Chemical formula: C₁₁H₆ClN₃O₆ Molecular mass: 311.63 g/mol PubChem compound: 44564
Lodoxamide, a mast cell stabiliser inhibits the in vivo Type I immediate hypersensitivity reaction in animals and man.
In vitro studies have demonstrated the ability of lodoxamide to stabilise mast cells and prevent the antigen specific induced release of histamine. In addition, lodoxamide prevents the release of other mast cell inflammatory mediators (i.e. SRS-A, slow reacting substances of anaphylaxis also known as the peptido-leukotrienes). Lodoxamide inhibits histamine release in vitro by preventing the movement of calcium into the mast cell after stimulation.
The oral bioavailability of 14C-lodoxamide in man is 71%, approximately 87% of the absorbed drug undergoes bio transformation. The metabolic transformation of lodoxamide results from stepwise hydrolysis of the oxylamide groups to form the monoxamate and the diamine. The diamine undergoes further hydroxylation followed by conjugation to either the O-glucuronide or O-sulphate. The O-glucuronide and O-sulphate metabolites account for 79% of the biotransformed lodoxamide, with the monoxamate and diamine accounting for 5% and 3% of the excreted metabolites. Only 2.7% of the absorbed dose is recovered as unchanged drug in the urine.
No further data.
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