Components:
Iobenguane I 123
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Name of the medicinal product

123I-MIBG

Qualitative and quantitative composition

Iobenguane I 123

Therapeutic indications

The information provided in Therapeutic indications of 123I-MIBG is based on data of another medicine with exactly the same composition as the 123I-MIBG of the medicine (Iobenguane I 123). Be careful and be sure to specify the information on the section Therapeutic indications in the instructions to the drug 123I-MIBG directly from the package or from the pharmacist at the pharmacy.
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123I-MIBG (iobenguane i 123 injection for intravenous use) is a radiopharmaceutical indicated for use in the detection of primary or metastatic pheochromocytoma or neuroblastoma as an adjunct to other diagnostic tests.

Dosage (Posology) and method of administration

The information provided in Dosage (Posology) and method of administration of 123I-MIBG is based on data of another medicine with exactly the same composition as the 123I-MIBG of the medicine (Iobenguane I 123). Be careful and be sure to specify the information on the section Dosage (Posology) and method of administration in the instructions to the drug 123I-MIBG directly from the package or from the pharmacist at the pharmacy.
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Radiation Safety

123I-MIBG (iobenguane i 123 injection for intravenous use) emits radiation and must be handled with appropriate safety measures to minimize radiation exposure to clinical personnel and patients. Radiopharmaceuticals should be used by or under the control of physicians who are qualified by specific training and experience in the safe use and handling of radionuclides, and whose experience and training have been approved by the appropriate government agency authorized to license the use of radionuclides. 123I-MIBG (iobenguane i 123 injection for intravenous use) dosing is based upon the radioactivity determined using a suitable calibration system immediately prior to administration.

To minimize radiation dose to the bladder, prior to and following 123I-MIBG (iobenguane i 123 injection for intravenous use) administration, encourage hydration to permit frequent voiding. Encourage the patient to void frequently for the first 48 hours following 123I-MIBG administration .

Thyroid Blockade

Before administration of 123I-MIBG (iobenguane i 123 injection for intravenous use) , administer Potassium Iodide Oral Solution or Lugol's Solution (equivalent to 100 mg iodide for adults, body-weight adjusted for children) or potassium perchlorate (400 mg for adults, body-weight adjusted for children) to block uptake of iodine 123 by the patient's thyroid. Administer the blocking agent at least one hour before the dose of 123I-MIBG .

Preparation and Administration

Inspect the 123I-MIBG (iobenguane i 123 injection for intravenous use) vial for particulate matter and discoloration prior to administration. Use aseptic procedures and a radiation shielding syringe during administration. Administer the dose as an intravenous injection over 1 to 2 minutes. A subsequent injection of 0.9% sodium chloride may be used to ensure full delivery of the dose.

Recommended Dose for Adults

For adults ( ≥ 16 years of age), the recommended dose is 10 mCi (370 MBq) .

Recommended Dose for Pediatric Patients

For pediatric patients < 16 years of age weighing ≥ 70 kg, the recommended dose is 10 mCi (370 MBq) .

For pediatric patients < 16 years of age weighing < 70 kg, the recommended dose should be calculated according to patient body weight as shown in Table 1 . The benzyl alcohol in 123I-MIBG (iobenguane i 123 injection for intravenous use) may cause serious adverse reactions in premature or low birth-weight infants .

Table 1: 123I-MIBG (iobenguane i 123 injection for intravenous use) Dose Preparation for Pediatric Patients*

Weight (kg) Fraction of adult activity 123I-MIBG (mCi) pediatric dose 123I-MIBG (MBq) pediatric dose
3 0.1 1 37
4 0.14 1.4 52
6 0.19 1.9 70
8 0.23 2.3 85.1
10 0.27 2.7 99.9
12 0.32 3.2 118.4
14 0.36 3.6 133.2
16 0.4 4 148
18 0.44 4.4 162.8
20 0.46 4.6 170.2
22 0.5 5 185
24 0.53 5.3 196.1
26 0.56 5.6 207.2
28 0.58 5.8 214.6
30 0.62 6.2 229.4
32 0.65 6.5 240.5
34 0.68 6.8 251.6
36 0.71 7.1 262.7
38 0.73 7.3 270.1
40 0.76 7.6 281.2
42 0.78 7.8 288.6
44 0.8 8 296
46 0.82 8.2 303.4
48 0.85 8.5 314.5
50 0.88 8.8 325.6
52 0.9 9 333
54 0.9 9 333
56 0.92 9.2 340.4
58 0.92 9.2 340.4
60 0.96 9.6 355.2
62 0.96 9.6 355.2
64 0.98 9.8 362.6
66 0.98 9.8 362.6
68 0.99 9.9 366.3
*Based on a reference activity for an adult scaled to body weight according to the schedule proposed by the European Association of Nuclear Medicine Paediatric Task Group.

Radiation Dosimetry

The estimated absorbed radiation doses to adults and children from intravenous administration of 123I-MIBG (iobenguane i 123 injection for intravenous use) are as shown in Table 2:

Table 2: Estimated Absorbed Radiation Dose from 123I-MIBG (iobenguane i 123 injection for intravenous use)

ORGAN/TISSUE ABSORBED DOSE PER UNIT ADMINISTERED ACTIVITY
ADULT 15-YEAR OLD 10-YEAR OLD 5-YEAR OLD 1-YEAR OLD NEONATES
µGy/ MBq rad/mCi µGy/ MBq rad/mCi µGy/ MBq rad/mCi µGy/ MBq rad/mCi µGy/ MBq rad/mCi µGy/ MBq rad/mCi
Adrenals 16 0.059 21 0.078 31 0.115 42 0.155 67 0.248 111 0.411
Brain 3.9 0.014 4.9 0.018 8.1 0.030 13 0.048 24 0.089 55.9 0.207
Breast 4.7 0.017 5.9 0.022 9.4 0.035 15 0.056 28 0.104 65.3 0.242
Gallbladder 20 0.074 24 0.089 34 0.126 51 0.189 95 0.352 200 0.740
GI Tract Stomach Wall 7.6 0.028 10 0.037 17 0.063 27 0.100 51 0.189 114 0.422
Small Intestine Wall 7.7 0.028 9.8 0.036 16 0.059 25 0.093 46 0.170 104 0.385
Colon Wall 8.1 0.030 10 0.037 16 0.059 26 0.096 46 0.170 104.3 0.386
Upper Large Intestine Wall 8.4 0.031 11 0.041 18 0.067 30 0.111 53 0.196 119 0.440
Lower Large Intestine Wall 7.7 0.028 9.6 0.036 15 0.056 21 0.078 38 0.141 84.9 0.314
Heart Wall 18 0.067 23 0.085 35 0.130 53 0.196 94 0.348 182 0.673
Kidneys 13 0.048 16 0.059 24 0.089 35 0.130 59 0.218 132 0.488
Liver 67 0.248 87 0.322 130 0.481 180 0.666 330 1.221 720 2.664
Lungs 16 0.059 23 0.085 32 0.118 48 0.178 89 0.329 215 0.796
Muscles 6 0.022 7.6 0.028 12 0.044 17 0.063 33 0.122 75.1 0.278
Esophagus 6 0.022 7.6 0.028 11 0.041 18 0.067 32 0.118 72.2 0.267
Osteogenic Cells 16 0.059 21 0.078 31 0.115 47 0.174 100 0.370 254 0.940
Ovaries 7.9 0.029 10 0.037 15 0.056 22 0.081 41 0.152 92.3 0.342
Pancreas 12 0.044 15 0.056 25 0.093 39 0.144 68 0.252 143 0.529
Red marrow 5.6 0.021 6.8 0.025 10 0.037 15 0.056 30 0.111 89.5 0.331
Skin 3.7 0.014 4.4 0.016 7.1 0.026 11 0.041 21 0.078 53.1 0.196
Spleen 20 0.074 27 0.100 42 0.155 64 0.237 110 0.407 282 1.043
Testes 5.4 0.020 7.1 0.026 11 0.041 16 0.059 30 0.111 69.9 0.259
Thymus 6 0.022 7.6 0.028 11 0.041 18 0.067 32 0.118 72.2 0.267
Thyroid 4.7 0.017 6.1 0.023 9.9 0.037 16 0.059 30 0.111 69.4 0.257
Urinary Bladder Wall 66 0.244 84 0.311 110 0.407 110 0.407 200 0.740 478.0 1.769
Uterus 11 0.041 14 0.052 21 0.078 28 0.104 51 0.189 110.0 0.407
Whole Body 8.1 0.030 10 0.037 16 0.059 24 0.089 44 0.163 104.0 0.385
EFFECTIVE DOSE µSv/MBq 13.7 18.1 26.7 37.6 68 162
mSv/mCi 0.507 0.670 0.988 1.39 2.52 6
*OLINDA/EXM calculation based on biodistribution data from Swanson et al. and Publication 53 of the ICRP (International Commission on Radiological Protection) [Annals of the ICRP 1987; 18 (1-4): 329-331]

The effective dose resulting from an administered activity amount of 10 mCi is 5.07 mSv in an adult.

Imaging Guidelines

Begin whole body planar scintigraphy imaging 24 ± 6 hours following administration of 123I-MIBG (iobenguane i 123 injection for intravenous use) . Single photon emission computed tomography (SPECT) may be performed following planar scintigraphy, as appropriate .

Contraindications

The information provided in Contraindications of 123I-MIBG is based on data of another medicine with exactly the same composition as the 123I-MIBG of the medicine (Iobenguane I 123). Be careful and be sure to specify the information on the section Contraindications in the instructions to the drug 123I-MIBG directly from the package or from the pharmacist at the pharmacy.
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123I-MIBG (iobenguane i 123 injection for intravenous use) is contraindicated in patients with known hypersensitivity to iobenguane or iobenguane sulfate.

Special warnings and precautions for use

The information provided in Special warnings and precautions for use of 123I-MIBG is based on data of another medicine with exactly the same composition as the 123I-MIBG of the medicine (Iobenguane I 123). Be careful and be sure to specify the information on the section Special warnings and precautions for use in the instructions to the drug 123I-MIBG directly from the package or from the pharmacist at the pharmacy.
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WARNINGS

Included as part of the PRECAUTIONS section.

PRECAUTIONS

Hypersensitivity Reactions

Hypersensitivity reactions have been reported following 123I-MIBG (iobenguane i 123 injection for intravenous use) administration. Prior to administration, question the patient for a history of prior reactions to iodine, an iodine-containing contrast agent or other products containing iodine. If the patient is known or strongly suspected to have hypersensitivity to iodine, an iodine-containing contrast agent or other products containing iodine, the decision to administer 123I-MIBG (iobenguane i 123 injection for intravenous use) should be based upon an assessment of the expected benefits compared to the potential hypersensitivity risks. Have anaphylactic and hypersensitivity treatment measures available prior to 123I-MIBG administration .

Risks for Benzyl Alcohol Toxicity in Infants

123I-MIBG (iobenguane i 123 injection for intravenous use) contains benzyl alcohol at a concentration of 10.3 mg/mL. Benzyl alcohol has been associated with a fatal “Gasping Syndrome” in premature infants and infants of low birth weight. Exposure to excessive amounts of benzyl alcohol has been associated with toxicity (hypotension, metabolic acidosis), particularly in neonates, and an increased incidence of kernicterus, particularly in small preterm infants. There have been rare reports of deaths, primarily in preterm infants, associated with exposure to excessive amounts of benzyl alcohol. .

Observe infants for signs or symptoms of benzyl alcohol toxicity following 123I-MIBG (iobenguane i 123 injection for intravenous use) administration. 123I-MIBG (iobenguane i 123 injection for intravenous use) safety and effectiveness have not been established in neonates (pediatric patients below the age of 1 month).

Increased Radiation Exposure in Patients with Severe Renal Impairment

123I-MIBG (iobenguane i 123 injection for intravenous use) is cleared by glomerular filtration and is not dialyzable. The radiation dose to patients with severe renal impairment may be increased due to the delayed elimination of the drug. Delayed 123I-MIBG (iobenguane i 123 injection for intravenous use) clearance may also reduce the target to background ratios and decrease the quality of scintigraphic images. These risks importantly may limit the role of 123I-MIBG (iobenguane i 123 injection for intravenous use) in the diagnostic evaluation of patients with severe renal impairment. 123I-MIBG (iobenguane i 123 injection for intravenous use) safety and efficacy have not been established in these patients .

Thyroid Accumulation

Failure to block thyroid uptake of iodine 123 may result in an increased long term risk for thyroid neoplasia. Administer thyroid blocking medications before 123I-MIBG administration .

Risks with Concomitant Medication Withdrawal

Drugs which interfere with norepinephrine uptake or retention may decrease the uptake of 123I-MIBG (iobenguane i 123 injection for intravenous use) in neuroendocrine tumors and lead to false negative imaging results. When medically feasible, stop these drugs before 123I-MIBG (iobenguane i 123 injection for intravenous use) administration and monitor patients for the occurrence of clinically significant withdrawal symptoms, especially patients with elevated levels of circulating catecholamines and their metabolites .

Hypertension

Assess the patient's pulse and blood pressure before and intermittently for 30 minutes after 123I-MIBG (iobenguane i 123 injection for intravenous use) administration. 123I-MIBG (iobenguane i 123 injection for intravenous use) may increase release of norepinephrine from chromaffin granules and produce a transient episode of hypertension, although this was not observed in the clinical study. Prior to 123I-MIBG (iobenguane i 123 injection for intravenous use) administration, ensure emergency cardiac and anti-hypertensive treatments are readily available.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Iobenguane sulfate was not mutagenic in vitro in the Ames bacterial mutation assay and in the in vitro mouse lymphoma test, and was negative in the in vivo micronucleus test in rats.

Long-term animal studies have not been conducted to evaluate 123I-MIBG (iobenguane i 123 injection for intravenous use) 's carcinogenic potential or potential effects on fertility.

Use In Specific Populations

Pregnancy

Pregnancy Category C: Any radiopharmaceutical, including 123I-MIBG (iobenguane i 123 injection for intravenous use) , has a potential to cause fetal harm. It is not known whether 123I-MIBG (iobenguane i 123 injection for intravenous use) can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Animal reproduction studies have not been conducted with 123I-MIBG (iobenguane i 123 injection for intravenous use) . 123I-MIBG (iobenguane i 123 injection for intravenous use) should be given to a pregnant woman only if clearly needed.

Nursing Mothers

It is not known whether 123I-MIBG (iobenguane i 123 injection for intravenous use) is excreted into human milk. However, iodine 123 is excreted into human milk. Because many drugs are excreted into human milk and because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to interrupt nursing after administration of 123I-MIBG (iobenguane i 123 injection for intravenous use) or not to administer 123I-MIBG (iobenguane i 123 injection for intravenous use) , taking into account the importance of the drug to the mother. Based on the physical half-life of iodine 123 (13.2 hours) nursing women may consider interrupting nursing for 6 days after 123I-MIBG (iobenguane i 123 injection for intravenous use) administration in order to minimize risks to nursing infants.

Pediatric Use

The safety and effectiveness of 123I-MIBG (iobenguane i 123 injection for intravenous use) have been established in the age groups 1 month to 16 years . Safety and effectiveness in pediatric patients below the age of 1 month have not been established .

Geriatric Use

The 123I-MIBG (iobenguane i 123 injection for intravenous use) clinical study did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly population should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy.

123I-MIBG (iobenguane i 123 injection for intravenous use) is excreted by the kidneys, and the risks of adverse reactions, increased radiation dose, and occurrence of falsely negative imaging results, may be greater in patients with severely impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection and image interpretation. Consider assessment of renal function in elderly patients prior to 123I-MIBG (iobenguane i 123 injection for intravenous use) administration..

Undesirable effects

The information provided in Undesirable effects of 123I-MIBG is based on data of another medicine with exactly the same composition as the 123I-MIBG of the medicine (Iobenguane I 123). Be careful and be sure to specify the information on the section Undesirable effects in the instructions to the drug 123I-MIBG directly from the package or from the pharmacist at the pharmacy.
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Clinical Study Experience

Serious adverse reactions were not observed in the 123I-MIBG (iobenguane i 123 injection for intravenous use) clinical study. The data described below reflect 123I-MIBG (iobenguane i 123 injection for intravenous use) exposure to 251 patients with known or suspected pheochromocytoma or neuroblastoma. The average ages were 49 years (range 17 – 88 years) for adults and, for pediatric patients, 4 years (range 1 month - 16 years). Slightly less than half the patients were male. All patients were monitored for adverse reactions over a 24 hour period following 123I-MIBG (iobenguane i 123 injection for intravenous use) administration.

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Adverse reactions were all mild to moderate in severity and were predominantly isolated occurrences ( ≤ 2 patients) of one of the following reactions: dizziness, rash, pruritus, flushing or injection site hemorrhage.

Postmarketing Experience

Because postmarketing reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Hypersensitivity reactions have uncommonly been reported during the postmarketing use of 123I-MIBG .

Overdose

The information provided in Overdose of 123I-MIBG is based on data of another medicine with exactly the same composition as the 123I-MIBG of the medicine (Iobenguane I 123). Be careful and be sure to specify the information on the section Overdose in the instructions to the drug 123I-MIBG directly from the package or from the pharmacist at the pharmacy.
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The major manifestations of overdose relate predominantly to increased radiation exposure, with the long term risks for neoplasia.

Pharmacodynamic properties

The information provided in Pharmacodynamic properties of 123I-MIBG is based on data of another medicine with exactly the same composition as the 123I-MIBG of the medicine (Iobenguane I 123). Be careful and be sure to specify the information on the section Pharmacodynamic properties in the instructions to the drug 123I-MIBG directly from the package or from the pharmacist at the pharmacy.
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123I-MIBG (iobenguane i 123 injection for intravenous use) is a diagnostic radiopharmaceutical which contains a small quantity of iobenguane that is not expected to produce a pharmacodynamic effect . To minimize radiation dose to the thyroid gland, this organ should be blocked before dosing . Since iobenguane is excreted mainly via the kidneys, patients with severe renal insufficiency may experience increased radiation exposure and impaired imaging results. Frequent voiding should be encouraged after administration to minimize the radiation dose to the bladder . The calculation of the estimated radiation dose is shown in Table 2 .

Pharmacokinetic properties

The information provided in Pharmacokinetic properties of 123I-MIBG is based on data of another medicine with exactly the same composition as the 123I-MIBG of the medicine (Iobenguane I 123). Be careful and be sure to specify the information on the section Pharmacokinetic properties in the instructions to the drug 123I-MIBG directly from the package or from the pharmacist at the pharmacy.
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Iobenguane is rapidly cleared from the blood and accumulates in adrenergically innervated tissues . Retention is especially prolonged in highly adrenergically innervated tissues (e.g., the adrenal medulla, heart, and salivary glands).

The majority of the iobenguane dose is excreted unaltered by the kidneys via glomerular filtration. A rapid initial clearance of circulating iobenguane is observed, followed by a slow clearance as iobenguane is released from other compartments. In patients with normal renal function, 70 to 90% of the administered dose is recovered unaltered in urine within 4 days. Iobenguane is not cleared by dialysis . Most of the remaining radioactivity recovered in the urine is in the form of the radioiodinated metabolite m-iodohippuric acid (MIHA) (typically ≤ 10%) and free radioiodide (typically ≤ 6%). The enzymatic process responsible for metabolism has not been well characterized and the pharmacologic activity of these metabolites has not been studied. Only a small amount ( < 1%) of the injected dose is eliminated via the feces.