Professional Information
Indium In 111 Oxyquinoline (Systemic)
VA CLASSIFICATION
Primary: DX201
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, radioactive (inflammatory lesions; thrombosis)—
Indications
Note: Bracketed information in the Indications section refers to uses that are not included in U.S. product labeling.
Accepted
Leukocytes, labeling of
Indium In 111 oxyquinoline is indicated for the labeling of autologous leukocytes. Indium In 111–labeled leukocytes are used for the following diagnostic studies:
Inflammatory lesions (diagnosis)—To locate inflammatory lesions such as abscesses. Indium In 111–labeled leukocytes are commonly used for the diagnosis of intra-abdominal abscesses, which may occur as complications of surgery, injuries, or inflammatory diseases of the gastrointestinal tract. Also, since labeled leukocytes localize in the inflamed gut mucosa, they are useful for demonstrating the presence, distribution, and extent of inflammatory bowel disease, including Crohn's disease and ulcerative colitis. In addition, labeled leukocytes are useful for demonstrating infections of prosthetic vascular grafts, and pyelonephritis and cystitis. Labeled leukocytes serve to evaluate acute and chronic osteomyelitis and are effective in demonstrating or excluding infection of orthopedic prostheses. The pattern of pulmonary uptake (diffuse vs. focal) of indium In 111–labeled leukocytes is used to rule out pulmonary or pleural infection, especially when chest x-rays are abnormal. {01} {02} {11} {14} {16} {17} {18} {22} {28} {35} {39} {41} {46}
—Indium In 111–labeled leukocyte scans have become useful as an adjunct to other diagnostic procedures in the detection of gastrointestinal and central nervous system (CNS) infections, such as focal encephalitis, cryptococcal meningitis, and cytomegalovirus encephalitis, in acquired immunodeficiency syndrome (AIDS) patients. {27} {28}
—Ultrasound or computed tomography may be the preferred method for anatomical delineation of the infectious process when the location of the abscess is fairly well known. Indium In 111 oxyquinoline–labeled leukocyte imaging is recommended when neither of those methods has been successful or when the results have been ambiguous. {01} {02} {04} {16} {21} {46}
[Platelets, labeling of]
Indium In 111 oxyquinoline is used for the labeling of autologous platelets to be used for the following studies: {07} {09} {10} {11} {25} {26} {34}
[Platelet survival studies]—For the evaluation of platelet kinetics in patients with thrombocytopenia of uncertain etiology (where accelerated platelet destruction may be a contributory mechanism).
[Thrombosis, cardiac (diagnosis)]; and
[Thrombosis, arterial and deep venous (diagnosis)]—For the scintigraphic localization of cardiac thrombi and arterial or deep venous thrombosis. {39} {41}
Physical Properties
Nuclear data {01} {41}:
| Radionuclide (half-life) |
Mode of decay |
Principal photon emissions (keV) |
Mean number of emissions/ disintegration |
|---|---|---|---|
| In 111 (2.83 days) |
Electron capture |
Gamma (171.3) Gamma (245.3) |
0.90 0.94 |
Pharmacology/Pharmacokinetics
Mechanism of action/Effect:
Labeling of leukocytes:
When incubated with leukocytes, which have been isolated from whole blood, the indium-oxyquinoline complex, being lipid-soluble, penetrates the cell membrane of the leukocytes. Within the cell the radioactive indium dissociates from oxyquinoline and becomes firmly attached to cytoplasmic components, while the nonradioactive oxyquinoline is released by the cell.
Diagnosis of inflammatory lesions: The radioactive autologous leukocytes are subsequently reinjected to permit the detection of inflammatory lesions based on the normal physiological accumulation of leukocytes at such sites. {01} {02} {03} {40} {41}
Labeling of platelets:
Diagnosis of thrombosis: The radiolabeled autologous platelets, when reinjected, deposit at sites of vascular endothelium injury as a normal hemostatic response. This permits detection of thrombi. {09} {10} {39}
Distribution:
Indium In 111–labeled leukocytes:
Distribution of labeled leukocytes is dependent on the predominance of the cell types labeled and their condition.
Leukocytes tend to concentrate at sites of inflammation (50 to 75% of circulating cells). However, there is an initial accumulation of radioactivity in the lungs, half of which is cleared in 15 minutes and the remainder slowly (by 4 hours after injection there is no notable radioactivity in normal lungs). Twenty-five to 50% of the radioactivity is subsequently distributed in spleen, liver, and bone marrow. Cells with lowered viability give high levels of activity in the liver, while a preparation with higher viability but contaminated with red cells and lymphocytes results in high levels of radioactivity in the spleen. {01} {33} {41} {42}
Radioactivity in liver and spleen reaches a plateau at 2 to 48 hours after injection with no significant clearance observed at 72 hours. {01} {03} {04} {41} {42}
Indium In 111–labeled platelets:
Some of the labeled platelets are rapidly taken up in the spleen and liver (about 30 and 10% of the injected dose, respectively). The remaining cells (60%) are cleared from the blood with a half-time of 4 to 5 days, and are distributed in red bone marrow, liver, spleen, and other tissues (about 25, 20, 5, and 10% of the injected dose, respectively). {33} {39}
Half-life:
Biological:
Clearance of indium In 111–labeled leukocytes from whole blood: 5 to 10 hours. {33} {39} {42}
Clearance of indium In 111–labeled platelets from whole blood: 7 to 10 days. {39} {43}
Time to radioactivity visualization:
Images of indium In 111–labeled leukocyte (or platelet) localization at inflammatory sites may be obtained as early as 4 hours after injection, but optimal images are obtained at 18 to 24 hours following administration. {01} {07} {10} {14} {28} {42}
Radiation dosimetry:
{01}{33}
| Organ |
Estimated absorbed radiation dose* |
|||
|---|---|---|---|---|
| Indium-labeled leukocytes† |
Indium-labeled platelets |
|||
| mGy/ MBq |
rad/ mCi |
mGy/ MBq |
rad/ mCi |
|
| Spleen |
5.5 |
20.35 |
7.5 |
27.75 |
| Liver |
0.71 |
2.63 |
0.73 |
2.70 |
| Red marrow |
0.69 |
2.55 |
0.36 |
1.33 |
| Pancreas |
0.52 |
1.92 |
0.66 |
2.44 |
| Bone surfaces |
0.35 |
1.30 |
0.23 |
0.85 |
| Kidneys |
0.33 |
1.22 |
0.41 |
1.52 |
| Adrenals |
0.31 |
1.15 |
0.37 |
1.37 |
| Stomach wall |
0.28 |
1.04 |
0.35 |
1.30 |
| Heart |
0.17 |
0.63 |
0.39 |
1.44 |
| Small intestine |
0.16 |
0.59 |
0.14 |
0.52 |
| Large intestine (upper) |
0.16 |
0.59 |
0.14 |
0.52 |
| Lungs |
0.16 |
0.59 |
0.28 |
1.04 |
| Large intestine (lower) |
0.13 |
0.48 |
0.097 |
0.36 |
| Ovaries |
0.12 |
0.44 |
0.098 |
0.36 |
| Uterus |
0.12 |
0.44 |
0.095 |
0.35 |
| Breast |
0.090 |
0.33 |
0.10 |
0.37 |
| Bladder wall |
0.072 |
0.27 |
0.066 |
0.24 |
| Thyroid |
0.061 |
0.23 |
0.081 |
0.30 |
| Testes |
0.045 |
0.17 |
0.043 |
0.16 |
| Other tissue |
0.11 |
0.41 |
0.12 |
0.44 |
| Radionuclide and impurities |
Effective dose* |
|||
|---|---|---|---|---|
| Indium-labeled leukocytes |
Indium-labeled platelets |
|||
| mSv/ MBq |
rem/ mCi |
mSv/ MBq |
rem/ mCi |
|
| In 111 |
0.59 |
2.18 |
0.70 |
2.59 |
| In 114m‡ |
69 |
255 |
83 |
307 |
† The actual leukocyte suspension used for labeling may also contain erythrocytes and thrombocytes, which become labeled at the same time. There may also be some unbound activity. Radiation contributions from these other fractions of activity have to be considered.
‡ Impurity. Radionuclidic impurity at calibration time is not greater then 0.037 MBq (1 microcurie) of indium In 114m per 37 MBq (1 millicurie) of indium In 111. {46}
Elimination:
Renal and fecal. Negligible amount (less than 1%) of the injected dose eliminated in 24 hours. {01} {33} {39}
Precautions to Consider
Carcinogenicity
Although earlier studies suggested oxyquinoline might have a carcinogenic potential, recent studies have not shown a carcinogenic effect in rats or mice given oxyquinoline in feed at concentrations of 1500 or 3000 parts per million for 103 weeks. In any case, the carcinogenic potential of oxyquinoline is of no real concern since the oxyquinoline that is released from the cell following radiolabeling is probably removed from the preparation by subsequent cell washings. {01} {39}
Pregnancy/Reproduction
Pregnancy—
The possibility of pregnancy should be assessed in women of child-bearing potential. Clinical situations exist where the benefit to the patient and fetus, from 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. {31}
For indium In 111 oxyquinoline–labeled leukocytes
Indium In 111 (injected as chloride) crosses the placenta. Studies have not been done in humans with indium In 111 oxyquinoline–labeled leukocytes.
Studies have not been done in animals. {01}
FDA Pregnancy Category C. {01}
Breast-feeding
Indium In 111 is excreted in breast milk in small concentrations (0.09 Bq/mL per megabecquerel [0.09 nCi/mL per millicurie] injected). Because of the potential risk to the infant from radiation exposure, temporary discontinuation of nursing is recommended for a short period of time (e.g., 24 hours), at the end of which milk should be expressed and discarded. {12} {29} {39} {44}
Pediatrics
Although indium In 111–labeled leukocytes (and platelets) are used in children, there have been no specific studies evaluating safety and efficacy of indium In 111 oxyquinoline in pediatric patients. When this radiopharmaceutical is used in children, the diagnostic benefit should be judged to outweigh the potential risk of radiation. {01} {15} {19} {20} {28} {31}
Geriatrics
Appropriate studies on the relationship of age to the effects of indium In 111–labeled leukocytes (or platelets) have not been performed in the geriatric population. However, no geriatrics-specific problems have been documented to date. {07} {28}
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 indium In 111–labeled leukocyte studies
Cell clumping{01} (clumping of cells in final preparation may produce false positive results, especially if images are taken early after injection [approximately 4 hours] because of focal accumulation of radioactivity in lungs {07} {08} {23})
Contamination by red blood cells or platelets{01} (red blood cells or platelets in final preparation may produce cardiac blood pool activity {01} {28} {39} {42})
Plasma contamination{01} (plasma contamination may impair labeling efficiency of leukocytes since transferrin in plasma competes for indium In 111 oxyquinoline {01} {41})
Due to other medications
Antibiotics, long-term therapy, or
Corticosteroids or
Hyperalimentation or
Lidocaine, with higher-than-therapeutic concentrations or
Procainamide, with higher-than-therapeutic concentrations (may produce false negative results because of decreased chemotaxis {07} {11} {39} {45})
Due to medical problems or conditions
Aspiration or
Atelectasis or
Congestive heart failure or
Cystic fibrosis or
Embolism, pulmonary or
Metastases or
Post-cardiopulmonary resuscitation or
Post-radiation therapy or
Pulmonary hemorrhage or
Respiratory distress syndrome, adult or
Uremia or
Vasculitis or
Wegener's granulomatosis (may produce diffuse pulmonary uptake of indium In 111–labeled leukocytes {35})
Gastrointestinal bleeding (may produce false positive images because of localization in bowel {14} {28})
Hematomas{04} (may produce false positive images)
Infection, chronic{04} (may produce false negative images)
Leukopenia{01} (may decrease leukocyte labeling efficiency because of small number of available leukocytes; the use of donor cells may be considered in leukopenic patients)
Pneumonitis or
Respiratory infections, upper (swallowed purulent sputum may cause false positive images {14} {28})
Due to other diagnostic tests
Gallium citrate Ga 67 scan, previous (background Ga 67 activity may preclude In 111–leukocyte study for at least 1 month {14})
With results of indium In 111–labeled platelet studies
Contamination by red blood cells{01} (red blood cells in final preparation may produce cardiac blood pool activity {01} {28} {39} {42})
Due to other medications
Heparin (although studies of the effect of heparin on In 111–labeled platelet accumulation on venous thrombi have yielded contradictory results, the possibility should be considered that false negative test results may occur in heparin-treated patients {25} {28} {30})
Due to medical problems or conditions
Hematoma (false positive images may result because of accumulation of indium In 111–labeled platelets at sites of bleeding [e.g., due to venipuncture] {39})
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 less frequent or rare
Allergic reaction (skin rash, hives, or itching)
pyrogenic reaction from indium In 111–labeled leukocytes (or platelets) (fever)—may also be clinical sign of abscess{01}{28}
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 radioactivity at sites of infection or thrombosis allows images to be obtained
Small amounts of radioactivity used in diagnosis; radiation received is low and considered safe
Before having this test
» Conditions affecting use, especially:
Pregnancy—Indium In 111 (administered as chloride) crosses the placenta; risk to fetus from radiation exposure as opposed to benefit derived from use should be considered
Breast-feeding—Small concentration of radioactivity 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
Precautions after having this test
No special precautions
Side/adverse effects
Signs of potential side effects, especially pyrogenic and allergic reactions
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 appropriate Federal or State agency, if required, or, outside the U.S., the appropriate authority.
Indium In 111 oxyquinoline solution is not administered directly. It is intended only for use in the preparation of indium In 111–labeled leukocytes (or platelets). {01} {28}
The manufacturer's package insert or other appropriate literature should be consulted for the specific method of labeling leukocytes and 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. {47}
Parenteral Dosage Forms
Note: Bracketed uses in the Dosage Forms section refer to categories of use and/or indications that are not included in U.S. product labeling.
INDIUM In 111 OXYQUINOLINE SOLUTION USP
Usual adult and adolescent administered activity
Diagnosis of inflammatory lesions
Intravenous, 7.4 to 18.5 megabecquerels (200 to 500 microcuries) of indium In 111 oxyquinoline–labeled leukocytes. {01} {46}
[Platelet survival studies]
Intravenous, 0.74 to 18.5 megabecquerels (20 to 500 microcuries) of indium In 111 oxyquinoline–labeled platelets. {39}
[Diagnosis of thrombosis]
Intravenous, 18.5 megabecquerels (500 microcuries) of indium In 111 oxyquinoline–labeled platelets. {10} {25} {39}
Usual pediatric administered activity
Dosage has not been established.
Note: In the diagnosis of acute inflammatory conditions, in children and adolescents, dosages of 0.26 to 0.30 megabecquerel (7 to 8 microcuries) of indium In 111 oxyquinoline–labeled leukocytes per kg of body weight have been used. However, in most clinical studies a total dosage of 1.8 to 3.7 megabecquerels (50 to 100 microcuries) is recommended for optimal imaging quality. {28} {39}
Usual geriatric administered activity
See Usual adult and adolescent administered activity .
Strength(s) usually available
U.S.—
37 megabecquerels (1 millicurie) per mL at calibration date (Rx)[Generic]
Note: Indium In 111 oxyquinoline solution is not administered directly. It is intended only for use in the preparation of indium In 111 oxyquinoline–labeled leukocytes (or platelets). {01} {28}
Canada—
Not commercially available.
Packaging and storage:
Store between 15 and 25 °C (59 and 77 °F), unless otherwise specified by manufacturer.
Note: The labeled leukocytes may be stored between 15 and 30 °C (59 and 86 °F), for up to 3 hours.
Stability:
Do not use if cell clumping is observed in final preparation.
Indium In 111 oxyquinoline solution should be used for labeling within 5 days after the calibration date.
Indium In 111 oxyquinoline–labeled leukocytes should preferably be administered within 1 hour of labeling. {01} {41} Administration of labeled leukocytes beyond 3 hours after preparation is not recommended since chemotaxis of granulocytes deteriorates during storage, causing false negative images. {01} {28}
Note: Caution—Radioactive material.
Revised: 08/02/1994
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