding the risk of the developing embryo's or fetus's exposure to MR. More studies are needed to establish the safety of MRI in pregnant patients. {08}

Studies in animals have not been done.

FDA Pregnancy Category C. {01}

Breast-feeding

It is not known whether perflubron is distributed into breast milk. {01}

Pediatrics

Appropriate studies on the relationship of age to the effects of perflubron have not been performed in the pediatric population. However, clinical trials, which included children, were conducted and pediatrics-specific problems that would limit the usefulness of this agent were not reported. {01}


Geriatrics


Appropriate studies on the relationship of age to the effects of perflubron have not been performed in the geriatric population. However, clinical trials, which included older patients, were conducted and geriatrics-specific problems that would limit the usefulness of this medication in the elderly were not reported. {07}


Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

With physiology/laboratory test values
Aspartate aminotransferase (AST [SGOT])    (although rare, serum values may be increased {01} {09})


Bilirubin, serum    (although rare, concentrations may be decreased {01} {09})


Leukocyte count    (may be increased rarely {01} {05} {09})


Diagnostic interference
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

With other diagnostic test results
Computed tomography studies and
Radiographic images    (perflubron may interfere with image interpretation if these studies are done prior to elimination of perflubron {01})


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problems exist
Bowel perforation, known or suspected or
Bowel obstruction, complete    (increased risk of absorption {01})


» Sensitivity to perflubron


Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
    
Abdominal fullness —incidence 5.1%
    
diarrhea —incidence 14.3%
    
nausea and vomiting —incidence 15.8%
    
oily taste in mouth —incidence 30%
    
rectal incontinence{01}{05}{09}
Note: The incidence of nausea and vomiting may be associated with the concurrent administration of glucagon; diarrhea may be dose-related. {01} {05}



Incidence less frequent (1–3%)
    
Abdominal pain —incidence 2.2%
    
rectal flatulence —incidence 2.2%
    
rectal leakage of solution{01}{05}

Incidence rare (<1%)
    
Chills
    
dizziness
    
headache
    
numb mouth
    
tremors
    
vasodilation {01}(flushing or redness of skin)





Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Perflubron (Diagnostic).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Description of use
Action in the body: Passage through gastrointestinal tract allows bowel delineation and improved visualization with MR imaging instruments

Before having this test
»   Conditions affecting use, especially:
Sensitivity to perflubron

Pregnancy—Safety concerns with use of magnetic and electric fields associated with MRI
Other medical problems, especially bowel perforation or complete obstruction

Preparation for this test
Special preparatory instructions may apply; patient should inquire in advance

Fasting for at least 4 hours prior to test is recommended to facilitate ingestion of large volume of contrast agent

Precautions after this test
Leakage of solution from rectum, for the first 3 hours, may require protection of clothing


General Dosing Information
Imaging of the upper abdominal region should begin within 15 minutes of ingestion of perflubron. Imaging of the pelvic region should begin 15 to 60 minutes after ingestion. {01} {05} {06}

Glucagon may be administered after ingestion of perflubron to reduce bowel motion and promote uniform gastrointestinal distribution of the contrast agent. This results in a greater degree of bowel darkening and, thus, increased clarity of bowel wall visualization. {05} {07}


Oral Dosage Forms

PERFLUBRON ORAL SOLUTION

Usual adult and adolescent dose
Gastrointestinal imaging, magnetic resonance
Oral, 9 mL per kg of body weight (usual range, 600 to 1000 mL total dose). {01}


Usual adult prescribing limits
Up to a total dose of 1000 mL. {01}

Usual pediatric dose
Dosage has not been established. {01}

Usual geriatric dose
See Usual adult and adolescent dose .

Size(s) usually available:
U.S.—


200 mL (Rx) [Imagent GI]

Canada—
Not commercially available.

Packaging and storage:
Store between 15 and 30 °C (59 and 86 °F), in a light-resistant container, unless otherwise specified by manufacturer. Protect from light. {01}



Developed: 01/25/1994



References
  1. Imagent GI package insert (Alliance—US), Rev 9/93.
  1. Long DM, Liu MS, Szanto PS, et al. Efficacy and toxicity studies with radiopaque perfluorocarbon. Radiology 1972; 105: 323-32.
  1. Mattrey RF, Hilpert PL, Levine D, et al. PFOB as a negative oral MR contrast agent identifies bowel: clinical results. Invest Radiol 1988; 23(9): S3.
  1. Mattrey RF. Perfluorooctylbromide: a new contrast agent for CT, sonography, and MR imaging. Am J Roentgenol 1989; 152: 247-52.
  1. Brown JJ, Duncan JR, Heiken JP, et al. Perfluorooctylbromide as a gastrointestinal contrast agent for MR imaging: use with and without glucagon. Radiology 1991; 181: 455-60.
  1. Mattrey RF, Trambert JJ, Brown JJ, et al. Results of the phase III trials with Imagent GI as an oral magnetic resonance contrast agent. Invest Radiol 1991; 26: S65-S66.
  1. Rubin DL, Muller HH, Nino-Murcia M, et al. Intraluminal contrast enhancement and MR visualization of the bowel: efficacy of PFOB. J Magn Reson Imaging 1991; 1: 371-80.
  1. National Institutes of Health Panel Issues Report. Consensus Development Conference: Magnetic resonance imaging 1987; Vol. 6 No. 14.
  1. Reviewers' comments as per 09/02/93 monograph revision.
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