Azedra Dosimetric (iobenguane iodine-131)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Iobenguane I 131, an iodine I 131 radiolabeled synthetic norepinephrine analog (iobenguane; also referred to as metaiodobenzylguanidine (MIBG)), is a highly specific radiopharmaceutical.
Iobenguane I 131, an iodine I 131 radiolabeled synthetic norepinephrine analog (iobenguane; also referred to as metaiodobenzylguanidine (MIBG)), is a highly specific radiopharmaceutical. Because of structural similarity to norepinephrine, iobenguane I 131 accumulates in highly sympathetically innervated tissues with high levels of norepinephrine transporters (e.g., heart, lung, adrenal medulla, salivary gland, liver, spleen, pheochromocytoma, paraganglioma). The radioactive component of iobenguane I 131 (I 131) induces apoptosis and tumor necrosis.
Iobenguane I 131 does not undergo hepatic metabolism. Iobenguane I 131 is eliminated principally by the kidneys; approximately 50 or 80% of the dose is excreted in urine within 24 or 120 hours, respectively. Unchanged I 131 accounts for a mean of 94 or 93% of radioactivity recovered in urine at 0-6 or 6-24 hours, respectively.
Minor metabolites include free I 131, metaiodohippuric acid (MIHA), and metaiodobenzyl bisguanidine (MMIBG). In vivo, nonradioactive iobenguane is 61-63% bound to plasma proteins. The mean terminal half-life of iobenguane I 131 is approximately 35 hours.
I 131 decays with beta and gamma emissions with a physical half-life of 8 days.
Generic name: iobenguane iodine-131
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
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Indications
The following indications are listed for Azedra Dosimetric:
- Paraganglioma
- Pheochromocytoma
Also known as: Chromaffin Cell Tumor, Medullary Chromaffinoma, Medullary Paraganglioma, Pheochromoblastoma.
Dosing
If adverse reactions occur, interruption of therapy, therapeutic dosage reduction, and/or discontinuance of iobenguane I 131 may be necessary based on severity of the adverse effect.
Iobenguane I 131 is administered by IV injection (dosimetric dose) or by IV infusion (therapeutic dose).
Precautions for reducing the risk of radiation exposure (i.e., use of water proof gloves, shielding, tongs) should be followed.
Iobenguane I 131 injection concentrate must be diluted prior to administration. Prior to administration, iobenguane I 131 injection should be inspected visually for particulate matter and discoloration. The solution should be clear and colorless to pale yellow; the solution should not be used if it is discolored or if particulate matter is present. Radioactivity levels of iobenguane I 131 vial(s) should be confirmed with a calibrated radioactivity measurement system prior to and after administration of the radiopharmaceutical.
The manufacturer's labeling and dosing and administration guide should be consulted for detailed information on infusion system requirements (e.g., components, set-up) and procedures for IV infusion of therapeutic doses of iobenguane I 131.
Administration sets and any partially used vials should be discarded according to local and federal regulations.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
In vitro studies indicate that nonradioactive iobenguane is not an inhibitor of cytochrome P-450 (CYP) isoenzymes 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A or inducer of CYP isoenzymes 1A, 2B6, 2C9, 2C19, or 3A.
In vitro, nonradioactive iobenguane is not a substrate or inhibitor of P-glycoprotein (P-gp).
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
The manufacturer states that there are no known contraindications to the use of iobenguane I 131.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Grade 3 or 4 adverse effects reported in at least 10% of patients receiving iobenguane I 131 include lymphopenia, neutropenia, thrombocytopenia, fatigue, anemia, elevated international normalized ratio (INR), nausea, dizziness, hypertension, and vomiting.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Safety and efficacy of iobenguane I 131 have not been established in pediatric patients younger than 12 years of age with unresectable, locally advanced, or metastatic pheochromocytoma or paraganglioma.
Safety and efficacy of iobenguane I 131 in pediatric patients 12 years of age or older with unresectable, locally advanced, or metastatic pheochromocytoma or paraganglioma have been established in the principal efficacy study (Study IB12B).
Because the absorbed dose of radiation is greater in pediatric patients and pediatric patients have a longer life expectancy than adults, the risk of adverse effects associated with radiation therapy is increased in pediatric patients. Prior to initiating therapy in pediatric patients, clinicians should assess whether the potential benefits of iobenguane I 131 therapy outweigh the risks of radiation exposure. (See Radiation Exposure under Cautions: Warnings/Precautions.)
Iobenguane I 131 may cause fetal harm if administered to pregnant women based on its mechanism of action. (See Fetal/Neonatal Morbidity and Mortality under Cautions: Warnings/Precautions.)
It is not known whether iobenguane I 131 distributes into milk in humans or animals or whether the radiopharmaceutical has any effects on nursing infants and on milk production. Because of the potential for serious adverse reactions to iobenguane I 131 in nursing infants, women should be advised to discontinue nursing during iobenguane I 131 therapy and for 80 days after the final dose.
The manufacturer makes no specific dosage recommendations for geriatric patients. (See Geriatric Use under Warnings/Precautions: Specific Populations, in Cautions.)
In clinical trials, 17% of patients receiving iobenguane I 131 were 65 years of age or older and 1% were 75 years of age and older. There is insufficient experience in patients 65 years of age and older to determine whether geriatric patients respond differently than younger adults.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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