In his poem "LAmethyste, ou les Amours de Bacchus et dAmethyste" (Amethyst or the loves of Bacchus and Amethyste), the French poet Remy Belleau (1528–1577) invented a myth in which Bacchus, the god of intoxication, of wine, and grapes was pursuing a maiden named Amethyste, who refused his affections. Amethyste prayed to the gods to remain chaste, a prayer which the chaste goddess Diana answered, transforming her into a white stone. Humbled by Amethystes desire to remain chaste, Bacchus poured wine over the stone as an offering, dyeing the crystals purple.Variations of the story include that Dionysus had been insulted by a mortal and swore to slay the next mortal who crossed his path, creating fierce tigers to carry out his wrath. The mortal turned out to be a beautiful young woman, Amethystos, who was on her way to pay tribute to Artemis. Her life was spared by Artemis, who transformed the maiden into a statue of pure crystalline quartz to protect her from the brutal claws. Dionysus wept tears of wine in remorse for his action at the sight of the beautiful statue. The gods tears then stained the quartz purple.This myth and its variations are not found in classical sources. However, the goddess Rhea does present Dionysus with an amethyst stone to preserve the wine-drinkers sanity in historical text. Other cultural associations
Tibetans consider amethyst sacred to the Buddha and make prayer beads from it. Amethyst is considered the birthstone of February.
Mechanism of action
The medication works by binding to and inhibiting the ATP-sensitive potassium channels (KATP) inhibitory regulatory subunit sulfonylurea receptor 1 (SUR1) in pancreatic beta cells. This inhibition causes cell membrane depolarization, opening voltage-dependent calcium channels. This results in an increase in intracellular calcium in the pancreatic beta cell and subsequent stimulation of insulin release.After a cerebral ischemic insult, the blood–brain barrier is broken and glibenclamide can reach the central nervous system. Glibenclamide has been shown to bind more efficiently to the ischemic hemisphere. Moreover, under ischemic conditions SUR1, the regulatory subunit of the KATP- and the NCCa-ATP-channels, is expressed in neurons, astrocytes, oligodendrocytes, endothelial cells and by reactive microglia.As per the research papers, this sulphonylurea drugs also has extra hepatic effects. It works by inhibiting the enzyme Carnityl Acyl Transferase I (CAT-I) indirectly which is present in the mitochondria. This prevents the transport of long chain fatty acids into the mitochondria for beta-oxidation. This prevents hyperglycemia for which it is prescribed. History
It was developed in 1966 in a cooperative study between Boehringer Mannheim (now part of Roche) and Hoechst (now part of Sanofi-Aventis). Society and culture
Names
Glibenclamide is available as a generic medication, is manufactured by many pharmaceutical companies and is sold under many brand names including Gliben-J, Daonil, Diabeta, Euglucon, Gilemal, Glidanil, Glybovin, Glynase, Maninil, Micronase and Semi-Daonil. It is also available in a fixed-dose combination drug with metformin that is sold under various trade names, e.g. Bagomet Plus, Benimet, Glibomet, Gluconorm, Glucored, Glucovance, Metglib and many others. References
External links
"Glyburide". Drug Information Portal.