Iodohippurate Sodium I 131 (Systemic)


VA CLASSIFICATION
Primary: DX201

Commonly used brand name(s): Hippuran; Hipputope.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Diagnostic aid, radioactive (renal disorders; urinary tract obstructions)—

Indications

Accepted

Renography—Iodohippurate sodium I 131 is indicated in renography to determine renal function, effective renal plasma flow, and urinary tract obstruction. {01} {10} {15} {16} {17}

Renal imaging, radionuclide—Iodohippurate sodium I 131 is indicated as an imaging agent to assess renal size, position, configuration, and function. {01} {04} {15}


Physical Properties

Nuclear data: {19}



Radionuclide
(half-life)
Mode of
decay
Principal
photon
emissions
(keV)
Mean number
of emissions/
disintegration
I 131
(8.08 days)
Beta
Beta (191.6)
Gamma (364.4)
0.90
0.81


Pharmacology/Pharmacokinetics

Mechanism of action/Effect:

Based on its excretion by both tubular secretion and glomerular filtration, which can be observed by appropriate imaging or detection systems. {17}

Half-life:

For iodohippurate sodium (biological)—Approximately 20 to 30 minutes. {05} {09}

Time to peak concentration:

Kidneys—Approximately 3 to 6 minutes. {05} {09} {17}

Radiation dosimetry:
{14}

Organ
Estimated absorbed radiation dose*
With normal
kidney function
With impaired
kidney function
mGy/
MBq
rad/mCi
mGy/
MBq
rad/mCi
Bladder wall
0.96
3.55
0.63
2.33
Uterus
0.35
1.30
0.039
0.14
Kidneys
0.30
1.11
0.15
0.56
Large intestine
(lower)
0.17
0.63
0.027
0.099
Ovaries
0.17
0.63
0.026
0.096
Testes
0.12
0.44
0.022
0.081
Small intestine
0.0078
0.029
0.022
0.081
Large intestine (upper)
0.0069
0.026
0.021
0.078
Red marrow
0.0049
0.018
0.019
0.070
Bone surfaces
0.0030
0.011
0.017
0.063
Adrenals
0.0028
0.010
0.021
0.081
Pancreas
0.0026
0.0096
0.019
0.070
Spleen
0.0024
0.0089
0.019
0.070
Stomach wall
0.0025
0.0093
0.018
0.067
Liver
0.0023
0.0085
0.025
0.093
Lungs
0.0016
0.0059
0.015
0.056
Thyroid
0.0014
0.0052
0.014
0.052
Other tissue
0.0054
0.020
0.018
0.067
Effective dose
0.066
mSv/MBq
0.24
rem/mCi
0.065
mSv/MBq
0.24
rem/mCi
* For adults; intravenous administration.
 Data based on the International Commission on Radiological Protection (ICRP) Publication 53—Radiation dose to patients from radiopharmaceuticals. {14}

Elimination:
    Renal, 50 to 75% within 25 minutes and 90 to 95% within 8 hours (primarily by tubular cell secretion [80%], but also by glomerular filtration [20%]). Iodide I 131 is eliminated in breast milk, also. {01} {04} {05} {16} {17}


Precautions to Consider

Pregnancy/Reproduction

Pregnancy—
Studies have not been done in humans with iodohippurate sodium I 131. However, iodide I 131 crosses the placenta and may cause severe and irreversible hypothyroidism in the newborn. Iodohippurate sodium I 131 is not recommended for use during pregnancy. {05} {06} {07} {08} {17}

The possibility of pregnancy should be assessed in women of child-bearing potential. Clinical situations exist where the benefit to the patient and fetus, based on information derived from radiopharmaceutical use, outweighs the risks from fetal exposure to radiation. In these situations, the physician should use discretion and reduce the radiopharmaceutical dose to the lowest possible amount. {12}

Studies have not been done in animals. {01}

FDA Pregnancy Category C. {01} {15}

Breast-feeding

Iodide I 131 is excreted in breast milk. Because of the potential risk to the infant from radiation exposure, temporary discontinuation of nursing is recommended for approximately 5 days. {01} {06} {08} {11} {17} {20}

Pediatrics

Although iodohippurate sodium I 131 is used in children, there have been no specific studies evaluating its safety and efficacy in children. When this radiopharmaceutical is used in children, the diagnostic benefit should be judged to outweigh the potential risk of radiation. {12} {17}


Geriatrics


Appropriate studies on the relationship of age to the effects of iodohippurate sodium I 131 have not been performed in the geriatric population. However, no geriatrics-specific problems have been documented to date.

Drug interactions and/or related problems
See Diagnostic interference.

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 results of this test

Due to other medications
Probenecid    (concurrent use may decrease kidney uptake of iodohippurate sodium I 131 due to a direct inhibition of the enzyme transport system in the proximal tubule by probenecid {09})


Due to medical problems or conditions
Dehydration    (kidney uptake of iodohippurate sodium I 131 may be reduced and renal transit time may be prolonged {15})

Due to other diagnostic tests
Retrograde pyelogram    (may alter renogram curve; renogram should be performed before or at least 24 hours after this procedure {04})

With other diagnostic test results
Thyroid function determinations and
Thyroid imaging    (Lugol's solution used prior to the administration of iodohippurate sodium I 131 may cause a decrease in radioactive iodine or pertechnetate ion uptake for several weeks)


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).

See also Diagnostic interference.

Risk-benefit should be considered when the following medical problem exists
Sensitivity to the radiopharmaceutical preparation


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
Incidence rare
—not clearly related to iodohippurate sodium I 131    
Fainting
    
nausea or vomiting{15}{17}





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

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

Description of use
Action in the body: Elimination by tubular cell secretion and glomerular filtration

Appearance, concentration, and elimination of iodohippurate sodium I 131 in kidneys allows monitoring and visualization

Small amounts of radioactivity used in diagnosis; radiation received is low and considered safe

Before having this test
»   Conditions affecting use, especially:
Sensitivity to the radiopharmaceutical preparation

Pregnancy—Risk to fetus from radiation exposure as opposed to benefit derived from use should be considered; possibility of hypothyroidism in newborn





Breast-feeding—Iodide I 131 excreted in breast milk; temporary discontinuation of nursing recommended because of risk to infant from radiation exposure





Use in children—Risk from radiation exposure as opposed to benefit derived from use should be considered


Preparation for this test
Special preparatory instructions may apply; patient should inquire in advance {09}


Precautions after having this test:
Possible interference with future thyroid tests



Side/adverse effects
Signs of potential side effects, especially fainting, nausea, or vomiting


General Dosing Information
Radiopharmaceuticals are to be administered only by or under the supervision of physicians who have had extensive training in the safe use and handling of radioactive materials and who are authorized by the Nuclear Regulatory Commission (NRC) or the appropriate Agreement State agency, if required, or, outside the U.S., the appropriate authority. {15} {18}

Approximately 25% of the free iodide content of iodohippurate sodium I 131 is taken up by the thyroid gland following intravenous administration. To help minimize thyroidal uptake of free iodide I 131, a thyroid blocking agent such as a saturated solution of potassium iodide or potassium perchlorate should be given prior to administration of iodohippurate sodium I 131 and for several days afterwards. {01} {05} {10} {15} {17}

To assure adequate urine flow, increased oral intake of fluids is recommended 1 hour prior to the diagnostic procedure, unless contraindicated because of the presence of edema or congestive heart failure. {09} {10}

Iodohippurate Sodium I 131 Injection USP is not intended for intra-arterial use. Also, precautions should be taken to avoid extravasation during intravenous administration. {01}

Safety considerations for handling this radiopharmaceutical
Improper handling of this radiopharmaceutical may cause radioactive contamination. Guidelines for handling radioactive material have been prepared by scientific, professional, state, federal, and international bodies and are available to the specially qualified and authorized users who have access to radiopharmaceuticals. {21}


Parenteral Dosage Forms

IODOHIPPURATE SODIUM I 131 INJECTION USP

Usual adult and adolescent administered activity
Renography
Intravenous, 0.0185 megabecquerel (0.5 microcurie) per kg of body weight.

Renal imaging, radionuclide
Intravenous, 0.1 to 0.185 megabecquerel (3 to 5 microcuries) per kg of body weight. {01} {15}


Usual pediatric administered activity
Dosage must be individualized by physician.

Usual geriatric administered activity
See Usual adult and adolescent administered activity .

Strength(s) usually available
U.S.—



At time of calibration: Per multiple-dose vial—


37 megabecquerels (1 millicurie) (Rx) [Hippuran] [Hipputope][Generic]


74 megabecquerels (2 millicuries) (Rx) [Hipputope][Generic]

Canada—


Various concentrations as per manufacturer's labeling (Rx)[Generic]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Note: Caution—Radioactive material.




Revised: 08/02/1994



References

Note: All references used in the development and earlier revisions of this monograph have not yet been incorporated into the computer database and, therefore, are not listed below. Citations for information not yet referenced in the monograph will be provided upon request.

  1. Package insert (Squibb).
  1. USP/NF.
  1. Report by Michael Stabin, Oak Ridge Assoc. University, Radiopharmaceutical Internal Dose Information Center, 4/84.
  1. Maynard CD. Clinical nuclear medicine. Philadelphia: Lea & Febiger, 1971: 228.
  1. American Hospital Formulary Service.
  1. Avery's drug treatment 1987. 3rd ed., 95, 116.
  1. Williams R, editor. Textbook of endocrinology. 6th ed. 1981: 220-1.
  1. AMA-Drug Evaluations.
  1. Hladik WB, Saha GB, Study KT. Essentials of nuclear medicine science. Baltimore: Williams & Wilkins, 1987: 26, 29, 30, 120, 219, 415.
  1. Chilton HM, Witcofski RL. Nuclear pharmacy—An introduction to the clinical application of radiopharmaceuticals. Philadelphia: Lea & Febiger, 1986: 127.
  1. Mountford PJ, Coakley AJ. A review of the secretion of radioactivity in human breast milk: data, quantitative analysis and recommendations. 1989; Nucl Med Commun 10: 15-27.
  1. USP Radiopharmaceuticals Advisory Panel meeting 5/91.
  1. Maisey MN, Britton KE, Gilday DL. Clinical nuclear medicine. 2nd ed. Philadelphia: J.B. Lippincott, 1991: 98.
  1. Task Group of Committee 2 of the International Commission on Radiological Protection. Annals of the ICRP. ICRP Publication 53—Radiation dose to patients from radiopharmaceuticals. New York: Pergamon Press, 1988: 311.
  1. Mallinckrodt package insert, rev 8/90.
  1. Blaufox MD. Procedures of choice in renal nuclear medicine. J Nucl Med 1991; 32: 1301-9.
  1. Swanson DP, Chilton HM, Thrall JH, editors. Pharmaceuticals in medical imaging. New York: Macmillan Publishing Company, 1990: 502, 515.
  1. USP Radiopharmaceuticals Advisory Panel meeting 8/4/92.
  1. Reviewers' comments on monograph revision of 10/05/92.
  1. Romney BM, et al. Radionuclide Administration to Nursing Mothers: Mathematically Derived Guidelines. Radiology 1986; 160: 549-54.
  1. Reviewers' responses to Ballot of 5/11/94.
  1. Eshima D, Fritzber AR, Taylor A Jr. Tc 99m renal tubular function agents: current status. Semin Nucl Med 1990; 20(1): 28-40.
  1. Thrall JH, Koff SA, Keyes JW. Diuretic radionuclide renography and scintigraphy in the differential diagnosis of hydroureteronephrosis. Semin Nucl Med 1981; 11(2): 89-104.
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