Chelation Definition:
- Chelation is the formation of complexes between drugs and metal ions (e.g., Ca²⁺, Fe³⁺, Mg²⁺).
Importance in Drug Action:
- Drug Absorption: Chelating with dietary minerals reduces absorption (e.g., tetracyclines + calcium).
- Toxicity Management: Chelating agents are used to remove heavy metals (e.g., lead, arsenic).
- Stability: It can enhance or reduce drug stability in formulations.
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Mechanism of Chelation:
- Ligand Coordination: Chelating agents typically have two or more donor atoms (such as oxygen, nitrogen, or sulfur) that can bind simultaneously to a metal ion, increasing the stability of the complex.
Examples of Chelation:
- Tetracyclines + milk (Ca²⁺): Decreased absorption.
- Deferoxamine: Used for iron poisoning.
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Biological and Therapeutic Relevance:
- Metal Ion Detoxification: Chelating agents are used to treat heavy metal poisoning (e.g., EDTA for lead poisoning).
- Enzyme Inhibition: Some drugs chelate essential metal ions in the active sites of enzymes, thereby inhibiting their activity.
- Stability: It can also stabilize certain drug formulations or influence the drug’s solubility and bioavailability.
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