Medication Guide App

Technetium Tc 99m Gluceptate (Systemic)


VA CLASSIFICATION
Primary: DX201

Commonly used brand name(s): Frosstimage Gluceptate; Frosstimage Gluco; Glucoscan; TechneScan Gluceptate.

Another commonly used name is
technetium Tc 99m glucoheptonate .
Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Diagnostic aid, radioactive (intracranial lesions; cerebral disorders; renal disorders)—

Indications

Accepted

Brain imaging, radionuclide—Technetium Tc 99m gluceptate is indicated as a brain imaging agent to detect and evaluate intracranial lesions, including brain tumors. {01} {08} {20}

Renal imaging, radionuclide—Technetium Tc 99m gluceptate is indicated as a renal imaging agent to evaluate kidney size, shape, and position, especially in parenchymal disorders. {01} {08} {20}

Brain perfusion studies or
Renal perfusion studies—Technetium Tc 99m gluceptate is indicated in dynamic brain and renal perfusion studies. {01} {08} {20}


Physical Properties

Nuclear data:



Radionuclide
(half-life)
Decay
constant
Mode
of
decay
Principal
photon
emissions
(keV)
Mean
number of
emissions/
disintegration
(³0.01)
Tc 99m
(6.0 hr)
0.1151 h -1
Isomeric
transition to
Tc 99
Gamma
(18)
0.062
Gamma
(140.5)
0.891


Pharmacology/Pharmacokinetics

Mechanism of action/Effect:


Diagnostic aid (intracranial lesions; cerebral disorders):

Technetium Tc 99m gluceptate accumulates, by passive diffusion, in intracranial lesions with an altered blood-brain barrier. The radionuclide emissions may then be detected to determine the presence and localization of the lesion. {17}



Diagnostic aid (renal disorders):

Based on its rapid clearance through the urinary tract. Urinary clearance of technetium Tc 99m gluceptate occurs by both glomerular filtration and tubular secretion; however, a sufficient amount is retained by the renal cortex to allow delayed static images to be performed for evaluation of cortical morphology. {05}


Distribution:

Rapidly distributed in and cleared from plasma; up to 15% of dose localizes in the tubules of the renal cortex by 3 hours. {01} {07} {17} {20}

Radiation dosimetry:


Estimated absorbed radiation dose*
Organ
mGy/MBq
rad/mCi
Bladder wall
0.056
0.21
Kidneys
0.049
0.18
Uterus
0.0077
0.029
Adrenals
0.0046
0.017
Ovaries
0.0046
0.017
Large intestine
wall (lower)

0.0044

0.016
Red marrow
0.0039
0.014
Spleen
0.0039
0.014
Small intestine
0.0037
0.014
Pancreas
0.0036
0.013
Large intestine
wall (upper)

0.0033

0.012
Testes
0.0029
0.011
Stomach wall
0.0027
0.010
Liver
0.0027
0.010
Bone surfaces
0.0026
0.0096
Lungs
0.0017
0.0063
Breast
0.0014
0.0052
Thyroid
0.0011
0.0041
Other tissue
0.0023
0.0085
Effective dose: 0.0090 mSv/MBq (0.033 rem/mCi)
* In adults; intravenous administration. Data based on the International Commission on Radiological Protection (ICRP) Publication 53—Radiation dose to patients from radiopharmaceuticals. {12}

Elimination:


Renal (by both glomerular filtration and renal tubular secretion) {07}
        Normal renal function: about 40% of the administered activity eliminated in 1 hour; about 70% of the administered activity eliminated within 24 hours.
        Renal function impairment: Urinary elimination is delayed. Hepatobiliary elimination may occur. {01} {14} {17}



Precautions to Consider

Carcinogenicity/Mutagenicity

Long-term animal studies to evaluate carcinogenic or mutagenic potential of technetium Tc 99m gluceptate have not been performed.

Pregnancy/Reproduction

Pregnancy—
Tc 99m (as free pertechnetate) crosses the placenta. However, studies have not been done with technetium Tc 99m gluceptate in humans.

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.

Studies have not been done in animals.

FDA Pregnancy Category C. {01} {09} {20}

Breast-feeding

Although it is not known whether technetium Tc 99m gluceptate is distributed into breast milk, it is known that Tc 99m as free pertechnetate is distributed into breast milk. Based on the assumption that the Tc 99m in breast milk is in the form of pertechnetate and based on the effective half-life of the radionuclide in breast milk, the daily volume of milk, a dose factor relating the radionuclide to its critical organ (thyroid) in the nursing infant, and the maximum permissible dose to that organ, a guideline has been proposed. According to this guideline, it has been calculated that nursing can be safely resumed when the concentration in breast milk reaches 30.3 × 10 -4 megabecquerels (8.2 × 10 -2 microcuries) per mL. This level of activity is probably reached, in the majority of patients, within 24 hours after administration of 740 megabecquerels (20 millicuries) of technetium Tc 99m–labeled radiopharmaceuticals. {05}

Pediatrics

Diagnostic studies performed in children have not demonstrated pediatrics-specific problems that would limit the usefulness of technetium Tc 99m gluceptate in children. However, when this radiopharmaceutical is used in children, the diagnostic benefit should be judged to outweigh the potential risk of radiation. {07} {16}


Geriatrics


Appropriate studies on the relationship of age to the effects of technetium Tc 99m gluceptate 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 brain imaging

Due to other medications
Corticosteroids, glucocorticoid    (uptake of technetium Tc 99m gluceptate in cerebral tumor or abscess may be decreased because of reduced peritumor edema caused by the corticosteroids {04})


Due to medical problems or conditions
Neurotoxicity, induced by such drugs as:
Cyclophosphamide or
Dactinomycin or
Doxorubicin or
Vincristine    (brain images may show increased activity due to chemotherapeutic neurotoxicity following therapy with these medications {13})

With results of renal imaging

Due to other medications
Penicillamine    (concurrent penicillamine therapy may cause transchelation of technetium Tc 99m gluceptate to a compound excreted through the hepatobiliary system, thus resulting in gallbladder visualization; gallbladder visualization may mimic abnormal kidney localization on posterior views of renal images)


Probenecid    (concurrent use may decrease kidney uptake of technetium Tc 99m gluceptate due to a direct inhibition of the enzyme transport system in the proximal tubule by probenecid {04})


Due to medical problems or conditions
Dehydration    (decreased urinary flow may result in poor renal images)


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 must 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 less frequent or rare
    
Allergic reaction (skin rash, hives, or itching){01}{04}





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: Concentration of radioactive gluceptate in brain lesions and kidneys

Retention of radioactivity in brain lesions and kidneys allows visualization

Small amount 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—Technetium Tc 99m (as free pertechnetate) crosses placenta; risk to fetus from radiation exposure as opposed to benefit derived from use should be considered





Breast-feeding—Not known if technetium Tc 99m gluceptate is distributed into breast milk, but Tc 99m as free pertechnetate is distributed into breast milk; temporary discontinuation of nursing may be 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 be given; patient should inquire in advance

Precautions after having this test
Increasing intake of fluids and voiding as often as possible for 4 to 6 hours after examination to minimize radiation dose to bladder


Side/adverse effects
Signs of potential side effects, especially allergic reaction


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.

Adequate hydration of the patient is recommended before and after examination to promote urinary flow. Also, urination is recommended as often as possible for 4 to 6 hours after the examination to reduce radiation dose to the bladder. {07} {17}

Manufacturer's package insert or other appropriate literature should be consulted for optimal times when imaging should be performed.

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. {19}


Parenteral Dosage Forms

TECHNETIUM Tc 99m GLUCEPTATE INJECTION USP

Usual adult and adolescent administered activity
Brain imaging or
Brain perfusion studies
Intravenous, 555 to 740 megabecquerels (15 to 20 millicuries). {08} {09}

Renal imaging or
Renal perfusion studies
Intravenous, 370 to 555 megabecquerels (10 to 15 millicuries). {08} {09} {14}


Usual pediatric administered activity
Brain imaging
Intravenous, 7.9 to 10.6 megabecquerels (0.21 to 0.28 millicuries) per kg of body weight, with a minimum total dosage of at least 74 megabecquerels (2 millicuries) and a maximum total dosage of 740 megabecquerels (20 millicuries). {15} {17}

Renal imaging
Intravenous, 5.3 to 10.6 megabecquerels (0.14 to 0.28 millicuries) per kg of body weight, with a minimum total dosage of at least 37 megabecquerels (1 millicurie) and a maximum total dosage of 370 megabecquerels (10 millicuries). {15} {17}


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

Strength(s) usually available
U.S.—


50 mg gluceptate calcium, 0.7 mg minimum stannous tin as stannous chloride dihydrate, and 1.1 mg maximum total tin as stannous chloride dihydrate (in a lyophilized form and under a nitrogen atmosphere), per10-mL reaction vial (Rx) [TechneScan Gluceptate]


200 mg gluceptate sodium, 0.06 mg minimum stannous tin as stannous chloride, and 0.07 mg maximum tin (in a lyophilized form and under a nitrogen atmosphere), per reaction vial (Rx) [Glucoscan]

Canada—


25 mg gluceptate calcium, 3 mg stannous chloride dihydrate (in lyophilized form under nitrogen atmosphere), per 10-mL reaction vial (Rx) [Frosstimage Gluceptate]


50 mg gluceptate calcium, 0.7 mg minimum stannous chloride dihydrate, and 1.1 mg maximum total tin expressed as stannous chloride dihydrate (in lyophilized form under nitrogen atmosphere), per 10-mL reaction vial (Rx) [Frosstimage Gluco]

Packaging and storage:
Store between 2 and 8 °C (36 and 46 °F). Protect from freezing. {17}

Note: Prior to labeling, kit can be stored at room temperature. {08} {09} {17}


Preparation of dosage form:
To prepare injection, an oxidant-free sodium pertechnetate Tc 99m solution is used. See manufacturer's package insert for instructions.

Stability:
Injection should be administered within 6 hours after preparation.

Incompatibilities:
If oxidants such as peroxides and hypochlorites are present in the sodium pertechnetate Tc 99m used for labeling, the final preparation may be adversely affected and should be discarded.

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 (Glucoscan—US), Rev 1984.
  1. Chilton HM, Witcofski RL: Nuclear Pharmacy—An introduction to the clinical application of radiopharmaceuticals. Philadelphia: Lea & Febiger, 1986: 99-101.
  1. Fleeger CA, editor. USAN 1993. USAN and the USP dictionary of drug names. Rockville, MD: The United States Pharmacopeial Convention, Inc., 1992.
  1. Hladik WB, Saha GB, Study KT. Essentials of nuclear medicine science. Baltimore: Williams & Wilkins, 1987: 219.
  1. USP Radiopharmaceuticals Advisory Panel meeting of 01/88.
  1. Hinkle GH, Basmadjian GP, Peek C, et al. Effects of concurrent drug therapy on technetium Tc 99m gluceptate biodistribution. Am J Hosp Pharm 1982; 39: 1930-3.
  1. Swanson DP, Chilton HM, Thrall JH, eds. Pharmaceuticals in medical imaging. New York: Macmillan Publishing Company, 1990: 312-6, 521-6.
  1. Frosstimage Gluco package insert (Frosst—Canada), Rev 01/90.
  1. TechneScan Gluceptate package insert (Mallinckrodt—US), Rev 03/89.
  1. USP Radiopharmaceuticals Advisory Panel meeting of 05/08/91.
  1. USP Radiopharmaceuticals Advisory Panel meeting of 08/04/92.
  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: 194.
  1. Hladik WB, Nigg KK, Rhodes BA. Drug-induced changes in the biologic distribution of radiopharmaceuticals. Semin Nucl Med 1982; 12(2): 208.
  1. Reviewers' comments per monograph revision of 07/84.
  1. Pediatric dosages submitted by USP Radiopharmaceuticals Advisory panelists 08/92.
  1. Ash JM, Antico VF, Gilday DL, et al. Special considerations in the pediatric use of radionuclides for kidney studies. Semin Nucl Med 1982; 12: 345-69.
  1. The United States pharmacopeia. The national formulary. USP 22nd revision (January 1, 1990). NF 17th ed (January 1, 1990). Rockville, MD: The United States Pharmacopeial Convention, Inc., 1990: 1315.
  1. Reviewers' comments per monograph revision of 11/25/92.
  1. Reviewers' responses to Ballot of 5/11/94.
  1. Package insert (TechneScan Gluceptate—US), Rev 5/83.
  1. Blaufox MD. Procedures of choice in renal nuclear medicine. J Nucl Med 1991; 32: 1301-9.
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