Consumer medicine information

Sodium Iodide (131I) Therapy Capsules

Sodium iodide (131I)

BRAND INFORMATION

Brand name

ANSTO Health Sodium Iodide (<sup>131</sup>I) Therapy Capsules

Active ingredient

Sodium iodide (131I)

Schedule

Unscheduled

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Sodium Iodide (131I) Therapy Capsules.

1 Medicine name

Sodium Iodide [131I]

2 Special advisory

Radiopharmaceuticals should be used only by physicians who are qualified by specific training in the safe use and handling of radionuclides produced by a nuclear reactor or particle accelerator, and whose experience and training have been approved by the appropriate government agency authorised to license the use of radionuclides.

Care should be taken to minimise radiation exposure to patients, consistent with proper patient management. As with other radioactive drugs, Sodium Iodide [131I] must be handled with care and appropriate safety measures should be used to minimise radiation exposure to clinical personnel.

3 Why am I using Sodium Iodide [131I] Therapy Capsule?

You are being given the Sodium Iodide (131I) Therapy Capsule for the treatment of hyperthyroidism, and the detection, treatment and ablation of residual functioning thyroid tissue in differentiated thyroid carcinoma.

Sodium Iodine (131I) is a radioisotope which emits high energy electrons (beta particles). When administered orally, the Iodine-131 from the capsules is taken up by the thyroid gland tissue. Beta radiation from the Iodine-131 help reduce the activity of the tissue in proportion to the amount of Iodine-131 absorbed.

If you have any concerns about being given this capsule, discuss them with your nuclear medicine specialist.

4 What should I know before I use Sodium Iodide [131I] Therapy Capsule?

All medicines and diagnostic agents have risks and benefits associated with their usage. Your nuclear medicine physician or specialist has weighed the small risk of your being treated with a Sodium Iodide (131I) therapy capsule against the benefits it is expected you will receive from it.

Before you are given Sodium Iodide [131I] Therapy Capsule, it is important to tell your nuclear medicine specialist or technologist if:

  1. You are pregnant or intend to become pregnant:
It is known that the Sodium Iodide (131I) contained in this capsule may be harmful to an unborn baby when administered to a pregnant woman.
Sodium Iodide (131I) will only be given in pregnancy after weighing the needs of the mother against any risk to the foetus.
If you intend to become pregnant consult your doctor about the advised waiting period.
  1. You are breast-feeding:
It is normal practice to stop breastfeeding and substitute formula feeding from the time you are given the capsule. It is known that Sodium Iodide (131I) passes into breast milk.
  1. You have eaten seafood, or foods with high iodine content lately:
Discuss your diet over the previous three days as iodine consumed in food may influence your treatment.

5 What if I am taking other medicines?

It is very important that you tell your doctors if you are taking any other medicines, including those you buy over the counter without a prescription from your pharmacy, supermarket, or health food store.

The constituents of medications you are taking could affect the results of this treatment. Your nuclear medicine specialist or technologist will advise you of what to do.

6How do I use Sodium Iodide [131I] Therapy Capsule?

(a)How it is given:

Sodium Iodide (131I) therapy capsules can only be administered by qualified staff with specific training in the safe use and handling of radiopharmaceuticals.

A Sodium Iodide (131I) therapy capsule is given with a drink. It must be swallowed whole – do not chew the capsule. You may be asked to take food and drink to aid digestion of the capsule.

(b) Test procedure:

After taking your capsule you may be asked to stay in hospital for a period (spanning from few hours to few days) to monitor the treatment.

After your treatment you may be asked to have another scan, similar to your original diagnostic scan, at a later date.

7 What should I know while using Sodium Iodide [131I] Therapy Capsule?

Preparation:

Usually no preparation is required for these tests. Specific instructions are given when any preparation is required.

After you are given the capsule:

  • Directly after swallowing the capsule you have radioactive material in you. You will be shielded from your surroundings for some time. Your stools, urine or vomit are considered radioactive and should be disposed of with care so they will not come into contact with others.
  • Urinate frequently in order to eliminate the product from your body.
  • Speak to your doctor if you are intending to father a child or intending to fall pregnant, you may have to wait for some period prior to this.

Your discharge from hospital and after you go home:

Continue your day-to-day activities. However, it is IMPORTANT to observe the following for one week after the treatment as the Iodine-131 continues to leave your body:

  • Avoid close physical contact with children and pregnant women.
  • Avoid being closer than 1 metre to other persons for an extended duration.
  • Drink plenty of fluids.
  • Observe good personal hygiene in order to prevent the spread of radioactive contamination.
  • Shower daily and frequently wash off excess perspiration.

Your doctor will tell you if you need to take any special precautions after receiving Sodium Iodide (131I) Capsule.

8 Are there any side effects?

Like all medicines, this medicine can cause side effects, although not everybody gets them. Tell your nuclear medicine specialist or technologist as soon as possible if you do not feel well after taking your Sodium Iodine (131I) therapy capsule.

Rare minor reactions such as nausea, vomiting, increased heartbeat, itching and rash have been reported with the use of Sodium Iodide (131I) therapy capsules.

When larger doses of Iodine-131 are used, reported sided effects include radiation thyroiditis, sialitis and transient worsening of hyperthyroidism.

Potential effects of a high dose of Iodine-131 include nausea, pulmonary fibrosis, bone marrow depression, leukaemia, and acute thyroid crisis.

9 Sponsor

ANSTO
New Illawarra Rd,
Lucas Heights
NSW 2234, Australia

Mailing address:
ANSTO, Locked Bag 2001
Kirrawee DC
NSW 2232, Australia

Telephone: 1800 251 572

E-mail: [email protected]
Website: www.ansto.gov.au

Product Code:
10020: 50MBq – 600MBq
10233: 700MBq – 6,000MBq

Australian Registration Number:
AUST R: 22808

10 Date of revision

18 January 2022

Published by MIMS November 2022

BRAND INFORMATION

Brand name

ANSTO Health Sodium Iodide (<sup>131</sup>I) Therapy Capsules

Active ingredient

Sodium iodide (131I)

Schedule

Unscheduled

 

1 Name of Medicine

Sodium iodide (131I).

2 Qualitative and Quantitative Composition

Description.

Sodium Iodide (131I) Therapy Capsules are supplied for oral administration as pale yellow gelatin capsules containing sodium iodide [131I] solution adsorbed on an inert filler (di-sodium hydrogen phosphate). A range of iodine-131 content is available, from 50 MBq to 6000 MBq at the time of calibration at 0900 hrs (Sydney time) each Monday.
Each capsule is contained in a glass serum vial sealed with a rubber stopper and red aluminium seal. The vial is in turn contained in an appropriate lead container. Decapping pliers can be supplied free of charge with the initial order.
For the full list of excipients, see Section 6.1 List of Excipients.

Physical characteristics for (131I).

Iodine-131 with a physical half-life of 8.04 days, decays by beta emission (average energy 182 keV) with associated gamma emission. Stable xenon-131 is formed in 98.9% of decays and radioactive xenon-131m (half-life 11.9 days) in 1.1% of decays. The principal beta emissions and gamma photons are listed in Table 1.
See Table 2.

External radiation.

The specific gamma ray constant for iodine-131 is 0.61 mGy per MBq-h at 1 cm. The first half-value thickness of lead for iodine-131 is 0.26 cm and a lead thickness of 2.6 cm will produce an attenuation factor of about 10-2. Attenuation by lead is given in Table 3.

3 Pharmaceutical Form

Yellow coloured gelatin capsule printed with an "ANSTO" logo and an "Ionising radiation trefoil" symbol.

4 Clinical Particulars

4.1 Therapeutic Indications

Sodium Iodide (131I) Therapy Capsule is indicated in the treatment of hyperthyroidism, and the detection and ablation of residual functioning thyroid tissue in differentiated thyroid carcinoma.

4.2 Dose and Method of Administration

The capsules are for oral administration and the dose ranges usually employed are as follows.

Thyrotoxicosis.

150-600 MBq.

Thyroid ablation.

800-2,000 MBq.

Thyroid carcinoma.

2,000-6,000 MBq.

Instructions for use.

(i) Prepare disposable gloves for staff and patient, absorbent paper tissues, empty disposable paper cup and a drink of water in a disposable paper cup.
(ii) Check expiry date of capsule, remove lid of lead container.
(iii) Measure the activity of the capsule while still in the sealed glass vial.
(iv) In a suitably ventilated enclosure remove the cap and closure from the glass vial, while still in the lead shipping container, using a decapping apparatus.
(v) With forceps or pliers, pick up the glass vial and tip the capsule into an empty disposable paper cup. Place the empty vial, and the closure in the lead container, and close the lead pot with the lid.

Note.

The empty vial and closure should be remeasured to confirm that no significant loss of activity has occurred from the capsule during transport and storage.
(vi) Present both disposable paper cups to the patient who should then swallow the capsule and take a drink of water if necessary. The patient should be advised not to bite the capsule.
(vii) Treat gloves, cups and the empty vial, stopper and cap as radioactive waste.

Radiation dosimetry.

The estimated absorbed radiation doses to euthyroid patients from an oral dose of iodine-131 is presented in Tables 4 - 7. This data has been taken from ICRP publication 128, Radiation Dose to Patients from Radiopharmaceuticals: a Compendium of Current Information Related to Frequently Used Substances; p.277-280.
The biokinetic model is described as a compartment model including inorganic iodide as well as organically bound iodine released to the body tissues following discharge from the thyroid. The ICRP model refers to oral administration. As part of the risk-benefit assessment it is advised that the effective dose and likely radiation doses to individual target organ(s) are calculated prior to administration. The activity might then be adjusted according to thyroid volume, biological half-life and the "re-cycling" factor which takes into account the physiological status of the patient (including iodine depletion) and the underlying pathology.
The radiation exposure mainly affects the thyroid. The radiation exposure of the other organs is in the range of thousandths lower than that of the thyroid. It depends on the dietary intake of iodine (the uptake of radioiodine is increased up to 90% in iodine deficient areas and it is decreased to 5% in iodine rich areas). It further depends on the thyroid function (eu-, hyper-, or hypothyroidism) and on the presence of iodine accumulating tissues in the body (e.g. the situation after excision of the thyroid, the presence of iodine accumulating metastases and on thyroid blockade). The radiation exposure of all other organs is correspondingly higher or lower, depending on the degree of accumulation in the thyroid.
In thyroid blocked patients, estimated radiation absorbed dose to various body organs per unit of 131I activity administered (mGy MBq-1) is presented in Table 4.
In Tables 5, 6 and 7, estimated radiation absorbed dose to various body organs per unit of 131I activity administered (mGy MBq-1) is given for low, medium, and high thyroid uptake scenarios respectively.
Dose calculations have been performed for standard (70 kg) adults, and for 15-, 10-, 5-, and 1-year-old children.

4.3 Contraindications

The use of this therapeutic radiopharmaceutical is absolutely contraindicated in women who are pregnant. Women of reproductive age should have a negative pregnancy test at the time of radionuclide therapy, and should take appropriate contraceptive measures.
The use of therapeutic iodine-131 is not recommended in persons with renal insufficiency, as delayed excretion will result in increased whole body radiation.
This therapy is contraindicated in patients who are being treated concurrently with thyroid hormone or antithyroid drugs, are vomiting or have diarrhoea.

Note.

"Iodine allergy" is not a contraindication for use, because of the very small chemical amounts of iodine in therapeutic capsules (e.g. approx. 3 microgram in a 500 MBq capsule).

4.4 Special Warnings and Precautions for Use

Warning.

Iodine-131 should not be administered to individuals below the age of 18 years unless such use is essential in the judgement of the clinician and the benefits outweigh any potential risks.

Precautions - general.

Radiopharmaceuticals should be used only by physicians who are qualified and licensed to handle radioisotopes.

Identified precautions - hyponatraemia.

Serious manifestations of hyponatraemia have been reported after sodium iodide [131I] therapy in elderly patients who have undergone total thyroidectomy. Risk factors include older age, female sex, use of thiazide diuretics and hyponatraemia at the start of sodium iodide [131I] therapy. Regular serum electrolyte measurements and monitoring should be considered for these patients.

Dose handling.

Radiation exposure to staff must be minimised. In particular, the capsules should not be handled directly. The glass vial containing the capsule may be contaminated externally with iodine-131 and appropriate handling precautions should be used.
As iodine-131 is volatile and the daughter radionuclide xenon-131m is gaseous, the vial containing the capsule should be uncapped in a ventilated enclosure. (Tests have failed to detect any diffusion of radioactivity from the sealed glass vial between manufacture and use). The activity of the capsule should be checked with a suitable instrument immediately prior to administration.

Patient care.

Care should be taken to minimise unwanted radiation exposure to patients, consistent with proper patient management, and to minimise radiation exposure to clinical personnel.
Patients should be encouraged to drink copious fluids before and after capsule administration and to void as often as possible after administration in order to reduce the radiation dose to the kidneys, stomach and bladder. A high standard of patient hygiene is desirable.

Discharge of patients after I-131 procedure.

Discharge of Patients Undergoing Treatment with Radioactive Substances should be in accordance with Radiation Protection Series Publication No. 4, published by Australian Radiation Protection and Nuclear Safety Agency (ARPANSA). https://www.arpansa.gov.au/sites/default/files/legacy/pubs/rps/rps4.pdf.
It is recommended that the ambient dose equivalent rate at a distance of 1 metre from a patient who is undergoing treatment with a radioactive substance should not exceed 25 microSv/hour at the time of the patient's discharge from the hospital.
Individualised instructions relevant to the patient's medical and social circumstances should be provided to each patient by the licensed medical specialist responsible for the treatment. The instructions should include, where appropriate, the need to restrict close proximity to other members of the household, especially children, young persons and pregnant women, the importance of good personal hygiene in order to prevent the spread of contamination, and the date when normal activities may be resumed.

Use in renal impairment.

The use of therapeutic iodine-131 is not recommended in persons with renal insufficiency, as delayed excretion will result in increased whole body radiation (see Section 4.3 Contraindications).

Use in the elderly.

No data available.

Paediatric use.

Safety and efficacy in children have not been established.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

The uptake of iodine-131 will be affected by recent intake of stable iodine in any form e.g. seafood, radiographic contrast media, and by antithyroid drugs and thyroxine. The patient's history should be fully investigated in this regard.
Antithyroid drugs should be withheld for at least 3 days prior to iodine-131 therapy, and thyroxine should be withdrawn for at least 4 weeks prior to therapy. Adequate trapping of iodide by thyroid tissue or thyroid cancer metastases should be demonstrated before the administration of a therapeutic dose of iodine-131.

Long-term effects.

Therapy using iodine-131 can induce hypothyroidism. To some extent, this effect is dose dependent, but life-long follow-up of patients treated with iodine-131 is advised.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

Adequate long-term studies have not been performed in animals to determine whether this drug affects fertility. After radioiodine therapy of thyroid carcinoma, a dose dependent impairment of fertility may occur in men and women. Depending on the activity dose, a reversible impairment of the spermatogenesis could occur in doses above 1,850 MBq. Clinical relevant effects including oligospermia and azoospermia and elevated serum FSH serum levels have been described after administration greater than 3,700 MBq.

Contraception in males and females.

Contraception for 6 months (for patients with benign thyroid conditions) or 12 months (for patients with thyroid cancer) is recommended for both sexes after therapeutic administration of sodium iodide (131I).
Men should not father a child for a time period of 6 months after radioiodine treatment to allow the replacement of irradiated by non-irradiated spermatozoa. Sperm banking should be considered for men who have extensive disease and therefore may need high sodium iodide (131I) therapeutic doses.

Women of childbearing potential.

When an administration of radiopharmaceuticals to a woman of childbearing potential is intended, it is important to determine whether or not she is pregnant. Any woman who has missed a period should be assumed to be pregnant until proven otherwise. If in doubt about her potential pregnancy (if the woman has missed a period, if the period is very irregular, etc.), alternative techniques not using ionising radiation (if there are any) should be offered to the patient. Women receiving sodium iodide (131I) should be advised not to become pregnant within 6-12 months after administration.
(Category X)
See Section 4.3 Contraindications.
There are no animal study data on the effects of sodium iodide [131I] on embryofetal development. The use of sodium iodide (131I) is contraindicated during established or suspected pregnancy or when pregnancy has not been excluded because transplacental passage of sodium iodide (131I) can cause severe and possibly irreversible hypothyroidism in neonates (the absorbed dose to the uterus for this medicinal product is likely to be in the range 20-270 mGy for therapeutic indications and 0.2 mGy for diagnostic indications, and the fetal thyroid gland avidly concentrates iodine during the second and third trimesters).
If a differentiated thyroid carcinoma is diagnosed during pregnancy, sodium iodide (131I) treatment should be postponed until after the childbirth.
As sodium iodide (131I) readily crosses the placenta, adverse effects are expected when used during pregnancy due to fetal thyroid accumulation of 131I that leads to neonatal hypothyroidism. Females and males of reproductive potential should use effective contraception during treatment and for at least 6 months after the last dose.
Iodine-131 is excreted in human milk. Before administering radiopharmaceuticals to a mother who is breast-feeding, consideration should be given to the possibility of delaying the administration of radionuclide until the mother has ceased breast-feeding, and what is the most appropriate choice of radiopharmaceuticals, bearing in mind the secretion of activity in breast milk. If the administration is considered necessary, breast-feeding must be discontinued at least 8 weeks before sodium iodide (131I) administration to allow sufficient time for involution to occur and to avoid excess concentration of sodium iodide [131I] in breast tissue and should not be resumed.
For radioprotection reasons following therapeutic doses, it is recommended to avoid close contact between mother and infants for 6 h.

4.7 Effects on Ability to Drive and Use Machines

The effects of this medicine on a person's ability to drive and use machines were not assessed as part of its registration.

4.8 Adverse Effects (Undesirable Effects)

Rare adverse reactions have been reported following the administration of iodine-131. Their relationship to the very small chemical amounts of iodine administered is not clear.
These reactions have included vomiting, nausea, tachycardia, pruritus and rash. Other reported side effects include radiation induced thyroiditis and sialitis and transient worsening of hypothyroidism.
Potential effects of a high dose of iodine-131 include radiation sickness, pulmonary fibrosis, bone marrow depression, acute leukemia, anaemia, acute thyroid crisis and death.

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at www.tga.gov.au/reporting-problems.

4.9 Overdose

See Section 4.8 Adverse Effects (Undesirable Effects).
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

The pharmacological active substance is sodium iodide (131I) in the form of sodium iodide that is taken up by the thyroid. The physical decay takes place essentially in the thyroid gland, where sodium iodide (131I) has a long residence time, delivering a selective irradiation to this organ.
In the amount used for therapeutic indications, no pharmacodynamic effects of sodium iodide (131I) are to be expected.
More than 90% of the radiation effects result from emitted β radiation which has a mean range of 0.5 mm. The β irradiation will dose dependently decrease cell function and cell division leading to cell destruction. The short range and almost absence of uptake of sodium iodide (131I) outside the thyroid lead to a negligible amount of irradiation exposure outside the thyroid gland.

Clinical trials.

No data available.

5.2 Pharmacokinetic Properties

Absorption.

After oral administration, sodium iodide (131I) is absorbed rapidly from the upper gastrointestinal tract (90% in 60 minutes). The absorption is influenced by gastric emptying. It is increased by hyperthyroidism and decreased by hypothyroidism.
Studies on the serum activities levels showed that after a fast increase, over 10 to 20 minutes, an equilibrium is reached after about 40 minutes. After oral administration of sodium iodide (131I) solution an equilibrium is reached at the same time.

Distribution and organ uptake.

The pharmacokinetics follows that of unlabelled iodide. After entering the blood stream it is distributed in the extra thyroidal compartment. From here it is predominantly taken up by the thyroid that extracts approximately 20% of the iodide in one pass or excreted renally. The iodide uptake in the thyroid reaches a maximum after 24-48 hours, 50% of the maximum peak is reached after 5 hours. The uptake is influenced by several factors: patient age, thyroid gland volume, renal clearance, plasmatic concentration of iodide and other drugs (see Section 4.5). The iodide clearance by the thyroid gland is usually 5-50 mL/min. In case of iodine deficiency the clearance is increased to 100 mL/min and in case of hyperthyroidism can be up to 1,000 mL/min. In case of iodide overload the clearance can decrease to 2-5 mL/min. Iodide also accumulates in the kidneys.
Small amounts of sodium iodide (131I) are taken up by salivary glands, gastric mucosa and they would also be localised in breast milk, the placenta and choroid plexus.
The iodide fixed by the thyroid enters the known metabolic path of thyroid hormones and is incorporated in the organic substances entering in the synthesis of thyroid hormones.

Biotransformation.

The iodide that has been taken up by the thyroid follows the known metabolism of the thyroid hormones and is incorporated in the organic compounds from which the thyroid hormones are synthesised.

Elimination.

Urinary excretion is 37-75%, faecal excretion is about 10%, with almost negligible excretion in sweat. Urinary excretion is characterised by the renal clearance, which constitutes about 3% of the renal flow and is relatively constant from one person to another. The clearance is lower in hypothyroidism and in impaired renal function and higher in hyperthyroidism. In euthyroidic patients with normal renal function 50-75% of the administered activity is excreted in urine within 48 hours.

Half-life.

The effective half-life of radioiodine in plasma is about 12 hours in blood plasma and about 6 days in the thyroid gland. Thus after administration of sodium iodide (131I) about 40% of the activity has an effective half-life of 6 hours and the remaining 60% of 8 days.

Renal impairment.

Patients with renal impairment may have a decrease in the radioiodine clearance, resulting in increased radiation exposure of sodium iodide (131I) administered. One study showed, for example, that patients with impaired renal function undergoing continuous ambulatory peritoneal dialysis (CAPD) have a clearance of radioiodine 5 times lower than patients with normal kidney function.

Note.

As with other iodine-131 gelatin capsules, some iodine-131 is lost due to binding of iodine-131 to the capsule material. This iodine-131 does not appear to be available for uptake by the thyroid.

5.3 Preclinical Safety Data

Genotoxicity.

The genotoxic potential of sodium iodine [131I] has not been evaluated under in vitro or in vivo conditions.

Carcinogenicity.

The carcinogenic potential of sodium iodide [131I] has not been evaluated in any animal studies.

6 Pharmaceutical Particulars

6.1 List of Excipients

Sodium phosphate dibasic anhydrous, sodium bicarbonate, sodium thiosulfate pentahydrate, water for injections.
Gelatin capsule hard: iron oxide yellow, titanium dioxide, gelatin, Tek Print SW-9008 black ink.

6.2 Incompatibilities

This medicinal product must not be mixed with other medicinal products except with those as required to achieve therapeutic indications given in Section 4.1 of this Product Information document.
Interaction of this medicine with others is also given in Section 4.5 of this Product Information document.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the ARTG. The expiry date can be found on the 'packaging' under this heading.

Note.

This product has an expiration period of 14 days from the date of calibration (shown on the product vial label).

6.4 Special Precautions for Storage

Store below 25 degrees Celsius.

6.5 Nature and Contents of Container

Primary.

The primary container is a labelled 10 mL serum vial of USP Type 1 (neutral) glass or equivalent with a 20 mm outer diameter neck. The closure is a 20 mm halo-butyl rubber stopper (or equivalent). The metal caps are plain 20 mm aluminium seals and are red in colour.

Secondary.

The outer container is a labelled lead pot of suitable thickness.

Tertiary.

For transport, the lead pot is packed in an approved Type A package.

6.6 Special Precautions for Disposal

Disposal of all radioactive wastes should be carried out in accordance with the "Code for the Disposal of Radioactive Wastes by the User - Radiation Protection Series, C-6, September 2018", published by Australian Radiation Protection and Nuclear Safety Agency (ARPANSA).
See Section 4.4 Special Warnings and Precautions for Use.
In Australia, any unused medicine or waste material should be disposed of in accordance with local requirements.

6.7 Physicochemical Properties

Chemical structure.

Molecular formula: Na131I.
Chemical structure: Na+........-I[131].

CAS number.

7790-26-3.

7 Medicine Schedule (Poisons Standard)

Unscheduled.

Summary Table of Changes