Potassium perchlorate
Potassium perchlorate Uses, Dosage, Side Effects, Food Interaction and all others data.
Potassium perchlorate is an inorganic salt with the chemical formula KClO4. It is a strong oxidizer with the lowest solubility of the alkali metal perchlorates. Potassium is most commonly used in flares and automobile airbags . The use of potassium perchlorate as a component in sealing gaskets for food containers has been revoked by the FDA following the use being abandoned by the industry . Potassium perchlorate acts as a competitive inhibitor of iodine uptake by the thyroid gland and attenuates the production of the thyroid hormone. Thus the use of potassium perchlorate has been extensive for hyperthyroidism during the last 50 years, particularly in the late 1950s and early 1960s . The therapeutic use of potassium perchlorate in thyroid disorders has been ceased due to a high risk for developing aplastic anemia and nephrotic syndrome .
Potassium perchlorate inhibits thyroid iodide transport. The clinical use of potassium perchlorate in hyperthyroidism, such as Graves' disease and amiodarone-induced hypothyroidism, have been investigated in various studies. Thyroid dysfunction occurs in about 15-20% of the patients receiving long-term amiodarone therapy . In patients with amiodarone-induced hypothyroidism, short-term administration of potassium perchlorate resulted in restoration of euthyroidism in most patients . Euthyroidism promoted by potassium perchlorate does not persist unless amiodarone treatment is withdrawn .
| Trade Name | Potassium perchlorate |
| Generic | Potassium perchlorate |
| Potassium perchlorate Other Names | Potassium perchlorate |
| Type | |
| Formula | ClKO4 |
| Weight | Average: 138.549 Monoisotopic: 137.912218056 |
| Protein binding | Displacement studies with thyroid hormones suggest that perchlorate ions may interfere with the binding of T4 to serum proteins . |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
No current FDA- or EMA-approved therapeutic indications.
How Potassium perchlorate works
Thyroxine (T4) and tri-iodothyronine (T3) are major thyroid hormones, or iodothyronines, that are synthesized and released from the thyroid. Iodine plays an essential role in the synthesis of these hormones. Via the sodium-iodide symporter (NIS), which is a protein located on the basolateral membrane of the thyroid follicular cell, iodine is transported from the blood into the thyroid gland where it is oxidized to . Perchlorate (ClO4−) is the dissociated anion of potassium perchlorate that exerts an inhibitory effect on iodide uptake by the thyroid gland in the cellular level . Due to its similarity in ionic size and charge to iodide, perchlorate inhibits the sodium-iodide symporter (NIS) without being translocated into the thyroid follicular cell . The inhibition constant, Ki, is estimated as 0.4 µmol to 24 µmol. At therapeutic dosage levels this competitive inhibition decreases the entrance of iodide into the thyroid, resulting in less available iodide for hormone synthesis and, therefore, a decrease in T3 and T4 synthesis . When ambient iodine intake is low or iodide uptake is sufficiently inhibited, perchlorate is capable in inducing goiter and hypothyroidism from inhibited iodide uptake . At high doses of potassium perchlorate, reduced T3 and T4 levels may be accompanied by increased TSH levels via a negative feedback loop, affecting the thyroid, pituitary and hypothalamus .
Toxicity
In a mice study, the LD50 was reported as 3621 mg/kg of following 33 weeks of oral administration . A study reports that at doses of 400 mg/d for several weeks had adverse effects such as GI irritation, skin rash, and lymphadenopathy but cited no serious complications . In patients treated with 400 to 1,000 mg perchlorate daily, cases of agranulocytosis and fatal aplastic anemia have been reported. Several deaths from aplastic anemia in patients treated with perchlorate at doses of 400 to 1000 mg/d for 8 to 33 weeks were also reported . The last report of fatal bone marrow toxicity related to treatment with potassium perchlorate was in the 1960s .
Volume of Distribution
No pharmacokinetic data on the volume of distribution. Perchlorate is likely to sequester into the thyroid gland, gastrointestinal tract, and possibly the skin .
Elimination Route
Perchlorate is rapidly absorbed from the gastrointestinal (GI) tract after ingestion . The time to reach peak plasma levels of perchlorate is approximately 3 hours following oral administration . As potassium perchlorate is an organic compound with complete ionization in water, dermal absorption through intact skin is unlikely .
Half Life
Perchlorate has a half-life in humans of approximately 6 to 8 hours .
Clearance
No pharmacokinetic data on clearance rate. Systemic clearance is biphasic with a slow terminal phase .
Elimination Route
Perchlorate is mainly excreted unchanged in the urine with the recovery rate of approximately 95% within 72 hours . It is reported that half of the total perchlorate ions administered orally are excreted during the first 5 hours post-dosing while the rest of the dose is excreted within 48 to 72 hours .
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