Chelators | Pharmacology Lecture | Medical Science V-Learn

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Chelators are the small molecules which efficiently bind with the heavy metals like lead, arsenic etc. They are employed as chelation therapy to alleviate heavy metal intoxication. Some of the chelators discussed in this medical lecture include dimercaprol and succimer alongside edetate calcium disodium, unithol and penicillamine. Also, deferoxamine is highlighted.

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Lecture Duration: 00:51:25
Released: December 2018

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GENERAL PROPERTIES
Chelators are used to prevent or reverse the toxicity caused by heavy metals. Excessive metal ions generates free radicals ultimately leading to cell death. An ideal chelator is the one with greater affinity and low toxicity associated with it. Some of the chelating agents used include EDTA, succimer and deferiprone. The process of chelation presents with its own benefits and drawbacks.

DIMERCAPROL AND SUCCIMER
Dimercaprol is a therapeutic antidote which is used against the toxicity caused by arsenic-containing warfare agent lewisite. It acts by inhibiting sulfhydryl-containing enzymes and is readily absorbed. On the other hand, succimer is a water-soluble analogue of dimercaprol. It protects against acute lethal effects of arsenic.

EDETATE CALCIUM DISODIUM AND UNITHOL
Edetate calcium disodium is also called ethylenediaminetetraacetic acid (EDTA). It is given as an IV infusion and gets rapidly excreted by glomerular filtration. It is employed for chelation of lead. Unithol, on the other hand, is a dimercapto chelating agents which is a water soluble analogue of dimercaprol. It has a bioavailability of 50% (orally).

PENICILLAMINE AND DEFEROXAMINE
Penicillamine is a white crystalline water-soluble derivative of penicillin. The preferred penicillamine is D-penicillamine. The other chelate, deferoxamine is isolated from Streptomyces pilosus. It is administered either intramuscularly or intravenously.

MISCELLANEOUS AGENTS
Deferasirox is a tridentate chelator with high affinity for iron and low affinity for other metals. Its use involves the oral treatment of iron overload caused by blood transfusion. Prussian blue, also called ferric hexacyanoferrate, is a hydrated crystalline compound in which ferrous and ferric ions are coordinated with cyanide groups in the lattice structure.
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