CALCIUM-CHANNEL BLOCKERS

CALCIUM-CHANNEL BLOCKERS are agents that literally block or close any of the many types of calcium channels. However, in common usage the term is mainly used to describe a class of drugs finding increasing application in therapeutics (also called calcium antagonists or calcium-entry blockers) typified by the dihydropyridines (DHPs). In a more general usage of the term, there are many different classes of calcium-channel blockers, and many types of calcium channels. See CALCIUM-CHANNEL ACTIVATORS. First, in the cell membrane, the voltage-gated calcium channels are of at least six types — termed L, N, T, P, Q, R — that may be differentiated by electrophysiological, molecular cloning and pharmacological criteria. The L- and N-channels are high-voltage activated, voltage-dependent and undoubtedly of great importance in normal physiology; L mainly in smooth, cardiac and skeletal muscle (and some neurons), but N only in neurons. T-channels are important in repetitive activity in cardiac SA node of the heart, neurons and some endocrine cells. The remainder have been found more recently in neurons. These channels are products of different genes, but they all share great structural similarity — both with respect to Read more […]

Herb-Drug Interactions: Grapefruit

Citrus paradisi Macfad. (Rutaceae) Synonym(s) and related species Citrus paradisi Macfad. Grapefruit is a hybrid of the Pummelo or Pomelo (Citrus maxima (Burm.) Merr) with the sweet orange (Citrus sinensis (L.) Osbeck). Constituents Grapefruit contains furanocoumarins including bergamottin, 6′,7′-dihydroxybergamottin, bergapten, bergaptol, geranyl-coumarin and paradisin A, flavonoid glycosides such as naringin and flavonoid aglycones galangin, kaempferol, morin, naringenin, quercetin and others. The peel contains a volatile oil, mostly composed of limonene. Note that some grapefruit seed extracts have been found to contain preservatives such as benzethonium chloride, triclosan and methyl-p-hydroxybenzoate, which might be present because of the methods of production. Use and indications Grapefruit is used as a source of flavonoids (citrus bioflavonoids), which are widely used for their supposed antioxidant effects, and are covered under flavonoids. Grapefruit seed extracts are used for their antimicrobial properties, but there is some controversy that this might be due to preservative content rather than natural constituents. Grapefruit and grapefruit juice are commonly ingested as part of the diet, Read more […]

Herb-Drug Interactions: Flavonoids

Bioflavonoids The flavonoids are a large complex group of related compounds, which are widely available in the form of dietary supplements, as well as in the herbs or foods that they are originally derived from. They are the subject of intensive investigations and new information is constantly being published. You may have come to this monograph via a herb that contains flavonoids. Note that the information in this general monograph relates to the individual flavonoids, and the reader is referred back to the herb (and vice versa) where appropriate. It is very difficult to confidently predict whether a herb that contains one of the flavonoids mentioned will interact in the same way. The levels of the flavonoid in the particular herb can vary a great deal between specimens, related species, extracts and brands, and it is important to take this into account when viewing the interactions described below. Types, sources and related compounds Flavonoids are a very large family of polyphenolic compounds synthesised by plants that are common and widely distributed. With the exception of the flavanols (e.g. catechins) and their polymers, the proanthocyanidins, they usually occur naturally bound to one or more sugar molecules Read more […]