Iodide I-131
Identification
- Summary
Iodide I-131 is a radioisotopic agent used for the treatment of hyperthyroidism and thyroid carcinomas that take up iodine.
- Brand Names
- Hicon
- Generic Name
- Iodide I-131
- DrugBank Accession Number
- DB09293
- Background
Iodide I-131 (as Sodium iodide I-131) is a radioisotopic drug used for the treatment and palliation of thyroid malignancy. Iodine-131 is notable for causing mutation and death in cells that it penetrates, which is due to its mode of beta decay. As a result of beta decay, approximately 10% of its energy and radiation dose is via gamma radiation, while the other 90% (beta radiation) causes tissue damage without contributing to any ability to see or image the isotope. Low levels of beta radiation are also known for causing cancer as this dose is highly mutagenic. For this reason, less toxic iodine isotopes such as I-123 are more frequently used in nuclear imaging, while I-131 is reserved for its tissue destroying effects. Because the thyroid gland naturally takes up iodine from the body, therapeutic methods using radioisotopes can take advantage of this mechanism for localization of drug to the site of malignancy.
Therapeutic solutions of Sodium Iodide-131 are indicated for the treatment of hyperthyroidism and thyroid carcinomas that take up iodine. Palliative effects may be observed in patients with advanced thyroid malignancy if the metastatic lesions take up iodine. It is also indicated for use in performance of the radioactive iodide (RAI) uptake test to evaluate thyroid function.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 130.9067
Monoisotopic: 130.906672748 - Chemical Formula
- I
- Synonyms
- Iodide I-131
- Iodide I-131 ion
- Iodide ion I 131
- Iodide ion, I-131
- Iodide-131
- iodine I-131
- Radioiodine
Pharmacology
- Indication
Therapeutic solutions of Sodium Iodide-131 are indicated for the treatment of hyperthyroidism and thyroid carcinomas that take up iodine. Palliative effects may be observed in patients with advanced thyroid malignancy if the metastatic lesions take up iodine. It is also indicated for use in performance of the radioactive iodide (RAI) uptake test to evaluate thyroid function.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Hyperthyroidism •••••••••••• Treatment of Thyroid carcinoma •••••••••••• Symptomatic treatment of Metastatic thyroid malignancy •••••••••••• Diagnostic agent Thyroid malignancy •••••••••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
The therapeutic effects of sodium iodide I-131 are a result of the ionizing radiation absorbed by the thyroidal tissue. Tissue damage is the result of direct insult to molecules by ionization and excitation and the consequent dissociation of those molecules. About 90% of local irradiation from sodium iodide I-131 is the result of beta radiation and 10% is the result of gamma radiation.
- Mechanism of action
Taken orally, sodium iodide I-131 is rapidly absorbed and distributed within the extracellular fluid of the body. The iodide is concentrated in the thyroid via the sodium/iodide symporter, and subsequently oxidized to iodine. The destruction of thyroidal tissue is achieved by the beta emission of sodium iodide I-131.
- Absorption
After oral administration, sodium iodide I-131 is absorbed rapidly from the upper gastrointestinal tract (90% in 60 minutes). Following absorption, the iodide is primarily distributed within the extra-cellular fluid of the body. It is trapped by the thyroid. The thyroid uptake of iodide is usually increased in hyperthyroidism and in goiter with impaired hormone synthesis, decreased in hypothyroidism, and normal to decreased in hypothyroidism receiving iodine. It should be noted that the uptake of radioactive iodide is a function of stable iodide concentration in the serum and the functional state of the thyroid.
- Volume of distribution
Not Available
- Protein binding
Sodium Iodide I-131 is not protein bound.
- Metabolism
Trapped iodide is oxidized to iodine and organically incorporated so rapidly that the iodide trap of the thyroid contains less than 0.2 % free iodide in comparison to the organically bound iodine. This process results in further concentration of iodine in the thyroid gland to about 500 times that in the blood.
- Route of elimination
Sodium Iodide I-131 is excreted by the kidneys. The normal range of urinary excretion is 37 to 75 % of the administered dose, varying with the thyroid and renal function of the patient.
- Half-life
Iodine I-131 decays by beta emission and associated gamma emission with a physical half-life of 8.04 days.
- Clearance
Not Available
- Adverse Effects
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- Toxicity
Adverse reactions that have been reported with doses of sodium iodide I-131 used in the treatment of benign disease include sialadenitis, chest pain, tachycardia, iododerma, itching skin, rash, hives, hypothyroidism, hyperthyroidism, thyrotoxic crisis, hypoparathyroidism, and local swelling. Adverse reactions that have been reported with doses of sodium iodide I-131 used in the treatment of malignant disease include radiation sickness, bone marrow depression, anemia, leucopenia, thrombocytopenia, blood dyscrasia, leukemia, solid cancers, lacrimal gland dysfunction, salivary gland dysfunction, congenital hypothyroidism, chromosomal abnormalities, cerebral edema, radiation pneumonitis, and pulmonary fibrosis.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAmiodarone Amiodarone may decrease effectiveness of Iodide I-131 as a diagnostic agent. Carbimazole The therapeutic efficacy of Iodide I-131 can be decreased when used in combination with Carbimazole. Ioversol The therapeutic efficacy of Iodide I-131 can be decreased when used in combination with Ioversol. Methimazole The therapeutic efficacy of Iodide I-131 can be decreased when used in combination with Methimazole. Potassium Iodide The therapeutic efficacy of Iodide I-131 can be decreased when used in combination with Potassium Iodide. - Food Interactions
- Drink plenty of fluids.
- Limit iodine intake. Consume a low iodine diet for two weeks before the administration of sodium Iodide I-131.
- Take on an empty stomach. Avoid eating for 2 hours before and after administering iodide I-131.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Sodium iodide I-131 29VCO8ACHH 7790-26-3 FVAUCKIRQBBSSJ-LAIFMVDKSA-M - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Hicon Solution 1000 mCi/1mL Oral Jubilant DraxImage Inc., dba Jubilant Radiopharma 2003-04-07 Not applicable US I 131 Mini Capsule 500 mCi/1 Oral Anazao Health Corporation 2012-05-23 Not applicable US I3odine MAXTM Solution 3500 mCi/1mL Oral International Isotopes Inc 2001-01-01 2016-10-25 US Iodotope Capsule, gelatin coated 130 mCi/1 Oral Bracco Diagnostics, Inc 1957-06-14 2008-06-19 US Sodium Iodide I 131 Capsule, gelatin coated 1 mCi/1mL Oral Mallinckrodt Nuclear Medicine Llc 2015-10-27 2018-07-01 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Sodium Iodide I-131 Kit 1000 mCi/1 Oral International Isotopes Inc 2020-03-16 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image I 131 Mini Sodium iodide I-131 (500 mCi/1) Capsule Oral Anazao Health Corporation 2012-05-23 Not applicable US I3odine MAXTM Sodium iodide I-131 (3500 mCi/1mL) Solution Oral International Isotopes Inc 2001-01-01 2016-10-25 US Sodium Iodide I-131 Sodium iodide I-131 (3500 mCi/1mL) Solution, concentrate Oral International Isotopes Inc 2010-09-01 Not applicable US
Categories
- ATC Codes
- V09FX03 — Sodium iodide (131i)
- V09FX — Various thyroid diagnostic radiopharmaceuticals
- V09F — THYROID
- V09 — DIAGNOSTIC RADIOPHARMACEUTICALS
- V — VARIOUS
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of inorganic compounds known as homogeneous halogens. These are inorganic non-metallic compounds in which the largest atom is a nobel gas.
- Kingdom
- Inorganic compounds
- Super Class
- Homogeneous non-metal compounds
- Class
- Homogeneous halogens
- Sub Class
- Not Available
- Direct Parent
- Homogeneous halogens
- Alternative Parents
- Not Available
- Substituents
- Homogeneous halogen
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 4GC1FOQ22U
- CAS number
- 14914-30-8
- InChI Key
- XMBWDFGMSWQBCA-RNFDNDRNSA-M
- InChI
- InChI=1S/HI/h1H/p-1/i1+4
- IUPAC Name
- (131I)iodide
- SMILES
- [131I-]
References
- General References
- Not Available
- External Links
- KEGG Drug
- D02259
- PubChem Compound
- 167195
- PubChem Substance
- 310265185
- ChemSpider
- 146281
- 1546394
- ChEMBL
- CHEMBL1201084
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Iodine-131
- FDA label
- Download (3.4 MB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Completed Not Available Thyroid Neoplasm 1 3 Unknown Status Treatment Thyroid Neoplasm 1 2 Active Not Recruiting Treatment Metastatic Thyroid Gland Carcinoma / Poorly differentiated thyroid carcinoma / Recurrent Thyroid Gland Carcinoma / Stage IV Thyroid Gland Follicular Carcinoma AJCC v7 / Stage IV Thyroid Gland Papillary Carcinoma AJCC v7 / Stage IVA Thyroid Gland Follicular Carcinoma AJCC v7 / Stage IVA Thyroid Gland Papillary Carcinoma AJCC v7 / Stage IVB Thyroid Gland Follicular Carcinoma AJCC v7 / Stage IVB Thyroid Gland Papillary Carcinoma AJCC v7 / Stage IVC Thyroid Gland Follicular Carcinoma AJCC v7 / Stage IVC Thyroid Gland Papillary Carcinoma AJCC v7 1 2 Completed Treatment Non-Hodgkin's Lymphoma (NHL) 2 2 Recruiting Treatment Follicular Thyroid Cancer / Metastatic Thyroid Cancer / Thyroid Cancer / Thyroid Cancer, Papillary / Thyroid Carcinoma / Unresectable Thyroid Gland Carcinoma 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral 3025 MBq Solution Oral 1000 mCi/1mL Solution Oral 37 GBq/mL Capsule Oral 500 mCi/1 Solution Oral 3500 mCi/1mL Capsule, gelatin coated Oral 3718.5 MBq Capsule, gelatin coated Oral 130 mCi/1 Solution Oral 5531 MBq Capsule Oral 3700 MBq Capsule Oral 1 mCi Capsule Oral 10 mCi Capsule Oral 100 mCi Capsule Oral 100 μCi Capsule Oral 125 mCi Capsule Oral 15 mCi Capsule Oral 150 mCi Capsule Oral 16 μCi Capsule Oral 175 mCi Capsule Oral 2 mCi Capsule Oral 20 mCi Capsule Oral 200 mCi Capsule Oral 25 mCi Capsule Oral 30 mCi Capsule Oral 5 mCi Capsule Oral 50 mCi Capsule Oral 50 μCi Capsule Oral 70 mCi Capsule Oral 75 mCi Solution Oral 1 mCi Solution Oral 10 mCi Solution Oral 100 mCi Solution Oral 125 mCi Solution Oral 15 mCi Solution Oral 150 mCi Solution Oral 175 mCi Solution Oral 2 mCi Solution Oral 20 mCi Solution Oral 200 mCi Solution Oral 25 mCi Solution Oral 250 mCi Solution Oral 30 mCi Solution Oral 300 mCi Solution Oral 350 mCi Solution Oral 400 mCi Solution Oral 450 mCi Solution Oral 5 mCi Solution Oral 50 mCi Solution Oral 500 mCi Solution Oral 60 mCi Solution Oral 75 mCi Solution Oral 80 mCi Solution Oral 18500 MBq Capsule Oral 3719 MBq Capsule Oral 0333 MBQ Capsule Oral 0592 MBQ Capsule Oral 1.11 MBQ Capsule Oral 2035 MBQ Capsule Oral 3.7 MBQ Capsule Oral 3718.5 MBq Solution Oral 74 MBQ/ML Solution Oral 925 MBQ/ML Injection, solution Intravenous 74 MBQ/ML Injection, solution Intravenous 925 MBQ/ML Injection Intravenous 74 MBq/ml Injection Intravenous 925 MBq/ml Capsule, gelatin coated Oral 1 mCi/1mL Capsule Oral 100 mCi/1 Capsule Oral 200 mCi/1 Kit Oral 1000 mCi/1 Solution, concentrate Oral 3500 mCi/1mL Solution Oral 25 mCi/1mL Solution Oral 5 mCi/1mL Capsule Oral 2793.5 MBq Capsule Oral 20 μg Capsule, coated Oral 5500 MBq Injection, solution Intravenous 740 MBq Capsule, coated Oral 7400 MBq - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source logP 1.02 Chemaxon pKa (Strongest Acidic) -9 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 0 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 0 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 13.95 m3·mol-1 Chemaxon Polarizability 5.07 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 115.60002 predictedDeepCCS 1.0 (2019) [M+H]+ 117.49543 predictedDeepCCS 1.0 (2019) [M+Na]+ 125.06797 predictedDeepCCS 1.0 (2019)
Drug created at October 30, 2015 14:22 / Updated at June 12, 2020 16:52