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ANTIHISTAMINIC AGENTS: Histamine

  • These are those agents or drugs or chemical substances which inhibits the action of histamine in human body.

  • Antihistamines are drug used to treat allergies, allergic rhinitis, the common cold, the flu, and other disorders.

Histamine

  • A chemical that cells release during allergic and inflammatory reactions, as well as in response to injury which causes smooth muscle contraction and vascular constriction.

  • Histamine = hist + amine. Hist word means “tissue” and amine means “NH2”. So, it is an amine compound that is releases by tissue.

  • It is a biological substance that is released by basophils and mast cells as a local response against parasite infection or to protect cells from any foreign substance.

  • Structure-

Biosynthesis of histamine

  • Histamine is synthesised by decarboxylation of histidine which is found in all organs and tissue of the human body. This synthesis is done in presence of catalyst enzyme L-histidine decarboxylase.

Storage of histamine

  • Most of the body's histamine is produced in granules by basophils and mast cells, these are the type of white blood cells (leukocytes).

  • Histamine (non- mast cell) is also present in a variety of tissues, including the brain's hypothalamus, where it works as a neurotransmitter.

  • The enterochromaffin-like (ECL) cell of the stomach is another important location for histamine storage and release.

  • Usually histamine is present in whole body, but its concentration is high in skin, mucosal cell of lungs, intestine, urinary tract.

  • Its concentration is also high in mammalian cerebro spinal fluid (brain).

Release of Histamine-

  • Histamine is released by the interaction of antigen with IgE antibodies on the surface of mast cell.

  • The antigen are protein and polysaccharides obtained from various source like dust, pollen gains, food stuff, venoms, toxins, detergents, and some other chemicals etc.,

  • There are some other inflammatory mediators release such as prostaglandins, kinin and platelets activating factor.

  • After the release of histamine from mast cell, it performs following physiological effects-

    • Hypersensitivity like itching, sneezing, watery eye and running nose.

    • contracts smooth muscles of lungs

    • inflammation which causes pain

    • allergic reactions

    • bronchospasm (hard to breath), cause due to inflammation and allergic reactions in the airways.

    • Vasodilation, cause hypotension

    • Gastric secretion, increase HCL secretion causes Acidity etc.,

Catabolism or degradation of histamine-

  • Diamine oxidase (DAO) and histamine-N-methyltransferase (HNMT) are mainly responsible for the degradation of histamine (HNMT)

  • Histamine inactivates by many reactions and enzymes which change the structure of histamine, after changing structure, histamine does not bind with receptor due to changes its structure.


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