GASTRIC SECRETION INHIBITORS

GASTRIC SECRETION INHIBITORS act at some stage in the control process to inhibit the enzymic or gastric acid secretions of the stomach, with the latter being a major therapeutic target. The neuronal, hormonal and paracrine control of gastric acid secretion from the parietal cells of the gastric mucosa is complex. The pathways involved include acetylcholine via the parasympathetic innervation of the stomach, the hormone gastrin. the paracrine agent histamine and possibly the paracrine hormone gastrin-releasing peptide. Anticholinergic agents have not proved very valuable in the long-run, having a limited ability to reduce acid secretion at doses that can be tolerated in view of widespread side-effects. Some more recently developed agents show gastric-selectivity (they are Mrcholinoceptor-preferring ligands, which may be the reason for their selectivity), e.g. pirenzepine and telenzepine: see muscarinic cholinoceptor antagonists. Gastrin receptor antagonists and gastrin-releasing peptide antagonists have now been developed for experimental use, but it is not yet clear if either will be useful clinically. See BOMBESIN RECEPTOR ANTAGONISTS; CHOLECYSTOKININ RECEPTOR ANTAGONISTS. Histamine H2-receptor antagonists Read more […]

Herb-Drug Interactions: St John’s wort

Hypericum perforatum L. (Clusiaceae) Synonym(s) and related species Hypericum, Millepertuis. Hypericum noeanum Boiss., Hypericum veronense Schrank. Pharmacopoeias St John’s Wort (British Ph 2009, European Ph 2008, US Ph 32); St John’s Wort Dry Extract, Quantified (British Ph 2009, European Ph, 6th ed., 2008 and Supplements 6.1, 6.2, 6.3 and 6.4). Constituents The main groups of active constituents of St John’s wort are thought to be the anthraquinones, including hypericin, isohypericin, pseudohypericin, protohypericin, protopseudohypericin and cyclopseudohypericin, and the prenylated phloroglucinols, including hyperforin and adhyperforin. Flavonoids, which include kaempferol, quercetin, luteolin, hyperoside, isoquercitrin, quercitrin and rutin; biflavonoids, which include biapigenin and amentoflavone, and catechins are also present. Other polyphenolic constituents include caffeic and chlorogenic acids, and a volatile oil containing methyl-2-octane. Most St John’s wort products are standardised at least for their hypericin content (British Pharmacopoeia 2009), even though hyperforin is known to be a more relevant therapeutic constituent, and some preparations are now standardised for both (The United Read more […]

Herb-Drug Interactions: Ginkgo

Ginkgo biloba L. (Ginkgoaceae) Synonym(s) and related species Fossil tree, Kew tree, Maidenhair tree. Salisburia adiantifolia Sm., Salisburia biloba Hoffmanns. Pharmacopoeias Ginkgo (US Ph 32); Ginkgo capsules (US Ph 32); Ginkgo dry extract, refined and quantified (British Ph 2009, European Ph 2008); Ginkgo leaf (British Ph 2009, European Ph, 6th ed., 2008 and Supplements 6.1, 6.2, 6.3 and 6.4); Ginkgo tablets (US Ph 32); Powdered ginkgo extract (The United States Ph 32). Constituents Ginkgo leaves contain numerous flavonoids including the biflavone glycosides such as ginkgetin, isoginkgetin, bilobetin, sciadopitysin, and also some quercetin and kaempferol derivatives. Terpene lactones are the other major component, and these include ginkgolides A, B and C, and bilobalide, Ginkgo extracts may be standardised to contain between 22 and 27% flavonoids (flavone glycosides) and between 5 and 12% terpene lactones, both on the dried basis. The leaves contain only minor amounts of ginkgolic acids, and some pharmacopoeias specify a limit for these. The seeds contain ginkgotoxin (4-O-methylpyridoxine) and ginkgolic acids. Use and indications The leaves of ginkgo are the part usually used. Ginkgo is often used Read more […]