Please Wait
Applying Filters...
Menu
Xls
2D Structure
Also known as: 7778-74-7, Perchloracap, Perchloric acid, potassium salt, Potassium;perchlorate, Perchloric acid, potassium salt (1:1), Mfcd00011362
Molecular Formula
ClKO4
Molecular Weight
138.55  g/mol
InChI Key
YLMGFJXSLBMXHK-UHFFFAOYSA-M
FDA UNII
42255P5X4D

Potassium Perchlorate is the potassium salt of perchloric acid and a member of the Hofmeister ions series with thyroid blocking properties. Potassium perchlorate is a competitive inhibitor of iodine uptake through inhibiting the sodium-iodide symporter (NIS) on the thyroid follicular cell membrane. This results in a potential decrease in thyroid hormone synthesis including thyroxine (T4) and tri-iodothyronine (T3). In addition, this agent decreases the accumulation of the radioactive imaging substance and Hofmeister series ion, pertechnetate Tc 99m, in the choroid plexus and in the salivary and thyroid glands through competitive displacing.
1 2D Structure

2D Structure

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
potassium;perchlorate
2.1.2 InChI
InChI=1S/ClHO4.K/c2-1(3,4)5;/h(H,2,3,4,5);/q;+1/p-1
2.1.3 InChI Key
YLMGFJXSLBMXHK-UHFFFAOYSA-M
2.1.4 Canonical SMILES
[O-]Cl(=O)(=O)=O.[K+]
2.2 Other Identifiers
2.2.1 UNII
42255P5X4D
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Perchloracap

2.3.2 Depositor-Supplied Synonyms

1. 7778-74-7

2. Perchloracap

3. Perchloric Acid, Potassium Salt

4. Potassium;perchlorate

5. Perchloric Acid, Potassium Salt (1:1)

6. Mfcd00011362

7. Potassium Perchlorate [usp]

8. Astrumal

9. Peroidin

10. 42255p5x4d

11. Potassium Perchlorate (usp)

12. Potassium Hyperchloride

13. Potassium Perchlorate (kclo4)

14. Hsdb 1222

15. Potassium Chlorate(vii)

16. Einecs 231-912-9

17. Un1489

18. Spectrex Fire Extinguishant Formulation A

19. Ccris 9379

20. Unii-42255p5x4d

21. Perchloracap (tn)

22. Potassium Perchlorate Anh

23. Potassium Perchlorate Salt

24. Ec 231-912-9

25. Potassium Perchlorate, Solid

26. Dsstox_cid_27003

27. Dsstox_rid_82046

28. Dsstox_gsid_47003

29. Potassium Perchlorate, Solution

30. Potassium Perchlorate, Solution [un1489] [oxidizer]

31. Potassium Perchlorate, Anhydrous

32. Chembl1200696

33. Dtxsid3047003

34. Potassium Perchlorate [mi]

35. Nsc41873

36. Potassium Perchlorate [hsdb]

37. Tox21_302192

38. Nsc-41873

39. Potassium Perchlorate [vandf]

40. Potassium Perchlorate (reagent Grade)

41. Potassium Perchlorate [mart.]

42. Akos015902938

43. Akos025243411

44. Potassium Perchlorate [who-dd]

45. Db09418

46. On-1489

47. Ncgc00256200-01

48. Cas-7778-74-7

49. Potassium Perchlorate [orange Book]

50. Potassium Perchlorate [ep Monograph]

51. Potassium Perchlorate [usp Monograph]

52. D07232

53. Q422434

54. Potassium Perchlorate, Solid [un1489] [oxidizer]

2.4 Create Date
2005-03-27
3 Chemical and Physical Properties
Molecular Weight 138.55 g/mol
Molecular Formula ClKO4
Hydrogen Bond Donor Count0
Hydrogen Bond Acceptor Count4
Rotatable Bond Count0
Exact Mass137.9122177 g/mol
Monoisotopic Mass137.9122177 g/mol
Topological Polar Surface Area74.3 Ų
Heavy Atom Count6
Formal Charge0
Complexity118
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count2
4 Drug and Medication Information
4.1 Therapeutic Uses

POTASSIUM PERCHLORATE, WHICH BLOCKS THYROID TRAPPING OF IODIDE, IS NO LONGER USED /AS ANTITHYROID DRUG/ SINCE IT CAUSES UNACCEPTABLY HIGH INCIDENCE OF APLASTIC ANEMIA & NEPHROTIC SYNDROME.

McEvoy G.K. (ed.). American Hospital Formulary Service-Drug Information 96. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 1996 (Plus Supplements)., p. 2767


GRAVES' DISEASE TREATED FOR 22 YR WITHOUT ILL EFFECT, THYROTOXICOSIS RECURRED 4 WK AFTER MEDICATION WAS WITHDRAWN, SUGGESTING THAT EUTHYROIDISM HAD BEEN MAINTAINED BY CHRONIC USE. LONG-TERM, LOW DOSE PERCHLORATE MAY BE NO MORE HAZARDOUS THAN ALTERNATIVE ANTITHYROID THERAPY.

PMID:6272249 Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2426142 CONNELL JM; POSTGRAD MED J 57 (670): 516 (1981)


4.2 Drug Warning

...NO SIDE EFFECTS REPORTED AFTER SINGLE-DOSE ADMIN...AS ADJUNCT TO SODIUM PERTECHNETATE TC 99M. IN HIGHER DOSES AS ANTITHYROID AGENT.../IT'S/ ASSOC WITH GASTRIC IRRITATION, NAUSEA, VOMITING, FEVER, SKIN RASHES, LYMPHADENOPATHY, NEPHROTIC SYNDROME & RARELY, LEUKOPENIA, AGRANULOCYTOSIS, PANCYTOPENIA, & FATAL APLASTIC ANEMIA.

McEvoy G.K. (ed.). American Hospital Formulary Service-Drug Information 96. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 1996 (Plus Supplements)., p. 2767


4.3 Drug Indication

No current FDA- or EMA-approved therapeutic indications.


5 Pharmacology and Biochemistry
5.1 Pharmacology

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.


5.2 ATC Code

H - Systemic hormonal preparations, excl. sex hormones and insulins

H03 - Thyroid therapy

H03B - Antithyroid preparations

H03BC - Perchlorates

H03BC01 - Potassium perchlorate


5.3 Absorption, Distribution and Excretion

Absorption

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.


Route of Elimination

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.


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.


Clearance

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


POTASSIUM PERCHLORATE IS ABSORBED FROM GI TRACT. PERCHLORATE IONS... /CONCENTRATE/ IN THYROID, CHOROID PLEXUS, SALIVARY GLANDS & GASTRIC MUCOSA. PEAK PLASMA LEVELS OF PERCHLORATE ARE REPORTED TO OCCUR ABOUT 3 HR AFTER ORAL ADMIN.

McEvoy G.K. (ed.). American Hospital Formulary Service-Drug Information 96. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 1996 (Plus Supplements)., p. 2767


PERCHLORATE IONS ARE...EXCRETED UNCHANGED IN URINE.

McEvoy G.K. (ed.). American Hospital Formulary Service-Drug Information 96. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 1996 (Plus Supplements)., p. 2767


5.4 Metabolism/Metabolites

Perchlorate ions are not reported to undergo metabolism.


PERCHLORATE IONS ARE NOT METABOLIZED...

McEvoy G.K. (ed.). American Hospital Formulary Service-Drug Information 96. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 1996 (Plus Supplements)., p. 2767


5.5 Biological Half-Life

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


PERCHLORATE IONS... ABOUT 1/2 OF ORAL DOSE ELIMINATED IN 5 HR & REMAINDER EXCRETED WITHIN 48-72 HR.

McEvoy G.K. (ed.). American Hospital Formulary Service-Drug Information 96. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 1996 (Plus Supplements)., p. 2767


5.6 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. 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 mol to 24 mol. 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.


POTASSIUM PERCHLORATE ADMIN ONCE A WK FOR 8 WK TO FRESHWATER CATFISH, HETEROPNEUSTES FOSSILIS, SIGNIFICANTLY REDUCED THYROIDAL ACTIVITY & ELEVATED TSH LEVEL OF PITUITARY GLAND. GONADOTROPIC POTENCY OF PITUITARY GLAND, & OVARIAN ACTIVITY, WERE EFFECTIVELY LOWERED AFTER TREATMENT.

SINGH R ET AL; GEN COMP ENDOCRINOL 31(4) 451 (1977)