NAV

Potassium perchlorate

Identification

Generic Name
Potassium perchlorate
DrugBank Accession Number
DB09418
Background

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 1. The use of potassium perchlorate as a component in sealing gaskets for food containers has been revoked by the FDA following the use being abandoned by the industry 7. 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 1. The therapeutic use of potassium perchlorate in thyroid disorders has been ceased due to a high risk for developing aplastic anemia and nephrotic syndrome 6.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Similar Structures
Weight
Average: 138.549
Monoisotopic: 137.912218056
Chemical Formula
ClKO4
Synonyms
  • Perchloric acid, potassium salt
  • Potassium perchlorate
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Pharmacology

Indication

No current FDA- or EMA-approved therapeutic indications.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

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 2. In patients with amiodarone-induced hypothyroidism, short-term administration of potassium perchlorate resulted in restoration of euthyroidism in most patients 4. Euthyroidism promoted by potassium perchlorate does not persist unless amiodarone treatment is withdrawn 2.

Mechanism of action

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 3. 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 3. 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 3. 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 3. When ambient iodine intake is low or iodide uptake is sufficiently inhibited, perchlorate is capable in inducing goiter and hypothyroidism from inhibited iodide uptake 3. 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 8.

TargetActionsOrganism
ASodium/iodide cotransporter
inhibitor
Humans
Absorption

Perchlorate is rapidly absorbed from the gastrointestinal (GI) tract after ingestion 3. The time to reach peak plasma levels of perchlorate is approximately 3 hours following oral administration 6. As potassium perchlorate is an organic compound with complete ionization in water, dermal absorption through intact skin is unlikely 8.

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 5.

Protein binding

Displacement studies with thyroid hormones suggest that perchlorate ions may interfere with the binding of T4 to serum proteins 5.

Metabolism

Perchlorate ions are not reported to undergo metabolism 6.

Route of elimination

Perchlorate is mainly excreted unchanged in the urine with the recovery rate of approximately 95% within 72 hours 3. 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 6.

Half-life

Perchlorate has a half-life in humans of approximately 6 to 8 hours 3.

Clearance

No pharmacokinetic data on clearance rate. Systemic clearance is biphasic with a slow terminal phase 5.

Adverse Effects
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Toxicity

In a mice study, the LD50 was reported as 3621 mg/kg of following 33 weeks of oral administration 9. 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 3. 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 3. The last report of fatal bone marrow toxicity related to treatment with potassium perchlorate was in the 1960s 3.

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
Integrate drug-drug
interactions in your software
AbacavirAbacavir may decrease the excretion rate of Potassium perchlorate which could result in a higher serum level.
AbciximabPotassium perchlorate may increase the anticoagulant activities of Abciximab.
AcalabrutinibThe therapeutic efficacy of Potassium perchlorate can be decreased when used in combination with Acalabrutinib.
AcebutololPotassium perchlorate may increase the hyperkalemic activities of Acebutolol.
AceclofenacPotassium perchlorate may increase the hyperkalemic activities of Aceclofenac.
Food Interactions
Not Available

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Perchloracap Capsule 200mgCapsule200 mgOralTyco Healthcare1989-12-312010-01-07Canada flag

Categories

ATC Codes
H03BC01 — Potassium perchlorate
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of inorganic compounds known as alkali metal perchlorates. These are inorganic compounds in which the largest oxoanion is perchlorate, and in which the heaviest atom not in an oxoanion is an alkali metal.
Kingdom
Inorganic compounds
Super Class
Mixed metal/non-metal compounds
Class
Alkali metal oxoanionic compounds
Sub Class
Alkali metal perchlorates
Direct Parent
Alkali metal perchlorates
Alternative Parents
Inorganic salts / Inorganic oxides
Substituents
Alkali metal perchlorate / Inorganic oxide / Inorganic salt
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
42255P5X4D
CAS number
7778-74-7
InChI Key
YLMGFJXSLBMXHK-UHFFFAOYSA-M
InChI
InChI=1S/ClHO4.K/c2-1(3,4)5;/h(H,2,3,4,5);/q;+1/p-1
IUPAC Name
potassium perchlorate
SMILES
[K+].[O-][Cl](=O)(=O)=O

References

General References
  1. Connell JM: Long-term use of potassium perchlorate. Postgrad Med J. 1981 Aug;57(670):516-7. [Article]
  2. Bogazzi F, Bartalena L, Tomisti L, Dell'Unto E, Cosci C, Sardella C, Tanda ML, Lai A, Gasperi M, Aghini-Lombardi F, Martino E: Potassium perchlorate only temporarily restores euthyroidism in patients with amiodarone-induced hypothyroidism who continue amiodarone therapy. J Endocrinol Invest. 2008 Jun;31(6):515-9. doi: 10.1007/BF03346400. [Article]
  3. Soldin OP, Braverman LE, Lamm SH: Perchlorate clinical pharmacology and human health: a review. Ther Drug Monit. 2001 Aug;23(4):316-31. [Article]
  4. Martino E, Mariotti S, Aghini-Lombardi F, Lenziardi M, Morabito S, Baschieri L, Pinchera A, Braverman L, Safran M: Short term administration of potassium perchlorate restores euthyroidism in amiodarone iodine-induced hypothyroidism. J Clin Endocrinol Metab. 1986 Nov;63(5):1233-6. doi: 10.1210/jcem-63-5-1233. [Article]
  5. Yu KO, Narayanan L, Mattie DR, Godfrey RJ, Todd PN, Sterner TR, Mahle DA, Lumpkin MH, Fisher JW: The pharmacokinetics of perchlorate and its effect on the hypothalamus-pituitary-thyroid axis in the male rat. Toxicol Appl Pharmacol. 2002 Jul 15;182(2):148-59. [Article]
  6. POTASSIUM PERCHLORATE - National Library of Medicine HSDB Database - Toxnet [Link]
  7. FDA is Revoking Food Additive Approval for the Use of Perchlorate in Sealing Gaskets for Food Containers Because its Use Has Been Abandoned [Link]
  8. Perchlorate Toxicity and Risk Assessment [Link]
  9. Toxicological Profile For Perchlorates [Link]
PubChem Compound
516900
PubChem Substance
347827848
ChemSpider
22913
RxNav
34318
ChEMBL
CHEMBL1200696
Wikipedia
Potassium_perchlorate
MSDS
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3TerminatedPreventionHeart Failure1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
CapsuleOral200 mg
CapsuleOral
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)Decomposes at 400 °CMSDS
water solubility17 g/L at 20 °CMSDS
Predicted Properties
PropertyValueSource
Water Solubility102.0 mg/mLALOGPS
logP-0.97ALOGPS
logP-0.098Chemaxon
logS-0.13ALOGPS
pKa (Strongest Acidic)-7.1Chemaxon
Physiological Charge-1Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area74.27 Å2Chemaxon
Rotatable Bond Count0Chemaxon
Refractivity11.91 m3·mol-1Chemaxon
Polarizability5.23 Å3Chemaxon
Number of Rings0Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-108.95883
predicted
DeepCCS 1.0 (2019)
[M+H]+111.76092
predicted
DeepCCS 1.0 (2019)
[M+Na]+119.9829
predicted
DeepCCS 1.0 (2019)

Targets

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Details1. Sodium/iodide cotransporter
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Mediates iodide uptake in the thyroid gland.
Specific Function
Iodide transmembrane transporter activity
Gene Name
SLC5A5
Uniprot ID
Q92911
Uniprot Name
Sodium/iodide cotransporter
Molecular Weight
68665.63 Da
References
  1. Soldin OP, Braverman LE, Lamm SH: Perchlorate clinical pharmacology and human health: a review. Ther Drug Monit. 2001 Aug;23(4):316-31. [Article]
  2. Perchlorate Toxicity and Risk Assessment [Link]

Carriers

Details1. Serum albumin
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Yamada T, Jones AE: Effect of thiocyanate, perchlorate and other anions on plasma protein-thyroid hormone interaction in vitro. Endocrinology. 1968 Jan;82(1):47-53. doi: 10.1210/endo-82-1-47. [Article]
  2. SCATCHARD G, BLACK ES: The effect of salts on the isoionic and isoelectric points of proteins. J Phys Colloid Chem. 1949 Jan;53(1):88-99. [Article]
  3. Yu KO, Narayanan L, Mattie DR, Godfrey RJ, Todd PN, Sterner TR, Mahle DA, Lumpkin MH, Fisher JW: The pharmacokinetics of perchlorate and its effect on the hypothalamus-pituitary-thyroid axis in the male rat. Toxicol Appl Pharmacol. 2002 Jul 15;182(2):148-59. [Article]

Drug created at November 30, 2015 19:10 / Updated at February 21, 2021 18:52