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
Thumb
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.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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
Adverseeffects
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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.
DrugInteraction
AmiodaroneAmiodarone may decrease effectiveness of Iodide I-131 as a diagnostic agent.
CarbimazoleThe therapeutic efficacy of Iodide I-131 can be decreased when used in combination with Carbimazole.
MethimazoleThe therapeutic efficacy of Iodide I-131 can be decreased when used in combination with Methimazole.
Potassium IodideThe therapeutic efficacy of Iodide I-131 can be decreased when used in combination with Potassium Iodide.
Potassium perchlorateThe therapeutic efficacy of Iodide I-131 can be decreased when used in combination with Potassium perchlorate.
PropylthiouracilThe therapeutic efficacy of Iodide I-131 can be decreased when used in combination with Propylthiouracil.
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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

Products2
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Product Ingredients
IngredientUNIICASInChI Key
Sodium iodide I-13129VCO8ACHH7790-26-3FVAUCKIRQBBSSJ-LAIFMVDKSA-M
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
HiconSolution1 mCi/1mLOralJubilant DraxImage Inc., dba Jubilant Radiopharma2003-04-07Not applicableUS flag
I 131 MiniCapsule500 mCi/1OralAnazao Health Corporation2012-05-23Not applicableUS flag
I3odine MAXTMSolution3500 mCi/1mLOralInternational Isotopes Inc2001-01-012016-10-25US flag
IodotopeCapsule, gelatin coated130 mCi/1OralBracco Diagnostics, Inc1957-06-142008-06-19US flag
Sodium Iodide I 131Capsule, gelatin coated1 mCi/1mLOralMallinckrodt2012-01-252017-07-01US flag
Sodium Iodide I 131Capsule, gelatin coated1 mCi/1mLOralMallinckrodt Nuclear Medicine Llc2015-10-272018-07-01US flag
Sodium Iodide I 131 DiagnosticCapsule100 mCi/1OralJubilant DraxImage Inc., dba Jubilant Radiopharma2006-05-01Not applicableUS flag
Sodium Iodide I 131 TherapeuticCapsule200 mCi/1OralJubilant Draximage Inc.2011-02-012012-02-07US flag
Sodium Iodide I-131Solution, concentrate3500 mCi/1mLOralInternational Isotopes Inc2010-09-01Not applicableUS flag
Sodium Iodide I-131 TherapeuticSolution5 mCi/1mLOralMallinckrodt Nuclear Medicine Llc2015-10-272018-07-01US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Sodium Iodide I-1311000 mCi/1OralInternational Isotopes Inc2020-03-16Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
I 131 MiniSodium iodide I-131 (500 mCi/1)CapsuleOralAnazao Health Corporation2012-05-23Not applicableUS flag
I3odine MAXTMSodium iodide I-131 (3500 mCi/1mL)SolutionOralInternational Isotopes Inc2001-01-012016-10-25US flag
Sodium Iodide I-131Sodium iodide I-131 (3500 mCi/1mL)Solution, concentrateOralInternational Isotopes Inc2010-09-01Not applicableUS flag

Categories

ATC Codes
V09FX03 — Sodium iodide (131i)V10XA01 — Sodium iodide (131i)
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
KEGG Drug
D02259
PubChem Compound
167195
PubChem Substance
310265185
ChemSpider
146281
RxNav
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
PhaseStatusPurposeConditionsCount
3CompletedNot AvailableNeoplasms, Thyroid1
3Unknown StatusTreatmentNeoplasms, Thyroid1
2Active Not RecruitingTreatmentMetastatic Thyroid Gland Carcinoma / Poorly Differentiated Thyroid Gland Carcinoma / Recurrent Thyroid Gland Carcinoma / Refractory 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 v71
2Active Not RecruitingTreatmentMetastatic Thyroid Gland Carcinoma / Poorly Differentiated Thyroid Gland 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 v71
2CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)2
2Not Yet RecruitingTreatmentThyroid Cancers1
0Active Not RecruitingTreatmentThyroid Cancers1
Not AvailableCompletedNot AvailableThyroid Cancers3
Not AvailableNot Yet RecruitingTreatmentThyroid Papillary Carcinoma1
Not AvailableUnknown StatusDiagnosticLacrimal Apparatus Diseases1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
CapsuleOral3025 MBq
SolutionOral1 mCi/1mL
SolutionOral37 GBq/mL
CapsuleOral500 mCi/1
SolutionOral3500 mCi/1mL
Capsule, gelatin coatedOral
Capsule, gelatin coatedOral130 mCi/1
SolutionOral18500 MBq
CapsuleOral
CapsuleOral3718.5 MBq
SolutionOral
Injection, solutionIntravenous
InjectionIntravenous74 MBq/ml
InjectionIntravenous925 MBq/ml
Capsule, gelatin coatedOral1 mCi/1mL
CapsuleOral100 mCi/1
CapsuleOral200 mCi/1
Solution, concentrateOral3500 mCi/1mL
SolutionOral25 mCi/1mL
SolutionOral5 mCi/1mL
CapsuleOral2793.5 MBq
Capsule, coatedOral5500 MBq
Injection, solutionIntravenous740 MBq
Capsule, coatedOral7400 MBq
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
logP1.02ChemAxon
pKa (Strongest Acidic)-9ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count0ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area0 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity13.95 m3·mol-1ChemAxon
Polarizability5.07 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Drug created on October 30, 2015 14:22 / Updated on June 12, 2020 16:52