Mequitazine

CAS No:
29216-28-2 Category:
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Product Details:

  • CAS No: 29216-28-2
  • AHFC code:
  • Synonyms: Mequitazina [INN-Spanish] Mequitazina [Spanish] Mequitazinum [INN-Latin]
  • ATC Code: R06AD07
  • Chemical Formula: C4H6N2S
  • Molecular Weight: 322.467
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB01071 (APRD00386)
  • SMILES: C(C1CN2CCC1CC2)N1C2=CC=CC=C2SC2=CC=CC=C12
  • InChl:
  • PubChem: 4066
  • IUPAC: 10-{1-azabicyclo[2.2.2]octan-3-ylmethyl}-10H-phenothiazine

Additional Details

Indication:
For the treatment of Hay fever, urticaria (hives) and allergic rhinitis
Pharmacodynamics:
In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Mequitazine is a histamine H1 antagonist. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.
Mode of Action:
Mequitazine binds to the histamine H1 receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Metabolism:
Toxicity:
General Reference:
Ramirez Chanona N, del Rio Navarro BE, Perez Martin J: [Efficacy of mequitazine (Primalan) on the relief of symptoms of allergic rhinoconjunctivitis in children. Documented clinical experience] Rev Alerg Mex. 2005 Nov-Dec;52(6):221-5. Pubmed Theunissen EL, Vermeeren A, van Oers AC, van Maris I, Ramaekers JG: A dose-ranging study of the effects of mequitazine on actual driving, memory and psychomotor performance as compared to dexchlorpheniramine, cetirizine and placebo. Clin Exp Allergy. 2004 Feb;34(2):250-8. Pubmed Nakamura K, Yokoi T, Kodama T, Inoue K, Nagashima K, Shimada N, Shimizu T, Kamataki T: Oxidation of histamine H1 antagonist mequitazine is catalyzed by cytochrome P450 2D6 in human liver microsomes. J Pharmacol Exp Ther. 1998 Feb;284(2):437-42. Pubmed Persi L, Dupin O, Arnaud B, Trinquand C, Michel FB, Bousquet J: Efficacy of mequitazine in comparison with placebo assessed by ocular challenge with allergen in allergic conjunctivitis. Allergy. 1997 Apr;52(4):451-4. Pubmed
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